替米沙坦治疗高血压用水胶体口腔溶膜的研制、优化及表征

IF 4.6 Q1 CHEMISTRY, APPLIED
Muzammil Husain , Vinit V. Agnihotri , Sameer N. Goyal , Yogeeta O. Agrawal
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引用次数: 3

摘要

替米沙坦是一种BCS II类抗高血压药物,由于首次代谢和溶解度差,口服生物利用度低,导致溶解问题。替米沙坦是快速释放给药系统的合适选择,因为它需要快速吸收以快速开始活性。本研究的目的是利用替米沙坦的水胶体结合口溶膜来创造和描述一种固体分散体。为了制作口腔溶膜,首先用捏合法制备固体分散体,然后用筛选载体的溶剂铸造法进一步配制,评估固体分散体的溶解度、药物含量和药物释放率。体外释药研究表明,固体分散体比纯药具有更好的溶解度和更快的释药速度。对制备的膜进行物理外观、表面PH、厚度均匀性、崩解时间、药物含量均匀性、折叠耐久性和体外药物释放等理化和力学参数的评价。采用32个水平的析因设计来改进该方法。考察了成膜聚合物(水胶体)组成和超崩解对成膜聚合物(水胶体)体外释放行为的影响。优化批的体外释药时间为91.83%,崩解时间为29秒。这些积极的结论表明,用HPMC E15作为成膜聚合物和乙醇酸淀粉钠作为超级崩解剂可以配制替米沙坦口腔溶膜,以提高生物利用度和治疗效果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development, optimization and characterization of hydrocolloid based mouth dissolving film of Telmisartan for the treatment of hypertension

Telmisartan, a BCS class II antihypertensive, has low oral bioavailability due to first-pass metabolism and a poor solubility profile, causing dissolving problems. Telmisartan is a suitable choice for the Rapid Release Drug Delivery System since it needs rapid absorption for a quick beginning of the activity. The goal of this research was to create and describe a solid dispersion employing hydrocolloid incorporated mouth dissolving film of Telmisartan. To make a Mouth Dissolving Film, first, prepare a solid dispersion using the Kneading Method, then use the Solvent Casting Metrpose of screening Carrier for the further formulation, solid dispersion is assessed for solubility, drug content, and drug release rate. The in-vitro drug release investigation revealed that solid dispersion had better solubility and rapid drug release than pure drug. Physical appearance, surface PH, thickness uniformity, disintegration duration, drug content uniformity, folding durability, and in-vitro drug release were among the physicochemical and mechanical parameters assessed on the produced films. A 32-level factorial design was used to improve the approach. The effects of film appearance, disintegrating time, and in-vitro drug release behavior on the composition of Film-forming polymer(hydrocolloids) and Super disintegration were investigated. The in-vitro drug release and disintegration time of the optimized batch were found to be 91.83 percent and 29 sec, respectively. These positive conclusions demonstrated that mouth dissolving film of Telmisartan can be formulated using HPMC E15 as a film-forming polymer and Sodium Starch Glycolate as a super disintegrant for improving bioavailability and therapeutic outcome.

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CiteScore
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