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Preparation method of doxazosin mesylate sustained-release dropping pill for treating hypertension and prostatic hyperplasia

A technology for doxazosin mesylate and benign prostatic hyperplasia, which is applied in the field of preparation of doxazosin mesylate sustained-release dripping pills, which can solve the cumbersome tablet production process, unfavorable overall health level, and physical hazards of staff and other problems to achieve the effect of avoiding the first-pass effect of liver and intestines, improving bioavailability and less side effects

Inactive Publication Date: 2013-03-13
北京博智绿洲医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The drug is currently commercially available as doxazosin mesylate tablets, which can treat hypertension and benign prostatic hyperplasia. As we all know, the production process of the tablet is cumbersome and the cost is high, so that the cost of the patient's medication is also increased, which is not conducive to Improving the ability of patients to seek medical treatment is not conducive to improving the overall health level of society
Especially in the preparation process, due to the granulation process, a large amount of dust pollution will be generated, which will cause harm to the health of the staff to a certain extent, and will also cause certain pollution to the environment.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Based on the total weight of 100 g, 70% of PEG4000, 20% of glycerol monostearate, and 10% of doxazosin mesylate. After the matrix is ​​heated and melted in a water bath, doxazosin mesylate is added, and the mixture is fully stirred to make the mixture. After mixing, drop the material into the condensation column filled with dimethyl silicone oil under the condition of 80 ℃ heat preservation. The temperature of the upper part of the condensate is 40 ℃, and the temperature of the bottom is 0 ℃. After forming, take it out and absorb it with absorbent paper. The dimethyl silicone oil adhering to the surface is dried under natural conditions.

[0025] The obtained product has a cumulative release percentage of 55-79% in 2 hours, a cumulative release percentage of 75-83% in 6 hours, and a cumulative release percentage of 79-93% in 10 hours, with good roundness and good hardness.

Embodiment 2

[0027] Based on the total weight of 100 g, 50% of PEG4000, 40% of glycerol monostearate, and 10% of doxazosin mesylate. After the base is heated and melted in a water bath, doxazosin mesylate is added, and the mixture is fully stirred to make the mixture. After mixing, drop the material into a condensation column filled with dimethyl silicone oil under the condition of 80 ℃ heat preservation. The temperature of the upper part of the condensate is 40 ℃, and the temperature of the bottom is 5 ℃. After forming, take it out and absorb with absorbent paper The dimethyl silicone oil adhering to the surface is dried under natural conditions.

[0028] The obtained product, the cumulative release percentage in 2 hours is 47-65%, the cumulative release percentage in 6 hours is 67-82%, and the cumulative release percentage in 10 hours is 79-100%, with good roundness and good hardness.

Embodiment 3

[0030] Based on the total weight of 100 g, 70% of PEG4000, 10% of glycerol monostearate, and 20% of doxazosin mesylate. After the substrate is heated and melted in a water bath, doxazosin mesylate is added, and the mixture is fully stirred to make the mixture. After mixing, drop the material into the condensation column filled with dimethyl silicone oil under the condition of 90 ℃ heat preservation. The temperature of the upper part of the condensate is 50 ℃, and the temperature of the bottom is 5 ℃. After forming, take it out and absorb it with absorbent paper. The dimethyl silicone oil adhering to the surface is dried under natural conditions.

[0031] The obtained product has a cumulative release percentage of 75-85% in 2 hours, a cumulative release percentage of 79-89% in 6 hours, and a cumulative release percentage of 95-100% in 10 hours. The roundness is good.

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PUM

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Abstract

The invention belongs to the technical field of pharmacy, and particularly relates to a preparation method of doxazosin mesylate sustained-release dropping pill for treating hypertension and prostatic hyperplasia. Based on doxazosin mesylate tablets, the invention employs existing dropping pill preparation technology to prepare the doxazosin mesylate sustained-release dropping pill. Compared to the prior art, the invention is the supplement for the defects of existing drug form production, and provides a drug, which has advantages of high bioavailability, rapid effectiveness, long-acting effect, little toxic or side effect, high drug content, small and accurate dosage, convenient usage, low price and convenience for carrying.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a preparation method of doxazosin mesylate sustained-release dropping pills for treating hypertension and benign prostatic hyperplasia. Background technique [0002] Doxazosin mesylate is a long-acting - Receptor blockers. This product selectively acts on post-holiday -Adrenergic receptors, dilate peripheral blood vessels, reduce peripheral vascular resistance and lower blood pressure, and have little effect on cardiac output. with other -Like blockers, doxazosin has a greater effect on orthostatic blood pressure and heart rate. This product acts on the smooth muscle of the prostate and bladder neck -Adrenergic receptors relax the smooth muscle of the bladder neck, prostate, and prostate capsule, and reduce the resistance of the urethra and bladder, thereby reducing the symptoms of urethral obstruction caused by benign prostatic hyperplasia. This product ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/517A61K47/34A61P9/12A61P13/08
Inventor 曲韵智王金强振君
Owner 北京博智绿洲医药科技有限公司