Garner John, Skidmore Sarah, Park Haesun, Park Kinam, Choi Stephanie, Wang Yan
Akina, Inc., 3495 Kent Avenue, Suite O-100, West Lafayette, IN 47906, USA.
Akina, Inc., 3495 Kent Avenue, Suite O-100, West Lafayette, IN 47906, USA.
Int J Pharm. 2015 Nov 10;495(1):87-92. doi: 10.1016/j.ijpharm.2015.08.063. Epub 2015 Aug 28.
Poly(lactide-co-glycolide) (PLGA) is the key component of long acting drug products responsible for providing sustained release in a controlled manner. The objective of the current study was to develop and validate an analytical protocol to determine key properties of PLGA used in commercial long-acting drug products. Procedures to isolate PLGA from commercial products have been established and the key properties of PLGA, such as polymer molecular weight, lactide:glycolide (L:G) ratio, and nature of polymer end-cap, have been determined. Identification of the polymer end-cap was confirmed by using two PLGA polymers with acid and ester end-caps. Trelstar(®) and Risperdal Consta(®) were chosen as model products. The calculated L:G ratios of PLGA used in Trelstar(®) and Risperdal(®) are 52:48 and 78:22, respectively. PLGAs from both Trelstar(®) and Risperdal Consta(®) possess ester end-caps. Since the properties of specific PLGA in clinically used formulations are not readily available, this protocol will be useful in developing PLGA-based long acting drug products.
聚（丙交酯-共-乙交酯）（PLGA）是长效药物产品的关键成分，负责以可控方式实现药物的缓释。本研究的目的是开发并验证一种分析方法，以测定用于商业长效药物产品的PLGA的关键特性。现已建立从商业产品中分离PLGA的方法，并已测定PLGA的关键特性，如聚合物分子量、丙交酯：乙交酯（L:G）比例以及聚合物端基的性质。通过使用两种具有酸端基和酯端基的PLGA聚合物，证实了聚合物端基的鉴定。选择曲普瑞林（Trelstar®）和利培酮长效注射剂（Risperdal Consta®）作为模型产品。曲普瑞林（Trelstar®）和利培酮（Risperdal®）中使用的PLGA的计算L:G比例分别为52:48和78:22。曲普瑞林（Trelstar®）和利培酮长效注射剂（Risperdal Consta®）中的PLGA均具有酯端基。由于临床使用制剂中特定PLGA的特性不易获得，该方法将有助于开发基于PLGA的长效药物产品。
