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Pharmaceutical composition of palipeddone

A kind of technology of paliperidone and composition, applied in the field of antipsychotic drugs, the pharmaceutical composition field of paliperidone

Inactive Publication Date: 2013-11-13
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to provide a paliperidone sustained-release pellet that effectively solves the problem of the industrialization of the existing paliperidone under the national conditions, and at the same time facilitates the medication of mental patients, and has a simple prescription process

Method used

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  • Pharmaceutical composition of palipeddone
  • Pharmaceutical composition of palipeddone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Ball core:

[0019] components Dosage (g) Paliperidone 3.0 lactose 100.0 sucrose 20.0 HPMC 60.0

[0020] Coating layer:

[0021] components 100 servings (g) Udrake RL100 3.0 Udrake RS100 6.0 PEG4000 1.8 60% ethanol 89.2

[0022] Preparation:

[0023] Add an appropriate amount of wetting agent according to the prescription amount of the pellet core and mix it to make a wet material, extrude the strip through a sieve plate, and make a pellet core in a spheronizer. After the pellet core is dried, it is coated on a fluidized bed to obtain pellets, and the weight gain of the coating is 10%.

Embodiment 2

[0025] Ball core:

[0026] components Dosage (g) Paliperidone 3.0 microcrystalline cellulose 36.0 lactose 90.0

[0027] Isolation layer:

[0028] components Dosage (g) HPMC-E5LV 6.0 PEG400 1500 talcum powder 5 60% ethanol 8.0

[0029] Coating layer:

[0030] components 100 servings (g) Udrake RL100 6.0 Udrake RS100 3.0 PEG4000 1.8 60% ethanol 89.2

[0031] The preparation method is the same as in Example 1.

Embodiment 3

[0033] Ball core:

[0034] components Dosage (g) Paliperidone 6.0 lactose 160.0 starch 42.0 EC 80.0 Eudragi RSPO 120.0

[0035] Coating layer:

[0036] components 100 servings (g) Udrake RL100 1.0 Udrake RS100 9.0 PEG4000 2.0 60% ethanol 88.0

[0037] The preparation method is the same as in Example 1.

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Abstract

The invention discloses a pharmaceutical composition of palipeddone, belongs to medicine field, and relates to an antipsychotic pharmaceutical composition, wherein the pharmaceutical composition comprises palipeddone active component, controlled-release auxiliary material and other acceptable auxiliary material in pharmacy. The pharmaceutical composition provided by the invention solves the problem of difficult medicine taking by mental patients, and has advantages of simple technology, low cost and easy industrialization, and can better satisfy clinic needs.

Description

technical field [0001] The invention belongs to the field of medicine and relates to antipsychotic drugs, in particular to a pharmaceutical composition of paliperidone. Background technique [0002] Paliperidone is the active metabolite of the atypical antipsychotic risperidone, 9-hydroxyrisperidone, which is a derivative of benzisoxazole, mainly by blocking 5-hydroxytryptamine 2A (5-HT 2A ) receptors and dopamine D 2 (DA 2 ) receptors exert antipsychotic effects. Paliperidone can treat schizophrenic patients through the control of various psychotic symptoms and the improvement of overall social function. Most of the adverse reactions of paliperidone, such as drowsiness, tachycardia, and extrapyramidal adverse reactions, are mild, do not cause physical discomfort or affect social function, and can be relieved after timely symptomatic treatment. [0003] Patients with schizophrenia have poor compliance with oral medications, which makes drug therapy have limitations in te...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/52A61K31/519A61K47/38A61K47/32A61P25/18
Inventor 马莉孟旻郭夏宋雪梅
Owner BEIJING VENTUREPHARM BIOTECH
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