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Paliperidone extended-release mini pill

A technology of paliperidone and sustained-release pellets, which is applied in the directions of organic active ingredients, nervous system diseases, bulk transportation, etc., to achieve the effects of uniform particle size, cost reduction, and simple preparation process

Inactive Publication Date: 2012-08-01
SICHUAN INDAL INST OF ANTIBIOTICS CHINA NAT PHARMA GROUP CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The production process is complicated and the cost is high
The existing gelatin capsule release paliperidone solution cannot make the sustained release of the drug stable

Method used

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  • Paliperidone extended-release mini pill
  • Paliperidone extended-release mini pill
  • Paliperidone extended-release mini pill

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Preparation of paliperidone ordinary pellets: mix microcrystalline cellulose and paliperidone raw material according to the prescription ratio, add purified water to prepare wet material, and extrude through an extrusion sieve plate (aperture 1.0mm) to obtain The strip-shaped material is placed in a spheronizer and spheronized into pellets, dried in a tumbling cylinder, and sieved to sieve pellets with a diameter of 0.85-1.25 mm.

[0057] Preparation of coated pellets: Dilute the coating solution Surelease® with water to a certain concentration, add the prescribed amount of porogen, and stir evenly. Put the paliperidone ordinary pellets prepared above into the coating machine, after the temperature of the pellets rises to 35 ℃ ~ 40 ℃, slowly spray into the prepared coating solution for slow-release coating according to the prescription amount, and then dry have to.

Embodiment 2

[0059] Preparation method is the same as embodiment 1

Embodiment 3

[0061] Preparation method is the same as embodiment 1

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Abstract

The invention provides a paliperidone extended-release mini pill, which solves the problems that a conventional extended-release tablet has a complex manufacturing process, high cost and side effects in taking. The paliperidone extended-release mini pill structurally comprises a pill core containing medicine and an extended-release coating layer from the inside out. The preparation method comprises the following steps: preparing a pill core containing medicine and wrapping the extended-release coating layer on the surface of the pill; and the grain diameter of the mini pill is 0.48 mm to 2.5 mm. The paliperidone extended-release mini pill can be released for 24 hours stably, lower than 30% of paliperidone extended-release mini pill is released within 2 hours, 40% to 60% of paliperidone extended-release mini pill is released within 12 hours, and more than 80% paliperidone extended-release mini pill is released at more than 20 hours. The paliperidone extended-release mini pill has the advantages of simple manufacturing process, low cost, uniform particle size, high yield and good release effect.

Description

Technical field: [0001] The invention relates to a sustained-release pharmaceutical dosage form of paliperidone. Background technique: [0002] Paliperidone (paliperidone), also known as 9-hydroxy-risperidone (9-hydroxy-risperidone), paliperidone (paliperidone), belongs to the atypical antipsychotic drugs of the benzoisoxazole class. Its chemical name is: (±)-3-[2-[4-(6-fluoro-1,2-benzoisoxazole-3-methyl)-1-piperidinyl]ethyl-6,7 ,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one with the formula C 23 h 27 FN 4 o 3 , and the relative molecular mass is 426.49. [0003] Paliperidone is the main plasma active metabolite of risperidone, and its pharmacological effects are similar to those of risperidone. The exact mechanism of action of paliperidone is not clear. Compared with traditional antipsychotic drugs, it has a lower affinity with dopamine (dopamine) D2 receptors and a lower affinity with 5-hydroxytryptamine receptors (hydroxytrytamine, 5-HT) 5- HT...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/52A61K31/519A61P25/18
Inventor 郑林邓盛齐任静陶静李楠
Owner SICHUAN INDAL INST OF ANTIBIOTICS CHINA NAT PHARMA GROUP CORP
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