Takada S, Uda Y, Toguchi H, Ogawa Y
DDS Research Laboratories, Takeda Chemical Industries, Limited, Osaka, Japan.
PDA J Pharm Sci Technol. 1995 Jul-Aug;49(4):180-4.
Copoly (dl-lactic/glycolic acid) microparticles for sustained release of a water-soluble drug (Thyrotropin releasing hormone: TRH) were prepared by a spray drying method. A higher entrapment ratio was achieved with the spray drying method with the in-water drying method. In order to avoid agglomeration of the microparticles, a double-nozzle spray drying method was designed using mannitol as an anti-adherent. The surface of the spray-dried microparticles was coated with mannitol, and the extent of agglomeration was decreased. Acetonitrile was the most suitable solvent for microencapsulation using the double-nozzle spray drying method because the initial burst of TRH from the microparticles during the first day was the smallest. When PLGA with a weight-average molecular weight of 14,000 was used, constant release of TRH continued for one month with a small initial burst. In conclusion, the production of biodegradable microparticles by the double-nozzle spray drying method appears to be an attractive alternative to conventional microencapsulation methods.
采用喷雾干燥法制备了用于持续释放水溶性药物(促甲状腺激素释放激素:TRH)的聚(dl-乳酸/乙醇酸)微粒。与水中干燥法相比,喷雾干燥法实现了更高的包封率。为避免微粒团聚,设计了以甘露醇为抗粘剂的双喷嘴喷雾干燥法。喷雾干燥微粒的表面用甘露醇包衣,团聚程度降低。乙腈是使用双喷嘴喷雾干燥法进行微囊化最合适的溶剂,因为第一天微粒中TRH的初始突释最小。当使用重均分子量为14,000的聚乳酸-羟基乙酸共聚物(PLGA)时,TRH持续恒速释放一个月,初始突释较小。总之,双喷嘴喷雾干燥法生产可生物降解微粒似乎是传统微囊化方法的一个有吸引力的替代方法。