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Allopurinol sustained-release pellets and preparation method thereof

A technology of sustained-release pellets and allopurinol, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, and medical preparations containing active ingredients, etc. It can solve the problems of difficult control of release uniformity and achieve uniform drug release Good performance, small particle size, large distribution area

Active Publication Date: 2015-09-02
HAINAN PULIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Allopurinol is a poorly soluble drug, and it is made into matrix-type sustained-release tablets, and the release uniformity is difficult to control.
[0005] The invention provides an allopurinol sustained-release pellet, which effectively solves the problem of release uniformity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Preparation of allopurinol sustained-release pellets.

[0025] Allopurinol 250g Microcrystalline Cellulose Core 250g

[0026] Povidone k30 25g Ethylcellulose 21g

[0027] Triethyl citrate 2.1g Talc powder 10g

[0028] Microcrystalline Cellulose 391g Lactose 168g

[0029] Low-substituted hydroxypropyl cellulose 110g Magnesium stearate 11g

[0030] Makes 1000 pieces

[0031] Preparation Process:

[0032] (1) Preparation of allopurinol pills:

[0033] Dissolve the prescribed amount of povidone in 75% ethanol solution to prepare a 3% povidone ethanol solution as an adhesive. Micronize allopurinol, weigh the prescription amount, pour it into the hopper, put the blank pellet core in the coating granulator, adjust the parameters, spray the adhesive, and start adding the medicine until all the medicine powder is added. After the medicine is finished, take it out and dry it at 60±5°C.

[0034] (2) Preparation of allopurinol sustained-release pellets:

[0035]...

Embodiment 2

[0038] Embodiment 2: Preparation of allopurinol sustained-release pellets

[0039] Allopurinol 300g Sucrose core 250g

[0040] Povidone k30 28g Eudragit NE30D 150g

[0041] Triethyl Citrate 4.5g Talc 45g

[0042] Microcrystalline Cellulose 480g Starch 68g

[0043] Crosslinked Povidone 110g Micronized Silica Gel 15g

[0044] Makes 1000 pieces

[0045] Preparation Process:

[0046] (1) Preparation of allopurinol pills:

[0047] Dissolve the prescribed amount of povidone in 75% ethanol solution to prepare a 3% povidone ethanol solution as an adhesive. Micronize allopurinol, weigh the prescription amount, pour it into the hopper, put the blank pellet core in the coating granulator, adjust the parameters, spray the adhesive, and start adding the medicine until all the medicine powder is added. After the medicine is finished, take it out and dry it at 60±5°C.

[0048] (2) Preparation of allopurinol sustained-release pellets:

[0049] Dissolve the prescribed amount of ethyl ...

Embodiment 3

[0052] Example 3: Preparation of allopurinol sustained-release pellets.

[0053] Allopurinol 300g Microcrystalline Cellulose 250g

[0054] Lactose 50g Stearic acid 12g

[0055] Hypromellose 20g Microcrystalline Cellulose 700g

[0056] Crosslinked Povidone 120g Micronized Silica Gel 15g

[0057] Makes 1000 pieces

[0058] Preparation Process:

[0059] (1) Preparation of allopurinol sustained-release pellets:

[0060] Dissolve the prescribed amount of hypromellose in 75% ethanol solution to prepare a 5% ethanol solution of hypromellose as a binder. Micronize allopurinol, weigh the prescription amount, mix evenly with microcrystalline cellulose, lactose and stearic acid, and use hypromellose ethanol solution to make soft material in a wet granulator. After discharging, extrude Prepare pellets by spheronizing and drying at 60±5°C.

[0061] (2) Preparation of allopurinol sustained-release pellets:

[0062] Weigh the allopurinol sustained-release pellets, microcrystalline cell...

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Abstract

The invention relates to a medicament for treating uarthritis, in particular to an allopurinol slow-release micro pill tablet and a preparation method thereof. The allopurinol slow-release micro pill tablet is prepared by tableting 30-65 percent by weight of allopurinol slow-release pills and 35-70 percent by weight of tablet auxiliary materials, wherein the tablet auxiliary materials include a filling agent; and the allopurinol slow-release micro pills are diaphragm-controlled slow-release micro pills or framework slow-release micro pills. The allopurinol slow-release micro pill tablet disclosed by the invention has the advantages of stable and effective blood concentration, high releasing uniformity, convenience for transporting, and the like.

Description

technical field [0001] The invention relates to a medicine for treating gout, in particular to an allopurinol sustained-release pellet tablet and a preparation method thereof. Background technique [0002] As a synthetic analog of hypoxanthine, allopurinol is currently the only drug that can inhibit the synthesis of uric acid, with few adverse reactions and can be taken for a long time. Its main pharmacological effect is that hypoxanthine and xanthine form uric acid through the catalysis of xanthine oxidase. Allopurinol and its metabolite oxyallopurinol are inhibitors of xanthine oxidase. Allopurinol is a competitive inhibitor of the enzyme at low concentrations and a non-competitive inhibitor at high concentrations. Oxyallopurinol is also a non-competitive inhibitor of enzymes, and it stays in the tissue for a long time, which further strengthens the pharmacological effects of allopurinol, resulting in hindered biosynthesis of uric acid, decreased uric acid concentration ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/26A61K31/519A61K47/32A61K47/38A61K47/44A61P19/06
Inventor 范敏华姜新东刘华
Owner HAINAN PULIN PHARMA
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