Pharmacy

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Prevalence and Predictors of Herb Use during Pregnancy (A study at Rafidia Governmental Hospital/ Palestine)
(2012) Deema Hilmi Adawi; Dr. Rowa’ Al-Ramahi; Dr. Nidal Jarradat
Abstract The use of herbal products among pregnant women is high Worldwide because they consider them safer than medication. They use herbs for nausea, vomiting, and other pregnancy related problems. Pregnant women like to use herbal products despite limited data on safety and efficacy. The objectives of this study are to measure the prevalence and predictors of herb use among a sample of Palestinian pregnant women and the possible influence of herbal consumption on pregnancy outcomes. This study was a questionnaire-based cross sectional descriptive study. It was conducted in the maternity ward of Rafedia Governmental Hospital between March and May 2012, a random sample of women who gave birth during the study period were met and asked to answer a face to face questionnaire. The results showed that the prevalence of using herbal products among pregnant women was 40.0%, the most common herbs were anise (61.7%), chamomile (53.3%), sage (55%), mixture of herbs (33.3%), and thyme (29.2%). The women preferred the herbs because they considered herbs safer than medications. There was no relation between herbal products use and any variable (age, educational level, living place, medical insurance, family income, work, chronic disease, parity and medication use). No negative relationship between herbal use and outcome on pregnant women and infants was found. This study found that the use of herbs during pregnancy is very common among Palestinian women. To provide the best care to pregnant women who use herb products, clinicians and pharmacist are recommended to stay up to date with herb use and their safety in pregnancy. The physicians are recommended to ask pregnant women about herb use because this practice is common among pregnant women, so doctors need to consider this to avoid any possible drug-herb interaction or negative outcomes on the mother or the fetus.
Community Pharmacists' Medication Knowledge: A Nation-wide Study in Palestine
(2012) Enass Majed Abd Alrahman Abu Arah; Prof. Waleed Sweileh; Dr. Adham Abu-Taha
Background: Community Pharmacists are easily accessible to the public. They have an important role and responsibility in monitoring the safety of medicines dispensed with or without a prescription. Objective: This study aims to assess medication knowledge of Palestinian community pharmacists. In specific, knowledge of community pharmacists about safety of medicines during pregnancy and evidence based therapy of herbal products will be assessed. Methodology: This is a cross-sectional survey study on community pharmacists. The medication knowledge was assessed by a set of questions specifically designed for this purpose. Scores of the test were presented as percentage from a total of 100. The internal consistency of each test was acceptable with a Cronbach alpha ≥ 0.6. Results: Approximately one third of chief community pharmacist in West-Bank, Palestine took part in the study. The sample consisted of 173 (50.6%) females and 169 (49.6%) males. The majority of the participants (303; 89.2%) had a B.Sc. degree in pharmacy while 37 (10.8%) had an M.S degree. Community pharmacists have the following median (Q1-Q3) scores: [70% (60-80)]; [40% (30-50)]; and [50% (40-70)] for the general knowledge, safety of medicines during pregnancy and in evidence based herbal therapy tests respectively. The total score was significantly and negatively correlated with the number of years since graduation (r= - 0.2; P<0.01). Female pharmacists had significantly better score than male pharmacists in all tests (general pharmacy, herbal pharmacotherapy, total parts) but not for drug safety during pregnancy (P values = 0.16, 0.008, 0.046) respectively.. Conclusion: Good proportion of the study sample lack adequate knowledge in certain important aspects of pharmacy practice such as medication safety during pregnancy, evidence based indication of herbal products, and herbal-drug interactions. This might negatively affect the role of Community pharmacists in patient counseling and education. Authorities need to improve the community pharmacists' role in healthcare system by providing continuous and up-to-date education for community pharmacists. Practice Implications: Professional development should be mandatory in Palestine. Inclusion of a course about drugs during pregnancy into pharmacy curriculum is recommended. Key Words: Community Pharmacist, Medication Knowledge, Pregnancy, Herbal Product, Palestine.
Assessing Appropriate Use of Inhaler Devices among Asthmatic Patients
(2013) Ola Adel Fawzi Salah; Prof. Waleed Sweileh; Dr. Samah Al-Jabi
Background: Appropriate use of inhaler devices such as metered-dose inhalers (MDIs) and dry-powder inhalers (DPIs) in clinical practice is not well studied in Palestine and few were carried out in the Arab world. Objectives: The objectives of this study were to assess patients’ administration technique of inhaler devices and its association with other variables. Method: A cross sectional observational evaluation was conducted at a pulmonary clinic in Nablus, Palestine. Administration technique was evaluated based on a pre-defined checklist. Asthma control was assessed using Asthma Therapy Assessment Questionnaire (ATAQ) scale. Results: MDIs (without spacer) and DPIs (turbuhalers and aerolizers) in patients with asthma disease were studied. The study included 149 patients with mean ± standard deviation (SD) age of 47.5 ± 18.5 years. Fifty five (36.9%) of the study patients had college education and higher. Forty two (28.2%) patients were using MDIs, 38 (25.5%) were using DPIs and 69 (46.3%) were using both devices. A total of 217 inhaler devices were evaluated: 111 (51.2%) for MDI and 106 (48.8%) for DPI. Mean scores ± SD for correct inhaler technique were 61 ± 20.1, 71.4 ± 14.9 and 66.2 ± 15.7 for MDIs, turbuhalers and aerolizers respectively (p = 0.00). For MDI and DPI devices, step 3 “exhale to residual volume” was the least correctly done (22.5% and 13.2% respectively). There was a significant relationship between correct score of handling inhaler device and educational level (r = 0.187; p=0.006) where higher educated patients had higher correct scores. Among patients, ATAQ scale indicated that 22 (14.8%) patients had well controlled asthma, 56 (37.6%) patients were not well controlled and 71 (47.7%) patients were poorly controlled. There was significant difference in scores of correct inhaler device handling and asthma control category (p < 0.01) where patients had higher correct scores were with higher control for their asthma. Among patients using inhaled corticosteroids (ICS), there was a significant difference between adherence score and correct handling scores (p = 0.002) where patients with better adherence had higher correct scores. Conclusion: Correct handling of inhaler devices was not common particularly among MDI devices. Regular checking of inhalation technique and proper practical teaching of patients is crucial for optimal use of most inhaler devices.
