Carbidopa-levedopa sustained-release dropping pill and preparation method thereof

A technology of sustained-release dripping pills and sustained-release preparations, which is applied in the direction of pharmaceutical formulas, medical preparations containing active ingredients, and medical preparations containing active ingredients. and other problems, to achieve the effect of reducing the number of medications, stabilizing drug release, and accurate dosage

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

Imported drugs that occupy all of the river's exports in the market have increased the financial burden on patients
At the same time, Xining is a controlled-release tablet with a single dosage form, short action time, and many daily doses. It is urgent to develop other dosage forms and varieties such as sustained release to meet domestic drug demand.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Based on the total weight of 100g, weigh the matrix PEG4000 37%, PEG6000 30%, PEG10000 5%, stearic acid 8%, glyceryl monostearate 10%, raw materials carbidopa 2%, levodopa 8%; Put the base in a heating container to heat and stir to melt it, add corresponding proportion of carvodopa, stir well, use a dropping pill machine, drop the melted or mixed liquid medicine into the container under the condition of heat preservation In the condensation column with simethicone oil, the temperature when heating and melting is 90°C, the temperature of the upper part of the condensate is 20°C, and the temperature of the bottom is -3°C; take it out after forming,

[0039]The obtained product has a 2-hour cumulative release percentage of 41%-52%, a 6-hour cumulative release percentage of 55%-77%, and a 10-hour cumulative release percentage of 79%-100%. The release degree is qualified and the roundness is good.

Embodiment 2

[0041] Based on the total weight of 100g, weigh the matrix PEG4000 35%, PEG6000 20%, PEG10000 10%, stearic acid 10%, but glyceryl stearate 5%, raw materials carbidopa 4%, levodopa 16%; Put the base in a heating container to heat and stir to make it melt, add the corresponding proportion of carvodopa, stir well, use a dropping pill machine, under the condition of heat preservation, drop the melted or mixed liquid medicine into In the condensation column filled with simethicone oil, the temperature when heating and melting is 85°C, the temperature of the upper part of the condensate is 25°C, and the temperature of the bottom is -1°C; take it out after molding,

[0042] The obtained product has a 2-hour cumulative release percentage of 45%-55%, a 6-hour cumulative release percentage of 56%-76%, and a 10-hour cumulative release percentage of 78%-99%. The release degree is qualified and the roundness is good.

Embodiment 3

[0044] Based on a total weight of 100g, weigh 35% of the matrix PEG4000, 25% of PEG6000, 20% of stearic acid, 5% of glyceryl monostearate, 3% of raw carbidopa, and 12% of levodopa; Heat and stir in the heating container to melt, add the corresponding proportion of carvodopa, stir well, use the dropping pill machine, and drop the molten or mixed liquid medicine into the liquid paraffin under the condition of heat preservation. In the condensing column, the temperature when heating and melting is 80°C, the temperature of the upper part of the condensate is 25°C, and the temperature of the bottom is 3°C; take it out after molding,

[0045] The obtained product has a 2-hour cumulative release percentage of 46%-66%, a 6-hour cumulative release percentage of 69%-80%, and a 10-hour cumulative release percentage of 861%-100%. The release degree is qualified and the roundness is good.

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PUM

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Abstract

The invention relates to a carbidopa-levedopa sustained-release dropping pill for the treatment of Parkinson's disease and a preparation method thereof. The invention aims to solve the insufficiencies of an oral preparation, and provides a carbidopa-levedopa sustained-release dropping pill, which has advantages of high bioavailability, rapid effectiveness, long action time, low frequency of drug taking, convenient administration, little toxic or side effect, convenient storage and transportation, and suitability for oral administration, and the preparation method thereof.

Description

technical field [0001] The invention relates to a carlevodopa slow-release preparation for treating Parkinson's disease and a preparation method thereof. Background technique [0002] Carbidopa is a compound containing carbidopa (C10H14N2O4.H2O) and levodopa (C9H11N04), with molecular weights of 244.25 and 197.2, respectively, and its chemical name is, carbidopa: (-)-levodopa -α-hydrazino-α-methyl-β-3,4-dihydroxyphenylpropionic acid monohydrate; Levodopa: (-)-L-α-amino-β-3,4-dihydroxyphenylpropane acid. [0003] Carbidopa raw material is white or off-white fluffy crystal, almost odorless. This product is slightly soluble in water or methanol, almost insoluble in ethanol or chloroform, and easily soluble in dilute hydrochloric acid. [0004] Levodopa raw material is white or off-white crystalline powder; odorless and tasteless. Slightly soluble in water, insoluble in ethanol, chloroform or ether; easily soluble in dilute acid. [0005] Carlevodopa is the main drug for th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/198A61K47/34A61K47/36A61P25/16
Inventor 曲韵智王金强振君
Owner 北京博智绿洲医药科技有限公司
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