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Compound medicine composition for improving oral bioavailability of paclitaxel and application of compound medicine composition

A technology of paclitaxel and its composition, which is applied in the field of compound pharmaceutical composition to improve the oral bioavailability of paclitaxel, can solve the unseen problems of cytotoxicity of human bone marrow cells, and achieve the goal of improving anti-tumor activity and oral bioavailability Effect

Inactive Publication Date: 2012-07-11
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the compatibility of traditional Chinese medicine monomers and paclitaxel to make a compound preparation (pharmaceutical composition) with a clear mechanism

Method used

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  • Compound medicine composition for improving oral bioavailability of paclitaxel and application of compound medicine composition
  • Compound medicine composition for improving oral bioavailability of paclitaxel and application of compound medicine composition
  • Compound medicine composition for improving oral bioavailability of paclitaxel and application of compound medicine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1 drug efficacy experiment

[0028] Experimental results of MDR1-MDCKⅡ cell model:

[0029] UPLC-MS / MS was used to determine the concentration of paclitaxel with a concentration of 1 μM transported to the AP surface through MDRI-MDCKII monolayer cells under the action of different concentrations of traditional Chinese medicine monomers. BL-AP Transport Apparent Permeability Coefficient P app See Table 1 for the values. The experimental results show that various traditional Chinese medicine monomers can inhibit the efflux of paclitaxel to a certain extent.

[0030] Table 1 Permeability coefficients of various traditional Chinese medicine monomers

[0031]

[0032] Effects of traditional Chinese medicine ingredients combined with oral administration of paclitaxel on tumor weight of human lung cancer A549 cell xenografts in nude mice:

[0033] After the administration, the tumor weights of each medication group were lower than those of the control gr...

Embodiment 2

[0038] The preparation of embodiment 2 capsules

[0039] Ratio of each API:

[0040] Paclitaxel 10g Glycyrrhizic Acid 10g

[0041] Preparation:

[0042] After the drug combination is mixed evenly, adopt the "gradual mixing method" to mix with 1980 grams of starch, add an appropriate amount of starch and stir, add an appropriate amount of talcum powder, mix evenly, pack into capsules to make capsules, and make 2000 capsules altogether.

Embodiment 3

[0043] Example 3 Preparation of Granules

[0044] Ratio of each API:

[0045] Paclitaxel 10g Glycyrrhizic Acid 10g

[0046] Preparation:

[0047] After the drug combination is mixed evenly, adopt the "gradual mixing method" to mix with 1980 grams of starch, add an appropriate amount of starch, stir, granulate, dry, make granules, and pack into 2000 bags.

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Abstract

This application is the divisional application of an inventive patent application with the application number of 201110004638.9, the application date of January 11th, 2011 and the name of compound medicine composition for improving oral bioavailability of paclitaxel and the application of the compound medicine composition. The invention discloses a compound medicine composition for improving oral bioavailability of paclitaxel and the application of the composition. The invention further discloses a medicine composition comprising the compound medicine composition and paclitaxel monomer compounds. The compound medicine composition provided by the invention can be used for improving the oral bioavailability of the paclitaxel; and when being used for preparing anti-cancer drugs, the compound medicine composition can improve the anti-cancer effect of the paclitaxel. In the compound medicine composition provided by the invention, the paclitaxel is the main anti-cancer ingredient; the monomer compounds are extracted by traditional Chinese medicine; the oral bioavailability and anti-cancer effect of the paclitaxel are improved by inhibiting the first pass effect of the paclitaxel. Experimental investigation shows that the compound medicine composition provided by the invention is prepared into oral medicines so as to improve blood concentration and anti-cancer effect of the paclitaxel after oral administration.

Description

technical field [0001] This application is a divisional application for an invention patent application with the application number 201110004638.9, the application date is January 11, 2011, and the title is "a compound pharmaceutical composition for improving the oral bioavailability of paclitaxel and its application". The invention relates to the field of pharmaceutical compositions, in particular to a compound pharmaceutical composition for improving the oral bioavailability of paclitaxel and its application. Background technique [0002] Paclitaxel, as a chemotherapy and anticancer drug with a special mechanism, is clinically used to treat a variety of malignant tumors, such as ovarian cancer, cervical cancer, breast cancer, laryngeal cancer, and esophageal cancer. Currently, paclitaxel preparations used clinically are injections. Due to the low solubility of paclitaxel in water, most of the injections currently used use polyoxyethylene castor oil / absolute ethanol (1:1, v...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/337A61K47/22A61P35/00
Inventor 蔡大可黄民金晶毕惠嫦古练权
Owner SUN YAT SEN UNIV
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