Problems Associated with Reconstitution, Administration, and Storage of Antibiotic Suspensions for Pediatrics in Nablus City-Palestine
(2013) Haya Ibrahim Anabousi; Dr.Rowa’ Al-Ramahi; Dr. Abd Al Naser Zaid
Pediatric infectious diseases either viral or bacterial remain a very common community health problem; in bacterial infection an antibiotic is the drug of choice, to achieve therapeutic effect and prevent treatment failure antibiotics must be properly used. The objective of this study is to evaluate the appropriateness of antibiotic suspensions use for pediatrics among Palestinian mothers including their reconstitution, dose administration, duration, and storage condition. This study was a questionnaire based cross sectional descriptive study. It was conducted at Ministry of Health (MoH) primary health care Al-Wosta clinic and a pediatric private clinic in Nablus city between 22 January, and 22 March 2013. A sample of400 mothers, 200 visited MOH, and 200 visited the private clinic were met and asked to answer a face to face questionnaire. The results showed that most common pediatric infections were bronchitis 110 (27.5%), throat infection (pharyngitis) 110 (27.5%), and otitis media 108 (27.0%), the most commonly prescribed antibiotic was amoxicillin, amoxicillin and clavulanic acid, and azithromycin. Regarding mothers' practice 347 (86.8%) of mothers told that they read instructions, 311 (77.8%) could understand manufacturer instructions, and 176 (44.0%) of mothers asked pharmacists for advice if they didn’t understand the instructions. In order to prepare antibiotic suspension 302 (75.5%) used boiled then cooled tap water, and 192 (84.4%) of mothers used syringe to measure the needed amount of water, and 304 (76.6%) of mothers added water in two steps, 392(98.0%) of mothers claimed that they shook the drug bottle before used. Regarding dose administration, 313 (78.2%) considered syringe as the most accurate tool for dose administration, most of mothers told that they gave drug dose with major meals when direction were to give three times daily. About use duration 6 (1.5%) of mothers claimed that they used antibiotic suspension after 2 weeks, and 26 (6.5%) gave left over antibiotic suspension to another child. One hundred seventy seven (44.2%) of mothers told they stored dry powder antibiotic in medicinal cabinet, while 226 (56.5%) of them stored suspension in refrigerator. Although our results reflect good knowledge about antibiotic suspension use between Palestinian mothers there is a room for improvement. The pharmacists are recommended to explain directions to mothers and confirm on them by writing, to supply them with syringe with suitable calibration for dose administration, and to tell them about storage condition and duration of use.
Analysis of beliefs about medicines and medication adherence in patients with chronic diseases at the Military Medical Services, Nablus, Palestine
(2014) Raniah Majed Fares Jamous; Prof. Waleed Sweileh; Dr. Adham Abu-Taha
Background: very few studies in the Arab world investigated patients’ behavior toward medications, particularly in those with multiple co-morbid and different chronic diseases. Furthermore, most studies in this field were carried out among patients with governmental insurance which could affect the reliability and validity of the results since medications are not always available in governmental pharmacies. Objective: to investigate how the presence of multiple chronic illnesses could affect the association between attitudes toward medicines and adherence practices in a non-governmental settings. Methodology: The Palestinian Medical Military Services in Nablus, Palestine was the main setting for the study. Presence and number of multiple chronic diseases were obtained from patients through interview setting and were confirmed by information available at the medical files. Attitudes toward medicines were evaluated by the Beliefs about Medicines Questionnaire (BMQ) while compliance / adherence behavior was evaluated by Morisky Medication Adherence Scale (MMAS-8). Results: One hundred and eighty seven patients were interviewed. Most participants (79.6%) had positive attitude that their medicines were necessary to maintain their good health status while 58.2% of the study sample were afraid and had negative attitude or concern about taking medicines on regular basis and 57.8% were afraid that they will get addicted and become dependent on their medicines. In the presence of multiple chronic diseases, demographic and clinical factors were not significantly associated with adherence practices. However, in patients with multiple chronic diseases, those who had higher positive attitudes and feeling of necessity had higher odds [1.4 (1.1 - 1.9)] of having adherence practices while those who had higher negative attitudes or concerns or fear about medicines had lower odds [0.8 (0.65 – 0.98)] of having adherence practices. Conclusions: In patients with multiple chronic diseases, positive and negative attitudes toward medicines are significant determinant of adherence practices.
Antimicrobial Utilizing Pattern in a Governmental Hospital in Palestine Measured Using WHO ATC/DDD Methodology
(2014) Marina Zeyad Bada; Dr. Adham Abu Taha; Prof. Waleed Swieleh
BACKGROUND: Increased consumption of antimicrobial agents is related to a worldwide increased in bacterial resistance, increased costs and dispensable effects of drugs on patients. OBJECTIVES: To investigate the pattern of antimicrobial consumption data using WHO ATC/DDD methodology in a governmental hospital in Palestine, and to assess the obstacles for implementing rational use of antimicrobial agents in hospital. METHODS: Antimicrobials consumption in Rafidia hospital was retrieved prospectively. The ATC/ DDD and DU90% methodologies were used. Defined Daily Dose (DDD) per 100 Bed-Days and DDD per 1000 inhabitants per day were calculated for total systemic antimicrobial use and by antimicrobial class. RESULTS: Antimicrobials were administered to 554 patients (55.4%) out of 1000 who were hospitalized in Rafidia hospital over two months period. The total consumption of antimicrobial agents was 1656.1 DDD that corresponding to 70.55 DDD/100 Bed-Days and 3.31 DDD/1000 Inhabitants/ Day. The most highly used antimicrobial were ceftriaxone followed by cefuroxime and metronidazole. The bulk prescription (DU90%) was made up of 8 out of 22 total antimicrobial agents. And the highest rates of antimicrobial use were found in intensive care unit (ICU) 132.64 DDD/100 Bed-Days and surgical department 98.52 DDD/100 Bed-Days. CONCLUSIONS: We found that antimicrobial utilization in Rafidia hospital was relatively high, and there were a high tendency for wide-spectrum antimicrobial utilization such as third-generation cephalosporins, carbapenems and aminoglycosides. This study proved that there is an urgent demand for national antimicrobial stewardship and education programs in infection control and prevention in Palestinian hospitals. Key words: Antibiotic, Consumptions.
