Rizatriptan drug absorbed through mouth mucosa

A technology of oral mucosa and rizatriptan, which is applied in the field of rizatriptan medicine, can solve the problem of affecting the efficacy of the drug and patient compliance, which is only 13-28%, and achieves the avoidance of the first-pass effect, rapid onset of action, and ease of use. convenient effect

Inactive Publication Date: 2013-06-19
重庆市力扬医药开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to reports, the first-pass effect of oral administration of rizatriptan benzoate is obvious, the bioavailability is 45%, and the headache relief rate is only 13-28% after oral administration for 30 minutes, which affects the efficacy of the drug and patient compliance to a certain extent

Method used

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  • Rizatriptan drug absorbed through mouth mucosa
  • Rizatriptan drug absorbed through mouth mucosa
  • Rizatriptan drug absorbed through mouth mucosa

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1 sublingual tablet

[0023] composition:

[0024]

[0025]

[0026] Preparation method: crush the raw material of rizatriptan benzoate, Tablettose 80, Ludipress and other auxiliary components through a 100-mesh sieve, mix evenly, and directly compress the tablet.

Embodiment 2

[0027] Embodiment 2 sublingual tablet

[0028] composition:

[0029]

[0030] Preparation method: Mix the prescription amount of rizatriptan benzoate with auxiliary ingredients such as pregelatinized starch and microcrystalline cellulose, add 0.4% xanthan gum aqueous solution, granulate, dry, granulate, add external cross-linked polymer Vitamin ketone and talcum powder are mixed evenly and compressed into tablets.

Embodiment 3

[0031] Embodiment 3 sublingual tablet

[0032] composition:

[0033]

[0034] Preparation method: The raw material of rizatriptan benzoate and auxiliary ingredients such as MicroceLac 100 and microcrystalline cellulose are pulverized through a 100-mesh sieve, mixed evenly, and directly compressed into tablets.

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Abstract

Disclosed is a rizatriptan drug absorbed through mouth mucosa. Malic acid rizatriptan is an effective drug ingredient, and the rizatriptan drug absorbed through mouth mucosa is jointly composed of malic acid rizatriptan and auxiliary ingredients which are acceptable in a mouth mucosa drug, wherein the auxiliary ingredients comprise a disintegrating agent, a filling agent, a flavoring agent, a bonding agent, a mucosa sorbefacient and a lubricating agent. Preparation forms of specific drugs comprise sublingual tablets, lozenges, mouth and check lozenges, mouth adhering tablets and mouth pasting tablets and the like. The drug can be completely or mainly absorbed through mouth mucosa such as hypogloeeis mucosa and / or mouth and cheek mucosa and is non-irritant to a mouth. Bioavailability and the curative effect of the drug can be obviously improved, and the rizatriptan drug absorbed through mouth mucosa can be taken conveniently, so that a patient is enabled to take the drug obediently.

Description

technical field [0001] The invention relates to a drug absorbed through the oral mucosa, specifically a rizatriptan drug that can be absorbed through the oral mucosa, including sublingual tablets, buccal buccal tablets, buccal tablets, oral adhesive tablets and oral patches Drug preparations that can be completely or mainly absorbed by oral mucosa such as sublingual mucosa and / or buccal mucosa. Background technique [0002] Migraine is a chronic neurovascular disorder, characterized by diffuse or unilateral attacks, severe pain, and recurrent attacks. Around the world, about 15% to 18% of women and 6% to 9% of men experience migraine every year; in my country, the incidence of migraine is 4.2% to 14.6%. Triptans are a new generation of migraine drugs that selectively agonize 5-HT 1B / D1 The receptor has strong specificity and clear efficacy. Since the first triptan-type migraine treatment drug sumatriptan was launched in February 1991, this type of drug has become the first...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4196A61P25/06
Inventor 刘星王显著吉杰标黄毅
Owner 重庆市力扬医药开发有限公司
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