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Nimudipin undertongue spraying agent

A nimodipine and spray technology, applied in the field of nimodipine dosage forms, can solve the problems of gastrointestinal side effects, unacceptable to patients, low bioavailability, etc., and achieves avoiding side effects, high bioavailability, and good patient compliance. Effect

Inactive Publication Date: 2004-09-08
张瑞琛 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The object of the present invention is to provide a kind of nimodipine sublingual spray, it is through scientific formula, and nimodipine is prepared as spray, and it can solve the low bioavailability and inconvenient use of existing technology clinically , It is difficult for patients to accept, and it has certain side effects on the gastrointestinal tract

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0009] Take 4kg of nimodipine and pulverize it to 500 mesh, sieve, take 30kg of polyethylene glycol-400 and 50kg of propylene glycol respectively, and put it on a water bath at 50°C, first dissolve nimodipine with an appropriate amount of polyethylene glycol-400, then add propylene glycol to mix Evenly, add 0.006kg of butylated hydroxytoluene (BHT) and 0.01kg of peppermint oil, mix evenly, filter and fill in a spray container.

Embodiment 2

[0011] Take 3kg of nimodipine and pulverize it to 500 mesh, sieve it, take 15kg of polyethylene glycol-400 and 20kg of propylene glycol respectively, put it on a water bath at 50°C, first dissolve nimodipine with an appropriate amount of polyethylene glycol-400, then add propylene glycol to mix Evenly, add 0.004kg of butylated hydroxytoluene (BHT) and 0.007kg of peppermint oil, mix evenly, filter and fill in a spray container.

Embodiment 3

[0013] Take 2kg of nimodipine and pulverize it to 500 mesh, sieve, take 20kg of polyethylene glycol-400 and 30kg of propylene glycol respectively, put it on a water bath at 50°C, first dissolve nimodipine with an appropriate amount of polyethylene glycol-400, then add propylene glycol to mix After diluting with 100kg of distilled water, add 0.003kg of butylated hydroxytoluene (BHT) and 0.005kg of peppermint oil, mix evenly, filter and fill in a spray container.

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PUM

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Abstract

A sublingual spray of nimodipine contains nimodipine (1-5 wt. portions), propanediol (10-50), polyethylene glycol-400 (10-30), BHT (0.001-0.01) and mint oil (0.001-0.02). Its advantages are high biological utilization rate, low dosage, and no first over effect.

Description

technical field [0001] The invention relates to the technical field of nimodipine dosage forms. Background technique [0002] Nimodipine is a second-generation pyridine calcium antagonist, which is similar to nitrendipine and nifedipine. The main difference is that although this drug can dilate blood vessels and peripheral blood vessels, it mainly dilates cerebral blood vessels selectively, and its antihypertensive effect is relatively low. Small, so it is currently used clinically for the treatment of cerebrovascular disease, that is, for ischemic cerebrovascular disease, prevention of migraine, treatment of mild or moderate hypertension, cerebral vasospasm caused by subarachnoid hemorrhage, etc. [0003] The raw material of nimodipine is light yellow crystalline powder, odorless and tasteless, easily soluble in acetone and chloroform, soluble in ethanol, slightly soluble in ether, but insoluble in water. The drug has been used as a clinical cerebrovascular drug for many y...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/12A61K31/4422A61P9/00A61P9/12
Inventor 张瑞琛陈延龙
Owner 张瑞琛
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