Formulation and evaluation of mucoadhesive buccal films of enalapril maleate.
Formulation and evaluation of mucoadhesive buccal films of enalapril maleate.
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DOI：
10.4103/0250-474x.78522
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发表时间：
2010-09
影响因子：
0.5
通讯作者：
Nautiyal U
中科院分区：
文献类型：
--
作者：
Semalty A;Semalty M;Nautiyal U
马来酸依那普利用于治疗高血压和心绞痛。由于肝脏首过代谢高，其生物利用度低。因此，本工作进行了马来酸依那普利口腔粘膜粘附膜的目的，以提高治疗效果，患者的依从性和生物利用度。本研究采用溶剂浇铸法制备了10种马来酸依那普利口腔粘膜粘附释药系统。使用羧甲基纤维素钠、羟丙基甲基纤维素、羟乙基纤维素和聚乙烯吡咯烷酮K-90作为粘膜粘附聚合物。制备的膜进行了评价，其重量，厚度，表面pH值，溶胀指数，药物含量均匀性，在体外停留时间，耐折性，体外释放和渗透研究。薄膜在渗透研究中表现出超过10小时的控释。结果表明，含20 mg马来酸依那普利的羧甲基纤维素钠2% w/v和羟乙基纤维素2% w/v（配方F5）的膜具有良好的溶胀性、方便的滞留时间和良好的药物控释性，因此可选择用于开发有效治疗用途的口腔膜剂。
Enalapril maleate is used in the treatment of hypertension and angina pectoris. It shows low bioavailability due to high hepatic first pass metabolism. Hence the present work was undertaken to formulate mucoadhesive buccal films of enalapril maleate with an objective to improve therapeutic efficacy, patient compliance and the bioavailability. In the present study ten formulations of mucoadhesive drug delivery system of enalapril maleate were prepared as buccal films, by solvent casting technique. Sodium carboxymethylcellulose, hydroxylpropylmethylcellulose, hydroxyethylcellulose and polyvinyl pyrrolidone K-90 were used as mucoadhesive polymers. Prepared films were evaluated for their weight, thickness, surface pH, swelling index, drug content uniformity, in vitro residence time, folding endurance in vitro release and permeation studies. Films exhibited controlled release over more than 10 h in permeation studies. It was concluded that the films containing 20 mg of enalapril maleate in sodium carboxymethylcellulose 2% w/v and hydroxyethyl cellulose 2% w/v (formulation F5), showed good swelling, a convenient residence time and promising controlled drug release, thus can be selected for the development of buccal film for effective therapeutic uses.