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Temozolomide brain-targeting pharmaceutical composition and application thereof

A technology of temozolomide and its composition, which is applied in the field of brain-targeted powder pharmaceutical composition, can solve the problems of inconvenient use for patients, teratogenic reproductive organs, unfavorable industrial production, etc.

Active Publication Date: 2012-07-04
BEIJING HUMANWELL JUNWEI PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is only temozolomide capsules on the market in China. Its dosage is large, which can cause cancer, teratogenicity and reproductive organ toxicity, and the treatment cost is expensive, which brings heavy financial and physical burdens to patients.
[0005] Temozolomide is commercially available in the form of capsules and freeze-dried powder injections. The research on other dosage forms of temozolomide mainly includes the following types according to published literature reports: temozolomide polylactic acid nanospheres (Chinese patent CN200610161653.3), temozolomide sustained-release implantation Drug (Chinese Patent CN200710203056.7), Temozolomide Controlled Release Drug Delivery System (Chinese Patent CN03134852.1), Temozolomide Multimer Local Sustained Release Drug (Chinese Patent CN200410043908.7), Temozolomide Brain Sustained Release Implant (Chinese Patent 200510024953.2) and temozolomide liposomes, dispersible tablets, etc., the above dosage forms have poor practicability, high cost, are not conducive to industrial production, and are inconvenient for patients to use

Method used

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  • Temozolomide brain-targeting pharmaceutical composition and application thereof

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Experimental program
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Effect test

Embodiment 1

[0059] Embodiment 1: Preparation of temozolomide powder composition

[0060] Weigh 30 g of temozolomide fine powder that has been pulverized through a 120 mesh sieve, and set aside. In addition, 65g of lactose, 3.5g of hydroxypropyl-β-cyclodextrin, and 1.5g of citric acid were accurately weighed and crushed to 120 meshes, and set aside. Temozolomide, lactose, hydroxypropyl-β-cyclodextrin, and stabilizer are uniformly mixed by an equal-volume increasing method, ground, and passed through a 200-mesh sieve for 3 times to obtain the temozolomide powder composition of the present invention, which can be used as temozolomide nasal powder For example in capsules or in containers with powder dosing valves. The average particle size of the particles was measured to be 185 microns.

Embodiment 2

[0061] Embodiment 2: Preparation of temozolomide powder composition

[0062] Weigh 60 g of temozolomide fine powder that has been pulverized through a 120 mesh sieve, and set aside. In addition, 38g of lactose, 1g of β-cyclodextrin, and 1g of tartaric acid were accurately weighed and crushed to 100 meshes, and set aside. Temozolomide, lactose, β-cyclodextrin, and stabilizer are uniformly mixed by an equal increase method, ground, and passed through a 200-mesh sieve for 3 times to obtain the temozolomide powder composition of the present invention, which can be used as temozolomide nasal powder, for example, in Capsules or dispensed in containers with powder dosing valves. The average particle size of the particles was measured to be 215 microns.

Embodiment 3

[0063] Embodiment 3: Preparation of temozolomide powder composition

[0064] Take by weighing 45g of temozolomide fine powder that has been pulverized through a 140 mesh sieve, and set aside. In addition, 42 g of mannitol, 10 g of hydroxypropyl-β-cyclodextrin, and 3 g of citric acid were accurately weighed and crushed to 140 mesh, and set aside. Temozolomide, hydroxypropyl-β-cyclodextrin, and stabilizer are uniformly mixed by an equal increase method, ground, and passed through a 200-mesh sieve for 3 times to obtain the temozolomide powder composition of the present invention, which can be used as temozolomide nasal powder, such as Dispensed in capsules or in containers with powder dosing valves. The average particle size of the particles was measured to be 185 microns.

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Abstract

The invention discloses a temozolomide brain-targeting pharmaceutical composition and application thereof. The pharmaceutical composition provided by the invention contains a therapeutic effective dose of temozolomide, an absorbefacient and a pharmaceutical carrier. The invention also provides a pharmaceutical composition which contains a therapeutic effective dose of temozolomide, a stabilizer and a pharmaceutical carrier. The invention further provides the application of the pharmaceutical compositions provided by the invention in the preparation of drugs for intranasal administration. The compositions provided by the invention can be used as nasal powder. The temozolomide nasal powder provided by the invention is formed by the temozolomide, the pharmaceutical carrier and the stabilizeror the absorbefacient and is a preparation which reaches the brain to treat brain tumors through the absorption of nasal mucosa.

Description

technical field [0001] The invention belongs to the technical field of medicine, and more specifically relates to a brain-targeted powder pharmaceutical composition of temozolomide and its application. The powder composition of the present invention is made into a nasal powder, which can be absorbed through nasal mucosa to achieve brain-targeted administration of temozolomide. Background technique [0002] More than 60% of adult primary brain tumors are gliomas and malignant melanomas. This is a very harmful malignant tumor with high morbidity and mortality. The survival period calculated from the initial diagnosis is only 9-12 months. It causes patients to lose multiple functions, such as movement disorders, epilepsy, visual disorders, language disorders, etc., and their quality of life is extremely poor. Although patients are treated with surgery, radiotherapy and chemotherapy, almost all patients will experience tumor recurrence. [0003] Temozolomide (Temozolomide, TM...

Claims

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Application Information

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IPC IPC(8): A61K31/4188A61K9/14A61P35/00
Inventor 高永良李颖边琳晶何群高翠仙
Owner BEIJING HUMANWELL JUNWEI PHARM TECH CO LTD
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