Oral nifedipine slow-release preparation and preparation method thereof

A technology of nifedipine and sustained-release preparations, which is applied in the field of medicine, can solve the problems of rapid release of dropping pills and lack of sustained-release characteristics, and achieve the effects of increasing drug dissolution, oral bioavailability, and increasing solubility or wettability Effect

Inactive Publication Date: 2009-04-29
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This kind of drop pill is suitable for oral and buccal administration, but both polyethylene glycol and poloxamer are water-soluble excipients, so the prepared drop pill has a relatively fast release rate and does not have sustained-release characteristics

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] The capsule of present embodiment 1 contains following composition by weight percentage:

[0056] Nifedipine................................4%

[0057] Gelucire 50 / 13................80%

[0058] Stearic acid .................................6%

[0059] Starch .............................10%

[0060] Preparation method: Melt nifedipine, Gelucire 50 / 13, and stearic acid in proportion and mix them uniformly, add a proportional amount of starch, mix uniformly, pour into capsules, and cool at room temperature to obtain nifedipine sustained-release capsules. Starch is an insoluble material, which can stabilize the solid dispersion and inhibit aging. Gelucire 50 / 13 is the matrix material in this formulation, and stearic acid acts as a blocker to further control the release rate of nifedipine. The drug is dispersed in the matrix material, and the release of the drug depends on the diffusion rate of the drug and the dissolution rate of the matrix.

Embodiment 2

[0062] The capsule of present embodiment 2 contains following composition by weight percentage:

[0063] Nifedipine................................4%

[0064] Gelucire 50 / 13................85%

[0065] Cetyl Alcohol................................8%

[0066] Starch................................3%

[0067] Preparation method: Melt nifedipine, Gelucire 50 / 13, and cetyl alcohol in proportion and mix them uniformly, add a proportional amount of starch, mix uniformly, pour into capsules, and cool at room temperature to obtain nifedipine sustained-release capsules. Starch is an insoluble material, which can stabilize the solid dispersion and inhibit aging. Gelucire 50 / 13 is the matrix material in this preparation, and cetyl alcohol is used as a blocker to further control the release rate of nifedipine. The drug is dispersed in the matrix material, and the release of the drug depends on the diffusion rate of the drug and the dissolution rate of the matrix.

Embodiment 3

[0069] The capsule of present embodiment 3 contains following composition by weight percentage:

[0070] Nifedipine................................4%

[0071] Gelucire 50 / 13................80%

[0072] Cetyl Alcohol................................10%

[0073] Hydroxypropyl Methyl Cellulose...................6%

[0074] Preparation method: Melt nifedipine, Gelucire 50 / 13, and cetyl alcohol in proportion and mix them evenly, add a proportional amount of hydroxypropyl methylcellulose (5cps), mix evenly, pour into capsules, cool at room temperature, and obtain Nifedipine extended-release capsules. Hydroxypropyl methylcellulose plays a certain role in stabilizing the solid dispersion and inhibiting aging. Gelucire 50 / 13 is the matrix material in this preparation, and cetyl alcohol is used as a blocker to further control the release rate of nifedipine. The drug is dispersed in the matrix material, and the release of the drug depends on the diffusion rate of the drug and the dis...

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Abstract

The invention provides an oral nifedipine sustained-release preparation which comprises the following ingredients by weight: 4 percent to 30 percent of nifedipine, 50 percent to 85 percent of excipients which have sustained-release function and are acceptable in pharmacy, and other medical excipients, the amount of which ranges from a proper amount to 100 percent and are acceptable in the pharmacy. Nifedipine sustained-release capsules of the invention can not only improve the solubility of the nifedipine in water, but also continuously release the nifedipine. The invention also provides a preparation method of the oral nifedipine sustained-release preparation, which comprises the step of evenly blending the nifedipine, the excipients which have sustained-release function and are acceptable in the pharmacy and other excipients acceptable in the pharmacy.

Description

technical field [0001] The invention relates to the technical field of medicine. Specifically, the present invention relates to an oral nifedipine sustained-release preparation and a preparation method thereof. Background technique [0002] The chemical name of nifedipine is: 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydro-3,5-dimethyl pyridinedicarboxylate, which is widely used clinically. Vascular drugs, which belong to the class of calcium channel antagonist drugs, are mainly suitable for the treatment of patients with hypertension and angina pectoris. And is listed as the drug of choice for the treatment of coronary heart disease, angina pectoris and hypertension. However, since the 1980s, it has been confirmed by medical practice that common preparations of nifedipine reflexively cause increased heart rate and activate the sympathetic nervous system, which is not conducive to the control of myocardial ischemia and heart failure, while long-acting calcium antagonists have a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4422A61K9/52A61K47/34A61P9/10A61P9/12A61K47/14
Inventor 王成港李桂龙王春龙刘衡阎卉龚莉
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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