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Solid dispersed Nimoldipine tablet and its prepn process

A nimodipine solid and dispersed technology is applied in the fields of nimodipine solid dispersible tablets and preparation thereof, calcium channel antagonist tablets containing active component nimodipine and preparation thereof, and calcium channel antagonist tablets, It can solve the problems of obvious first-pass effect, loss of first-pass effect, poor water solubility, etc., and achieve the effect of improving drug effect, small loss and improving dissolution.

Inactive Publication Date: 2005-04-27
SHANGHAI NEW ASIATIC PHARMA MINHANG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drug has been used as a clinical cerebrovascular drug for many years, but due to its own physical and chemical properties, it has disadvantages such as poor water solubility and obvious first-pass effect, which directly affect the clinical efficacy.
It has been clinically proven that due to the difference in the preparation process and dosage form of nimodipine, there is a large gap in their bioavailability and vasodilation efficacy. The nimodipine tablets and capsules of the traditional preparation process are absorbed through the gastrointestinal tract and need to undergo The liver metabolizes, enters the surrounding capillaries or lymphatic vessels, and then enters the blood circulation. There is a long-term absorption and distribution process in the middle, and the drug loses about 80% in the whole process. The first-pass effect is very obvious.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] 1. Mix 5g of nimodipine and 40g of povidone K30 in a heating pot;

[0019] 2. Add 110g of ethanol and heat to 65°C to dissolve;

[0020] 3. Add 55g of cross-linked polyvinylpyrrolidone to absorb and sieve to granulate, dry at 60°C, granulate, compress into tablets, and coat.

Embodiment 2

[0022] 1. Mix 10g of nimodipine and 45g of povidone K30 in a heating pot;

[0023] 2. Add 110g of ethanol and heat to 65°C to dissolve;

[0024] 3. Add 45g of cross-linked polyvinylpyrrolidone to absorb and sieve to granulate, dry at 60°C, granulate, compress into tablets, and coat.

Embodiment 3

[0026] 1. Mix 15g of nimodipine and 35g of povidone K30 in a heating pot;

[0027] 2. Add 110g of ethanol and heat to 65°C to dissolve;

[0028] 3. Add 50g of cross-linked polyvinylpyrrolidone to absorb and sieve to granulate, dry at 60°C, granulate, compress into tablets, and coat.

[0029] In the 15% ethanol medium of the present invention, the dissolution rate in vitro is 89.76%, while that of domestic similar products is only 30.04%.

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PUM

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Abstract

The present invention relates to solid dispersed Nimoldipine tablet and features that solid dispersed Nimoldipine tablet is prepared with Nimoldipine in 5-15 wt%, polyvidon K30 in 25-45 wt% and cross-linked PVP in 45-65 wt%, and through the following steps: heating and mixing Nimoldipine and polyvidon K30, adding alcohol in 1.1 times and heating to 65-70 deg.c for dissolving, adding cross-linked PVP for adsorption, sieving and pelletizing, drying and finishing at 55-65 deg.c, tabletting and coating. The present invention has the advantages of raised intracorporal leaching rate of Nimoldipine, less loss of the medicine during absorption and raised medicine effect.

Description

technical field [0001] The invention relates to a nimodipine solid dispersion tablet and a preparation method thereof, relates to a calcium channel antagonist tablet, in particular to a calcium channel antagonist tablet containing nimodipine as an active component and a preparation method thereof, which can be used for treating Cerebral infarction, migraine, stroke, arachnoid hemorrhage and sudden deafness belong to the technical field of nimodipine tablets. Background technique [0002] Nimodipine is a dihydropyridine calcium channel antagonist. Its action is characterized by being able to pass through the blood-brain barrier and effectively acting on the cerebrovascular. It has obvious effects on the treatment of cerebral infarction, migraine, stroke, arachnoid hemorrhage and sudden deafness. It also has a great effect on promoting memory enhancement and the treatment of senile dementia. [0003] The raw material of nimodipine is light yellow crystalline powder, odorless ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4422A61P9/10A61P25/06A61P27/16
Inventor 安惠声
Owner SHANGHAI NEW ASIATIC PHARMA MINHANG
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