KR920007625A - Clathrate consisting of Silybinin, preparation method thereof and pharmaceutical composition containing the same - Google Patents

Abstract

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Description

Clathrate consisting of Silybinin, preparation method thereof and pharmaceutical composition containing the same

As this is a public information case, the full text was not included.

FIG. 1 shows the X-raygraphs for silybinin, β -cyclotextrin, their physical mixtures and the complexes of Example 1. FIG.

Figure 2 shows the X-ray diffractogram of the silybinin, DIMEB and the complex of Example 7.

Figure 3 shows the X-ray diffractograms of the silybinin, HP β CD and the complex of Example 8.

Claims (11)

A water-soluble clathrate consisting of cyclodextrin and silybinin selected from α- , β- , r -cyclodextrins and appropriate derivatives thereof. The complex of claim 1 wherein the molar ratio of silybinin: cyclotextrin is 1: 1 to 1: 4. The complex of claim 1 or 2, wherein said cyclodextrin is β -cyclodextrin. The complex of claim 3 wherein the molar ratio of silybinin: β -cyclodextrin is 1: 2, 1: 2.75 or 1: 4. 3. The cyclodextrin according to claim 1 or 2, wherein the cyclodextrin is Ephthakis-2,6-0-dimethyl- β -cyclodextrin, Eftagi-2,3,6-0-trimethyl- β -cyclodextrin. And a complex selected from the group consisting of 0-hydroxypropyl- β -cytodextrin. The complex according to any one of claims 1 to 5, wherein the solubility (release) in water is at least 60% as measured by the usp XI paddle method. A method for preparing the clathrate of claim 1, comprising preparing an aqueous solution of silybinin and cyclodextrin at a pH of 7 or above and adjusting the pH to 7 or less by adding an appropriate acid to the solution. The method of claim 7, wherein the silicinine is suspended in water, an appropriate base is added to dissolve the silybinin, and cyclodextrin is added thereto, the acid is lowered to below pH 7 by addition of an appropriate acid, or the complex is separated or water Suspending silybini and cyclodextrin in water, adding the appropriate base to dissolve the components, adjusting the pH to below 7 by adding the appropriate acid, and then separating the complex. A pharmaceutical composition containing at least one complex of any one of claims 1 to 6 in a therapeutically effective amount, optionally together with a pharmaceutically acceptable carrier and / or adjuvant. A pharmaceutical composition of claim 9 comprising providing a therapeutically effective amount of one or more complexes of any one of claims 1 to 6 bound in any pharmaceutically acceptable diluent and / or adjuvant. How to manufacture. A method of using at least one complex according to any one of claims 1 to 6 to prepare a pharmaceutical composition for liver treatment. ※ Note: The disclosure is based on the initial application.