Temozolomide injectable composition and preparation method thereof

A technology for temozolomide and composition, which is applied in the field of temozolomide injectable composition and its preparation field, can solve the problems of potential safety hazards for patients, long reconstitution time and high cost

Active Publication Date: 2018-04-06
SHANGHAI ACEBRIGHT PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This solution can greatly increase the dissolution rate, but it also contains organic solvents, and there will be some organic solvent residues after the preparation is lyophilized, which is not conducive to safe administration
[0009] In summary, the prior art has the following disadvantages: 1. The composition without organic solvent has a slow dissolution rate during preparation, temozolomide is degraded more during the preparation process, and the content of related substances is relatively high, causing potential safety hazards to patients. And the preparation time is long and the cost is high
At the same time, the reconstitution time is longer, which is not conducive to clinical application
2. Although the composition containing organic solvent can improve the dissolution rate, after freeze-drying, there is a problem of organic solvent residue, which is not conducive to safe administration

Method used

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  • Temozolomide injectable composition and preparation method thereof
  • Temozolomide injectable composition and preparation method thereof
  • Temozolomide injectable composition and preparation method thereof

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preparation example Construction

[0077] The present invention also provides a preparation method of the temozolomide composition of the present invention, comprising the steps of:

[0078] 1) Dissolve other excipients except the active ingredient in water for injection, and adjust the pH to 2.5-5.0;

[0079] 2) Add the active ingredient, stir to dissolve, and constant volume;

[0080] 3) filter;

[0081] 4) Packing;

[0082] 5) freeze-drying.

[0083] Preferably, the preparation method comprises the following steps:

[0084] 1) Dissolve glycine, sodium sulfobutylbeta cyclodextrin, nonionic surfactant, buffer, and lyoprotectant in water for injection, add a pH regulator to adjust the pH to 3.5-4.5, and control the temperature of the solution 30°C or below (such as 5-29°C or 15-29°C);

[0085] 2) adding temozolomide or a pharmaceutically acceptable salt thereof, stirring to dissolve, and constant volume;

[0086] 3) sterile filtration;

[0087] 4) sub-package injection bottles;

[0088] 5) freeze-drying...

Embodiment 1

[0104] Dissolve 12.0 g of glycine, 4.0 g of sodium sulfobutylbeta cyclodextrin, 12.0 g of Tween 80, 20.0 g of sodium citrate, and 60.0 g of mannitol in 3.2 L of water for injection, and add about 13.0 g of hydrochloric acid to adjust the pH to 3.8. Control the solution temperature to 20°C. Add 10.0 g of temozolomide, stir to dissolve, dilute to 4 L, filter aseptically, divide 40 ml / bottle into injection vials, lyophilize, stopper, and seal.

Embodiment 2

[0106] Dissolve 15.0g glycine, 1.0g sodium sulfobutylbeta cyclodextrin, 15.0g polyethylene glycol hydroxystearate, 10.0g sodium citrate, and 120.0g mannitol in 3.2L water for injection, and add about 6.0 g of hydrochloric acid was used to adjust the pH to 4.0. Control the solution temperature to 25°C. Add 10.0 g of temozolomide, stir to dissolve, dilute to 4 L, filter aseptically, divide 40 ml / bottle into injection vials, lyophilize, stopper, and seal.

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Abstract

The invention relates to a temozolomide injectable composition and a preparation method thereof. Concretely, the invention discloses a temozolomide composition and a preparation method thereof. The composition is an injectable composition. Glycine and sulfobutylether-beta-cyclodextrin are used as solubilizing agents; organic dissolvants are not added. The temozolomide injectable composition has various advantages of obviously improving the dissolution speed, reducing the solution state existing time of temozolomide during the industrial production, reducing the relevant substance level and thelike.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a temozolomide injectable composition and a preparation method thereof. Background technique [0002] Glioma originating from the ectoderm is the most common primary tumor of the nervous system, accounting for more than 50% of primary intracranial tumors. According to data, about 60% of primary brain tumors are malignant brain tumors. The incidence of malignant brain tumors in China is 8-10 cases / 100,000. It is estimated that there are more than 200,000 new malignant brain tumor patients in China every year. It is characterized by rapid growth, strong invasiveness, easy recurrence after surgery, and high mortality. Gliomas accounted for 1.4 percent of all new tumors, and gliomas accounted for 2.4 percent of all cancer deaths. Although surgical treatment has significantly improved the survival of patients with glioma, drug treatment is still one of the important met...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/40A61K47/18A61K31/4188A61P35/00
CPCA61K31/4188A61K47/183A61K47/40
Inventor 安晓霞蔡伟惠刘薇于娟
Owner SHANGHAI ACEBRIGHT PHARMA CO LTD
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