Fu J C, Moyer D L, Hagemeier C
J Biomed Mater Res. 1978 May;12(3):249-54. doi: 10.1002/jbm.820120302.
The daily in vitro release of hydrocortisone from composite polymer capsules is reported here for over 120 days. Increase in vinyl acetate comonomer content of the ethylene-vinyl acetate copolymer matrix brought about an increase in the diffusion rate. Variation in the initial drug content of the capsules from 40 mg to 20 mg affects the daily drug release less significantly than the variation in copolymer ratio. The correlation between vinyl acetate comonomer content and the percent crystallinity of the copolymer matrix is suggested as one of the possible major factors in controlling diffusion rate from this drug-polymer system. The diffusion constant (D) calculated was 0.212 X 10(10) cm2/sec when the copolymer carrier has 30% vinyl acetate content and 0.430 X 10(11) cm2/sec when the copolymer carrier has 20% vinyl acetate content for capsules with 20 mg initial drug content, and 0.118 X 10(-11) cm2/sec and 0.226 X 10(-11) cm2/sec, respectively, for capsules with 40 mg initial drug content.
本文报道了复合聚合物胶囊中氢化可的松超过120天的每日体外释放情况。乙烯-醋酸乙烯酯共聚物基质中醋酸乙烯酯共聚单体含量的增加导致扩散速率提高。胶囊初始药物含量从40毫克变化到20毫克,对每日药物释放的影响不如共聚物比例变化显著。醋酸乙烯酯共聚单体含量与共聚物基质结晶度百分比之间的相关性被认为是控制该药物-聚合物体系扩散速率的可能主要因素之一。对于初始药物含量为20毫克的胶囊,当共聚物载体醋酸乙烯酯含量为30%时,计算得到的扩散常数(D)为0.212×10⁻¹⁰平方厘米/秒;当共聚物载体醋酸乙烯酯含量为20%时,扩散常数为0.430×10⁻¹¹平方厘米/秒。对于初始药物含量为40毫克的胶囊,扩散常数分别为0.118×10⁻¹¹平方厘米/秒和0.226×10⁻¹¹平方厘米/秒。