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Zolmitriptan fast-release tablet and preparation method thereof

An immediate-release tablet and tablet compression technology, which is applied in pill delivery, cardiovascular system diseases, drug combination, etc., can solve the problems of decreased renal clearance rate, etc., and achieve the effects of improving reliability and effectiveness, rapid release, and simple preparation

Inactive Publication Date: 2014-04-30
SHANGHAI TIANLONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In patients with moderate to severe renal impairment compared with healthy subjects, although the area under the curve of the parent compound and its active metabolite was only slightly increased (16% and 35%, respectively), the half-life was increased, but Zomi Renal clearance of triptan and its metabolites is reduced (7-8 times)

Method used

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  • Zolmitriptan fast-release tablet and preparation method thereof
  • Zolmitriptan fast-release tablet and preparation method thereof
  • Zolmitriptan fast-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] prescription:

[0025]

[0026] Preparation: Grind the above excipients and pass through a 60-mesh sieve; fully mix zolmitriptan and poloxamer 188, sieve and mix with calcium hydrogen phosphate and cross-linked carboxymethyl starch sodium, and dry granulate Preparation into granules includes pressing into large tablets, crushing, passing through a 14-mesh sieve for granulation, adding micro-powder silica gel to press into tablets, and the product is obtained.

Embodiment 2

[0028] prescription:

[0029]

[0030] Preparation: crush the above-mentioned excipients and pass through a 60-mesh sieve; fully mix zolmitriptan and sodium dodecyl sulfate, sieve and mix with compressible starch and low-substituted hypromellose, and add micropowder silica gel Tablets, ready to use.

Embodiment 3

[0032] prescription:

[0033]

[0034] Preparation: crush the above-mentioned auxiliary materials and pass through a 60-mesh sieve; fully mix zolmitriptan and sodium alginate, sieve and mix with lactose and cross-linked polyvinylpyrrolidone, add micro-powder silica gel to press into tablets, and obtain the product.

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PUM

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Abstract

The invention provides a zolmitriptan fast-release tablet, comprising the active component zolmitriptan, one or more selected from the group consisting of a filler, a disintegrating agent, a binder, a lubricant, a flow aid, a flavoring agent, a smell adjusting agent and a coloring agent, and a release promoter capable of promoting release of the active component. The release promoter may be selected from the group consisting of sodium dodecyl sulfate, poloxamer, Tweens, brominated cetane trimethylamine, sodium lauryl sulfate, stearyl alcohol sulfonate, polyoxyethylene high-grade fatty alcohol, sucrose ester, sorbitol fatty ester, soyabean lecithin, alginic acid, sodium alginate and colloid aluminium-magnesium silicate; and the usage amount of the release promoter is 0.1 to 5% of the total weight of the tablet.

Description

technical field [0001] The present invention relates to a solid oral preparation for the treatment of cardiovascular diseases, such as myocarditis, cardiomyopathy, ischemic encephalopathy and other diseases, in particular to a rapid-release zolmitriptan tablet, and the present invention also relates to the Method for the preparation of tablets. Background technique [0002] Zolmitriptan chemical name: (S)-4-[3-[2-(dimethylamino)ethyl]-1H-indole-5-methyl]-2-oxazolidinone, is A selective 5-HTIB / ID receptor agonist. It is clinically used for the treatment of migraine with aura or non-aura in adults. Its therapeutic effect is through stimulating the 5-HTIB / ID receptors on intracranial blood vessels (including arteriovenous anastomoses) and sympathetic nerves of the trigeminal nervous system, causing intracranial vasoconstriction and inhibiting the release of pro-inflammatory neuropeptides. [0003] Zolmitriptan is rapidly absorbed after oral administration. It can reach 75% ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/422A61P9/10
Inventor 丁杰
Owner SHANGHAI TIANLONG PHARMA
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