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Compound pharmaceutical composition for improving oral bioavailability of paclitaxel and application thereof

A technology of paclitaxel and a composition, which is applied in the field of compound pharmaceutical compositions for improving oral bioavailability of paclitaxel, can solve the problems such as unseen and cytotoxicity of human bone marrow cells, and achieves the technology of improving antitumor activity and improving oral bioavailability. Effect

Inactive Publication Date: 2012-08-01
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 pharmaceutical composition for improving oral bioavailability of paclitaxel and application thereof
  • Compound pharmaceutical composition for improving oral bioavailability of paclitaxel and application thereof
  • Compound pharmaceutical composition for improving oral bioavailability of paclitaxel and application thereof

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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PUM

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Abstract

This application is a provisional application of Ser. No. 201110004638.9, entitled Compound Pharmaceutical Composition for Improving Oral Bioavailability of Paclitaxel and Application thereof, filed on Jan. 11, 2011. The invention discloses a compound pharmaceutical composition for improving oral bioavailability of paclitaxel and application thereof. The invention also discloses a pharmaceutical composition containing the compound pharmaceutical composition and a monomeric compound of paclitaxel. The compound pharmaceutical composition provided in the invention can be used for improving oral bioavailability of paclitaxel and for preparing anti-cancer drugs and can enhance the anti-cancer effect of paclitaxel. In the compound pharmaceutical composition provided in the invention, paclitaxel is used as an anti-cancer main component, and the monomeric compound extracted from a traditional Chinese medicine improves oral bioavailability and the anti-cancer effect of paclitaxel by inhibiting the first pass effect of paclitaxel. According to experiments and research, the compound pharmaceutical composition, prepared into an oral drug, can enhance plasma concentration and the antineoplastic effect of paclitaxel.

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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IPC IPC(8): A61K31/357A61K31/337A61P35/00
Inventor 蔡大可黄民金晶毕惠嫦古练权
Owner SUN YAT SEN UNIV
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