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Levodopa / benserazide hydrochloride compound sustained-release suspension and preparation method thereof

A technology of benserazide hydrochloride and levodopa, which is applied in directions such as pharmaceutical formulations, medical preparations containing active ingredients, and emulsion delivery, to achieve the effects of solving difficulty in swallowing and being convenient to take.

Inactive Publication Date: 2014-07-30
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

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0033] 2. Impregnation of drug resin

[0034] Take an appropriate amount of drug-loaded resin, add it to 20% PEG6000 aqueous solution, stir for 0.5 hour, dry and sieve to obtain impregnated drug resin.

[0035] 3. Preparation of Drug Resin Microcapsules

[0036] The acrylic resin is dissolved in acetone, then the impregnated drug-loaded resin and PEG400 are added, stirred for a certain period of time, and the latter two are evenly dispersed to form a suspension. Add this suspension to the homogeneously mixed liquid paraffin and span80 mixture under stirring conditions, then stir in a water bath at 30°C for 4 hours, filter the obtained microcapsules with suction, wash with petroleum ether, and store at 40°C Drying under heat to obtain drug resin microcapsules.

[0037] 4. Preparation of Drug Resin Microcapsule Suspension

[0038] Take a certain amount of drug-resin microcapsules, an appropriate amount of suspending agent (one or more of PVP, HPMC, tragacanth gum, Carbopol, A...

Embodiment 1

[0046] 100 mg of the drug-loaded resins were taken, respectively added to 10 ml of 20% PEG6000 aqueous solution, stirred for 0.5 hour, dried and sieved to obtain impregnated drug resins.

[0047] 3. Preparation of Drug Resin Microcapsules

[0048] Dissolve 40mg of acrylic resin in 8ml of acetone, then add 200mg of impregnated levodopa resin and 1ml of PEG400, and magnetically stir for a certain period of time to disperse the latter two evenly to form a suspension. Add this suspension to the mixed solution of 24ml liquid paraffin and 1ml span80 which has been mixed homogeneously under the condition of stirring, then stir in a water bath at 30°C for 4 hours, filter the obtained microcapsules with suction, wash with petroleum ether, and in Dry at 40°C to obtain drug resin microcapsules.

[0049] Dissolve 50mg of acrylic resin in 8ml of acetone, then add 200mg of impregnated benserazide hydrochloride resin and 1ml of PEG400, and stir magnetically for a certain period of time to d...

Embodiment 2

[0055] 2. Impregnation of drug resin

[0056] Take 100 mg of the drug-loaded resin, add 10 ml of 20% PEG6000 solution, stir for 0.5 hour, dry and sieve to obtain the impregnated drug resin.

[0057] 3. Preparation of Drug Resin Microcapsules

[0058] Dissolve 60mg of acrylic resin in 8ml of acetone, then add 200mg of impregnated levodopa resin and 1ml of PEG400, and stir for a certain period of time to disperse the latter two evenly to form a suspension. Add this suspension to the mixed solution of 24ml liquid paraffin and 1ml span80 which has been mixed homogeneously under the condition of stirring, then stir in a water bath at 30°C for 4 hours, filter the obtained microcapsules with suction, wash with petroleum ether, and in Dry at 40°C to obtain drug resin microcapsules.

[0059] Dissolve 75mg of acrylic resin in 8ml of acetone, then add 200mg of impregnated benserazide hydrochloride resin and 1ml of PEG400, and stir for a certain period of time to disperse the latter two e...

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Abstract

The invention discloses a levodopa / benserazide hydrochloride compound sustained-release suspension. The preparation contains by weight 10-50% of levodopa, 10-50% of benserazide hydrochloride and 10-50% of accessories. Compared with a solid preparation, the invention has the following advantages: the drug is coated in resin to improve drug stability; the preparation can be taken by doses to solve the problem that a large dose of drug prepared into an oral solid sustained release preparation is difficult to swallow; a multiple unit drug delivery system, in which drug release behavior is the sum of the drug release behavior of each particle, has better reproducibility and consistency; the preparation can avoid the situation of high local concentration caused by fragmentation of the oral solid sustained release preparation, and can cover the adverse taste of drugs and increase palatability. The sustained release preparation provided by invention can be used clinically as an anti-parkinsonian drug.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a levodopa / benserazide hydrochloride 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. [0003] At present, there are patents related to levodopa / benserazide hydrochloride; the Chinese patent application whose publication number is CN101623278 discloses a "medicine composition containing levodopa and benserazide hydrochloride"; the Chinese patent application whose publication number is CN101879153A The patent application discloses a "a combination of levodopa methyl ester and benserazide mixed drug sustained-release microsphere composition and its preparation method". [0004] The above domestic and foreign patents have not yet seen reports on the compound sustained-release suspension preparation of levodopa / b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/198A61K9/10A61P25/16A61K31/165
Inventor 刘宏飞丁慧曹进于小凤朱源师双双
Owner JIANGSU UNIV
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