摘要
本文用差示扫描量热法(DSC)筛选确定双炔失碳酯与PVP按1:7～1:9比例以溶剂法制得共沉淀物,其中已不存在双炔失碳酯晶体。用X射线衍射法研究了1:8共沉淀物,证明无双炔失碳酯的晶体衍射峰。经溶出速率测定结果20 min的药物溶出度1:8共沉淀物比原药约大38倍。用导数热重法(DTG)求得1:8共沉淀物与双炔失碳酯的热解动力学参数,其活化能分别为182.8和133.4 kJ/mol,1:8共沉淀物的热解稳定性明显大于原药。小鼠抗着床试验结果表明空白对照组着床数为4.8,53抗孕片(剂量10.6 mg/kg)组为0.9(P<0.05),1:8共沉淀物(剂量5 mg/kg)组为0.2(P<0.01),即1:8共沉淀物抗着床的有效剂量小于53抗孕片的一半。
The copreeipitate of anordrin (AD)—PVP was prepared by solvent method. The DSC (differential scanning calorimetry) revealed that AD did not have crystalline structure in copreeipitates of 1:7～1:9. X-ray diffraction spectrum of 1:8 coprecipitate (COPPT) showed no crystalline structure of AD. The dissolution rate of AD was about 38 times higher for 1:8 COPPT than pure AD. Activation energies determined by DTG (derivative thermogravimetry) were 182.8 and 133.4 kJ/mol, respectively, showing that the 1:8 COPPT is much more ’ stable than pure AD in thermal degradation. The experimental results showed that antiimplantation effect of the 1:8 COPPT was much better than that of AD tablets: the number of implantation sites of mice administrated 1:8 COPPT (Smg/kg) was 0.2 (P<0.01) and that of mice administrated AD tablets (10.6 mg/kg) was 0.9 (P<0.05); effective dose of 1:8 COPPT was less than half of that of AD tablets.
出处
《药学学报》
CAS
CSCD
北大核心
1989年第3期219-224,共6页
Acta Pharmaceutica Sinica
关键词
双炔失碳酯
共沉淀物
差示扫描量热分析
抗着床
避孕药
Anordrin
Coprecipitate
Differential scanning calorimetry
Antiimplantation
Contraceptive agents
