Tamsulosin hydrochloride sustained release microgranules and preparation method thereof

A technology of tamsulosin hydrochloride and slow-release microparticles, which can be used in pharmaceutical formulations, microcapsules, medical preparations of non-active ingredients, etc., and can solve problems such as unfavorable taking by patients

Active Publication Date: 2020-01-21
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] CN 1758903A discloses a kind of tamsulosin intestinal sustained-release microparticles, the preparation is an orally disintegrating enteric-coated sustained-release microparticle tablet, and excessive auxiliary materials are added for tablet compression, which is unfavorable for patients to take
US2004096502A1, CN103585112A, and CN102579359A disclose tamsulosin hydrochloride slow-release microparticles including multi-particles. The microparticles are composed of tamsulosin hydrochloride, microcrystalline cellulose and excipients with slow and controlled release, so that the drug is gradually released from the matrix of the granules. but did not address the effect of food on drug absorption

Method used

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  • Tamsulosin hydrochloride sustained release microgranules and preparation method thereof
  • Tamsulosin hydrochloride sustained release microgranules and preparation method thereof
  • Tamsulosin hydrochloride sustained release microgranules and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Prescription of pill core containing drug coating layer:

[0048]

[0049] Enteric coating layer coating solution prescription (weight gain 2.5%):

[0050]

[0051] Sustained-release coating layer coating solution prescription (weight gain 6%):

[0052]

[0053] The preparation method of tamsulosin hydrochloride slow-release microparticles, the steps are as follows:

[0054] Step (1), take the prescribed amount of tamsulosin hydrochloride and hypromellose, add purified water, stir until dissolved, and obtain a drug-containing solution;

[0055] Step (2), taking a blank microcrystalline cellulose pellet core and placing it in a fluidized bed, setting the coating parameters of the fluidized bed, and using the drug-containing solution prepared in step (1) for coating to obtain a drug-containing pellet core;

[0056] Step (3), take the prescribed amount of triethyl citrate and talcum powder and disperse them in an appropriate amount of purified water, place them ...

Embodiment 2

[0081] Prescription of pill core containing drug coating layer:

[0082]

[0083] Enteric coating layer coating solution prescription (weight gain 2%):

[0084]

[0085] Sustained-release coating layer coating solution prescription (weight gain 6%):

[0086]

[0087] Preparation method: with embodiment 1.

[0088] Determination of release rate: according to the second method of appendix XD of the 2015 edition of Chinese Pharmacopoeia, the release test method under the WS1-(X-333)-2003Z item is measured (n=12), and the average release rate is 23% (2h), respectively. 54% (3h) and 89% (5h), the release rate meets the regulations.

Embodiment 3

[0090] Prescription of pill core containing drug coating layer:

[0091]

[0092] Enteric coating layer coating solution prescription (weight gain 3%):

[0093]

[0094] Sustained-release coating layer coating solution prescription (weight gain 6%):

[0095]

[0096] Preparation method: with embodiment 1

[0097] Determination of release rate: According to the second method of appendix XD of the 2015 edition of the Chinese Pharmacopoeia, the release test method under the item WS1-(X-333)-2003Z is measured (n=12), and the average release rate is 21% (2h), respectively. 57% (3h) and 83% (5h), comply with the regulations.

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Abstract

The invention discloses tamsulosin hydrochloride sustained release microgranules. The tamsulosin hydrochloride sustained release microgranules take blank pill cores as pill cores, and the pill cores are successively coated with a medicine-containing coating layer, an enteric coating layer and a sustained release coating layer; the medicine-containing coating layer is obtained by being sprayed by an aqueous solution of tamsulosin hydrochloride and an adhesive; and the enteric coating layer is obtained by being sprayed by an enteric coating solution containing an enteric coating material, a plasticizer and an anti-viscosity agent. According to the tamsulosin hydrochloride sustained release microgranules, absorption or bioavailability of tamsulosin is not influenced by the food effect and physiological changes of gastrointestinal tract before and after meals, a stable blood concentration curve and long-term action time can be obtained, occurrence of cardiovascular side effects can be reduced, and the safety, effectiveness and compliance of patient medication can be greatly improved.

Description

technical field [0001] The invention relates to tamsulosin hydrochloride slow-release microparticles and a preparation method thereof. Background technique [0002] Benign prostatic hyperplasia is a common urological disease in elderly men, which refers to the benign adenomatous hyperplasia of cells in the periurethral area of ​​the prostate. Tamsulosin hydrochloride is an alpha 1 adrenergic receptor antagonist used to relieve benign prostatic hyperplasia. Tamsulosin hydrochloride sustained-release microparticles can obtain a stable blood drug concentration curve and long-term action time, reduce the occurrence of cardiovascular side effects, and greatly improve the safety, effectiveness and compliance of patients taking medicine. [0003] Using the same drug for the same disease, some people have achieved good curative effect, while some people not only have no obvious curative effect, but also have serious adverse reactions. In addition to individual differences, the reas...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/38A61K47/32A61K31/18A61P13/08
CPCA61K9/5078A61K9/5026A61K9/5047A61K31/18A61P13/08
Inventor 李剑丁静周建平黄春玉许润田丽娟谢俊徐向阳
Owner CHINA PHARM UNIV
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