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比格犬口服维生素K1制剂后的生物利用度评估。

Evaluation of bioavailability upon oral administration of phytonadione preparations in beagle dogs.

作者信息

Tokumura T, Tsushima Y, Machida Y, Kayano M, Nagai T

机构信息

Tsukuba Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan.

出版信息

Biol Pharm Bull. 1993 Mar;16(3):319-21. doi: 10.1248/bpb.16.319.

Abstract

Bioavailability of phytonadione was investigated after oral administration to beagle dogs. The administrations of phytonadione in a surfactant solution (preparation a) and in an oleic acid solution (preparations b) greatly increased the bioavailability of phytonadione. The AUCs of preparations a and b were about 2.5 times larger than those of commercially available tablets A and C. This result well corresponded to the results of the dissolution test previously reported. The absorption of phytonadione from the gastro-intestinal tract was affected by food and the bioavailability was largely increased under non-fasted conditions. However, a large scatter was observed in the data, and it was found that the evaluation of the bioavailability of phytonadione preparations could not be done in non-fasted animals.

摘要

在给比格犬口服后,研究了维生素K₁的生物利用度。将维生素K₁溶于表面活性剂溶液(制剂a)和油酸溶液(制剂b)中给药,大大提高了维生素K₁的生物利用度。制剂a和b的AUC约为市售片剂A和C的2.5倍。该结果与先前报道的溶出度试验结果非常吻合。胃肠道对维生素K₁的吸收受食物影响,在非空腹条件下生物利用度大幅提高。然而,数据中观察到较大的离散度,并且发现无法在非空腹动物中评估维生素K₁制剂的生物利用度。

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