Solid-state molecule disperse preparations of pennogenin series compounds

Abstract

The invention relates to a special preparation form which takes the compounds of pennogenyl saponins as active ingredients. The solid-state molecule dispersion preparation of the compounds of pennogenyl saponins consists of the ingredients with the following weight percentage ratio: 0.5 to 40 percent compounds of pennogenyl saponins, 60 to 99 percent cyclodextrin and 0.1 to 10 percent hydroxy acid. Generally, as the volume of the molecular space of the compound with the molecular weight more than 1000 is too big, the compound is not easy to be embedded by cyclodextrin, the invention has the advantage that the compounds of pennogenyl saponins are embedded in cyclodextrin in a dispersion state of single molecule, the dispersion degree is smaller than nanoparticle by more than 10 times, whenthe invention enters the gastrointestinal tract, the invention is easy to be absorbed by the human body, and the bioavailability can be improved by more than 2 times. The second advantage is that theinvention overcomes the shortcoming of slow dissolution caused by easy aging of the PEG solid dispersion. The preparation of the invention is mainly used in the treatment of gynecological blood syndromes, including hemostasis, blood formation and gynecological inflammation.

Description

[0001] This application is a divisional application of 200510010873.1, the filing date of the original application is June 24, 2005, the application number is 200510010873.1, and the name of the invention is: pinanoside compound solid molecular dispersion preparation. technical field [0002] The invention relates to a special preparation form with pinanoside compounds as active components. Background technique [0003] 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. [0004] 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 ...

AI Technical Summary

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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