Evaluation of Prescribing Pattern and Compliance to Treatment Guidelines in Hemodialysis Patients in Hebron Governmental Hospital
(2015) Bayan Jamal AL-Deen Nammourah; Dr. Rowa’ Al-Ramahi
Background: Chronic kidney disease (CKD) including end-stage renal disease (ESRD) is a growing epidemic. Hemodialysis (HD) is the most commonly used renal replacement therapy in addition to the management of diabetes, hypertension, dyslipidemia, anemia, and bone mineral disorder in hemodialysis patients. Objectives: The objectives of this study were to asses prescribing pattern and to evaluate compliance to treatment guidelines in hemodialysis patients. Method: This study was an observational retrospective cohort study, it was conducted at Hebron governmental hospital / Palestine between March and April 2014. All adult on chronic HD there were included. All information were collected from governmental electronic health record (AviCenna HIS program), and patients were asked to answer some questions when data was not found in the system. Statistical analysis was performed by using Statistical Package for Social Sciences (SPSS) program. Results: During the study period 158 HD patients were prescribed 1567 medication orders of 103 different medications, 49 medications for the management of chronic illness, and 54 medications for acute illness. The patients were taking a minimum of 2 and a maximum of 18 medications, with a mean of 9.92±2.94. The most commonly prescribed medications were calcium carbonate (91.8%), followed by alfacalcidol (84.8%), then iron/folic acid (69.6 %). About (36.7%) of the patients had diabetes, and hemoglobin A1c (HbA1c) test which reflect average blood sugar level for the past 2-3 months was not performed for these patients. Insulin mixtard, insulin actrapid, and glibenclamide were used to control diabetes . A majority of the patients (72.2%) had Hypertension. The target predialysis blood pressure of <140/90 mmHg were achieved in 77.2% of the patients (70.5% of the males vs 87.3% of the females; P- value =0.014) , and post dialysis blood pressure of < 130/80 were achieved 57.6% of the patients. Target predialysis correlate with postdialysis blood pressure ( r=0.236, P- value =0.003) and amlodipine was the most commonly used drug for the management of hypertension which is differ from what the guidelines advise. Atorvastatin was the most prescribe medication for dyslipidemia (39.9%). Patients with total cholesterol levels of < 200 mg/dl were 78.3% patients. Regarding triglycerides levels, 96.2% had levels of < 500 mg/dl. There was an association between the control of the total cholesterol and triglycerides as 80.1% of the patients had total cholesterol of < 200 mg/dl ( P- value =0.006). In the management of anemia, patients who reached goal hemoglobin (Hb) of 11-12 mg/dl according to the national kidney foundation (NKF) guidelines were 8.9% patients only. If kidney disease improving global outcome (KDIGO) guidelines are used, these guidelines accept a Hb level between 9-11.5 mg/dl but not to exceed 13 mg/dl, the patients in this range was 43.0% cases. Transferrin levels were not measured. Iron was used by 69.9% of the patients, and erythropoietin stimulating agents (ESA) by 5.1% of the patients as it was not available in the hospital, and very expensive to purchased by the patient’s own accounts. No data was available for calcium, and parathyroid hormone levels to manage bone mineral disorder, Target phosphorus level was obtained in 12% of the patients according to the NKF guidelines. If serum phosphorus normal range of 2.5–4.5 mg/dl is used according to KDIGO guidelines, this target was achieved in 4.4% patients only. Calcium carbonate was used by 91.8%, sevelamir by 15.8%, and alfacalcidol by 84.8% of the HD patients. Conclusion: The results reflect a poor compliance to treatment guidelines according to NKF and KDIGO guidelines for diabetes, hypertension, dyslipidemia, anemia, and bone mineral disorder. The target levels for treatment are not achieved in many HD patients. The medications are not prescribed optimally to the patients and many investigations and laboratory tests are not performed.
Attitudes, Knowledge and Practices of Health-Care Practitioners Toward Splitting or Crushing Oral Solid Dosage Forms in Palestine: Safety and Therapeutic Implications
(2015) Yaser Mustafa Mahmood Abdallah; Prof. Dr. Abdel Naser Zaid; Dr. Saed Zyoud
Background: Tablet splitting and crushing is a widespread practice among health-care providers and patients for different reasons, such as: (i) increasing dose flexibility, (ii) making tablet parts easier to swallow, and (iii) allowing cost savings for medications. However, this practice may be dangerous because some formulations and classes of drugs are unsuitable for crushing or splitting and may cause significant problems, especially in drugs with low therapeutic indices. Objectives: This thesis was conducted to examine the attitudes, knowledge and practice of pharmacists and nurses toward splitting or crushing oral solid dosage forms (OSDFs) in Palestine. It also aimed to determine the factors that affect health-care practitioners with regard to splitting or crushing OSDFs, in addition to determining the differences in attitudes and knowledge between nurses and pharmacists regarding this very important issue, and to determine the safety and therapeutic problems that resulted from splitting or crushing OSDFs. Methodology: This is a self-administered cross-sectional questionnaire survey involving 550 respondents and was conducted during the period May 2013 to August 2013 among pharmacists and nurses who work at community pharmacists and hospitals in the West Bank area of Palestine. Data were collected using a pretested questionnaire consisting of four sections and analysed using descriptive statistics and correlation. Results: A total of 615 questionnaires were distributed and 550 were completed. About 67.3% of the pharmacists and only 5.6% of the nurses had good knowledge. Nearly 69% of the pharmacists and 36.4% of the nurses had a good attitude. There was a positive correlation (p=0.002, r=0.18) between knowledge and attitude scores among pharmacists. There was a positive correlation (p<0.001, r = 0.24) between knowledge and attitude scores among nurses. Approximately 83.7% of the pharmacists and 41.6% of the nurses had good practices. Conclusion: This study has identified knowledge, attitude and practice gaps among health-care practitioners, especially among nurses. Therefore improving appropriate knowledge regarding splitting and crushing OSDFs is required by planning and developing programs for local health education purposes
