Poka Madan Sai, Milne Marnus, Wessels Anita, Aucamp Marique
Department of Pharmaceutical Sciences, School of Pharmacy, Sefako Makgatho Health Sciences University, Molotlegi Street, Pretoria 0208, South Africa.
Centre of Excellence for Pharmaceutical Sciences (Pharmacen), North-West University, Hoffman Street, Potchefstroom 2520, South Africa.
Pharmaceutics. 2023 Oct 30;15(11):2557. doi: 10.3390/pharmaceutics15112557.
Crystalline carriers such as dextrose, sucrose, galactose, mannitol, sorbitol, and isomalt have been reported to increase the solubility, and dissolution rates of poorly soluble drugs when employed as carriers in solid dispersions (SDs). However, synthetic polymers dominate the preparation of drugs: excipient SDs have been created in recent years, but these polymer-based SDs exhibit the major drawback of recrystallisation upon storage. Also, the use of high-molecular-weight polymers with increased chain lengths brings forth problems such as increased viscosity and unnecessary bulkiness in the resulting dosage form. An ideal SD carrier should be hydrophilic, non-hygroscopic, have high hydrogen-bonding propensity, have a high glass transition temperature (), and be safe to use. This review discusses sugars and polyols as suitable carriers for SDs, as they possess several ideal characteristics. Recently, the use of low-molecular-weight excipients has gained much interest in developing SDs. However, there are limited options available for safe, low molecular excipients, which opens the door again for sugars and polyols. The major points of this review focus on the successes and failures of employing sugars and polyols in the preparation of SDs in the past, recent advances, and potential future applications for the solubility enhancement of poorly water-soluble drugs.
据报道,当葡萄糖、蔗糖、半乳糖、甘露醇、山梨醇和异麦芽糖等结晶载体用作固体分散体(SDs)的载体时,可提高难溶性药物的溶解度和溶解速率。然而,合成聚合物在药物制剂中占主导地位:近年来已制备出药物-辅料固体分散体,但这些基于聚合物的固体分散体存在储存时重结晶的主要缺点。此外,使用链长增加的高分子量聚合物会带来诸如粘度增加和所得剂型不必要的体积庞大等问题。理想的固体分散体载体应具有亲水性、不吸湿性、高氢键倾向、高玻璃化转变温度()且使用安全。本文综述讨论了糖类和多元醇作为适合固体分散体的载体,因为它们具有几个理想特性。最近,低分子量辅料在固体分散体开发中的应用引起了广泛关注。然而,安全的低分子辅料选择有限,这再次为糖类和多元醇打开了大门。本文综述的重点是过去在固体分散体制备中使用糖类和多元醇的成功与失败、最新进展以及未来提高难溶性药物溶解度的潜在应用。