Karnachi A A, Reddy I K, Degennaro M D, Khan M A
Division of Pharmaceutics, School of Pharmacy, Northeast Louisiana University, Monroe.
J Drug Target. 1997;4(5):297-301. doi: 10.3109/10611869708995845.
The ulcerogenic activity of indomethacin was studied in rats following single and chronic doses of indomethacin in the form of pure drug, solid dispersions and coprecipitates. Each formulation was administrated as a suspension in a 2% methylcellulose solution. Gastrointestinal ulceration was assessed, four hours after a single dose and 24 hours following the last dose of a chronic four day dosing regimen, by counting the number of lesions and ulcers present. A rating scale was employed to evaluate the severity index. The coprecipitate formulation produced less severe ulceration than the solid dispersion and pure drug. This suggests that the severity of ulceration than the solid dispersion and pure drug. This suggests that the severity of ulceration may be related to the preparation methodology and drug release kinetics.
以纯药物、固体分散体和共沉淀物的形式,对大鼠单次和长期给予吲哚美辛后,研究了其致溃疡活性。每种制剂均以2%甲基纤维素溶液中的悬浮液形式给药。在单次给药后4小时以及慢性4天给药方案的最后一剂后24小时,通过计数出现的损伤和溃疡数量来评估胃肠道溃疡情况。采用评分量表来评估严重程度指数。共沉淀物制剂产生的溃疡比固体分散体和纯药物轻。这表明溃疡的严重程度可能与制备方法和药物释放动力学有关。 这表明溃疡的严重程度比固体分散体和纯药物轻。这表明溃疡的严重程度可能与制备方法和药物释放动力学有关。 (注:原文中“This suggests that the severity of ulceration than the solid dispersion and pure drug.”表述重复且有误,翻译时尽量按正确理解翻译,但保留了原文的重复问题。)