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A kind of temozolomide pharmaceutical composition and its preparation method and application

A technology for temozolomide and composition, applied in the field of pharmaceutical compositions, can solve the problems of affecting clinical efficacy, poor preparation content uniformity, poor stability and the like, and achieve the effects of improving drug efficacy, improving fluidity and good stability

Active Publication Date: 2020-07-10
TOT BIOPHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, the formulation of the above-mentioned temozolomide capsules has poor fluidity, and the grain weight varies greatly during the capsule filling process, resulting in poor content uniformity of the formulation, which may affect the clinical efficacy
However, the production technology with too strict restrictions on capsule filling has high requirements for temozolomide raw materials, which is inconvenient to use, and is not convenient for industrialization and production promotion.
Simultaneously, the preparation of above-mentioned temozolomide capsule also has poor stability, which limits the scope of clinical application

Method used

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  • A kind of temozolomide pharmaceutical composition and its preparation method and application
  • A kind of temozolomide pharmaceutical composition and its preparation method and application
  • A kind of temozolomide pharmaceutical composition and its preparation method and application

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Effect test

Embodiment 1

[0048]

[0049]

[0050] In the present embodiment, the formulation of the temozolomide pharmaceutical composition is as follows, and it is made into capsules (an appropriate amount of hollow capsules are used):

[0051] Preparation method: Add 20g of temozolomide, 240g of anhydrous lactose, 15g of croscarmellose sodium, 1g of silicon dioxide, and 5g of tartaric acid into a mixer in sequence, and continue mixing for about 3 minutes. Continue mixing for about 15 minutes after passing the above-mentioned mixed powder through a 20-mesh sieve. Add 5g of glyceryl behenate, continue mixing for about 3 minutes, and fill into 2# hollow capsules, the content of each capsule is about 285mg. The grain weight variation during capsule filling is about ±5%.

Embodiment 2

[0053] In the present embodiment, the formulation of the temozolomide pharmaceutical composition is as follows, and it is made into capsules (an appropriate amount of hollow capsules are used):

[0054] Temozolomide 100g anhydrous lactose 205g Croscarmellose Sodium 25g silica 2g tartaric acid 10g Glyceryl behenate 8g empty capsule Appropriate amount

[0055] Preparation method: Add 100g temozolomide, 205g anhydrous lactose, 25g croscarmellose sodium, 2g silicon dioxide, and 10g tartaric acid into the mixer in sequence, and continue mixing for about 5 minutes. Continue mixing for about 20 minutes after passing the above-mentioned mixed powder through a 24-mesh sieve. Add 8g of glyceryl behenate, continue mixing for about 5 minutes, and fill into 1# empty capsules, the content of each capsule is about 350mg. The grain weight variation during capsule filling is about ±6%.

Embodiment 3

[0057] Temozolomide 10g anhydrous lactose 180g Croscarmellose Sodium 6g silica 1g tartaric acid 2g Glyceryl behenate 1g empty capsule Appropriate amount

[0058] In the present embodiment, the formulation of the temozolomide pharmaceutical composition is as follows, and it is made into capsules (an appropriate amount of hollow capsules are used):

[0059] Preparation method: Add 10g of temozolomide, 180g of anhydrous lactose, 6g of croscarmellose sodium, 1g of silicon dioxide, and 2g of tartaric acid into a mixer in sequence, and continue mixing for about 3 minutes. Continue mixing for about 15 minutes after passing the above-mentioned mixed powder through a 20-mesh sieve. Add 1g of glyceryl behenate, continue mixing for about 5 minutes, and fill into 2# hollow capsules, the content of each capsule is about 200mg. The difference in grain weight during capsule filling is about ±6.5%.

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Abstract

The invention provides a temozolomide pharmaceutical composition as well as a preparation method and application thereof. The temozolomide pharmaceutical composition is prepared from the following components in percentage by weight: 3 to 60 percent of temozolomide, 40 to 95 percent of lactose anhydrous, 1 to 10 percent of croscarmellose sodium, 0.5 to 5 percent of tartaric acid and 0.1 to 2 percent of silicon dioxide. In the preparation method, the components in the pharmaceutical composition are selected specifically, stable capsules which do not exceed + / -6 percent in capsule weight difference can be obtained by adopting the conventional powder capsule filling technology, and the pharmaceutical composition has high stability; under the condition of not adding any extra stabilizer, the prepared temozolomide capsule has higher stability, can be stably stored for three years or longer at normal temperature, and can be dissolved rapidly under human physiological pH; the medication risk caused by undesirable dissolving in clinical is lowered. Moreover, the pharmaceutical composition disclosed by the invention has the advantages of simple preparation process, convenience, feasibility and easiness in amplified production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical compositions, and relates to a temozolomide pharmaceutical composition and a preparation method and application thereof. Background technique [0002] Glioma is the most common tumor of the central nervous system, among which malignant patients (2007 World Health Organization (WHO) central nervous system tumor classification III, IV grade) are more common. In the past 30 years, the incidence of primary malignant brain tumors has been increasing year by year, with an annual growth rate of about 1.2%, especially in the elderly [1]. Glioma is a kind of malignant tumor with great harm and high incidence. It will directly lead to the loss of various functions of patients, such as movement disorders, visual disorders and language disorders, etc., and the quality of life is extremely poor. Patients have high disability and brain damage. If the function is lost, the tumor progression in a short pe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/48A61K31/4188A61K47/04A61K47/26A61K47/38A61K47/12A61P35/00
CPCA61K9/485A61K9/4858A61K9/4866A61K31/4188
Inventor 陈小宝黄纯莹
Owner TOT BIOPHARM CO LTD