Nimodipine pulse sustained release mircopill preparation and preparing method thereof

A technology of sustained-release pellets and pulses, which is used in pharmaceutical formulations, medical preparations containing active ingredients, cardiovascular system diseases, etc. problems, to achieve the effect of reducing the frequency of medication, reducing side effects, and facilitating medication

Active Publication Date: 2008-07-30
SHENZHEN SOUTH CHINA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the large daily dosage of nimodipine, which is almost insoluble in water, and the particularity of other physical and chemical properties, the release rate of the drug is difficult to control, and it is difficult to make a pulse sustained-release preparation that is administered once a day and has time characteristics.

Method used

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  • Nimodipine pulse sustained release mircopill preparation and preparing method thereof
  • Nimodipine pulse sustained release mircopill preparation and preparing method thereof
  • Nimodipine pulse sustained release mircopill preparation and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1. nimodipine contains pill core, and composition is as follows:

[0047] Nimodipine 24g

[0048] Lactose 41g

[0049] Microcrystalline Cellulose 20g

[0050] Bolosham 4g

[0051] water 30g

[0052] Preparation:

[0053] Mix nimodipine, lactose, and microcrystalline cellulose evenly, make a soft material with boloxamer aqueous solution, place it on an extrusion spheronizer, extrude, and the extrusion speed is 14Hz; spheronize, the spheronization speed is 23Hz 0.5min , 17Hz 2.5min; drying at 60°C.

[0054] In vitro release test

[0055] Adopt the device of " Chinese Pharmacopoeia 2005 edition two appendices XC dissolution test method first method, get nimodipine sustained-release pellets (equivalent to nimodipine 120mg) six parts, be 1.0 with 1000mL containing 30% isopropanol pH The hydrochloric acid solution is the release medium, the rotation speed is 100 revolutions per minute, 5mL samples are taken at a certain time, and the same temperature and the...

Embodiment 2

[0057] Example 2. Sustained-release pellets with stomach-soluble coating layer

[0058] Composition of pill core: (based on 200 capsules)

[0059] Nimodipine 24g

[0060] Sodium Lauryl Sulfate 4g

[0061] Lactose 16g

[0062] Microcrystalline Cellulose 45g

[0063] water 40g

[0064] Coating material:

[0065] Eudragit E PO 9g

[0066] Preparation:

[0067] Mix nimodipine, sodium lauryl sulfate, lactose, and microcrystalline cellulose evenly, make a soft material with an aqueous solution, place it on an extrusion spheronizer, extrude, spheronize, dry at 60°C, and use Eudragit E PO Aqueous dispersion for coating. Sustained-release pellets with a gastric-soluble coating layer were obtained.

[0068] Fill the above-mentioned coated sustained-release pellets into empty capsules, each containing 120 mg of nimodipine, to obtain a capsule of sustained-release pellets.

[0069] In vitro release test

[0070] Get 6 capsules, test according to the method under the in vitro re...

Embodiment 3

[0072] Example 3. Sustained-release pellets with enteric coating layer

[0073] Composition of pill core: (based on 200 capsules)

[0074] Nimodipine 24g

[0075] Sodium Lauryl Sulfate 6g

[0076] Lactose 37g

[0077] Microcrystalline Cellulose 29g

[0078] water 35g

[0079] Coating material:

[0080] Eudragit S100 20g

[0081] Preparation:

[0082] Mix nimodipine, sodium lauryl sulfate, lactose, and microcrystalline cellulose evenly, make a soft material with an aqueous solution, place it on an extrusion spheronizer, extrude, and spheronize; dry; use Eudragit S100 water dispersion Perform coating. Sustained-release pellets coated with enteric coating layer were obtained.

[0083] The above-mentioned coated sustained-release pellets are filled in empty capsules, each containing 120 mg of nimodipine. Capsules of sustained-release pellets.

[0084] In vitro release test

[0085] The test was carried out according to the method under the in vitro release test item in...

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PUM

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Abstract

The invention relates to a pulsed sustained-release pellet comprising nimodipine and a preparation method is also provided. The sustained-release pellet comprises: one of gastric-dissolved and medicines containing sustained-release pellets and enteric-coated and medicines containing sustained-release pellets, or the combination. The preparation method is that: making medicines containing pellets using nimodipine and excipents, coating the medicines containing pellets with the gastric coating or the enteric coating, mixing the sustained-release pellets coated with gastric coating and enteric coating in proportion and putting the sustained-release pellets into capsules or tabletting. The pulsed sustained-release pellet of the invention has a special release behavior and needs to be taken only once per day. The release curve agrees well with the disease circadian rhythm of cerebrovascular disease patients, playing a role of the best prevention and treatment.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a preparation method of pulse sustained-release pellets containing nimodipine. technical background [0002] Nimodipine is a dihydropyridine calcium ion antagonist, which is highly selective for brain tissue receptors and easily penetrates the blood-brain barrier. By effectively preventing calcium ions from entering cells and inhibiting smooth muscle contraction, the purpose of releasing vascular smooth muscle is achieved, thereby protecting brain neurons, stabilizing their function, increasing cerebral blood perfusion, improving cerebral blood supply, and increasing tolerance to hypoxia. At present, it is widely used in cerebrovascular disease and nootropic drugs in clinical practice. The main indications are: (1) prevention and treatment of subarachnoid hemorrhage and cerebral vasospasm; (2) prevention of vascular headache attacks; (3) For the treatment of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/22A61K9/52A61K31/4422A61P9/10A61P9/12A61P25/06
Inventor 巩洪刚张四喜张翠娟邓树海
Owner SHENZHEN SOUTH CHINA PHARMA
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