Tamsulosin Hydrochloride sustained-release preparation, preparation method and applications thereof

A technology for tamsulosin hydrochloride and sustained-release preparations, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, urinary system diseases, etc., can solve the problems of large differences in drug release, affecting drug release behavior, and poor reproducibility. Achieve the effect of overcoming large fluctuations in release degree and reducing toxic side effects and adverse reactions

Active Publication Date: 2015-08-05
ZHEJIANG HAILISHENG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The tamsulosin hydrochloride matrix sustained-release preparation disclosed in the aforementioned literature is either a single release system or a membrane-controlled pellet release system, wherein the matrix granulation size, tabletting pressure fluctuation, and membrane-controlled pellet coating in the single release system Changes in the membrane and drug release pores will significantly affect the drug release behavior, which will lead to defects such as large drug release differences between batches and poor reproducibility in small-dose tamsulosin hydrochloride sustained-release preparations, while the release system of membrane-controlled pellets has initial defects. Defects such as insufficient drug release

Method used

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  • Tamsulosin Hydrochloride sustained-release preparation, preparation method and applications thereof
  • Tamsulosin Hydrochloride sustained-release preparation, preparation method and applications thereof
  • Tamsulosin Hydrochloride sustained-release preparation, preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Example 1 Preparation of Tamsulosin Hydrochloride Sustained Release Capsules

[0066] 1) The composition of the matrix sustained-release pellets:

[0067]

[0068] Among them, hydroxypropyl methylcellulose is a slow-release material, lactose is used as a porogen, and polyvinylpyrrolidone K30 (PVPk30) is used as a binder. The porogen dissolves in the digestive juice to form micropores in the skeleton. Slow and smooth release from the hole.

[0069] 2) Composition of film-controlled slow-release coating film

[0070]

[0071] 3) Composition of drug-containing immediate-release layer

[0072]

[0073] The preparation method of tamsulosin hydrochloride slow-release preparation of the present embodiment comprises the following steps:

[0074] 1) Disperse the required amount of hydroxypropyl methylcellulose in purified water, heat it to about 80°C, and add the prescribed amount of tamsulosin hydrochloride under stirring conditions until a slurry is formed; then ...

Embodiment 2

[0078] Example 2Preparation of Tamsulosin Hydrochloride Sustained Release Capsules (12h Sustained Release Preparation)

[0079] 1) The composition of the matrix drug-containing sustained-release pellets:

[0080]

[0081]

[0082] 2) Composition of film-controlled slow-release coating film

[0083]

[0084] 3) Composition of drug-containing immediate-release layer

[0085]

[0086] The preparation method of tamsulosin hydrochloride sustained-release capsules in this embodiment is the same as in embodiment 1.

Embodiment 3

[0087] Example 3 Preparation of Tamsulosin Hydrochloride Sustained Release Tablets (24h Sustained Release Formulation)

[0088] 1) The composition of the matrix drug-containing sustained-release tablet core:

[0089]

[0090] Among them, hydroxypropyl methylcellulose is a slow-release material, lactose is used as a porogen, and polyvinylpyrrolidone K30 (PVPk30) is used as a binder. The porogen dissolves in the digestive juice to form micropores in the skeleton. Slow and smooth release from the hole.

[0091] 2) Composition of film-controlled slow-release coating film

[0092]

[0093] 3) Composition of drug-containing immediate-release layer

[0094]

[0095] The preparation method of tamsulosin hydrochloride slow-release preparation of the present embodiment comprises the following steps:

[0096] 1) Disperse the required amount of hydroxypropyl methylcellulose in pure water, heat to about 80°C, and add the prescribed amount of tamsulosin hydrochloride under sti...

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Abstract

The present invention relates to a tamsulosin hydrochloride sustained-release preparation, a preparation method and applications thereof. The preparation comprises, by weight, 5-95% of framework type medicine-containing sustained-release micro-pills, 1-20% of a film control type sustained-release coating film, and 1-10% of a medicine-containing rapid-release layer, wherein the framework type medicine-containing sustained-release micro-pills comprise 0.01-1% of tamsulosin hydrochloride, 5-50% of a sustained-release material, 1-10% of an adhesive, and 5-50% of a pore forming agent, the film control type sustained-release coating film comprises 1-40% of a sustained-release material, 1-5% of a plasticizer, 10-60% of a pore forming agent, and 1-5% of an anti-adhesion agent, and the medicine-containing rapid-release layer comprises 0.01-1% of tamsulosin hydrochloride, 1-95% of a rapid-release material, and 1-10% of an adhesive. The tamsulosin hydrochloride sustained-release preparation has advantages of fast, stable, sustained, and long-lasting effect, low side effect, controllable quality, suitability for mass production and the like.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a tamsulosin hydrochloride sustained-release preparation, a preparation method thereof and an application thereof. Background technique [0002] Tamsulosin hydrochloride (structure shown in formula I, also known as tamsulosin hydrochloride) is a potent and highly selective α1-adrenergic receptor inhibitor (blocker), clinically used for the treatment of benign prostate Dysuria due to hyperplasia (BPH) and enlarged prostate. In vitro tests have shown that tamsulosin hydrochloride has a better curative effect than the similar drug terazosin hydrochloride. However, oral preparations of tamsulosin hydrochloride have rapid absorption and rapid onset of action, which may cause adverse reactions such as hypotension and dizziness, so tamsulosin hydrochloride sustained-release preparations are often used clinically. [0003] [0004] At present, tamsulo...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/18A61K47/38A61K47/32A61K47/34A61P13/00
Inventor 郑海辉夏志国迟玉峰周波
Owner ZHEJIANG HAILISHENG PHARM CO LTD
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