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Injectable parenteral medicinal preparation of temozolomide and preparation method thereof

A technology of external drug, temozolomide, which is applied in the field of parenteral pharmaceutical preparations, can solve the problems of patients doubting the quality of drugs, reducing patient compliance and acceptance, and achieve the convenience of clinical medication, reducing the time of thermal degradation and increasing stability. Effect

Active Publication Date: 2012-02-08
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above-mentioned freeze-dried powder of temozolomide can change from white to light pink under long-term and accelerated conditions, which indicates that there may be certain problems in its quality or stability
The change of the color of the freeze-dried powder can easily make patients doubt the quality of the drug, and reduce the patient's compliance and acceptance.

Method used

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  • Injectable parenteral medicinal preparation of temozolomide and preparation method thereof
  • Injectable parenteral medicinal preparation of temozolomide and preparation method thereof
  • Injectable parenteral medicinal preparation of temozolomide and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Pharmaceutical preparation of the present invention is usually made through the following steps:

[0058] 1. Weigh the prescribed amount of stabilizer, wetting agent, excipient, buffer, stir and dissolve in at least one water-based diluent, the water-based diluent is about 90% of the prescribed amount, and the water temperature is controlled at 0-60°C .

[0059] 2. Weigh the prescribed amount of temozolomide, stir and dissolve in the above solution, measure the pH value of the solution after completely dissolving, and adjust the pH value of the solution with a pH regulator as required.

[0060] 3. Add the aqueous diluent to the final volume, and continue to stir the solution until the mixture is uniform.

[0061] 4. Filter sterilize the above solution.

Embodiment 2

[0063] Weigh 3.00g polysorbate-80, 4.00g L-cysteine ​​hydrochloride monohydrate, 25.00g mannitol, 9.90g acetic acid, 2.04g sodium acetate, add 900mL water for injection, and place in a water bath at 40°C Stir to dissolve, add 2.50g temozolomide (Jiangsu Hengrui Medicine Co., Ltd., the same source in the following examples), stir to dissolve, add water to 1000mL, filter with a 0.22 μm microporous membrane, sub-package, and freeze-dry to obtain temozolomide freeze-dried pink.

Embodiment 3

[0065] Weigh 3.00g polysorbate-80, 4.00g L-cysteine ​​hydrochloride monohydrate, 15.00g mannitol, 2.35g sodium citrate dihydrate, 0.63g hydrochloric acid, add 900mL water for injection, in 40 Stir to dissolve in a water bath at ℃, add 2.50 g of temozolomide, stir to dissolve, add water for injection to 1000 mL, filter through a 0.22 μm microporous membrane, subpackage, and freeze-dry to obtain temozolomide freeze-dried powder.

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Abstract

The invention relates to an injectable parenteral medicinal preparation of temozolomide and a preparation method thereof. The medicinal preparation comprises (1) temozolomide or pharmaceutically acceptable salt thereof, (2) at least one stabilizer, and (3) at least one aqueous diluent, wherein the stabilizer is selected from L-alanine, L-glycine, L-cysteine, L-cysteine hydrochloride anhydride, L-cysteine hydrochloride monohydrate, acetyl cysteine, S-carboxymethyl-L-cysteine, L-ethyl cysteine hydrochloride, L-methyl cysteine hydrochloride, vitamin C or a mixture thereof. The invention further relates to lyophilized power containing the medicinal preparation and products thereof.

Description

technical field [0001] The invention relates to an injectable pharmaceutical preparation for parenteral use, which comprises at least one stabilizer of the antineoplastic drug temozolomide and at least one aqueous diluent. Background technique [0002] Temozolomide chemical name: 3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-amide, which is imidazole Tetrazines are alkylating agents with antitumor activity, developed by Schering-Plough. Temozolomide is indicated for newly diagnosed glioblastoma multiforme, initially in combination with radiotherapy and subsequently as adjuvant therapy; temozolomide is also indicated for glioblastoma multiforme or anaplastic star tumors that have relapsed or progressed after conventional therapy. shape cell tumor. In 1998, Temozolomide capsules were first launched in the European Union, and then in 1999 in the United States with the approval of the US FDA. Temozolomide is currently the first-line drug for the treatment of ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4188A61K47/22A61K47/18A61K47/20A61K9/19A61P35/00
CPCA61K31/4188A61K9/0019A61K9/19A61K47/183A61K31/495A61K47/20A61P35/00
Inventor 孙飘扬张辉吴玉霞
Owner JIANGSU HENGRUI MEDICINE CO LTD
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