Levodopa/carbidopa compound sustained-release suspension and preparation method thereof

A technology of levodopa and suspension preparations, which is applied in the direction of medical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as dysphagia, poor swallowing ability, and poor drug stability. Achieve the effects of good reproducibility and consistency, convenient administration, and increased plasticity

Inactive Publication Date: 2014-03-12
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention solves the problems of dysphagia and poor drug stability
The present invention aims at the deficiencies of the existing preparations. The levodopa unilateral preparations and compound preparations currently on the market are all solid preparations and injections, and no liquid preparations are on the market. It can solve the problem that the elderly are difficult to swallow solid medicine, and significantly improve the patient's compliance

Method used

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  • Levodopa/carbidopa compound sustained-release suspension and preparation method thereof
  • Levodopa/carbidopa compound sustained-release suspension and preparation method thereof
  • Levodopa/carbidopa compound sustained-release suspension and preparation method thereof

Examples

Experimental program
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preparation example Construction

[0033] 1. Preparation of Drug Resin

[0034] The cation exchange resin is added into the levodopa solution and stirred at room temperature. Samples were taken regularly to determine the concentration of the drug in the solution. When the drug concentration no longer changes with time, the equilibrium is reached, the unbound drug on the surface of the resin is washed away with double distilled water, and the drug-loaded resin is obtained by drying at 40°C-60°C.

[0035] Add the cation exchange resin to the carbidopa solution and stir at room temperature. Samples were taken regularly to determine the concentration of the drug in the solution. When the drug concentration no longer changes with time, the equilibrium is reached, the unbound drug on the surface of the resin is washed away with double distilled water, and the drug-loaded resin is obtained by drying at 40°C-60°C.

[0036] 2. Impregnation of drug resin

[0037] Take an appropriate amount of drug-loaded resin, add i...

Embodiment 1

[0046] 1. Preparation of Drug Resin

[0047]Take 200 mg of ion exchange resin and add 200 ml of 1.0 mg / ml levodopa solution (dissolved in 0.001 mol / L HCl solution), and stir at room temperature for 2 hours. Wash the unbound drug on the surface of the resin with double distilled water, and dry at 60°C to obtain the drug-loaded resin.

[0048] Take 200 mg of ion exchange resin and add 200 ml of 1.0 mg / ml carbidopa solution (dissolved in 0.001 mol / L HCl solution), and stir at room temperature for 2 hours. Wash the unbound drug on the surface of the resin with double distilled water, and dry at 60°C to obtain the drug-loaded resin.

[0049] 2. Impregnation of drug resin

[0050] Take 100 mg of drug-loaded resin, add 10 ml of 20% PEG6000 solution, stir for 0.5 hour, dry and sieve to obtain impregnated drug resin.

[0051] 3. Preparation of Drug Resin Microcapsules

[0052] Dissolve 40mg of acrylic resin in 8ml of acetone, then add 200mg of impregnated drug-loaded resin and 1ml ...

Embodiment 2

[0056] 1. Preparation of Drug Resin

[0057] Take 200 mg of ion exchange resin and add 200 ml of 5.0 mg / ml levodopa solution (dissolved in 0.001 mol / L HCl solution), and stir at room temperature for 2 hours. Wash the unbound drug on the surface of the resin with double distilled water, and dry at 60°C to obtain the drug-loaded resin.

[0058] Take 200 mg of ion exchange resin and add 200 ml of 5.0 mg / ml carbidopa solution (dissolved in 0.001 mol / L HCl solution), and stir at room temperature for 2 hours. Wash the unbound drug on the surface of the resin with double distilled water, and dry at 60°C to obtain the drug-loaded resin.

[0059] 2. Impregnation of drug resin

[0060] Take 100 mg of drug-loaded resin, add 10 ml of 20% PEG6000 solution, stir for 0.5 hour, dry and sieve to obtain impregnated drug resin.

[0061] 3. Preparation of Drug Resin Microcapsules

[0062] Dissolve 60mg of acrylic resin in 8ml of acetone, then add 200mg of impregnated drug-loaded resin and 1ml...

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Abstract

The invention discloses a levodopa / carbidopa compound sustained-release suspension and a preparation method thereof. The preparation comprises the following components in percentage by weight: 10-50% of levodopa, 10-50% of carbidopa and 10-50% of accessory realizing a sustained-release effect. Compared with a solid preparation, the suspension disclosed by the invention has the advantages that the drug is coated in resin so that the drug stability is improved; the suspension can be taken in divided dose, so that the problem that the oral solid sustained-release preparation prepared from large-dose drugs is hard to swallow is solved; in a multi-unit drug release system, the drug release action is the total of the drug release actions of particles, and the reproducibility and consistency are better; the phenomenon of excessively high local concentration often caused after the oral solid sustained-release preparation is ground can be avoided; the bad smell of the drug can be covered, and the palatability of the preparation is improved. The sustained-release preparation disclosed by the invention is to be clinically used as an anti-paralysis agitans drug.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a levodopa / carbidopa compound sustained-release suspension and a preparation method thereof. Background technique [0002] Currently, levodopa is the drug of choice for Parkinson's patients over 65 years of age and with multiple symptoms. Parkinson's disease generally begins at the age of 50 to 65, and the incidence rate gradually increases with age. With the aggravation of symptoms and complications after long-term application of drugs, the application of long-acting levodopa compound preparations is the most effective. Levodopa is the precursor compound of dopamine. After decarboxylation, dopamine is generated. Dopamine is difficult to pass through the blood-brain barrier, and the dose entering the central nervous system is only 1% of the dose. Not only the curative effect is weakened, but also the peripheral adverse reactions increase. If taken together with carbidopa, it...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/198A61K9/10A61K47/38A61K47/32A61P25/16
Inventor 刘宏飞丁慧曹进于小凤夏国华师双双
Owner JIANGSU UNIV
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