Preparation and Characterization of Carvedilol-Loaded Poly (D, L) Lactide Nanoparticles/Microparticles as a Sustained Release System
(2015) Majd Suleiman Mahmoud Bani-Odeh; Dr. Mohyeddin Assali; Prof. Abdel Naser Zaid
Background: Polymeric nano and micro particles are promising delivery systems for the enhancement of the bioavailability of highly lipophilic drugs prone to ﬁrst pass metabolism. Purpose: This study aims at preparing carvedilol polymeric nanoparticles and microparticles with high loading efficiency. Other objective was to study carvedilol release profile from the obtained particles at room and body temperatures. Method: Carvedilol PDLLA nanoparticles and microparticles were prepared using nano-precipitation method. PVA was used as emulsifying agent. The effect of the solvents (acetone, tetrahydrofuran, acetonitrile, ethanol and dichloromethane) and the polymer amount on the size, size distribution and morphology of the formed particles were studied using atomic force microscope (AFM). Results: Spherical polymeric particles were obtained in all solvents used. The used method is easy, rapid, reproducible, effective (high loading capacity of carvedilol) and consequently can be used as new strategy for the development of carvedilol controlled release dosage forms. The in vitro release profile of carvedilol has shown a sustained release pattern with a little rapid release rate at body temperature in comparison to that at room temperature. Conclusion: The carvedilol loaded PDLLA nanoparticles have been successfully prepared with high loading efficacy and small particle size when acetone was used as the organic solvent and 12.5 mg of PDLLA polymer was used. Microparticles obtained when dichloromethane was used. The Korsmeyer Peppas with T lag model was the best one to explain the sustained release behavior.Chapter One
Analytical and Dissolution Method Development and Validation for a Home Formulated Rutin Tablet
(2015) Jumana Saleh Mohamed Mansour; Dr. Murad Abualhasan; Dr. Nidal Jaradat
Rutin can be classified as flavone, colorant and vitamin. It is highly available in some foods, fruits, vegetables and plant-based beverages. Rutin is highly attracted to the researchers due to its variant beneficial medical effects making rutin used in the treatment of various ailments. Rutin is available in different oral dosage forms such as tablets or capsules either alone or in combination with other active ingredients. Rutin pharmaceutical preparations are widely available in international market as well as Palestinian market. In this study we formulated a 250mg rutin tablet and we developed an easy and simple validated analytical method to quantify rutin in our formulated tablet as well as the internationally marketed Rutin® tablet of Solgar. The method was validated in accordance to international guidelines of the ICH and USP. The dissolution profile of our formulated tablet was also inspected. The shelf and the accelerated stability of the locally formulate tablet was studied. The results clearly show that our developed method was a valid method with a good linearity, precision and accuracy. The validated method was sensitive with LOD and LOQ value of 4.34*10-3 and 0.013mg/ml respectively. The locally formulated rutin tablet was stable under accelerate as well as room temperature for 150 days, only with slight and tolerable drop in the %assay with no detrimental effect on the physical properties of the tablets. The dissolution profile of our locally formulated tablet show slightly better dissolution in phosphate buffer compared with the internationally marketed Rutin® tablet of Solgar. Our study encourages and helps companies that manufacture herbal products especially those present in Palestine to improve their formulated herbals and apply validation analytical methods to check their product quality. In conclusion we succeeded in developing a validated analytical method to quantify rutin in our locally formulated rutin tablet as well as the available rutin formulations present in the local and international markets. Our formulated tablet showed a slight improvement in the dissolution profile and was stable in normal as well as under stress condition
Biowaiver monograph for ascorbic acid immediate release solid oral dosage forms
(2016) Helen Najdi Naji Al-Masri; Dr. Ramzi Shawahna; Dr. Amjad Hussien
Background: Demonstrating similarity in terms of safety and efficacy between innovator pharmaceutical products and their generic versions is a critical step in granting marketing authorizations (MAs) for generics. Similarity often proved by conducting in vivo bioequivalence (BE) studies in healthy volunteers. Health regulatory bodies issue MAs for generic versions after furnishing a proof of similarity with their innovator counterparts. BE studies are expensive, time consuming and risky studies since they are conducted in healthy volunteers. Today, the biopharmaceutical classification system (BCS) introduced by Amidon and adapted by various regulatory authorities and organizations like the US Food and Drug Administration (FDA), European Medicines Agency (EMA) and the World Health Organization (WHO) has significantly changed the processes of drug development and approval. Regulatory bodies now allow waiver of in vivo BE studies using surrogate in vitro dissolution testing for immediate release (IR) solid oral dosage forms containing high solubility and high permeability (BCS class I) drugs. Objectives: The objectives of this thesis were to systematically evaluate the possibility of granting biowaiver for immediate release (IR) formulations containing ascorbic acid as an active pharmaceutical ingredient (API). The release characteristics of two formulations containing ascorbic acid were also assessed. Methods:Solubility studies were conducted to determine the aqueous solubility of ascorbic acid at different pH points in the range of 1-7.5 at 37 ºC and to assign a correct solubility class for ascorbic acid. According to the BCS, and the FDA guidelines, a drug substance is considered highly soluble when the highest dosestrength is soluble in 250 ml or less of aqueous media over the pH range of 1–7.5. A standard shake-flask method was applied using three different aqueous media with pH values of 1.0 (maleate buffer), 4.5 (acetate buffer), and 7.5 (phosphate buffer) at 