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Pharmaceutical composition of paclitaxel

A composition, paclitaxel technology, applied in the field of medicine, can solve problems such as increased substance content, increased degradation products of the main drug, and impact on product quality

Active Publication Date: 2015-09-23
吴静
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Paclitaxel will be degraded to varying degrees under conditions of light, alkali, acid, and high temperature, especially in high alkalinity and high heat, which will increase the content of related substances. Therefore, terminal sterilization after the injection preparation and filling is completed The process (generally using 115°C for 30 minutes) may affect the product quality, increase the degradation products (related substances) of the main drug, and bring the risk of clinical use

Method used

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  • Pharmaceutical composition of paclitaxel
  • Pharmaceutical composition of paclitaxel
  • Pharmaceutical composition of paclitaxel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] Paclitaxel 30g, polyoxyethylene castor oil 2650g, adipic acid 32.1g, disodium hydrogen phosphate 42.9g, ethanol 3950g.

[0092] The above paclitaxel content was 100.04%, the paclitaxel content was 0.09%, the 7-epi-10-deacetyl paclitaxel content was 0.04%, the 7-epi-paclitaxel content was not detected, and the total impurity content was 0.15%. Relative density of ethanol: equivalent to containing C 2 h 6 O is 99.5% (g / g).

[0093] Preparation method: Take ethanol, add acid, add polyoxyethylated castor oil, stir evenly, pass through a 0.45 μm filter element, add paclitaxel, dissolve completely, filter with a 0.22 μm filter element, fill with nitrogen and seal at a temperature above 300 ° C, In ampoules sterilized for more than 10 minutes. Sterilize at 115°C for 30 minutes to obtain 1000 tubes.

Embodiment 2

[0095] Paclitaxel 3g, polyoxyethylene castor oil 265g, adipic acid 2.50g, disodium hydrogen phosphate 5.00g, ethanol 395g.

[0096] The paclitaxel content was 100.04%, the paclitaxel content was 0.09%, the 7-epi-10-deacetyl paclitaxel content was 0.04%, the 7-epi-paclitaxel content was not detected, and the total impurity content was 0.15%. Relative density of ethanol: equivalent to containing C 2 h 6 O is 99.5% (g / g).

[0097] Preparation method: Take ethanol, add acid, add polyoxyethylated castor oil, stir evenly, pass through a 0.45 μm filter element, add paclitaxel, dissolve completely, filter with a 0.22 μm filter element, fill with nitrogen and seal at a temperature above 300 ° C, In ampoules sterilized for more than 10 minutes. Sterilize at 115°C for 30 minutes to obtain 1000 tubes.

Embodiment 3

[0099] Paclitaxel 3g, polyoxyethylene castor oil 265g, adipic acid 2.81g, disodium hydrogen phosphate 4.69g, ethanol 395g.

[0100] The paclitaxel content was 100.04%, the paclitaxel content was 0.09%, the 7-epi-10-deacetyl paclitaxel content was 0.04%, the 7-epi-paclitaxel content was not detected, and the total impurity content was 0.15%. Relative density of ethanol: equivalent to containing C 2 h 6 O is 99.5% (g / g).

[0101]Preparation method: Take ethanol, add acid, add polyoxyethylated castor oil, stir evenly, pass through a 0.45 μm filter element, add paclitaxel, dissolve completely, filter with a 0.22 μm filter element, fill with nitrogen and seal in a warp above 300 ° C, In ampoules sterilized for more than 10 minutes. Sterilize at 115°C for 30 minutes to obtain 1000 tubes.

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Abstract

The invention belongs to the technical field of medicines, discloses a pharmaceutical composition of paclitaxel, and particularly relates to a pharmaceutical composition of paclitaxel, polyoxyethylated castor oil, sodium dihydrogen phosphate, hexanedioic acid and ethanol. The pharmaceutical composition disclosed by the invention is prepared into an injection; the single impurity and total impurities accord with the quality requirements by virtue of a high-temperature and highlight test. The preparation prepared from the pharmaceutical composition disclosed by the invention has the advantages of high stability and low impurity content.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition containing paclitaxel as an active ingredient. Background technique [0002] Paclitaxel, English name: Paclitaxel, alias Taxol, [0003] [0004] Chemical name 5β,20-epoxy-1,2α,4,7β,10β,13α-hexahydroxytaxane-11-en-9-one-4,10-diacetate-2-benzoate -13[(2'R,3'S)-N-benzoyl-3-phenylisoserine ester], molecular weight 853.92, molecular formula C 47 h 51 NO 14 . [0005] Microtubules, a constituent of eukaryotic cells, are formed by dimers of microtubules composed of two similar polypeptide (a and p) subunits. Under normal conditions, there is a dynamic equilibrium between microtubules and tubulin dimers. Paclitaxel can lose this dynamic balance between the two, induce and promote tubulin polymerization, prevent depolymerization, and stabilize microtubules. These effects lead to the failure of cells to form spindles and spindle fibers d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/337A61K9/08A61K47/02A61K47/12A61K47/10A61P35/00
Inventor 吴静
Owner 吴静