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Sustained-release dropping pills of Troxerutin and method for preparing the same

A technology for slow-release dropping pills and dropping pills, which is used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Low bioavailability, high manufacturing and medical costs, to achieve the effects of labor protection and environmental protection, improved bioavailability, and short production cycle

Inactive Publication Date: 2008-10-01
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

[0004] Clinically used oral dosage forms have lower dissolution rate and bioavailability, and slower onset of action than injections
Injections are often prone to allergic reactions or adverse reactions, etc., but also have the disadvantages of difficult operation, great pain for patients, high manufacturing and medical costs, and heavy economic burden for patients.
[0005] The State Patent Office has disclosed a troxerutin dripping pill with a patent number of 03153227.6 and a preparation method thereof. It can be known from the content of the disclosed invention patent that the dripping pill has high bioavailability, rapid drug release, and rapid effect effects. It overcomes the shortcomings of other oral dosage forms of troxerutin such as low bioavailability and dissolution rate, but takes more medications and has a shorter half-life

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Based on the total weight of 100g, weigh 25% of the matrix PEG4000, 20% of PEG6000, 15% of PEG10000, 30% of stearic acid, and 10% of the raw material troxerutin; it is prepared according to the above method.

[0035] The resulting product has a 2-hour cumulative release percentage of 37%-63%, a 6-hour cumulative release percentage of 64%-85%, a 10-hour cumulative release percentage of 82%-93%, and a 12-hour cumulative release percentage of 95%-100%. , better release rate, qualified dissolution time limit, better roundness.

Embodiment 2

[0037] Based on the total weight of 100g, weigh 20% of the matrix PEG4000, 20% of PEG6000, 10% of PEG10000, 17% of stearic acid, 13% of glycerol monostearate, and 20% of the raw material troxerutin; prepared according to the above method.

[0038] The resulting product has a 2-hour cumulative release percentage of 35%-57%, a 6-hour cumulative release percentage of 55%-73%, a 10-hour cumulative release percentage of 80%-91%, and a 12-hour cumulative release percentage of 92%-100%. , better release rate, qualified dissolution time limit, better roundness.

Embodiment 3

[0040] Based on the total weight of 100g, weigh 15% of the matrix PEG4000, 15% of PEG6000, 10% of polyoxyethylene monostearate, 20% of stearic acid, and 40% of the raw material troxerutin; prepared according to the above method.

[0041]The obtained product has a 2-hour cumulative release percentage of 65%-77%, a 6-hour cumulative release percentage of 75%-85%, a 10-hour cumulative release percentage of 80%-97%, and a 12-hour cumulative release percentage of 92%-100% , the release degree is good, the dissolution time is qualified, and the roundness is good.

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PUM

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Abstract

The invention relates to a troxerutin sustained-release drop pill for the treatment of hemiplegia, aphasia, arteriosclerosis, central retinitis, thrombophlebitis, varicose veins and other symptoms caused by cerebral thrombosis and cerebral embolism, as well as a preparation method thereof. The invention aims at utilizing the sustained-release pharmaceutical technology to make up for the shortcomings of the prior art and providing the troxerutin sustained-release drop pill with high bioavailability, few administration times, long-term effect, no toxicity, no side effects and convenient usage and carrying, as well as the preparation method thereof. The troxerutin is taken as raw material, a hydrophilic skeleton material and a hydrophobic skeleton material are added according to certain weight percentages to be taken as matrixes and evenly mixed, the mixed materials are heated till melting, evenly stirred and arranged in a special pill dropping machine, and then dropped into condensate liquid at appropriate speed for preparation.

Description

technical field [0001] The invention relates to a sustained-release therapeutic drug and a preparation method thereof for treating hemiplegia, aphasia, arteriosclerosis, central retinitis, thrombophlebitis, varicose veins and the like caused by cerebral thrombosis and cerebral embolism. Background technique [0002] Troxerutin is the dried flowers and flower buds of poplar poplar, a leguminous plant, which is obtained through screening, crushing, extraction, and refined processing. Its pharmacological action can inhibit the aggregation of red blood cells and platelets, and has the effect of preventing thrombus formation. At the same time, it can resist vascular damage caused by 5-hydroxytryptamine and bradykinin, increase capillary resistance, reduce capillary permeability, and prevent edema caused by increased vascular permeability. It has a significant protective effect on acute ischemic brain injury. It is suitable for hemiplegia, aphasia and pre-myocardial infarction s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/7048A61K47/34A61P9/10A61P9/14A61P9/00A61K47/10A61K47/12A61K47/14A61K47/42A61K47/44
Inventor 曲韵智
Owner 北京博智绿洲医药科技有限公司
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