Pharmacy & Pharm.D

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    Diclofenac nanomicelles: Synthesis and anti-inflammatory activity
    (2015-05-30) Raeda Alhawareen; Haifa Najajreh; Oraib Rabaya
    Diclofenac is the most well-known globally non-steroidal anti-inflammatory drug (NSAIDs), Diclofenac produces analgesic, antipyretic, and anti- inflammatory effects and is widely used for the treatment of moderate pain and inflammation, its absorption may be influenced by gastric emptying rate and mechanical agitation in the stomach, and it has low solubility and low dissolution profile, so in this study we try to develop a novel drug delivery system of diclofenac derivative which have amphiphilic structure that is capable to self assemble to form nanomicelles which will be more water soluble with high efficiency of loading capacity that will work as a sustained release system. By using different polymers (triethylene glycol TEG, polyethylene glycol PEG 400, PEG 600) presenting the hydrophilic chain, linking the chain with the hydrophobic drug (Diclofenac). We successfully synthesize the diclofenac derivatives and their characterization using Nuclear Magnatic Resonance (NMR), then formation of the nanomicelles of the amphiphilic derivative and their characterization by atomic force microscopy (AFM)obtaining a spherical shape of the micelles with average diameters of 200nm for Dic-PEG400-Dic, 80-140nm for Dic-PEG600-Dic. The critical micelle concentration (cmc) has been calculated using Pyrene method obtaining cmc 2.7 x 10 -5 mg/ml for Dic-PEG400-DicAnd 1 x 10 - 4 mg/ml forDic-PEG600-Dic. We also study the in vitro diclofenac release profile by esterase enzyme PLE,Quantitative analysis showed that conversion of free Diclofenac was completed within 35 hrs. After 24 hrs, ≈95% was released from Dic-PEG400-Dic derivative micelles. More than 85% of Dic-PEG600-Dic derivative was converted within 30 hours. Then we determined the anti-inflammatory activity by testing TNF-α production in LPS-stimulated Balb/c mice.diclofenac derivative dose-dependently and significantly suppressed TNF production after a 5mg/kg dose were given. After 1.5 hr, 3hr, 6hr, 24 and 48 hr the derivative reduce the TNF level in a proportion of 51.3+ 28.1, 46.2+ 2.2, 44.8 + 10.8, 38.6 + 27.7 and 66.7 + 34.2 respectively, while diclofenac reduced the TNF level after 1.5 hr, 3hr, 6hr, 24, and 48 hr in a proportion of 37.7 + .6, 36 + 1.6, 38.8 + 20.3, 46.8 + 13.5 and 49.7+ 10 .9 respectively.Dic-PEG400-Dic micelles have stronger anti-inflammatoryeffect and lasted for a longer period than diclofenac only.we conclude thatthe diclofenac derivative (micelles) will have more water solubility with high efficiency of loading capacity than that of the diclofenac alone, that will work as a sustained release system.
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    Analytical Method Development and Validation of High-Performance Liquid Chromatography for Simultaneous Determination of Oxytetracycline Hydrochloride and Flunixin in Veterinary Injectable Solution
    (2021-08-26) Rand Abdullah; Aseel Mansour; Mais Mansour; Naser Shraim
    A linear, precise, specific and accurate high performance liquid chromatographic validation method was developed for determination of Oxytetracycline and Flunixine in an injectable pharmaceutical dosage form (Fenox®). The purpose of high performance liquid chromatography (HPLC) analysis of any drug is to confirm the identity of a drug and provide quantitative results and also to monitor the progress of the therapy of a disease. The aim of the study is to develop and validate a liquid chromatographic method to quantify and determine two active ingredients simultaneously in one dosage form. The proposed method is rapid, cost-effective and can be used as a quality-control tool for routine quantitative analysis of these two active ingredients in the injectable dosage form. The HPLC analysis was performed on the phenomixc18, 15cm column, which was of a diameter of 4.5 mm and a particle size of 5 µm. Different mobile phases were then tested by using different mixture of ACN and buffer solution to obtain a suitable retention time and a pH 8.5. The UV detection was performed at the wavelength (λmax) range of 200-500 nanometers and the retention time of ocytetracycline 1.343 and flunixine 4.573 min. Analytical method validation was done in accordance to ICH guidelines. The linearity of the calibration curve was then established in the concentration range of 0.16-0.64 mg\ml of Oxytetracycline and 0.032-0.128 mg/ml of Flunixine. The mean recovery of 101.4 % -100.2%. The values of LOD Oxytetracycline 0.011949 flunixine 0.005281 and LOQ oxytetracycline 0.036209 flunixine 0.016003. According to the accuracy outcome results the RSD value for all Oxytetracycline samples is 0.283841 and for Flunixine samples is 0.304195, which represents good accuracy of the used method. As well the developed method showed excellent linearity, accuracy, precision, specificity, robustness, LOD and LOQ results within the acceptance criteria.
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    Antioxidant, Anti Lipase, Anti Amylase Activity Evaluation of Basil (Ocimum Basilicum) Seeds Oil in Palestine
    (2021-06-28) Mohammad Shakhsheer; Noor Nawahdah; Ali Hanbali; Ahmad Eid