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Solid-state molecular dispersible preparation of pennogenin compound

A technology of pinanoside and molecular dispersion, which is applied in the field of special preparations, can solve the problems of low bioavailability, and achieve the effects of overcoming slow dissolution, improving bioavailability, and easy absorption

Inactive Publication Date: 2006-12-27
YUNNAN BAIYAO GROUP
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  • Description
  • Claims
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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.

Method used

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  • Solid-state molecular dispersible preparation of pennogenin compound
  • Solid-state molecular dispersible preparation of pennogenin compound

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Experimental program
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Embodiment Construction

[0046] result:

[0047] (1), in the above examples, the dissolution rate and bioavailability of pinanosides were obviously improved. The preparation with cyclodextrin as the main auxiliary material has excellent stability and is not easy to age.

[0048] (2) Water-soluble polymers such as PVP and PEG obviously improve the dissolution rate of the pinanoside compound-cyclodextrin complex, and obviously increase the bioavailability of the pinanoside compound.

[0049] (3) The hydroxy acid can obviously improve the dissolution rate of the pinanoside compound-cyclodextrin complex, and obviously improve the bioavailability of the pinanoside compound.

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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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K9/00A61P15/00A61P7/04A61P7/06
Inventor 唐书明
Owner YUNNAN BAIYAO GROUP
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