Molokhia A M
Res Commun Chem Pathol Pharmacol. 1984 Aug;45(2):219-24.
Three brands of locally available cephalexin capsules were stored in paper bags at 40 degrees C/90% relative humidity. Samples were taken at different time intervals and tested for the effect of storage on disintegration, dissolution and drug content for up to 70 days. Bioavailability testing was carried by administering the capsules to four volunteers before storage and after 70 days of storage. Two brands (A and B) showed increase in disintegration time associated with decrease in the rate of dissolution. The third brand (C) showed similar effect but later on irregular disintegration and dissolution were observed. Such behavior was found to be a result of storage effect on the capsule shell. No effect on drug content was observed for brands A and B but significant loss of activity was observed with some samples of brand (C). Bioavailability testing based upon urine analysis for excreted drug indicated that the rate but not the extent of drug absorption for brands A and B decreased by storage. The results with brand C showed serious fluctuations in absorption after storage for more than 25 days. These findings point out to the importance of proper formulation and protection of solid dosage forms handled in places where high temperature and humidity conditions are likely to exist.
将当地可获得的三种品牌的头孢氨苄胶囊存放在纸袋中，温度为40摄氏度，相对湿度为90%。在不同时间间隔取样，测试储存长达70天对崩解、溶出和药物含量的影响。通过在储存前和储存70天后给四名志愿者服用胶囊进行生物利用度测试。两个品牌（A和B）的崩解时间增加，同时溶出速率下降。第三个品牌（C）表现出类似的效果，但后来观察到不规则的崩解和溶出。发现这种行为是储存对胶囊壳影响的结果。品牌A和B的药物含量未受影响，但品牌（C）的一些样品观察到活性显著损失。基于尿液中排泄药物分析的生物利用度测试表明，品牌A和B的药物吸收速率而非吸收程度因储存而降低。品牌C的结果显示，储存超过25天后吸收出现严重波动。这些发现指出了在可能存在高温高湿条件的地方，妥善配制和保护固体剂型的重要性。
