Enhanced Efficacy of Carvedilol by Utilization of Solid Dispersion and Other Novel Strategies: A Review.

Lakshita Rao, Bigul Yogeshver Bhardwaj, Mahek Chugh, Ashish Sharma, Rashmi Shah, Neha Minocha, Parijat Pandey
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Abstract

Carvedilol is classified as a second class drug of Biopharmaceutical classification system (BCS), and it is an excellent beta blocker and vasodilating agent. It is used in a diverse range of disease states. Despite having tremendous advantages, the drug cannot be used effectively and productively due to aquaphobicity and poor bioavailability. To overcome this limitation, numerous novel approaches and tactics have been introduced over the past few years, such as Selfmicro emulsifying drug delivery systems (SMEDDS), nanoparticles, solid dispersions and liposomal drug delivery. The present review aims to accentuate the role of solid dispersion in improving the dissolution profile and aqua solubility of carvedilol and also to emphasize other novel formulations of carvedilol proposed to prevail the limitations of carvedilol. Solid dispersion and other novel approaches were found to play a significant role in overcoming the drawbacks of carvedilol, among which solid dispersion is the most feasible and effective approach being used worldwide. Reduced particle size, more wettability, and large surface area are obtained by the implementation of solid dispersion technique, hence improving carvedilol solubility and bioavailability.

利用固体分散体和其他新策略增强卡维地洛的疗效综述。
卡维地洛被生物制药分类系统(BCS)列为第二类药物,是一种优良的受体阻滞剂和血管舒张剂。它用于多种疾病状态。尽管具有巨大的优势,但由于疏水性和生物利用度差,药物不能有效地利用和生产。为了克服这一限制,在过去的几年中,已经引入了许多新的方法和策略,例如自微乳化药物递送系统(SMEDDS)、纳米颗粒、固体分散体和脂质体药物递送。本文着重介绍了固体分散体在改善卡维地洛的溶出度和水溶性方面的作用,并介绍了卡维地洛的其他新配方,以克服卡维地洛的局限性。固体分散和其他新方法在克服卡维地洛的缺点方面发挥了重要作用,其中固体分散是目前世界范围内最可行、最有效的方法。通过固体分散技术的实施,获得了更小的颗粒尺寸、更大的润湿性和更大的表面积,从而提高了卡维地洛的溶解度和生物利用度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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