Rotigotine hydrochloride or free alkali film-forming gel preparation and preparation method thereof

A technology of gel preparation and hydrochloride, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., which can solve the problem of large adverse reactions, instability, and low bioavailability of patches and other problems, to achieve the effect of good transdermal absorption, smooth gel, and good air permeability

Inactive Publication Date: 2012-06-20
长春斯菲尔生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The invention provides a film-forming gel preparation of rotigotine, which is applied externally and administered through the skin, which solves the problem of low bioavailability of rotigotine oral preparations (bioavailability can reach 50%) and large adverse reactions of patches. Unstable Disadvantages

Method used

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  • Rotigotine hydrochloride or free alkali film-forming gel preparation and preparation method thereof
  • Rotigotine hydrochloride or free alkali film-forming gel preparation and preparation method thereof
  • Rotigotine hydrochloride or free alkali film-forming gel preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Rotigotine film-forming gel formulation

[0030] Prepare the gel (by 100g) according to the following recipe:

[0031] Rotigotine Free Base 0.5g, Hydroxypropyl Cellulose 2.5g, Carbomer 934 0.5g, Silicone Elastomer SF600A (Guangzhou Biaomei Company) 5.0g, Glycerin 20.0g, Triethanolamine 0.5g, Ethanol 10ml, The remainder is distilled water.

[0032] Weigh 0.5g of carbomer 934 and 2.5g of hydroxypropyl cellulose, mix and sprinkle into 60ml of deionized water to swell naturally. The next day, add 0.5g triethanolamine to adjust the pH to neutrality, weigh 0.5g rotigotine free base and dissolve it in 10ml absolute ethanol, stir and dissolve, slowly add it dropwise to the above gel, weigh 5.0g silicone elastic Body SF600A (Guangzhou Biaomei Co., Ltd.), 20.0g glycerin, add water to make up to 100g, add it to the gel, stir and mix well, that's it.

Embodiment 2

[0034] Rotigotine film-forming gel formulation

[0035] Prepare the gel (by 100g) according to the following recipe:

[0036] Rotigotine free base 1.0g, hydroxyethyl cellulose 0.5g, carbomer 934 10.0g, silicone elastomer ST-Elastomer 10 (Dow Corning) 3.0g, glycerin 15.0g, triethanolamine 5.0g, ethanol 15ml , the remainder is distilled water.

[0037] Weigh 10.0g of carbomer 934 and 0.5g of hydroxyethyl cellulose, mix and evenly sprinkle it into 60ml of deionized water to swell naturally. The next day, an appropriate amount of triethanolamine (about 5.0 g) was added to adjust the pH to neutrality. 1.0 g of rotigotine free base was weighed and dissolved in 15 ml of absolute ethanol. After stirring and dissolving, it was slowly added dropwise to the above gel. g silicone elastomer ST-Elastomer 10 (Dow Corning Corporation), 15.0 g of glycerin, add water to make up to 100 g, add it to the gel, stir and mix, and that’s it.

Embodiment 3

[0039] Rotigotine film-forming gel formulation

[0040]Prepare the gel (by 100g) according to the following recipe:

[0041] Rotigotine Free Base 2.0g, Hypromellose 1.0g, Carbomer 940 9.0g, Silicone Elastomer ST-Elastomer 10 (Dow Corning) 2.0g, Glycerin 5.0g, Triethanolamine 4.0g, Ethanol 18ml, the balance is distilled water.

[0042] Weigh 9.0g of carbomer 934 and 1.0g of hydroxypropyl methylcellulose, mix and sprinkle into 60ml of deionized water to swell naturally. The next day, an appropriate amount of triethanolamine (about 4.0 g) was added to adjust the pH to neutrality, and 2.0 g of rotigotine free base was weighed and dissolved in 18 ml of absolute ethanol. g silicone elastomer ST-Elastomer 10 (Dow Corning), add 5.0 g of glycerol, add water to make up to 100 g, add it to the gel, stir and mix well, and that’s it.

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Abstract

The invention provides rotigotine hydrochloride or free alkali film-forming gel preparation and a preparation method thereof. The rotigotine hydrochloride or free alkali film-forming gel preparation is prepared according to the following steps: mixing a gel matrix and a film-forming matrix uniformly, and adding into deionized water to swell naturally; adding a pH value adjusting agent to adjust the pH value until the pH value of the mixture is neutral; dissolving rotigotine free alkali into anhydrous alcohol, stirring to dissolve, and dropwise adding the solution into gel slowly; adding waterinto organosilicon elastomers and glycerin to supplement the organosilicon elastomers and the glycerin until the organosilicon elastomers and the glycerin reach the prescription dosage; adding the organosilicon elastomers and the glycerin into the gel, stirring and mixing uniformly. Due to the adoption of the adopted gel matrix, the film-forming matrix and the organosilicon elastomer gel, the percutaneous absorption amount of rotigotine can be greatly improved by about 5 times compared with the prior art, the rotigotine can take effect to the whole body, the continuous and stable release of the rotigotine can be ensured, the fluctuation of the concentration of the rotigotine, which is caused by intravenous pulsatile delivery of the rotigotine, can be avoided or reduced, the dyskinesias can be alleviated or delayed, and the life quality of the patient with Parkinson's disease can be greatly improved.

Description

technical field [0001] The present invention is an improvement to the dosage form of rotigotine, and further discloses a film-forming gel preparation of rotigotine hydrochloride or free alkali. The present invention also provides a preparation method of the preparation, which belongs to medical pharmacy technology field. Background technique [0002] Drug Rotigotine (-)-(S)-2-[N-Propyl-N-[2-(2-thiophene)ethyl]amino]-5-hydroxy-1,2,3,4-tetra Hydronaphthalene is a dopamine receptor agonist that can be used to treat Parkinson's disease. Clinical studies have proved that rotigotine cannot be simply administered orally because it is inactivated by the first-pass effect of the liver after it enters the body orally. If the drug is given by ordinary injection, as a long-term treatment drug, one or more injections per day will obviously increase the pain and discomfort of the patient, and there is evidence that pulsatile drug administration will cause the clinical manifestation of "...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/381A61K47/38A61K47/34A61P25/16
Inventor 李想刘伟刘喜明史亚楠孙凤英李又欣
Owner 长春斯菲尔生物科技有限公司
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