Exemestane sustained-release capsule

A technology of sustained-release capsules and exemestane, which is applied in drug delivery, organic active ingredients, medical preparations containing active ingredients, etc., and can solve the problems of ineffective control of the release amount, poor safety, and poor effectiveness

Inactive Publication Date: 2014-07-30
赵辉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The object of the present invention is to provide a kind of exemestane sustained-release capsule, it can overcome the current exemestane common dosage form medicine release amount and can not effectively control, cause the shortcoming that safety, effectiveness are relatively poor, and can reduce medication total dose and good efficacy

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0018] The preparation process of the above-mentioned exemestane sustained-release capsules adopts the following several processes to prepare:

[0019] (1) Extrusion spheronization method: use an extrusion spheronizer to mix the raw material medicine and excipients through an 80-mesh screen, spray the mixed powder with a binder in the extrusion spheronizer, and then extrude and spheronize Make pellets, dry and sieve to obtain drug-containing pellets with a certain mesh size. Coating with ethyl cellulose aqueous dispersion in a fluidized bed coating pan;

[0020] (2) Powder coating method: use a non-porous coating pan, a water chestnut-shaped coating pan, a fluidized bed top spray (or bottom spray) coating machine, and a fluidized bed tangential spray to make pellets. Take the water chestnut-shaped coating pot as an example: mix the medicinal powder and excipients through an 80-mesh sieve, take a certain number of pellets (sucrose pills or microcrystalline cellulose pills) int...

Embodiment 1

[0024] An exemestane sustained-release capsule is composed of 5% exemestane, 90% excipient, 3% film coating material, 1% wetting agent and 1% binder. Wherein the excipient is microcrystalline cellulose, the film coating material is ethyl cellulose aqueous dispersion, the wetting agent is 75% ethanol solution, and the binder is aqueous solution of hydroxypropyl methyl cellulose. A kind of preparation technology of exemestane sustained-release capsule, it adopts following technology to prepare:

[0025] Utilize extruding spheronization method: utilize extruding spheronizing granulator, crude drug and microcrystalline cellulose are mixed and crossed 80 mesh screens, mix powder with the aqueous solution of hydroxypropyl methylcellulose in extruding spheronizing granulator After spraying wet, extrude and spheronize to form pellets, and after drying, sieve to obtain drug-containing pellets with a certain mesh size, which are coated with ethyl cellulose aqueous dispersion in a fluidi...

Embodiment 2

[0027] An exemestane sustained-release capsule, wherein the sustained-release capsule is made up of 20% exemestane, 63% excipient, 10% film coating material, 5% wetting agent and 2% binding agent . Wherein the excipient is starch, the film coating material is ethyl cellulose aqueous dispersion, the wetting agent is aqueous solution, and the binding agent is alcohol solution of polyvinylpyrrolidone.

[0028] A kind of preparation technology of exemestane sustained-release capsule, it adopts following technology to prepare:

[0029] Powder coating method: use a non-porous coating pan, a water chestnut-shaped coating pan, a fluidized bed top spray (or bottom spray) coating machine, and a fluidized bed tangential spray pellet machine to make pellets. Take the water chestnut-shaped coating pot as an example: mix the medicine powder and starch through an 80-mesh sieve, take 30-35 mesh pellets (sucrose pills or microcrystalline cellulose pills) into the water chestnut-shaped coating...

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Abstract

The invention discloses an exemestane sustained-release capsule. The exemestane sustained-release capsule is composed of 5-20wt% of exemestane, 58-95wt% of excipient, 3-10wt% of film coating material, 0-10wt% of wetting agent and 1-2wt% of adhesive; and a preparation method for the same comprises the step of preparing by (1) an extrusion rounding method, (2) a powder coating method, and (3) a liquid deposition method to obtain the exemestane sustained-release capsule.

Description

field of invention [0001] The invention relates to a sustained-release capsule, in particular to an exemestane sustained-release capsule. Background of the invention [0002] Breast cancer is one of the most common malignant tumors among women in the world. The incidence rate is increasing year by year. In today's elderly population, women over 65 years old, about 26% suffer from breast cancer, and about 1 / 3 of the tumor growth requires high estrogen levels to maintain, that is, estrogen dependence Characteristics. Estrogen-dependent breast cancer occurs more frequently in postmenopausal women. Antiestrogens are commonly used in patients with estrogen-dependent breast cancer. Tamoxifen has been used as the first-line treatment drug, but the effect of tamoxifen is better when it is first used, and long-term use is prone to drug resistance, leading to disease recurrence. Another class of aromatase inhibitors whose mechanism of action is different from tamoxifen is effective...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/5685A61P35/00
Inventor 赵辉赵冠淇苏天慧胡晓川
Owner 赵辉
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