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Glipizide film-controlled slow-release pellet capsule

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

Active Publication Date: 2013-07-24
内蒙古天衡医院管理有限公司
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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 glipizide membrane-controlled sustained-release pellets prepared by water dispersion coating, the present invention provides a membrane-controlled membrane-controlled pellet that can maintain stable release performance throughout the validity period. Type Glipizide Sustained-release Pellet Capsule Capsules, characterized in that the core of the pellets contains sodium carboxymethyl starch with high water-swellability, and the sustained-release coating film is deformed by water-absorbing swelling, thereby offsetting the film Ageing

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The glipizide sustained-release pellet capsule of the common pellet core of embodiment 1

[0029] 1. Prescription

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

[0031]

[0032]

[0033] 2. Prescription of sustained-release film coating solution

[0034]

[0035] 3. No. 0 stomach-dissolving gelatin capsule shells, 1,000 capsules.

[0036] Second, the preparation process:

[0037] 1. Ball core preparation process:

[0038] (1) Glipizide is passed through an 80-mesh sieve;

[0039] (2) Take glipizide, microcrystalline cellulose PH101, lactose, sodium lauryl sulfate of prescription quantity, put in the wet granulator and mix uniformly;

[0040] (3) make soft material with 2% carboxymethylcellulose sodium 10% ethanol solution;

[0041] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0042] (5) spheronization, the spheronization speed is 900~1000rpm, drying in the fluidized bed;

[0043] (6) Sieve, and tak...

Embodiment 2

[0071] Example 2 Glipizide Sustained-release Pellet Capsules Containing 5% Sodium Carboxymethyl Starch

[0072] 1. Prescription

[0073] 1. Pill core prescription (1000 capsules)

[0074]

[0075] 2. Prescription of sustained-release film coating solution: same as in Example 1

[0076] 3. No. 0 stomach-soluble gelatin capsule shell 1000 capsules

[0077] Second, the preparation process:

[0078] 1. Ball core preparation process:

[0079] (1) Glipizide is passed through a 60-mesh sieve;

[0080] (2) Glipizide, microcrystalline cellulose PH101, lactose, carboxymethyl starch sodium, sodium lauryl sulfate are taken by weighing prescription quantity, put in the wet granulator and mix uniformly;

[0081] (3) make soft material with 2% carboxymethylcellulose sodium 10% ethanol solution;

[0082] (4) Extrude on the extruder, the screen aperture is 1.0mm, and the extrusion speed is 20-30rpm;

[0083] (5) spheronization, the spheronization speed is 900~1000rpm, drying in the f...

Embodiment 3

[0100] Example 3 Glipizide Sustained-release Pellet Capsules Containing 10% Sodium Carboxymethyl Starch

[0101] 1. Prescription

[0102] 1. Pill core prescription (1000 capsules)

[0103]

[0104] 2. Prescription of sustained-release film coating solution: same as in Example 1.

[0105] 3. No. 0 stomach-dissolving gelatin capsule shells, 1,000 capsules.

[0106] Second, the preparation process:

[0107] 1. Ball core preparation process: with embodiment 2.

[0108] 2. The preparation process of the slow-release film coating solution: the same as in Example 1.

[0109] 3. Coating (sustained release film):

[0110] 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 22.1% and 26.8%.

[0111] 4, heat treatment: with embodiment 1

[0112] 5. Capsule filling: same as in Example 1.

[0113] 3. Release, content determination and results

[0114] Assay method: with embodiment 1, ...

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Abstract

The invention relates to a glipizide film-controlled slow-release pellet capsule. A slow-release film of the glipizide film-controlled slow-release pellet utilizes Eurdragit RL 30D as a film-formation material. A pellet core of the glipizide film-controlled slow-release pellet contains sodium carboxymethyl starch having high expansibility, and also contains pharmaceutically-acceptable common excipients for the slow-release pellet, wherein preferably, the excipients comprise microcrystalline cellulose, lactose and sodium dodecyl sulfate, and the pellet core comprises 5 to 20wt% of sodium carboxymethyl starch. 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 17 to 36%. The glipizide film-controlled slow-release pellet comprises the pellet core containing sodium carboxymethyl starch having high water expansibility and thus after absorbing water, the glipizide 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 the permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the glipizide film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept in the period of validity.

Description

technical field [0001] The invention relates to a glipizide membrane-controlled sustained-release pellet capsule, in particular to a glipizide membrane-controlled sustained-release pellet capsule whose pellet core contains sodium carboxymethyl starch, and belongs to the field of pharmaceutical preparations. Background technique [0002] Glipizide is an oral hypoglycemic drug of the sulfonylurea class, which can promote the secretion of insulin by pancreatic β cells and enhance the effect of insulin on target tissues; it can also stimulate pancreatic α cells to inhibit the secretion of glucagon, as well as inhibit glycogen Protolysis, promoting muscle utilization and consumption of glucose, for the treatment of type 2 diabetes. [0003] Glipizide is almost insoluble in water, and the earliest common preparation on the market needs to be taken 3 times a day, the blood concentration fluctuates greatly, the peak concentration is too high, and the adverse reactions are serious. ...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/64A61K47/32A61K47/36A61K47/38A61P3/10
Inventor 姜庆伟狄媛吕玉珠唐亚坤刘俊轶
Owner 内蒙古天衡医院管理有限公司
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