Acipimox film-controlled slow-release pellet capsule

A technology of acyclolimus film and sustained-release pellets, which is applied in the field of pharmaceutical preparations and can solve the problems of aging and release of the film and the like

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

[0007] In order to solve the problem of release decline caused by film aging of acipimus film-controlled sustained-release pellets prepared by aqueous dispersion coating, the present invention provides a film-controlled film-controlled pellet that can maintain stable release performance throughout the validity period. Type acipimox sustained-release pellet capsules, characterized in that the core of the pellets contains low-substituted hydroxypropyl cellulose with high water-swellability, and the sustained-release coating film is deformed by water swelling, thereby offsetting the membrane aging

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The acipimox 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) Acipimox is passed through a 60-mesh sieve;

[0038](2) Take by weighing acipimox, microcrystalline cellulose PH101, lactose of prescription quantity, put in the wet granulator and mix evenly;

[0039] (3) 1% 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.

[0043] 2. Pr...

Embodiment 2

[0066] Example 2 Containing 10% low-substituted hydroxypropyl cellulose acipimox sustained-release pellet capsules

[0067] 1. Prescription

[0068] 1. Pill core prescription (1000 capsules)

[0069]

[0070] 2. Prescription of sustained-release film coating solution: same as in Example 1.

[0071] 3. No. 0 stomach-dissolving gelatin capsule shells, 1,000 capsules.

[0072] Second, the preparation process:

[0073] 1. Ball core preparation process:

[0074] (1) Acipimox is passed through a 60-mesh sieve;

[0075] (2) Acipimox, microcrystalline cellulose PH101, lactose, and low-substituted hydroxypropyl cellulose are taken by weighing the prescription amount, and mixed uniformly in a wet granulator;

[0076] (3) 1% carboxymethylcellulose sodium 10% ethanol solution to make soft material;

[0077] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0078] (5) spheronization, the spheronization speed is 900~1000rpm, drying i...

Embodiment 3

[0095] Example 3 Acilimus Sustained-release Pellet Capsules Containing 20% ​​Low-Substituted Hyprolose

[0096] 1. Prescription

[0097] 1. Pill core prescription (1000 capsules)

[0098]

[0099]

[0100] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0101] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0102] Second, the preparation process:

[0103] 1. Ball core preparation process: with embodiment 2.

[0104] 2. The preparation process of the slow-release film coating solution: the same as in Example 1.

[0105] 3. Coating (sustained release film):

[0106] 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 26.2% and 31.6%.

[0107] 4, heat treatment: with embodiment 1.

[0108] 5. Capsule filling: the coated pellets are filled into capsules.

[0109]3. Release, content determination and results

[0110] Assay...

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Abstract

The invention relates to an acipimox film-controlled slow-release pellet capsule. A slow-release film of the acipimox film-controlled slow-release pellet utilizes Eurdragit NE 30D as a film-formation material. A pellet core of the acipimox film-controlled slow-release pellet contains low-substituted hydroxypropyl cellulose having high expansibility, and also contains pharmaceutically acceptable common excipients for the slow-release pellet, wherein preferably, the excipients comprise microcrystalline cellulose and lactose, and the pellet core comprises 10 to 40wt% of the low-substituted hydroxypropyl cellulose. The slow-release film comprises the Eurdragit NE 30D, triethyl citrate as a plasticizer and talcum powder as an antiplastering aid, wherein preferably, a ratio of Eurdragit NE 30D to triethyl citrate to talcum powder is 30: 2: 4 and coating weight gain is in a range of 20 to 39%. The acipimox film-controlled slow-release pellet comprises the pellet core containing low-substituted hydroxypropyl cellulose having high water expansibility and thus after absorbing water, the acipimox film-controlled slow-release pellet obviously expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore size is increased; and permeability is improved and permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the acipimox film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept prior to expiration date.

Description

technical field [0001] The invention relates to an acipimox membrane-controlled sustained-release pellet capsule, in particular to an acipimox membrane-controlled sustained-release pellet capsule with a pellet core containing low-substituted hydroxypropyl cellulose, belonging to the field of pharmaceutical preparations . Background technique [0002] Acilimus is a niacin derivative, which can inhibit the decomposition of adipose tissue, reduce the release of free fatty acids from adipose tissue, thereby reducing the synthesis of triglyceride (TG) in the liver, and inhibiting very low-density lipoprotein (VLDL) and the synthesis of low-density lipoprotein (LDL), so that the concentration of triglyceride (TG) and total cholesterol (TC) in the blood is reduced, and it is used for the treatment of hypertriglyceridemia (type IV), hypercholesterolemia (IIa type), high triglycerides combined with hypercholesterolemia (type IIb). The basic clinical requirement for this type of dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K9/16A61K31/4965A61K47/38A61P3/06
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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