Sustained-release suspension preparation containing levodopa and benserazide hydrochloride and preparation method thereof

A technology of benserazide hydrochloride and suspension preparations, which is applied to medical preparations containing active ingredients, medical preparations with non-active ingredients, and pharmaceutical formulas, which can solve problems such as instability and easy oxidation and decomposition, and achieve low cost , reduce irritation, fast absorption effect

Inactive Publication Date: 2018-09-21
WUYI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the raw materials contain 2-3 phenolic hydroxyl groups, they are very unstable. They are easy to oxidize and decompose when placed in the air, and they are even more unstable in aqueous solution.

Method used

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  • Sustained-release suspension preparation containing levodopa and benserazide hydrochloride and preparation method thereof
  • Sustained-release suspension preparation containing levodopa and benserazide hydrochloride and preparation method thereof
  • Sustained-release suspension preparation containing levodopa and benserazide hydrochloride and preparation method thereof

Examples

Experimental program
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preparation example Construction

[0051] The present invention also includes a preparation method of the above-mentioned sustained-release suspension preparation, comprising the following steps:

[0052] First weigh levodopa and benserazide hydrochloride with a mass ratio of 1.5:1 to 6:1 respectively, and mix the weighed levodopa and benserazide hydrochloride with the cation exchange resin respectively to prepare two kinds of loaded drug resin, and then impregnate the above two drug-loaded resins in the impregnating agent respectively. After mixing other auxiliary materials, the sustained-release suspension preparation is obtained.

[0053] From the above description, it can be seen that the beneficial effects of the present invention are: using cation exchange resin to encapsulate the drug, and using skeleton materials and retarders to effectively realize the sustained release effect, and then adding suspending agent and other additives to prepare a suspension , can be taken in divided doses, the dose is acc...

Embodiment 1

[0061] Embodiment 1 of the present invention is: a preparation method of a sustained-release suspension preparation containing levodopa and benserazide hydrochloride, comprising the following steps:

[0062] S1. Preparation of drug-loaded resin:

[0063] Weigh 500mg The cross-sectional area of ​​RP69 resin is 4cm 2 In the dynamic exchange column, 1mg·mL -1 The hydrochloric acid solution of levodopa (dissolved in 0.01mol·L -1 HCl) into the resin column, adjust the lower hole plug to make it 1mL min -1 The flow rate is uniform, and the drug loading temperature is set to 37.0°C±0.5°C. The drug loading time is 2.5h (reaching the breakthrough point); after the drug loading is completed, the wet resin is washed three times with deionized water to remove the free drug on the surface, and finally it is put into an oven to dry at 40°C to 60°C. drug-loaded resin loaded with levodopa;

[0064] 100mg RP69 was poured into 100mL benserazide hydrochloride solution (the solvent was 0...

Embodiment 2

[0076] Example 2 of the present invention is: a preparation method of a sustained-release suspension preparation containing levodopa and benserazide hydrochloride, which differs from Example 1 only in that: the sustained-release dopaserazide in the step S4 Among the microcapsules, the drug-loaded resin microcapsules loaded with levodopa contained 150 mg of levodopa and the drug-loaded resin microcapsules loaded with benserazide hydrochloride contained 50 mg of benserazide hydrochloride, and other operations were the same as in Example 1.

[0077] The sustained-release suspension preparation containing levodopa and benserazide hydrochloride prepared by the above operations was subjected to a stability test. 1) High temperature experiment: place the prepared slow-release mixture, levodopa hydrochloric acid solution and benserazide hydrochloride solution at 60°C for 10 days at the same time, recover and detect the contents of levodopa and benserazide hydrochloride in the solution ...

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Abstract

The invention discloses a sustained-release suspension preparation containing levodopa and benserazide hydrochloride and a preparation method thereof. The sustained-release suspension preparation is prepared from cation exchange resin, levodopa, benserazide hydrochloride, an impregnating agent, plasticizers, suspending aids, framework materials, retardants and other auxiliary materials. The levodopa and the benserazide hydrochloride are firstly and respectively weighed; the weighed levodopa and the weighed benserazide hydrochloride are respectively mixed with the cation exchange resin; two kinds of medicine carrying resin are prepared; then, the two kinds of medicine carrying resin are respectively impregnated in the impregnating agent; after the impregnating is completed, the framework materials and the plasticizers are respectively used for preparing a medicine carrying resin microcapsule; finally, the suspending aids, the retardants and other auxiliary materials are added and are then mixed; the sustained-release suspension preparation is prepared. Compared with the prior art, the scheme has the advantages that the problem that old people are difficult to swallow solid medicineis solved; the adaptability of patients is obviously improved.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a sustained-release suspension preparation containing levodopa and benserazide hydrochloride and a preparation method thereof. Background technique [0002] Parkinson's syndrome is a chronic disease with a very high incidence rate at present. For Parkinson's patients over 65 years old and with multiple symptoms, levodopa (levodopa, LD) is the drug of choice in the treatment process. The onset of 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 a prodrug of dopamine, which itself has no pharmacological activity. It acts by converting into dopamine after entering the brain and increasing the amount of dopamine in the striatum. Bens...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K47/69A61K47/44A61K47/12A61K47/38A61K47/36A61K47/32A61K31/198A61P25/16A61K31/165
CPCA61K9/10A61K31/165A61K31/198A61K47/12A61K47/32A61K47/36A61K47/38A61K47/44A61K47/6951A61P25/16A61K2300/00
Inventor 刘宏飞李冬利杜仪
Owner WUYI UNIV
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