首页> 外文期刊>Journal of Drug Delivery and Therapeutics >FORMULATION AND EVALUATION OF MUCOADHESIVE CLOTRIMAZOLE VAGINAL TABLET USING LIQUISOLID TECHNOLOGY
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FORMULATION AND EVALUATION OF MUCOADHESIVE CLOTRIMAZOLE VAGINAL TABLET USING LIQUISOLID TECHNOLOGY

机译:液体固溶技术制备粘胶性克霉唑唑阴道片剂的研制与评价

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Liquisolid technology is very effective technique for improving the solubility and dissolution properties of poorly water soluble drug formulations like Clotrimazole. Clotrimazole is a BCS Class II, antifungal drug used for treatment for Vaginal Candidiasis. In this liquisolid technique the drug soluble in non volatile solvents and then it converted into free flowing, non adherent powder, which can be compressed into tablet. Here N-methyle-2-pyrrolidone and propylene glycol is used in the ratio of 1:1 as a solvent. Neusilin US2 and Aerosil 200 used as Coating and Carrier material respectively. For mucoadhesion on vaginal wall Sodium carboxymethyle cellulose used as a mucoadhesive agent. Mucoadhesive tablets were prepared using direct compression technique. Magnesium Stearate used as a glidant. Mucoadhesive liquisolid tablets were evaluated as precompression evalutions and post compression evaluations. Future tablets were evaluated as In vitro and Ex vivo evaluations. The optimized batch showed that In vitro release in simulated vaginal fluid pH 4.5 in 6 hr was 99%. Ex vivo diffusion studies of optimized batch showed 80% of drug diffusion in 6 hr. Mucoadhesive strength showed high mucoadhesion of optimized batch that is 36 gm. From this study it was concluded that liquisolid technology is an effective technique to improve solubility and dissolution properties of poorly water soluble drug formulations like Clotrimazole.
机译:Liquisolid技术是一种非常有效的技术,可改善水溶性差的药物制剂(如克霉唑)的溶解度和溶出度。克霉唑是一种BCS II类抗真菌药,用于治疗念珠菌性阴道病。在这种液体固体技术中,药物可溶于非挥发性溶剂中,然后转化为自由流动的非粘附性粉末,可将其压制成片剂。在此,N-甲基-2-吡咯烷酮和丙二醇以1:1的比例用作溶剂。 Neusilin US2和Aerosil 200分别用作涂层和载体材料。用于阴道壁粘膜粘附羧甲基纤维素钠用作粘膜粘附剂。使用直接压片技术制备粘膜粘附片剂。硬脂酸镁用作助流剂。将粘膜粘着性液体固体片剂评估为压缩前评估和压缩后评估。将来的片剂被评估为体外和离体评估。优化的批次显示,在模拟阴道液pH 4.5中,在6小时内的体外释放率为99%。优化批次的离体扩散研究显示6小时内80%的药物扩散。粘膜粘附强度显示最佳批次的粘膜粘附力为36 gm。从这项研究得出的结论是,液固技术是一种提高水溶性差的药物制剂(如克霉唑)的溶解性和溶解性的有效技术。

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