Kalepu Sandeep, Nekkanti Vijaykumar
Department of Pharmaceutical Technology, Shri Vishnu College of Pharmacy, Bhimavaram 534202, Andhra Pradesh, India.
College of Pharmaceutical Sciences, Western University of Health Sciences, Pomona, California 91766, USA.
Acta Pharm Sin B. 2015 Sep;5(5):442-53. doi: 10.1016/j.apsb.2015.07.003. Epub 2015 Aug 24.
The emerging trends in the combinatorial chemistry and drug design have led to the development of drug candidates with greater lipophilicity, high molecular weight and poor water solubility. Majority of the failures in new drug development have been attributed to poor water solubility of the drug. Issues associated with poor solubility can lead to low bioavailability resulting in suboptimal drug delivery. About 40% of drugs with market approval and nearly 90% of molecules in the discovery pipeline are poorly water-soluble. With the advent of various insoluble drug delivery technologies, the challenge to formulate poorly water soluble drugs could be achieved. Numerous drugs associated with poor solubility and low bioavailabilities have been formulated into successful drug products. Several marketed drugs were reformulated to improve efficacy, safety and patient compliance. In order to gain marketing exclusivity and patent protection for such products, revitalization of poorly soluble drugs using insoluble drug delivery technologies have been successfully adopted by many pharmaceutical companies. This review covers the recent advances in the field of insoluble drug delivery and business prospects.
组合化学和药物设计领域的新趋势导致了具有更高亲脂性、高分子量和低水溶性的候选药物的开发。新药开发中的大多数失败都归因于药物的低水溶性。与低溶解度相关的问题可能导致生物利用度低,从而导致药物递送不理想。约40%已获市场批准的药物以及发现阶段近90%的分子水溶性较差。随着各种难溶性药物递送技术的出现,配制难溶性药物的挑战有望得到解决。许多溶解度差和生物利用度低的药物已被制成成功的药品。几种上市药物进行了重新配方,以提高疗效、安全性和患者依从性。为了获得此类产品的市场独占权和专利保护,许多制药公司已成功采用难溶性药物递送技术来振兴难溶性药物。本综述涵盖了难溶性药物递送领域的最新进展和商业前景。