Solid-state molecular dispersible preparation of pennogenin compound

Abstract

The present invention relates to a special preparation form using pennogenin composite as an active constituent. Said pennogenin composite solid molecule dispersing preparation is formed by the mass percent of 0.5 to 40% pennogenin composite and 60 to 99.5% cyclodextrin. Composites with molecular weight over 1000 are generally supposed to be hard buried by cyclodextrin due to their big molecular space volume. The present invention is characterized in burying the pennogenin composite in cyclodextrin in a dispersing state in single molecule with the dispersing degree over ten times smaller than that of nanometer grains, which is quickly disintegrated and dispersed and absorbed by human body after entering into gastrointestinal tract, which as a result, improves the biological utility ratio by over two times. And the invention is also characterized in overcoming the shortcoming of PEG solid dispersant easily aging which results in slow dissolving-out speed. The present preparation is mainly used to cure gynecological blood diseases including hemostasis, hematopoiesis and gynecological inflammation.

Description

technical field [0001] The invention relates to a special preparation form with pinanoside compounds as active components. Background technique [0002] Pinanoside is not very widely distributed in the plant kingdom, and its content is low. Chinese Patent Application No. 02150907.7 discloses a "17-hydroxy C#-[27] steroid compound, its synthesis method and its use", which can be used for the synthesis of pinatogenin or dihydro pinanogenin. [0003] At present, there have been literatures publicly reporting the application of pinanosides in pharmaceuticals. However, pharmacokinetic studies have shown that the bioavailability of pinanoside compounds is extremely low, and more than 90% of them are excreted from the feces in the original form. Only a small amount of the original drug and no metabolites were detected in blood, bile and urine samples. Contents of the invention [0004] The object of the present invention is to provide a solid molecular dispersion preparation of...

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Problems solved by technology

However, pharmacokinetic studies have shown that the bioavailability of pinanosides is extremely low, and more than 90% are excreted from the feces in the original form. Only a small amount of the original drug was detected in the blood, bile and urine samples, and no metabolites were detected.

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