Nimodipine oral fast dissolving tablets and preparation method thereof

A nimodipine buccal, nimodipine technology, applied in nimodipine buccal instant tablets and its preparation field, can solve the problems of unacceptable and inconvenient use for patients, achieve simple preparation process, easy industrial production, avoid gastric Effects of intestinal first-pass

Inactive Publication Date: 2011-04-27
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] When nimodipine tablets and capsules are administered orally, they will be metabolized by the liver before being absorbed through the gastrointestinal tract, enter the surrounding capillaries or lymphatic vessels, and then enter the blood circulation. There is a long period of absorption an

Method used

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  • Nimodipine oral fast dissolving tablets and preparation method thereof
  • Nimodipine oral fast dissolving tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (1) Preparation of nimodipine solid dispersion: take nimodipine and polyvinylpyrrolidone in a ratio of 1:3, dissolve together in absolute ethanol, and ultrasonically mix the mixed solution for 15 minutes to form a uniform transparent liquid, then this The mixed solution is placed in a spray dryer for spray drying, and the dry powder is collected to obtain a nimodipine solid dispersion. The parameters of the spray dryer are set as: feed flow rate 20ml / min; spray pressure 7bar; atomizer rotation speed 50Hz; inlet air temperature 55-65°C; outlet air temperature 40-50°C.

[0030] (2) Preparation of nimodipine oral instant tablet: take 80 grams of nimodipine solid dispersion, 40 grams of microcrystalline cellulose, 24 grams of sodium bicarbonate, 30 grams of cross-linked polyvinylpyrrolidone, 10 grams of citric acid, cyclamate 10 grams, 5 grams of micropowder silica gel and 1 gram of magnesium stearate, after sieving and mixing evenly, use the powder direct compression metho...

Embodiment 2

[0034] (1) Preparation of nimodipine solid dispersion: take nimodipine and polyvinylpyrrolidone in a ratio of 1:6, dissolve together in absolute ethanol, and ultrasonically mix the mixed solution for 15 minutes to form a uniform transparent liquid, and then this The mixed solution is placed in a spray dryer for spray drying, and the dry powder is collected to obtain a nimodipine solid dispersion. The parameters of the spray dryer are set as: feed flow rate 20ml / min; spray pressure 7bar; atomizer rotation speed 50Hz; inlet air temperature 55-65°C; outlet air temperature 40-50°C.

[0035] (2) Preparation of nimodipine oral instant tablet: take 140 grams of nimodipine solid dispersion, 84 grams of microcrystalline cellulose, 40 grams of sodium bicarbonate, 84 grams of cross-linked polyvinylpyrrolidone, 20 grams of citric acid, cyclamate 20 grams, 10 grams of micro-powdered silica gel and 2 grams of magnesium stearate, sieved and mixed evenly, and compressed by direct powder compr...

Embodiment 3

[0039] (1) Preparation of nimodipine solid dispersion: take nimodipine and polyethylene glycol in a ratio of 1:3, dissolve them in absolute ethanol together, and ultrasonically mix the mixed solution for 15 minutes to form a uniform transparent liquid, and then mix The mixed solution is placed in a spray dryer for spray drying, and the dry powder is collected to obtain a nimodipine solid dispersion. The parameters of the spray dryer are set as: feed flow rate 20ml / min; spray pressure 7bar; atomizer rotation speed 50Hz; inlet air temperature 55-65°C; outlet air temperature 40-50°C.

[0040] (2) Preparation of nimodipine oral instant tablet: take 80 grams of nimodipine solid dispersion, 32 grams of microcrystalline cellulose, 22 grams of sodium bicarbonate, 40 grams of cross-linked polyvinylpyrrolidone, 10 grams of citric acid, cyclamate 10 grams, 5 grams of micropowder silica gel and 1 gram of magnesium stearate, after sieving and mixing evenly, use the powder direct compressio...

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Abstract

The invention belongs to the field of medicinal preparations. Nimodipine serving as a clinical cerebrovascular medicament is applied for years; however, the nimodipine has the defects of poor water solubility, obvious first pass effect and the like due to the physicochemical property of the nimodipine, which directly influence clinical medicinal effect. The invention provides nimodipine oral fast dissolving tablets and a preparation method thereof. The preparation method comprises the following steps of: preparing a nimodipine solid dispersion with high water solubility from a nimodipine raw material and a hydrophilic carrier by a spray drying process; mixing the solid dispersion and suitable auxiliary materials; and preparing the oral fast dissolving tablets by a direct powder compression method. The preparation process is simple and industrial production is easy to realize. The prepared nimodipine oral fast dissolving tablets can be administrated without water. After being administrated, the nimodipine oral fast dissolving tablets are rapidly dissolved and absorbed in an oral cavity in 30 seconds so as to avoid the first pass effect of the gastrointestinal tract, greatly improve the dissolution rate of the medicament and improve the bioavailability of the medicament.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an oral instant tablet of nimodipine and a preparation method thereof. Background technique: [0002] Nimodipine, also known as nifedipine, is a second-generation pyridine calcium antagonist. At present, it is mostly used in clinical treatment of cerebrovascular disease, namely for ischemic cerebrovascular disease, treatment of mild or moderate hypertension, prevention and treatment of cerebral vasospasm, sudden deafness, migraine after subarachnoid hemorrhage, etc. . [0003] Nimodipine has been used as a clinical cerebrovascular drug for many years, but due to its own physical and chemical properties, it has shortcomings such as poor water solubility and obvious first-pass effect, which directly affects the clinical efficacy. On the one hand, the saturated solubility of the hydrophobic drug nimodipine in water is only 4 μg / ml. After entering the body, m...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4422A61K47/38A61P9/10A61P9/12A61P25/06
Inventor 钟延强张翮杨凌鲁莹邹豪陈琰俞媛高静刘俊杰孙治国
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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