37 °C. The establishment of equilibrium was confirmed by comparing the solubility at 24 h and 48h.Drug levels in the samples were analyzed using UV spectrophotometric assay of ascorbic acid at 260nm. Dissolution experiments on two IR tablets containing ascorbic acid 500 mg were carried out. Dissolution profiles of ascorbic acid 500 mg tablets were generated in 900 ml of deionized water at pH points of 1.2, 4.5 and 6.8 adjusted using 0.1 N HCl or NaOH solutions. A paddle type dissolution apparatus was used and dissolution was tested in according to the USP type-II method. Paddles rotated at 75 rpm and the temperature of the dissolution media was maintained at 37 ± 0.5 ºC. Aliquots of 5 mL were withdrawn at predetermined time intervals of 5, 10, 15, 20, 25, 30, 45 and60 min.Samples were suitably diluted and analyzed at260 nm using UV spectrophotometer. Molecular descriptors like polar surface area (PSA), n-octanol/water partition coefficient (log P), distribution-coefficient at pH 7.4 (log D7.4), number of hydrogen bond acceptors, number of hydrogen bond donors and pKa were calculated using software packages. Literature databases were searched for solubility, permeability and dissolution related parameters. Results:The solubility measurements show that the maximum dose listed on the WHO’s EML list was soluble in less than 250 mL of water over the pH range specified by the regulatory agencies at 37 °C. The calculated dose number was in the range 0.00011 of 0.00029 in the pH range of 1.2-7.5. These results suggest that ascorbic acid should unequivocally be assigned a “high solubility” BCS class. Based on the predicted physicochemical properties and observed in vivo behavior, ascorbic acid behave like high permeability BCS class drugs. Therefore, we suggest that ascorbic acid should be assigned to BCS class I drugs. Visual as well as similarity (ƒ2) and difference (ƒ1) factors comparisons between the two IR oral formulations containing ascorbic acid(C-Tamin tablets, and Vitamin C tablets) as a single API showed the ascorbic acid was released differently in the tested dissolution media. Conclusions:Ascorbic acid is a high solubility and high permeability drug, and therefore is classified as a BCS class 1 compound. The risk of bioinequivalence is manageable as long as the use of ascorbic acid is safe. For these reasons, we consider ascorbic acid to be a good candidate for waiver of in vivo BE studies. Conducting in vitro dissolution could reveal the quality of IR oral formulations. Key words:absorption; bioavailability; bioequivalence; biopharmaceutical classification system (BCS); biowaiver; ascorbic acid; pharmacokinetics; permeability; solubility
Biological and phytochemical screening of Erodium laciniatum and Lactuca orientalis
(An-Najah National University, 2017-01-12) Othman, Dua'a; Jaradat, Nidal
From ancient times, various herbal remedies and various medical agents containing flavonoids, tannins and phenols have been utilized for prevention and treatment of different diseases and disorders. Currently, such groups of bioactive compounds have become the subject of many antimicrobials researches, with possessed antiviral, antifungal and antibacterial activities. Moreover, many of high quality studies assessed the relationship between flavonoid's, tannin's and phenol's chemical structures and their antibacterial activities, and also studied their mechanisms of action on the microbial growth. These investigations approved that such classes of natural compounds can possess many therapeutic properties, including oestrogenic, antiinflammatory, enzyme inhibition and antimicrobial activities. In this study we aimed to screen Erodium laciniatum and Lactuca orientalis phytoconstituents and to evaluate their total flavonoids, tannins and phenols contents. An additional aim is to evaluate their antioxidant and antimicrobial activities. Phyto-constituents, total flavonoids, phenols and tannins were screened and evaluated by using standard analytical and phytochemical methods. Antioxidant activity was evaluated by using DPPH method meanwhile antibacterial activities were examined by using several reference bacterial strains obtained from the American Type Culture Collection (ATCC) and multidrug resistant clinical isolates. The tested strains included Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), Staphylococcus aureus (MRSA Positive), Enterococcus faecium (ATCC 700221), Shigella sonnei (ATCC 25931), Enterobacter cloacae (clinical) and Klebsiella pneumoniae (clinical). In addition to that anti-fungal activities of these extracts were also examined against two reference strains Candida albicans (ATCC 90028) and Epidermatophyton floccosum (ATCC 52066). Antibacterial and antifungal activity of all prepared Erodium laciniatum and Lactuca orientalis organic and aqueous extracts were determined by using several methods including agar diffusion well-variant method, agar diffusion disc-variant method and broth micro-dilution method. The results of the phytochemical screening showed that L. orientalis and E. laciniatum contain phenols, tannins, flavonoids, saponins, monosaccharides, reducing sugars, carbohydrates, cardiac glycosides, and steroids, while alkaloids were not detected in both of the studied species. However, proteins, starch and terpenoids were not detected in L. orientalis and detected in E. laciniatum which means that E. laciniatum had more phyto-constituents than L. orientalis. Moreover, total flavonoid, tannins and phenols content in E. laciniatum extract were higher than the L. orientalis extracts. The IC50 values of the antioxidant activity were almost the same in L. orientalis and E. laciniatum extracts. Additionally the lowest value of MIC was for organic extract of E. laciniatum against Staphylococcus aureus. The same organic extract also showed to have the largest diameter of inhibition against Enterococcus faecium. However, L. orientalis aqueous extract showed to have the largest diameter of inhibition against Staphylococcus aureus. Whereas, the antifungal activity which was tested by using agar dilution method against Epidermatophyton floccosum showed that the organic extract of E. laciniatum had the lowest MIC which was 0.391mg/ml. In conclusion, both of the studied species have a mixture of phytochemicals and rich in flavonoids, phenols and tannins and have potential antioxidant and antimicrobial activities which can be used as therapeutic agents or can be used in cosmeceutical and pharmaceutical industries.
