Rothen-Weinhold A, Besseghir K, De Zelicourt Y, Gurny R
University of Geneva, School of Pharmacy, Geneva, Switzerland.
J Control Release. 1998 Mar 2;52(1-2):205-13. doi: 10.1016/s0168-3659(97)00216-2.
In recent years peptides and proteins have received much attention as candidate drugs. For many peptides, particularly hormones, it is desirable to release the drug continuously at a controlled rate over a period of weeks or even months. Polylactic acid and poly (lactic-co-glycolic) acid are well known biocompatible biodegradable materials with wide applications including the design of controlled-release systems for pharmaceutical agents. Polylactic acid implants containing vapreotide were prepared by an extrusion method and drug release was evaluated in vivo in rats using an RIA method The development of an injectable, biodegradable depot formulation of a somatostatin analogue (vapreotide) is described which ensures satisfactory peptide blood level in rats over approximately 250 days. A modification of this formulation by means of a wear coating allows minimisation of the initial burst a feature rarely discussed.
近年来，肽和蛋白质作为候选药物受到了广泛关注。对于许多肽，尤其是激素而言，期望在数周甚至数月的时间内以可控的速率持续释放药物。聚乳酸和聚（乳酸-共-乙醇酸）是众所周知的具有生物相容性的可生物降解材料，其应用广泛，包括药物控释系统的设计。采用挤出法制备了含伐普肽的聚乳酸植入物，并通过放射免疫分析法在大鼠体内评估了药物释放情况。本文描述了一种生长抑素类似物（伐普肽）的可注射、可生物降解长效注射剂的研发过程，该制剂可确保大鼠体内肽的血药浓度在约250天内保持在令人满意的水平。通过磨损涂层对该制剂进行改良，可将初始突释降至最低，这一特性鲜少被讨论。
