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含纳米晶酮洛芬的基质微丸的体内评价

In vivo evaluation of matrix pellets containing nanocrystalline ketoprofen.

作者信息

Vergote G J, Vervaet C, Van Driessche I, Hoste S, De Smedt S, Demeester J, Jain R A, Ruddy S, Remon J P

机构信息

Laboratory of Pharmaceutical Technology, Ghent University, Harelbekestraat 72, 9000, Ghent, Belgium.

出版信息

Int J Pharm. 2002 Jun 20;240(1-2):79-84. doi: 10.1016/s0378-5173(02)00114-x.

Abstract

The aim of this study was to evaluate the in-vivo behaviour of matrix pellets formulated with nanocrystalline ketoprofen after oral administration to dogs. No significant differences in AUC-values were seen between pellet formulations containing nanocrystalline or microcrystalline ketoprofen and a commercial ketoprofen formulation (reference: Rofenid 200 Long Acting). C(max) of the formulations containing nano- or microcrystalline ketoprofen was significantly higher compared to reference, whereas t(max) was significantly lower. The in-vivo burst release observed for the spray dried nanocrystalline ketoprofen matrix pellets was reduced following compression of the pellets in combination with placebo wax/starch pellets. These matrix tablets sustained the ketoprofen plasma concentrations during 5.6 and 5.4 h for formulations containing nano- and microcrystalline ketoprofen, respectively.

摘要

本研究的目的是评估口服给予犬纳米晶酮洛芬制成的基质微丸的体内行为。含纳米晶或微晶酮洛芬的微丸制剂与市售酮洛芬制剂(对照:洛芬尼德200长效制剂)之间的AUC值未见显著差异。与对照相比,含纳米或微晶酮洛芬的制剂的C(max)显著更高,而t(max)显著更低。喷雾干燥的纳米晶酮洛芬基质微丸与安慰剂蜡/淀粉微丸压片后,体内突释现象减少。这些基质片分别使含纳米和微晶酮洛芬的制剂在5.6小时和5.4小时内维持酮洛芬血浆浓度。

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