马来酸氯苯那敏制剂的研制及评价

K. Rajitha, G Rashmitha, B. Sharanya, A. Swathi
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摘要

本研究旨在制备马来酸氯苯那敏(又称氯苯那敏)制剂。马来酸氯苯胺(Chlorpheni-ramine maleate, CPM)是第一代烷基胺抗组胺药,用于预防鼻炎和荨麻疹等过敏性疾病的症状,口服生物利用度约为25-50%,经过一次代谢。以黄原胶、金合胶、HPMC K4M、黄原胶和瓜尔胶为聚合物,采用非水造粒技术制备了含CPM的微球。研究了不同聚合物浓度对马来酸氯苯那敏(CPM)释放的影响。采用差示扫描量热法和x射线粉末衍射光谱法进行了理化表征。对所制片剂的平均质量、硬度、卡尔氏指数、轻叩密度、脆性、崩解性、含量均匀性等参数进行了评价。所有的参数都在规格书中。用紫外分光光度计在261 nm处测定药物含量。在37±10℃、pH值为6.8的人工唾液中对制剂进行体外释药研究。在所有使用的聚合物中,由于黄原胶的结合能力较小,药物释放量最高。采用零级、一级、Higuchi、korsemyer - peppas、Hixon crowell、糜烂等体外释放模型,建立含片的释药机理和释药动力学。
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Formulation and Evaluation of Chlorpheniramine Maleate Troches
The present study was sought to prepare Chlorphenamine (also called chlorpheniramine) maleate troches. Chlorpheni-ramine maleate (CPM) is a first-generation alkyl amine anti histamine used in the prevention of the symptoms of allergic conditions such as rhinitis and urticarial having oral bio availability about 25-50%, it undergoes first pass metabolism. Troches containing CPM was prepared by non-aqueous granulation technology using Xanthum gum, Gum acacia, HPMC K4M and tragacanth and guar gum as the polymers.  The effect of varying the concentration of polymer on release of Chlorpheniramine maleate (CPM) from troches was investigated. Differential scanning calorimetry and X-ray powder diffraction spectroscopy were used for physicochemical characterization. Tablets prepared were evaluated for different parameters such as average weight, hardness, Carr’s index, tapped density, friability, disintegration, content uniformity test. All the parameters were found within the specifications. The drug content was estimated by UV spectrophotometer at 261 nm. In vitro drug release studies of troches formulations were performed in artificial saliva pH 6.8 at 37±1oC. Among the all polymers used the highest drug release is shown with xanthum gum due to its less binding capacity. The in vitro release data was subjected to zero order, first order, Higuchi, Korsemeyer-Peppas, Hixon crowell and erosion model in order to establish the drug release mechanism and kinetics of drug release from the lozenge tablets.
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