Nifedipine film-controlled slow-release pellet capsule

A technology of slow-release pellets and horizontal film, which is applied in the direction of medical preparations of non-active ingredients, cardiovascular system diseases, organic active ingredients, etc., and can solve the problems of film aging and release decline

Active Publication Date: 2013-07-24
北京天衡药物研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In order to solve the problem of release decline caused by membrane aging of nifedipine membrane-controlled sustained-release pellets prepared by aqueous dispersion coating, the present invention provides a membrane-controlled membrane-controlled pellet that can maintain stable release performance throughout the validity period. Nifedipine slow-release pellet capsules are characterized in that the core of the pellets contains croscarmellose sodium with high water-swellability, and the sustained-release coating film is deformed by water swelling, thereby offsetting the film aging

Method used

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  • Nifedipine film-controlled slow-release pellet capsule
  • Nifedipine film-controlled slow-release pellet capsule
  • Nifedipine film-controlled slow-release pellet capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The nifedipine slow-release pellet capsule of embodiment 1 common ball core

[0029] 1. Prescription

[0030] 1. Pill core prescription (1000 capsules)

[0031]

[0032] 2. Prescription of sustained-release film coating solution

[0033]

[0034] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0035] Second, the preparation process:

[0036] 1. Ball core preparation process:

[0037] (1) Nifedipine is passed through an 80 mesh sieve;

[0038] (2) Take by weighing nifedipine, microcrystalline cellulose PH101, lactose, PEG 4000 of prescription quantity, put in wet granulator and mix uniformly;

[0039] (3) 2% carboxymethylcellulose sodium 10% ethanol solution to make soft material;

[0040] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0041] (5) spheronization, the spheronization speed is 900~1000rpm, drying in the fluidized bed;

[0042] (6) Sieve, and take ball cores between 16 and 30 mesh. ...

Embodiment 2

[0063] Embodiment 2 Containing 5% croscarmellose sodium nifedipine sustained-release pellet capsule

[0064] 1. Prescription

[0065] 1. Pill core prescription (1000 capsules)

[0066]

[0067] 2. Prescription of sustained-release film coating solution: same as in Example 1.

[0068] 3. No. 0 stomach-dissolving gelatin capsule shells, 1,000 capsules.

[0069] Second, the preparation process:

[0070] 1. Ball core preparation process:

[0071] (1) Nifedipine is passed through a 60 mesh sieve;

[0072] (2) Take nifedipine, microcrystalline cellulose PH101, lactose, PEG 4000, croscarmellose sodium of recipe quantity by weighing, put in the wet granulator and mix uniformly;

[0073] (3) make soft material with 2% carboxymethylcellulose sodium 10% ethanol solution;

[0074] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0075] (5) spheronization, the spheronization speed is 900~1000rpm, drying in the fluidized bed;

[00...

Embodiment 3

[0093] Example 3 Nifedipine Sustained-release Pellet Capsules Containing 10% Croscarmellose Sodium

[0094] 1. Prescription

[0095] 1. Pill core prescription (1000 capsules)

[0096]

[0097] 2. Prescription of sustained-release film coating solution: same as in Example 1.

[0098] 3. No. 0 stomach-dissolving gelatin capsule shells, 1,000 capsules.

[0099] Second, the preparation process:

[0100] 1. Ball core preparation process: with embodiment 2.

[0101] 2. The preparation process of the slow-release film coating solution: the same as in Example 1.

[0102] 3. Coating (sustained release film):

[0103] The ball core is placed in a fluidized bed for coating, and the weight gain of the coating film is controlled, and the weight gain of the coating is 23.5% and 28.4%.

[0104] 4, heat treatment: with embodiment 1.

[0105] 5. Capsule filling: same as in Example 1.

[0106] 3. Release, content determination and results

[0107] Assay method: with embodiment 1, th...

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PUM

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Abstract

The invention relates to a nifedipine film-controlled slow-release pellet capsule. A slow-release film of the nifedipine film-controlled slow-release pellet utilizes Eurdragit RL 30D as a film-formation material. A pellet core of the nifedipine film-controlled slow-release pellet contains croscarmellose sodium having high water expansibility. Excipients comprise microcrystalline cellulose and lactose as fillers and PEG 4000 as a solubilizer. The pellet core comprises 5 to 20wt% of croscarmellose sodium. The slow-release film comprises Eurdragit RL 30D, triethyl citrate as a plasticizer, and talcum powder as an antiplastering aid, wherein preferably, a ratio of Eurdragit RL 30D to triethyl citrate to talcum powder is 30: 3: 4 and a film weight increasing ratio is in a range of 21 to 35%. After absorbing water, the nifedipine film-controlled slow-release pellet obviously expands so that the slow-release film is stretched; the water-permeable micropore size is increased; and permeability is improved and the permeability reduction caused by film aging is counteracted. Therefore, the nifedipine film-controlled slow-release pellet keeps stable release performances in the period of validity.

Description

technical field [0001] The invention relates to a nifedipine film-controlled sustained-release pellet capsule, in particular to a nifedipine film-controlled sustained-release pellet capsule with a pellet core containing croscarmellose sodium, belonging to the field of pharmaceutical preparations . Background technique [0002] Nifedipine is a calcium antagonist, which selectively antagonizes the influx of calcium ions in vascular smooth muscle, relaxes peripheral resistance vessels, reduces peripheral resistance, and is used for the treatment of hypertension; inhibits myocardial contraction, reduces myocardial metabolism, and reduces myocardial oxygen consumption. For the treatment of angina pectoris. [0003] Nifedipine is almost insoluble in water, and the earliest common preparation on the market needs to be taken twice a day, the blood concentration fluctuates greatly, the peak concentration is too high, and the adverse reactions are serious. [0004] Bayer has launche...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K9/16A61K31/4422A61K47/38A61P9/12A61P9/10
Inventor 姜庆伟狄媛吕玉珠唐亚坤刘俊轶
Owner 北京天衡药物研究院有限公司
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