Composition containing paclitaxel and preparation method thereof

A paclitaxel and composition technology, applied in the field of paclitaxel-containing composition and its preparation, can solve the problems of high drug safety risk, toxicity, and poor patient compliance, and achieve the effects of avoiding hemolytic reaction, preventing drug degradation, and improving compliance

Active Publication Date: 2014-04-23
李宏 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The paclitaxel injection in the prior art is a solution injection, specifically an injection made of absolute ethanol and polyoxyethylene castor oil at a ratio of 1:1, wherein ethanol has obvious irritation, and the auxiliary material polyoxyethylene castor oil has obvious Toxicity, clinical manifestations of severe allergic reactions, in order to avoid allergic reactions, 5-10 mg (mg) dexamethasone, 300 mg cimetidine or intramuscular injection of 50 mg diphenhydramine is often required 30 minutes before use, and Clinical monitoring is required, and the mixed solvent of ethanol and polyoxyethylene castor oil will dissolve the plasticizer in the infusion tube during the administration process. Therefore, the existing paclitaxel injection has high drug safety risks and poor patient compliance

Method used

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  • Composition containing paclitaxel and preparation method thereof
  • Composition containing paclitaxel and preparation method thereof
  • Composition containing paclitaxel and preparation method thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0068] The preparation method of colostrum is as follows: in parts by weight, 27.5 parts of glycerin, 0.025 parts of calcium sodium edetate and 6.25 parts of polyethylene glycol 400 are dissolved in water to form an aqueous phase solution; 1 part of paclitaxel is mixed with a little anhydrous Ethanol wetting and 250 parts of medium chain oil, 15 parts of egg yolk lecithin, 0.375 parts of VE, 0.75 parts of oleic acid mixed solution for high-speed shearing, volatilization of ethanol to form an oil phase solution; add the oil phase to the water phase under high-speed shearing at 12000rpm , forming colostrum. Four equal parts of colostrum were divided, and the pH value of the colostrum was adjusted to the pH value shown in Table 5 respectively. After 800bar high-pressure homogenization to form a homogeneous liquid, it is filled in an ampoule Instantly. The content of impurities before sterilization was determined by high performance liquid chromatography, and the results are show...

Embodiment 1～3

[0103] Examples 1-3 Preparation of Paclitaxel Fat Emulsion Injection 1-3 Test

[0104] Table 9 1000mL emulsion prescription of Examples 1-3

[0105]

[0106] The preparation method of the paclitaxel fat emulsion injection of embodiment 1 is as follows:

[0107] Take the glycerin, EDTA-CaNa2 and PEG400 in the amount shown in Table 9 and dissolve them in water at 60°C to form an aqueous phase; take the paclitaxel in the amount shown in Table 9 and wet it with absolute ethanol and mix with medium chain oil, egg yolk lecithin PL100, VE (Vitamin E) and oleic acid are mixed, dissolved in a 60°C water bath at 12000r / min high-speed shear, volatilizes ethanol to form an oil phase; in a 60°C water bath, add the oil phase to water under a 12000r / min high-speed shear Phase, cut for 10 minutes to form colostrum, adjust the pH value of the colostrum to 5.5; homogenize the adjusted pH value of the colostrum 8 times under 800bar high pressure to form a paclitaxel homogeneous solution, adj...

Embodiment 4～6

[0112] Examples 4-6 Preparation of Paclitaxel Fat Emulsion Injection 4-6 Test

[0113] Table 10 1000mL emulsion prescription of Examples 4-6

[0114]

[0115] The preparation method of the paclitaxel fat emulsion injection in Example 4 was consistent with Example 1 except that the dosage was shown in Table 10, to obtain Injection 4;

[0116] The preparation method of the paclitaxel fat emulsion injection of embodiment 5 adopts the dosage shown in Table 10 except that the dosage is the same as that of embodiment 2, and the injection 5 is obtained;

[0117] The preparation method of the paclitaxel fat emulsion injection in Example 6 was the same as in Example 3, except that the dosage was used as shown in Table 10, and the injection 6 was obtained.

[0118] Table 12 shows the quality inspection results of injections 1-6 sterilized by F0>12.

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Abstract

The invention relates to the technical field of antitumor drugs, and discloses a composition containing paclitaxel and a preparation method thereof. The composition containing paclitaxel comprises 1 part by weight of paclitaxel and 1.2-15 parts by weight of egg yolk lecithin; the pH value range of the composition is 4.0-6.0. According to the composition containing paclitaxel of the invention, egg yolk lecithin is adopted as an emulsifier; the pH value of the composition is adjusted to be within a proper range; no polyoxyethylated castor oil with large toxicity is adopted; no ethanol is contained; the medication risk of the composition containing paclitaxel is reduced; and the patient compliance is improved.

Description

technical field [0001] The invention relates to the technical field of antitumor drugs, in particular to a paclitaxel-containing composition and a preparation method thereof. Background technique [0002] Paclitaxel is a natural anticancer drug developed by Bristol-Myers Squibb at the end of the 20th century. It is a cytostatic drug with a unique mechanism of action and is effective for many drug-resistant patients. Inhibit the depolymerization of microtubules, stabilize the microtubules, lead to abnormal arrangement of microtubules, cause the pituitary gland to lose its normal function and lead to cell death, and have outstanding curative effects on breast cancer and ovarian cancer. Neck cancer and prostate cancer also have some effect. [0003] The paclitaxel injection in the prior art is a solution injection, specifically an injection made of absolute ethanol and polyoxyethylene castor oil at a ratio of 1:1, wherein ethanol has obvious irritation, and the auxiliary mater...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/24A61K9/107A61K9/19A61K31/337A61P35/00
Inventor 刘新红李宏岳昌林晏敏红
Owner 李宏
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