Sustained release temozolomide capsules and preparation method thereof

A technology of temozolomide and capsules, applied in the field of medicine, can solve the problems of short half-life of temozolomide, unstable blood drug concentration, etc., and achieve the effects of easy industrial production, reduction of the number of times of taking medicines, and long action time.

Active Publication Date: 2018-05-11
BEIJING SL PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the problems of short half-life of temozolomide and unstable blood drug concentration during ...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A temozolomide sustained-release capsule, containing 5 temozolomide microtablets, each tablet core contains temozolomide 2mg, tablet weight is 8mg, it includes the following components, and the dosage per 10000 tablets is:

[0039] Temozolomide 20.00g;

[0040] Thinner 17.00g;

[0041] Sustained release agent 38.00g;

[0042] Antioxidant 1.60g;

[0043] Adhesive 2.60g;

[0044] Lubricant 0.80g;

[0045] Described diluent is lactose;

[0046] The sustained-release agent is hypromellose;

[0047] Described antioxidant is tartaric acid;

[0048] Described binding agent is povidone K30;

[0049] Described lubricant is talcum powder and stearic acid, and talcum powder 0.2g, stearic acid 0.6g;

[0050] A preparation method for Temozolomide Gastric Sustained Release Capsules, comprising the following steps:

[0051] 1) Weigh each component according to the above formula, and pulverize the weighed temozolomide through a 100-mesh sieve, and pass the diluent and sustaine...

Embodiment 2

[0058] A temozolomide sustained-release capsule, containing 4 temozolomide microtablets, each tablet core containing temozolomide 5mg, tablet weight 20mg, it includes the following components, and the dosage per 10000 tablets is:

[0059] Temozolomide 50.00g;

[0060] Thinner 30.00g;

[0061] Sustained release agent 115.00g;

[0062] Antioxidant 3.00g;

[0063] Lubricant 2.00g;

[0064] Described diluent is lactose, microcrystalline cellulose, and lactose 20g, microcrystalline cellulose 10g;

[0065] The sustained-release agent is Eudragit RS;

[0066] Described antioxidant is citric acid;

[0067] Described lubricant stearic acid and silicon dioxide, and stearic acid 1.5g, silicon dioxide 0.5g;

[0068] A preparation method for Temozolomide Gastric Sustained Release Capsules, comprising the following steps:

[0069] 1) Weigh each component according to the above formula, and pulverize the weighed temozolomide through a 100-mesh sieve, and pass the diluent and sustained...

Embodiment 3

[0075] A temozolomide sustained-release capsule, containing 5 temozolomide microtablets, each tablet core containing temozolomide 10mg, tablet weight 35mg, it includes the following components, and the dosage per 10000 tablets is:

[0076] Temozolomide 100.00g,

[0077] Diluent 72.00g;

[0078] Sustained release agent 160.00g;

[0079] Antioxidant 5.00g;

[0080] Lubricant 3.00g;

[0081] Described thinner is lactose, starch, and lactose is 42g, and starch is 30g;

[0082] The sustained release agent is hypromellose, Eudragit NE, and hypromellose 100g, Eudragit NE60g;

[0083] Described antioxidant is citric acid;

[0084] Described lubricant stearic acid and silicon dioxide, and stearic acid 2.4g, silicon dioxide 0.6g;

[0085] A preparation method for Temozolomide Gastric Sustained Release Capsules, comprising the following steps:

[0086] 1) Weigh each component according to the above formula, and pulverize the weighed temozolomide through a 100-mesh sieve, and pass ...

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Abstract

The invention relates to sustained release temozolomide capsules and a preparation method thereof, and belongs to the technical field of medicine. Each sustained release temozolomide capsule comprises2-20 sustained release micro-tablets and a capsule shell, wherein each micro-tablet contains 2-20 mg of temozolomide. The sustained release micro-tablets comprise raw and auxiliary materials in percentage by weight as follows: 5%-50% of temozolomide, 5%-40% of a diluent, 10%-70% of a sustained release agent, 0.5%-2% of an antioxidant, 0-5% of an adhesive and 0.5%-2% of a lubricant. The inventionfurther discloses the preparation method of the sustained release temozolomide capsules. The materials are pelletized or mixed and pressed into the micro-tablets directly, and the micro-tablets are loaded to hollow capsules quantitatively. The sustained release temozolomide capsules have the advantages of being good in dissolution, convenient to use, stable in plasma concentration and long in acting time, compliance of patients is improved, the preparation process is simple and lower in cost, and industrial production is easy.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a sustained-release capsule of an antitumor drug, in particular to a sustained-release capsule of temozolomide and a preparation method thereof. Background technique [0002] Temozolomide (TMZ) is used for the treatment of malignant glioma that has progressed or recurred after conventional treatment and as a first-line treatment for advanced melanoma that has metastasized. Temozolomide can effectively treat brain tumors through the blood-brain barrier. Combined with radiotherapy to treat brain metastases from lung cancer, it can significantly improve the objective response rate of brain metastases, prolong survival, and prevent brain metastases from lung cancer. [0003] Studies on the pharmacokinetics of temozolomide in mice have shown that temozolomide is absorbed very rapidly, with a half-life of 1.13h (i.p.) and 1.29h (p.o.). In the phase I clinical trial of temozolomide, it ...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/4188A61K47/38A61K47/32A61P35/00A61P35/04
CPCA61K9/4808A61K9/4866A61K31/4188
Inventor 李学海刘成东周伟李好好杨彩霞刘媛媛窦学义白玉倩肖秀英宋木娇穆甲俊翟芳刘亚楠徐明波
Owner BEIJING SL PHARMA
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