Nimodipine capsule containing semi-solid combination and preparation

A technology for nimodipine capsules and nimodipine solids, which is applied in the field of pharmaceutical preparations, can solve the problems of reduced dissolution rate, low dissolution rate, easy aging, etc., and achieves the effects of increased dissolution rate, fast dissolution rate, and easy aging.

Inactive Publication Date: 2008-09-03
武汉星福海药业有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Purpose of the invention: the present invention provides a kind of content is the high dissolution rate nimodipine capsule of semi-solid composition and preparation method thereof, and its purpose is to solve the low dissolution rate of nimodipine drug in the past and existing nimodipine solid dispersion The body is easy to age, resulting in problems such as a decrease in dissolution rate

Method used

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  • Nimodipine capsule containing semi-solid combination and preparation

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Effect test

Embodiment 1

[0024] Embodiment 1: prepare nimodipine capsule according to the following steps:

[0025] a. the preparation of nimodipine solid dispersion: take copovidone S630 and Eudragit E100 as carrier, get 3 parts of micronized nimodipine, 5 parts of Eudragit E100 and 2 parts of copovidone S630 (by weight ), after uniform mixing, add to the feeding hopper of the twin-screw melting extruder, set the temperature in the first zone to 115°C, the temperature in the second, third, and fourth zones are all 130°C, and the number of revolutions is 36 rpm, and the extrudate is placed in ( -70) ℃ refrigerator quenching, crushing, passing through a 120-mesh sieve to obtain nimodipine solid dispersion.

[0026] b. The preparation of nimodipine capsules: get semi-solid matrix copovidone S630 / 72g, polyoxyethylene sorbitan fatty acid ester (Tween 80) / 96g, semi-solid matrix polyethylene glycol 400 / 360g, polyethylene glycol Diol 6000 / 8.4g, heat and stir at 90°C, add nimodipine solid dispersion powder / 1...

Embodiment 2

[0028] Embodiment 2: prepare nimodipine capsule according to the following steps:

[0029] a. Preparation of Nimodipine Solid Dispersion: Take copovidone S630 as carrier, get 2 parts of micronized nimodipine and 8 parts of copovidone S630 (by weight), after uniform mixing, add twin-screw melt extrusion In the feeding hopper of the machine, set the temperature of the first zone to 115°C, the temperature of the second, third, and fourth zones to be 125°C, and the number of rotations to be 30 rpm, and put the extruded product in a (-30)°C refrigerator to quench, crush, and pass through 100 mesh sieve to obtain nimodipine solid dispersion.

[0030] b. Preparation of Nimodipine Capsules: Take sorbitan fatty acid lipid (Span 60) / 120g, semi-solid matrix polyethylene glycol 400 / 300g, glycerin / 72g, polyethylene glycol 8000 / 12g, and heat at 80°C After stirring evenly, add nimodipine solid dispersion powder / 120g, continue to stir until uniform, cool down to 60°C, and quantitatively fill...

Embodiment 3

[0031] Embodiment 3: prepare nimodipine capsule according to the following steps:

[0032]a. Preparation of Nimodipine Solid Dispersion: Take Acrylic Resin No. 4 as carrier, get 3 parts of micronized Nimodipine, 7 parts of Acrylic Resin No. 4 (by weight), after uniform mixing, add single-screw melt extrusion In the feeding hopper of the machine, set the temperature of the first zone to 105°C, the temperature of the second, third, and fourth zones to be 135°C, and the number of rotations to be 24 rpm. The extruded product is cooled at room temperature, crushed, and passed through a 100-mesh sieve to obtain Ni Modipine solid dispersion.

[0033] b. Preparation of Nimodipine Capsules: Take poloxamer 188 / 120g, glycerin 300g, heat and stir at 75°C until uniform, add nimodipine solid dispersion powder / 120g, continue to stir until uniform, cool to 70°C, The liquid-filled capsule filling machine quantitatively fills the contents into cellulose capsules, each capsule contains about 45...

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Abstract

The invention discloses a nimodipine capsule with high dissolution and semi-solid composition as content and a preparation method thereof, and belongs to the pharmaceutical preparation field. The method comprises the following steps of mixing micronized nimodipine and a hydrophilic carrier, preparing into solid dispersion by melting extrusion method, cooling, pulverizing, mixing with semi-solid matrix, surfactant, melting point regulator under heating, and filling the content into hard capsule with a capsule filling machine. The invention combines the melting extrusion technique and semi-solid filling hard capsule technique, and after the prepared novel nimodipine capsule is administered into human body, the nimodipine quickly diffuses in molecular form and saturates metabolic enzymes, so as to improve bioavailability. The inventive nimodipine capsule solves the low dissolution and low utilization ratio problems of prior nimodipine preparation; and has the advantages of high dissolution, good stability, simple preparation method, and applicability to industrial production.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a high-dissolution nimodipine capsule whose content is a semisolid composition and a preparation method thereof. Background technique: [0002] Using solid dispersion technology to improve the dissolution rate of poorly water-soluble drugs is a relatively effective method that is more commonly used in recent years. Solid dispersion refers to the dispersion system formed by uniformly dispersing the drug in a certain solid carrier substance in the state of molecule, colloid, amorphous, microcrystalline and so on. The rapid release mechanism is that the dissolution rate of the drug is closely related to its specific surface area, that is, the larger the specific surface area of ​​the drug per unit volume, the higher the dissolution rate, and the carrier itself can promote the dissolution of the drug. In recent years, focusing on the convenience of industrial ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/66A61K31/435A61K9/48A61P9/10A61P9/12A61P25/28
Inventor 李从福唐星孙蕴哲
Owner 武汉星福海药业有限公司
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