酮康唑微海绵外用凝胶的制备及评价

Joshna Booravilli, Janaki Devi Sirisolla, Shivani Saluru
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引用次数: 1

摘要

微海绵是那些药物输送系统,其目的是以某种方式输送最小剂量的药物或药用活性成分,以增加制剂的稳定性,改变药物释放谱。酮康唑是一种咪唑类抗真菌药,属BCSⅱ类。本研究的主要目的是通过准乳状法,以不同的聚合物如苦楝子S-100、苦楝子L-100按1:2、1:3、1:4、1:5的比例制备酮康唑外用微海绵,并对其进行评价。所制备的制剂根据比率标记为es2。e3、e4、e5适用于e5 -100, e2、e3、e4、e5适用于e5 -100。通过包封效率、产率、药物含量等评价试验,结果表明:L-100 (EL - 5)和S-100 (ES - 5)配方效果较好。对es5和EL 5配方进行了优化,并进行了体外溶出度研究等试验,结果表明,es5配方释放时间长达8小时,可用于凝胶制剂。凝胶(GES5)由含有1% w/w的药物酮康唑的微海绵制备,并掺入由Carbopol 934组成的凝胶基中。微海绵经过筛分,分散在Carbopol凝胶中。评估测试,如pH测量,目视检查,扩散研究,药物含量和体外扩散研究。这种配制微海绵的方法改善了药物的递送,因此有助于提高药物的生物利用度,并且还作为通过皮肤的有效载体。
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Formulation and Evaluation of Ketoconazole Microsponge Topical Gel
Microsponges are those drug delivery systems which are intended in a way to deliver a minimum dose of the drug or pharmaceutically active ingredient to increase the stability of formulation, to alter drug release profile. Ketoconazole is an imidazole anti-fungal agent  belonging to BCS class II. The main objective of this research work is to formulate and evaluate ketoconazole microsponge for topical  delivery by using various polymers such eudragit S-100, eudragit L-100 in four ratios 1:2, 1:3, 1:4, 1:5 by quasi emulsion method. The  formulations prepared were labelled based on the ratios as ES 2. ES 3, ES 4, ES 5 for eudragit S-100 and EL 2, EL 3, EL 4, EL 5 for eudragit L-100. Evaluation tests like entrapment efficiency, production yield, drug content was performed and formulation of eudragit L-100 (EL 5) and eudragit S-100 (ES 5) showed better results. ES 5 and EL 5 formulations were optimized and tests like in vitro dissolution studies  were conducted which showed that the formulation ES 5 showed released upto 8 hours and can be used in the formulation of gel. The  gel (GES5) was prepared by usingmicrosponges containing the drug ketoconazole equivalent to 1 % w/w and was incorporated into  the gel base made up of Carbopol 934. The microsponges were sieved and were dispersed in Carbopol gel. Evaluation tests like pH  measurement, visual inspection, spreadability studies, drug content and in vitro diffusion studies. This method of formulating  microsponges has improved drug delivery therefore helping in the enhancement of the bioavailability of the drug and also acts as an efficient carrier through the skin.
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