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采用D-甘露醇的固体分散技术在改善氨苯蝶啶口服吸收方面的应用。

The application of solid dispersion technique with D-mannitol to the improvement in oral absorption of triamterene.

作者信息

Arias M J, Gines J M, Moyano J R, Rabasco A M

机构信息

Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, Spain.

出版信息

J Drug Target. 1994;2(1):45-51. doi: 10.3109/10611869409015892.

Abstract

Present paper proposes a new system to administer triamterene, a sparing potassium diuretic which presents absorption problems when administered as a free powder, due to its low solubility in water. To increase the dissolution rate and subsequent oral bioavailability of this drug, it has been formulated as solid dispersion. This method involves preparation by the melting carrier method using D-mannitol as matrix. These systems were subjected to USP XXII dissolution rate determination. The results revealed a marked dissolution rate increase of included triamterene in solid dispersions when compared with micronized drug. Further in vivo assays have demonstrated the absorption efficiency for the proposed systems when referred to pure drug. In vitro-in vivo correlation between the parameter T80% (from dissolution rate studies) and the pharmacokinetic one Ke, has found to be acceptable. All the results obtained make this system suited for further formulation in the pharmaceutical industry.

摘要

本论文提出了一种新的氨苯蝶啶给药系统。氨苯蝶啶是一种保钾利尿剂,以游离粉末形式给药时存在吸收问题,因为它在水中的溶解度较低。为了提高这种药物的溶解速率及随后的口服生物利用度,已将其制成固体分散体。该方法涉及采用D - 甘露醇作为基质通过熔融载体法制备。这些体系进行了美国药典XXII溶出速率测定。结果显示,与微粉化药物相比,固体分散体中包载的氨苯蝶啶的溶出速率显著提高。进一步的体内试验证明了所提出的体系相对于纯药物的吸收效率。已发现参数T80%(来自溶出速率研究)与药代动力学参数Ke之间的体外 - 体内相关性是可接受的。所获得的所有结果使得该体系适合在制药行业进一步制剂化。

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