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吲哚美辛缓释胶囊与普通胶囊的生物利用度比较
Camparison of bioavailability between the sustained release Indometacin capsule and a commercially available capsule in human
【摘要】 本文比较了吲哚美辛(消炎痛)缓释胶囊和一种普通胶囊在体外的溶出速率以及在人体内生物利用度。吲哚美辛血清浓度用高效液相色谱(HPLC)测定。结果表明,2种胶囊制剂的溶出速率显著不同。在8名受试者中,2种胶囊的吸收程度基本一致;但缓释胶囊的峰药浓度(Cmax)显著低于普通胶囊(P<0.01),其达峰时间(Tmax)也明显延迟(P<0.01)。给予单剂量(50mg)缓释胶囊后,在给药后h4至h12,其血清浓度显著高于普通胶囊(P<0.05)。提示该缓释剂可避免普通制剂初期的高峰药浓度,可延长给药间隔时间。
【Abstract】 The in vitro dissolution rates and the comparison of a cross-over bio-availability in 8 adult health volunteers between the sustained release indometacin capsule and a commercially available capsule were examined. The serum samples were assayed for indometacin by HPLC. The in vitro dissolution behaviour of the two capsule formulations exhibited a significant difference. The in vivo bioavaila-bility of different capsule formulations, although their absorped degree(AUC ,14 h) were almost the same, Cmax and Tmax of the sustained release capsule were significantly lower and latter than that of the commercially available capsule (P< 0.01).The sustained release capsule demonstrated a higher and smooth concentration-time curves than that of the commercially available capsule from 4-12 k following a single dose(50 mg) of indorriete.cin, and their serum level were significantly higher than that of the latter(P<0.05).The results suggest that the sustained release indometacin capsule can avoid high initial peak of the commercially available capsule arid increase the interval between dosage.
【Key words】 indometacin; biological availability; high pressure liquid chromato-graphy;
- 【文献出处】 新药与临床 , 编辑部邮箱 ,1990年02期
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