A transdermal drug delivery system comprising rivastigmine and its preparation method

A technology for a transdermal drug delivery system and a composition, applied in the field of pharmacy, can solve the problems of high cost, complicated production process, expensive silicone pressure-sensitive adhesive and the like, and achieve the effects of low cost and simple preparation process

Active Publication Date: 2019-08-09
RUNBIO BIOTECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the silicone pressure-sensitive adhesive itself is expensive, and in order to prepare such a silicone pressure-sensitive adhesive matrix layer, a specific coating process is required on the release film of the product
Therefore, the production process of "EXELON PATCH" (EXELON PATCH) is more complicated and the cost is higher

Method used

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  • A transdermal drug delivery system comprising rivastigmine and its preparation method
  • A transdermal drug delivery system comprising rivastigmine and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Get 12g rivastigmine tartrate, 16g polyvinylpyrrolidone K-90F, 22.4g diethylene glycol monoethyl ether, 2.8g ethyl lactate, 0.08g α-tocopherol, and 72g cosolvent into the conical flask, and use Ultrasonic instrument was used for ultrasonic dissolution for more than 4 hours to ensure that the solution was completely miscible, and 72g of acrylic pressure-sensitive adhesive DURO-TAK 87-2287 (containing 51% dry glue) was added, and stirred with a magnetic stirrer at 300 rpm for 4 hours. Until the solution is completely dissolved; let the solution in the Erlenmeyer flask stand for at least 1 hour or until all the bubbles disappear before use. Use a knife coater or hand-coat the obtained uniform glue onto a single-layer siliconized PET polyester film protective layer material (SCOTCH PAK 1022, 3M, St.Paul, US) and dry at 80°C for 30 minutes In order to remove the co-solvent, it is pressed with the backing layer (SCOTCH PAK 1109, 3M, St. Paul, US), punched, and packaged to obt...

Embodiment 2 to 3

[0042] The formula composition is basically the same as in Example 1, and ethyl lactate is replaced by butyl lactate di and monolauryl lactate in Example 1 respectively. The patch was prepared according to the method of Example 1 and the transdermal release rate of rivastigmine in the permeate was determined. The results are shown in Table 1.

[0043] The results in Table 1 show that Examples 1 to 3 all show good drug permeability, and wherein Example 1 has the best effect. On the other hand, when a single penetration enhancer is used, because there is no synergistic effect, the penetration enhancement effect of rivastigmine will be significantly reduced, as shown in Comparative Examples 1 to 2 in Table 1;

[0044] Table 1:

[0045]

Embodiment 4

[0047] Take 24g of rivastigmine tartrate, 16g of Eudragit RL 100, 22.4g of diethylene glycol monoethyl ether, 5.6g of lauryl lactate, 0.08g of α-tocopherol, and 72g of cosolvent into a conical flask, and use an ultrasonic instrument Ultrasonic dissolving for more than 4 hours to ensure that the solution is completely miscible, add 72g of acrylic pressure-sensitive adhesive DURO-TAK 87-2287 (containing 51% dry glue), stir with a magnetic stirrer at 300 rpm for 4 hours, according to the example The patch was prepared by the method of 1 and the transdermal release rate of rivastigmine in the permeate was measured. The results are shown in Table 2.

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Abstract

The invention discloses a rivastigmine cutaneous penetration system which comprises an acrylic pressure sensitive adhesive composition of (meth)acrylate, a penetration enhancer, an antioxidant and active medicine. The acrylic pressure sensitive adhesive composition of (meth)acrylate is composed of the mixture of at least one of acrylic pressure sensitive adhesives of (meth)acrylate containing hydroxyl and at least one of polyvinylpyrrolidone or polyalkyl methacrylate copolymer. The penetration enhancer is composed of ethylene glycol monoethyl ether and at least one of lactic acid or lactate compounds. The antioxidant is at least one of alpha-tocopherol, vitamin C palmitate or 2,6-Di-tert-butyl -p-cresol (BHT). The active medicine is rivastigmine or pharmaceutically acceptable salt thereof. The rivastigmine cutaneous penetration system is relatively simple in preparation process, high in cutaneous releasing speed and capable of keeping the enough stability, and patch products with the smaller area can be prepared.

Description

technical field [0001] The present invention relates to the field of pharmacy. In particular, it relates to a transdermal drug delivery system containing rivastigmine and a preparation method. Background technique [0002] With the aging of the population, the number of senile dementia patients is increasing year by year, becoming the fourth largest senile disease after heart, cerebrovascular diseases and malignant tumors. Most provinces and cities in China have entered into an aging population structure. According to the survey, the incidence rate of dementia patients over 60 years old is 5%, 10% over 75 years old, and 25% over 85 years old. Since the pathogenesis of senile dementia is still not very clear, there is no effective drug to completely cure senile dementia, and it only plays a role in improving cognition and delaying deterioration. Cholinesterase inhibitors are currently the mainstream drugs for the treatment of senile dementia on the market, and rivastigmine ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K47/32A61K47/10A61K47/12A61K47/14A61K47/22A61K31/27A61P25/28
CPCA61K9/7061A61K31/27A61K47/10A61K47/12A61K47/14A61K47/22A61K47/32
Inventor 杨明京吴树明
Owner RUNBIO BIOTECH CO LTD
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