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Slow released doxazosin mesilate capsule and its prepn process

A technology for doxazosin mesylate and sustained-release capsules, which is applied in the field of doxazosin mesylate sustained-release capsules, can solve the problems of cumbersome preparation process, high requirements on production conditions, complexity and the like, and achieves simple preparation process, Improve safety and efficacy, good reproducibility

Inactive Publication Date: 2007-01-03
SHANDONG INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] US 4,765,989 and Pfizer’s doxazosin mesylate controlled-release tablets are based on laser drilling and coating film controlled-release technology. The preparation process is cumbersome and complicated, and the production conditions are high and require special equipment.

Method used

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  • Slow released doxazosin mesilate capsule and its prepn process
  • Slow released doxazosin mesilate capsule and its prepn process
  • Slow released doxazosin mesilate capsule and its prepn process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] prescription:

[0033] Doxazosin Mesylate 4g

[0034] Blank ball core 200g

[0035] Hypromellose 2g

[0036] Eudragit RL100 4.0g

[0037] Triethyl citrate 0.66g

[0038] Talc powder 2.2g

[0039] Preparation:

[0040]The preparation method of the doxazosin mesylate sustained-release pellets is as follows: slowly add 2 g of hypromellose into 90 ml of 60% ethanol with a stirring device, and keep stirring until it dissolves into a clear solution. Add 4 g of doxazosin mesylate to 200 ml of anhydrous ethanol in the dark until dissolved. The above two liquids were combined as a coating liquid. Put 220g of blank pellet cores in the coating pan, set the peristaltic pump speed at 20±5 rpm, air pressure at 0.5~0.65Mpa, material bed temperature at 45~50°C, spray speed at 5ml / min, and use atomization The spray gun evenly sprays the drug-containing solution onto the ball core, and operates intermittently. After spraying the coating solution, first dry it in a coating pan for...

Embodiment 2

[0042] prescription:

[0043] Doxazosin Mesylate 4g

[0044] Blank ball core 200g

[0045] Hypromellose 2g

[0046] Eudragit RS100 4.5g

[0047] Triethyl citrate 0.66g

[0048] Talc powder 2.2g

[0049] Preparation:

[0050] The preparation method of doxazosin mesylate sustained-release pellets is the same as in Example 1.

Embodiment 3

[0052] prescription:

[0053] Doxazosin Mesylate 4g

[0054] Blank ball core 200g

[0055] Hypromellose 2g

[0056] Eudragit RL100 2.0g

[0057] Eudragit RS100 2.0g

[0058] Triethyl citrate 0.66g

[0059] Talc powder 2.2g

[0060] Preparation:

[0061] The preparation method of doxazosin mesylate sustained-release pellets is the same as in Example 1.

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PUM

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Abstract

The present invention relates to slow released doxazosin mesilate preparation, and is especially slow released doxazosin mesilate capsule. The slow released doxazosin mesilate capsule has filler comprising doxazosin mesilate 1.0-4.0 wt%, blank pill core 70-95 wt%, adhesive 0.5-3.0 wt%, slow releasing material polyacrylic resin and / or ethyl cellulose 1.0-10.0 wt%, plasticizer 0.2-3.0 wt% and anti-sticking agent 2.0-10.0 wt%. The preparation process includes: preparing medicine-containing coating liquid, coating the medicine-containing layer, preparing slow releasing coating liquid, coating the slow releasing film and encapsulating. The slow released doxazosin mesilate preparation of the present invention can maintain effective and stable blood medicine concentration for 24 hr and less side effects.

Description

technical field [0001] The invention relates to an oral sustained-release preparation of doxazosin mesylate, in particular to a sustained-release capsule of doxazosin mesylate, which produces regular and stable blood drug concentration after oral administration. Background technique [0002] Doxazosin mesylate is a selective alpha 1 Adrenoceptor blockers, by blocking α receptors to dilate blood vessels, reduce vascular resistance, lower blood pressure; by selectively blocking α adrenergic receptors in the smooth muscle matrix, capsule and bladder neck of the prostate, improve the health of patients with benign prostatic hyperplasia symptom. Its structural formula is as follows: [0003] [0004] This product is mainly absorbed in the gastrointestinal tract, and the absorption is rapid, and age and gender have no effect on absorption. Doxazosin mesylate is a product developed by Pfizer of the United Kingdom and was granted a compound patent in 1978. In 1988, doxazosin ...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/517A61K47/38A61K47/34A61P9/12A61P13/08A61K47/32
Inventor 逄书明孙玲孙杰
Owner SHANDONG INST OF PHARMA IND
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