含有甲氨蝶呤(MTX)的牛血清白蛋白(BSA)微球 I. 制剂学部分

含有甲氨蝶呤(MTX)的牛血清白蛋白(BSA)微球 I. 制剂学部分

石庭森, 陈小平

军事医学科学院毒物药物研究所, 北京 100850;

收稿日期:1992-03-23 修回日期:1992-12-22 出版日期:1993-06-15 发布日期:1993-06-15

Bovine Serum Albumin (BSA) Microspheres Containing Methotrexate (MTX) I. Pharmaceutical Aspects

Ting-Sen Shi, Xiao-Ping Chen

Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850

Received:1992-03-23 Revised:1992-12-22 Online:1993-06-15 Published:1993-06-15

摘要/Abstract

摘要： 用乳化技术制备了三种微球体系, 分别命名为I、II、III。I是乳剂通过戊二醛交联的方法制成, II是在戊二醛交联的基础上用甘氨酸处理的产品, III是乳剂通过加热固化法而制得的微球。结果发现, 相同的乳剂经交联法制得的微球其直径比加热固化法制得的微球大。微球II和微球I有更好的亲水性。微球I和II中MTX 的含量分别为2.73±0.05%和2.87±0.12%。Ⅲ是空白微球表面吸附了MTX 结晶的一种体系。微球中MTX 的体外释放实验证实, I和II在pH 7.4的磷酸盐缓冲液中, 药物释放达24小时之久其机理属Higuchi 扩散。

关键词: 亲水性蛋白微球, 乳化技术, 甲氨蝶呤(MTX), 药物释放动力学

Abstract: Microspheres I, II and III were produced by emulsion technique.Microsphere I was solidified by glutaraldehyde crosslinking, microsphere II was solidified by glutaraldehyde crosslinking and further treated with glycine solution and microsphere Illwas solidified by heating denaturation only.The results showed that the microsphere diameter produced by cross[inking was bigger than that prepared by heating.The microsphere II had higher hydrophilicity than Microsphere I had.The methotrexate (MTX) contents in microspheres I and II were 2.73±0.053%, 2.87±0.119% respectively. microsphere III was only blank microspheres with MTX adsorbed on their surfaces.In vitro release studies, microspheres I and I have maintained sustained release of MTX till the next day, it was found that the drug releases from microspheres I and II were governed by Higuchi diffusion law.

Key words: Hydrophillic albumin microspheres, Emulsion technique, Methotrexate, Drug release kinetics

Supporting:

石庭森, 陈小平. 含有甲氨蝶呤(MTX)的牛血清白蛋白(BSA)微球 I. 制剂学部分[J]. .

Ting-Sen Shi, Xiao-Ping Chen. Bovine Serum Albumin (BSA) Microspheres Containing Methotrexate (MTX) I. Pharmaceutical Aspects[J]. .