Synthesis, characterization & biological activity of Isopropyl Thiazole derivatives of the natural products Distamycin & Proximicin
(An-Najah National University, 2017-05-04) عبد الرحمن, امجد عبد الرحمن موسى; النيص, حسن
Minor groove binders (MGBs) are molecules which bind selectively to the minor groove of DNA. Distamycin and netropsin are naturally occurring MGBs, and are members of the polypyrrole class of compounds. They have potential antiviral, antibacterial, and anticancer properties. However, they also have toxic properties. These biological effects arise from the molecule binding to DNA in regions where there are short runs of A: T base pairs. Much work has been carried out in developing analogues of distamycin and netropsin which have improved their biological activities and reduced their toxicity profile. This project was concerned with developing a novel synthetic pathway of MGBs which allows for more varied substituents at the tail and head position of these molecules and replacing the N-methyl pyrrole with more lipophilic aromatic rings which, to date, has not been fully investigated. Aromatic rings such as benzene, pyridine, morpholine and indole were added to the structure of these compounds, in order to enhance the lipophilicity and membrane permeability to generate biologically active compounds. The tail group is significant as it plays a key role in both DNA binding, and transportation of these compounds to within cells. These structural variations will allow libraries of compounds with small molecular weight to be prepared. In this project, we developed simple and novel routes for the synthesis of potential minor groove binders. The outcome of such a study would be of great importance regarding the development of new analogues of distamycin and netropsin as potential antibacterial and anticancer agents. The synthetic pathway of the compounds started from the preparation of the isopropyl thiazole ring using the Darzen reaction and coupling the epoxide intermediate with thiourea. The second step was reacting the amine terminal of the isopropyl thiazole ring with various acid chlorides to give the second intermediate compounds in the synthetic pathway. After that the intermediate compounds where ether refluxed with an amine directly, or, where hydrolyzed and converted to acyl chlorides to be then reacted with various amines to give the final products. NMR spectroscopy was used to confirm the chemical structures of the investigated compounds, which were tested against different bacterial strains, and showed variable activities among the different compounds with the compound MGB 10 being the most active of the synthesized compounds.
Bio-Functionalization of SWCNTs with Combretastatin A4 for Targeted Cancer Therapy
(An-Najah National University, 2017-05-25) حمد, ديمه فهيم محمد رشدي; العسالي, محي الدين
Chemotherapy is a mainstay approach in the management of cancer. Unfortunately, it can affect not only the cancerous cells but also the healthy ones resulting in a number of severe side effects. Therefore, many researchers are keen to developing new Drug Delivery Systems (DDS) that may in one hand help reducing the used doses and on the other hand target the delivery of the chemotherapy to cancer cells. Some modern investigational DDS in this field are based on carbon nanotubes (CNTs) technology. The aim of this work is to covalently functionalize single walled carbon nanotubes (SWCNTs) with Combretastatin A4 (CA4) through click reaction in the presence of tetraethylene glycol linker to improve the solubility and dispersibility of the developed nano-drug. Moreover, in order to specifically target the cancer cells, a targeting agent folic acid was also loaded on the nano-system. The characterization of the developed nano-drug by scanning electron microscopy (SEM) and transmission electron microscopy (TEM) showed good dispersibility of the functionalized SWCNTs with diameters of (5-15) nm. Moreover, the efficiency of functionalization was determined by thermogravometric analysis (TGA) showing 45% of functionalization in the case of CA4-SWCNTs (7) and 50% for CA4-FA-SWCNTs (13). The in vitro release profile of CA4 showed that approximately 90% of the loaded drug was released over 50 hrs at pH 7.4 and 37 ºC. MTS proliferation test was implemented to determine the suitable concentration for the CA4-SWCNTs (7), which was found to be 15 ng/ml. After that the cytotoxic activity of the nano-drug was evaluated by flow cytometry using Annexin V/Propidium iodide (PI) test. In comparison with free CA4, CA4-SWCNTs (7) treatment demonstrated a significant increase in necrotic cells (around 50%) at the expense of the proportion of the apoptotic cells. Moreover, cell cycle PI test demonstrated that free CA4 and CA4-SWCNTs (7) caused G2/M arrest. However with CA4 treatment higher proportion of cells were in the S-phase while with CA4-SWCNTs treatment greater proportion of cells appeared to be in the G1-phase. Taken together, the provided data suggest that the novel CA4-SWCNTs (7) has a significant anticancer activity that might be superior to that of free CA4. The anticancer activity of CA4-FA-SWCNTs (13) is under investigation.
Evaluation of Food Effect on the Absorption of Clarithromycin using Physiological Modeling
(جامعة النجاح الوطنية, 2017-08-08) جيوسي, رند خليل عبداللطيف; رضوان, أسماء
Background: Food may affect the oral absorption of drugs by inducing physiological changes in the gastrointestinal physiology, such as: gastrointestinal pH, gastric residence time, bile salt secretion and drug metabolism. Purpose: The aim of the present study was to investigate the influence of food on the oral absorption of Clarithromycin by evaluating the effect of media parameters such as; pH, bile secretions and food composition, on the release of the drug from immediate release tablet, using in vitro and in silico assessments Method: The solubility, disintegration and dissolution profiles of Clarithromycin 500 mg immediate release tablets in compendial media with/without the addition of homogenized FDA meal as well as in biorelevant simulated intestinal media mimicking fasting and fed conditions were determined. These in vitro data were input to GastroPlusTM to make computational simulation in order to anticipate the effect of food on Clarithromycin absorption profiles under fasted and fed states. In vivo plasma concentration curves were used for compartmental modeling of pharmacokinetic data. Level A in vitro – in vivo linear correlations were established using mechanistic absorption modeling based deconvolution approach. Gastroplus™ was used for developing a physiological absorption model for Clarithromycin, which is capable of predicting the in vivo performance Results: Media pH has a profound effect on drug solubility, tablet disintegration and drug release. Clarithromycin has lower solubility in the biologically biorelevant media compared to other media, due to complex formation with bile salts. Clarithromycin tablets exhibited prolonged disintegration times and reduced dissolution rates in the presence of the standard FDA meal. The simulation model predicted no significant food effect on the oral bioavailability of Clarithromycin. The developed IVIVC model considered SIF, acetate, and FaSSIF buffer media to be the most relevant from the physiological standpoint. Conclusion: the intake of standard FDA meal with Clarithromycin may have no significant effect on oral bioavailability of Clarithromycin from immediate release tablets. This may suggest that the dissolution conditions recommended by ICH are sufficient to demonstrate interchangeability between generic and brand Clarithromycin, a class II drug, especially during the developmental phase of the generic product.
