论文部分内容阅读
作者发现,用脂溶性基质制备的氨茶碱或其水溶性衍生物的栓剂,在治疗过程中很难达到有效的血药浓度(10～20μg/ml)。本文目的是设计一种释药迅速和完全的氨茶碱栓剂。实验测得无水氨茶碱和含有1分子结晶水的氨茶碱的溶解速度分别为1.158和1.091mg/cm~(-2)/min~(-1);无水氨茶碱于37°时在水中溶解度为11.03mg/ml~(-1)。由于脂溶性基质的氨茶碱生物利用度低,作者乃选用PEG等水溶性基质。选择PEG的原则为:①能溶解药物;②能使药物很易释放。为达到这个目的,作者测定不同分子量的PEG和可可豆脂的介电常数,得出PEG分子量愈高,介电常数愈低,分子量低介电常
The authors found that suppositories of aminophylline or its water-soluble derivatives prepared with lipid-soluble matrices are very difficult to achieve effective plasma concentrations (10-20 μg / ml) during the course of treatment. The purpose of this paper is to design a quick and complete release of aminophylline suppository. The experimental results showed that the dissolution rates of anhydrous aminophylline and aminophylline containing 1 molecule of crystal water were 1.158 and 1.091 mg / cm ~ (-2) / min ~ When in water solubility of 11.03mg / ml ~ (-1). Due to the low bioavailability of aminophylline in fat-soluble matrices, the authors chose water-soluble matrices such as PEG. Select the principle of PEG as: ① to dissolve the drug; ② make the drug is easy to release. To this end, the authors measured the dielectric constants of PEG and cocoa butter of different molecular weights, yielding the higher PEG molecular weight, the lower the dielectric constant, the lower molecular weight