Functionalization of graphene sheets and their antibacterial activity
(An-Najah National University, 2017-08-08) Alsouqi, Deema Ghaleb; Assali, Mohyeddin
Graphene is a thin flat monolayer of carbon atoms tightly packed into a two-dimensional (2D) honeycomb lattice. It is one of the most studied materials nowadays because it has a high surface area and unique properties. However, graphene is considered a hydrophobic material (has a low solubility and dispersability in physiological solution), which leads to aggregation and precipitation in cell tissue and causing toxicity for different types of cells. For this purpose, functionalization of graphene has its purpose to improve its dispersability in water and its biocompatibility for various biomedical applications. The aim of this work is to covalently functionalize the graphene sheets with various charged groups (positive, negative and neutral) to improve its water dispersability, study its antibacterial activity and to determine the effect of charge on the activity. The graphene sheets had successfully functionalized covalently with three different groups (COOH, amine and tetraethylene glycol). The functionalization was confirmed by infrared spectroscopy and transmission electron microscope images. The functionalization demonstrates good dispersability in water and the degree of functionalization was quantified using the thermogravimetric analysis obtaining 32% of the functionalization in the case of graphene-TEG, 33% of graphene-amine and 47% of graphene-COOH. The antibacterial activity was determined primarily by agar diffusion disk- and well-variant method. Agar diffusion well-variant demonstrated the presence of the antibacterial activity for all graphene derivatives. In additional step, the antibacterial activity was detected and quantified through determining the MIC of the graphene derivatives by broth microdilution method. MIC was 250µg/ml for graphene-amine and graphene-TEG and 125µg/ml in the case of graphene-COOH. Moreover, the reduction of bacterial concentration after exposure to graphene derivatives was detected by the plate count method, the result shows that the bacterial reduction was increased in functionalized graphene nanomaterials with the complete growth inhibition in the case of graphene-COOH on both bacteria (E. coli and S. aureus). Graphene toxicity mechanism was investigated by in vitro graphene-mediated oxidation of glutathione, the loss of glutathione activity was the maximum for graphene-COOH with a reduction of 83%. Finally, graphene-COOH and graphene-TEG showed good hemo-compatibility, which supports their further in vivo studies.
Synthesis, Formulation and Analytical Method Validation of Rutin Prodrugs
(An-Najah National University, 2017-11-01) سرحان, تالا محمد أحمد; أبو الحسن, مراد
Background: Rutin is a plant extract that belongs to the flavonoid group of compounds. Many studies showed that Rutin has a potential pharmacological uses such as antioxidant, anti-inflammatory and antihypertensive activities. Rutin is widely used as medicinal product and food supplement and marketed in different pharmaceutical dosage formulations. However, rutin suffered from low systemic bioavailability due to its low absorption from the gastrointestinal tract and its low water solubility. In this study, we aimed to improve the water solubility and consequently its dissolution profile by synthesizing a more soluble derivative of rutin. Method: Decaacetylated ester of rutin was first synthesized. Then selective partial deacetylation was performed to produce the hexaacetylated ester of rutin. Water solubility of the new derivative as well as its dissolution was compared to rutin. An evaluation of the antioxidant activity of the hexaacetylated derivative was tested using 2,2-diphenyl-1-picrylhydrazyl reduction method. Moreover, A Ultraviolet/Visible spectrophotometric method was developed and validated for the analysis of a tablet formulation of the newly synthesized derivative. An ultraviolet spectrophotometric quantitative analytical method for rutin derivative as active particle ingredient and in a tablet dosage form was developed and validated according to the International Conference on Harmonization and international guidelines. Results: The hexaacetylated ester derivative of rutin was successfully synthesized and the derivative structure was confirmed by nuclear magnetic resonance. Moreover, the water solubility and the dissolution profile were improved by approximately two fold increase compared to that of the original rutin. Water solubility of the partially acetylated product has been increased from 0.07 to 0.15 mg/mL and its dissolution increased from 22% to 37.5% compared to the original rutin. Moreover, the antioxidant activity results showed that the newly synthesized derivative preserved the antioxidant activity of the original rutin. An easy and feasible analytical method was developed and validated. The developed method was found to be linear, precise, accurate and selective with a lowest limit of detection and lowest limit of quantification of 0.00854 and 0.0259 mg/mL respectively. The formulated tablets of hexaacetylated rutin in our research laboratory were found to be stable under accelerated conditions as well as long term conditions for three months. Conclusion: An improvement on the solubility of rutin was achieved by selective acetylation of some of the OH groups of rutin. The tablet formulation of the partially acetylated ester derivative of rutin gives a better dissolution over the already marketed rutin tablets.
Chemical composition and pharmacological screening of Micromeria fruticosa serpyllifolia volatile oils collected from West Bank-Palestine
(An-Najah National University, 2018-02-26) سلامه, نهاية محمد يوسف; شريم, نصر
Background and Objectives Micromeria fruticosa subspecies serpyllifolia (M. Bieb.) is one of the Medicinal Aromatic Plants (MAP) which are dominated in the eastern Mediterranean regions including Palestine, has pleasant minty fragrance, in hot summer provide sensation of coolness. The objective of the current work was to screen and compare the chemical constituents and potential pharmacological properties of Micromeria fruticosa serpyllifolia volatile oils collected from three different regions in the West Bank -Palestine. Methods The volatile oils of three samples of Micromeria fruticosa serpyllifolia were extracted using Microwave - ultrasonic apparatus method. The volatile oils samples were analyzed for chemical constituents using GC-MS. The antioxidant activity of the volatile oils of the three samples were screened by the inhibition of 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical. The antilipase activity was evaluated using porcine pancreatic lipase (PL) and p-nitrophenyl butyrate (PNPB). The anti amylase activity was assessed using porcine pancreatic α- amylase, starch and 3,5-dinitrosalicylic (DNSA). The antimicrobial activity was examined using broth microdiltution method separate for antibacterial and then for antifungal and agar dilution method for fungal assessment. Nine bacterial strains were used four Gram-positive: Staphylococcus aureus, Staphylococcal enterotoxin B (SEB), Enterococcus faecium, "methicillin"-resistant Staphylococcus aureus (MRSA), and five Gram-negative strains; Proteus mirabilis, Pseudomonas aeruginosa, Escherichia coli, Shigella sonnie, Klebsilla pneumoniae and one fungus Epidermophyton floccosum and one yeast Candida albicans. Results Plant extracts yield range was (0.67 to 0.99%) (w/w%). GC-MS analysis showed the high percentages of oxygenetated components with the range of (86.1-89.88%), non oxygenated components in the range of (4.38-4.71%), the total identified compounds range was (90.48-94.44%). Seven components were observed, pulegone was the most abundant components in the three samples in the range of (74.43-86.04%), isomenthone was the second abundant components with the range of (3.16-14.41%).The sample from Ramallah (middle region) showed the potent antioxidant agent with IC50 0.45 µg/mL, the sample from Hebron (southern region) was the potent antilipase agent with IC50 85.00 µg/mL. The sample from Nablus (northern region) was the potent antiamylase agent with IC50 3.00 µg/mL. The three samples exhibited broad antimicrobial activity; the three samples showed potent antifungal activity at minimum inhibitory concentration (MIC) with the range of (0.206 to 0.781 mg/mL). The sample from Hebron (southern region) showed the highest potency against Shigella sonnie with lowest reported MIC value (1.56 mg/mL), the sample of Nablus (northern region) demonstrated the least potency against Staphylococcal enterotoxin B (SEB) and 'methicillin" resistance Staphylococcus Aureus (MRSA) with highest MIC value (6.250 mg/mL). However, the three samples showed broadspectrum antibactreial activity with MIC value (3.125 mg/mL). Conclusion The study showed that Micromeria fruticosa serpyllifolia volatile oils samples from different regions in Palestine contained different proportions of phytochemicals which provided different potential biological activities such as: antioxidant, antiobesity, antidiabetes and antimicrobial activities that were in line with traditional uses of the plant extracts. The plant extracts showed higher antioxidant, antilipase and antiamylase potency higher than that of the relative references and there were significant differences in these activities compared to each other. Further in vivo studies are required to evaluate the potential pharmacological activities, safety and toxicity of plant extract. Also further studies are needed to isolate, identify and characterize the main components responsible for potential pharmacological activities..
Dual functionalization of single-walled carbon nanotubes for targeted cancer therapy
(An-Najah National University, 2018-05-07) نعيم كتانة, محي الدين العسالي
Chemotherapy is a mainstay strategy in the management of cancer. Regrettably, they suffer from serious side effects due to their effect on healthy cells besides cancerous cells. Therefore, many researchers are eager to develop new drug delivery systems that may help to decrease the side effects and the effective dose of the drug in addition to target delivery of the chemotherapy to cancer cells. One of the epochal drug delivery systems in this field are based on carbon nanotubes technology. The aim of this work is the covalent functionalization of single walled carbon nanotubes with Doxorubicin in the presence of tetraethylene glycol linker to improve the solubility and dispersibility of the developed nano-drug. Moreover, in order to target the cancer cells, a targeting agent mannose was also loaded on the nano-system. The characterization of the developed nano-drug by transmission electron microscopy showed good dispersibility of the functionalized single walled carbon nanotubes with diameters (6-10) nm. Moreover, the percentage of functionalization was determined by thermogravometric analysis showing 25% of functionalization in the case of Dox-SWCNTs (7) and 51% for Dox-mannose-SWCNTs (11). The in vitro release profile of Dox from Dox-SWCNTs (7) showed 45% of the loaded drug was released over 18 hr at pH 7.4 and almost complete release at pH 5.5 at 37 ºC. However, the in vitro release profile of Dox from Dox-mannose-SWCNTs (11) showed 75% of the loaded drug was released over 5hr at pH 5.5 at 37 ºC. The cytotoxity effect of the compounds was studied at different concentrations and different pH conditions and compared with Dox alone. The maximum cytotoxity effect was observed at 4μg/ml and at pH 6.5. After that, the pre-incubation with any of the tested concentrations of mannose reduced the cytotoxicity of Dox-mannose-SWCNT by approximately 40-57%, suggesting that the entry of this complex might be dependent on mannose receptors, which imparts this complex a kind of selectivity for cancer cells that overexpress this type of receptors.
Extemporaneous Compounding and Physiological Modeling of Amlodipine/Valsartan Suspension
(An-Najah National University, 2018-05-13) عابد, وفاء جاسم محمود; رضوان, أسماء
Background: In case of absent liquid dosage form, crushing a tablet or dispersing a capsule would be the most convenient option for using these drugs in patients with dysphagia difficulties. However, no bioequivalence or stability studies are conducted for these extemporaneous preparations, which leads to confusion regarding its efficacy and safety. In silico and in vitro tools have proven to be useful in predicting the in vivo performance of drugs depending on its physicochemical properties and it’s in vitro dissolution profiles. No liquid formulation of combination Amlodipine and Valsartan is available in the pharmaceutical market for use in pediatric population with hypertension. Purpose: The aim of the present study was to prepare an extemporaneous suspension of Amlodipine and Valsartan from available commercial tablets, and to evaluate the stability and dissolution properties of the compounded suspension. Method: Amlodipine/Valsartan extemporaneous suspension was prepared from available commercial tablets Valzadepine®. The dissolution profiles for the extemporaneous preparation and the commercial tablet was determined in different pH media. The physical, chemical and microbial stability of the compounded formulation was evaluated over one month period at room temperature. Moreover, In silico modeling using GastroPlus TM software was used to build absorption models for both drugs based on the in vitro dissolution data. The simulated plasma profile for both active ingredients were compared with the in vivo plasma profile to examine the similarity of the extemporaneous suspension and the commercial tablets. Results: The Amlodipine/Valsartan extemporaneous suspension was successfully prepared with acceptable organoleptic properties. The suspension was stable for four weeks period preserving its physical and chemical features. The release profiles of valsartan and Amlodepine from the suspension were similar to that from source tablet Valzadepine®. In silico modeling predicted similarity of the extemporaneous suspension and the commercial tablets. Conclusion: Amlodipine/Valsartan extemporaneous suspension could be prepared from available commercial tablets. Moreover, GastroPlusTM can be applied along with the in vitro dissolution in order to affirm similarity in extemporaneous compounding situations.

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