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Paliperidone osmotic pump type controlled release tablet

A paliperidone and osmotic pump technology, applied in the field of pharmaceutical preparations, can solve the problems of large side effects of patients, low blood drug concentration, poor curative effect of common dosage forms, etc.

Inactive Publication Date: 2017-10-24
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Because the common dosage form can reach a high plasma peak concentration in a short time after taking it, and the blood drug concentration is very low when the next medication is taken, especially in the early morning when the local ischemia is the most serious, the curative effect of the common dosage form is poor, and the harm brought to the patient Side effects are relatively large, so it is necessary to develop an oral osmotic pump formulation of paliperidone to meet market needs

Method used

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  • Paliperidone osmotic pump type controlled release tablet
  • Paliperidone osmotic pump type controlled release tablet
  • Paliperidone osmotic pump type controlled release tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] 1. Prescription

[0046] 1) Tablet core prescription, based on 1000 tablets:

[0047] Drug-containing layer:

[0048] Paliperidone 6g

[0049] Sucrose 120g

[0050] 15g pregelatinized starch

[0051] Microcrystalline Cellulose 60g

[0052] Sodium Carboxymethyl Cellulose 45g

[0053] Magnesium Stearate 2g

[0054] Boost layer:

[0055] Hydroxypropyl Methyl Cellulose 28g

[0056] Sodium chloride 46g

[0057] Sucrose 34g

[0058] Polyethylene oxide 50g

[0059] Magnesium Stearate 1g

[0060] 2) Prescription of semi-permeable membrane coating solution

[0061] Cellulose acetate 54g

[0062] Polyethylene glycol 14g

[0063] Ethanol 1000ml

[0064] 3) Prescription of film coating solution

[0065] Gastric coating powder 10g

[0066] water 100ml

[0067] 2. Detailed preparation process

[0068] 1. Preparation process of Paliperidone tablet core: The tablet core is a double-layer tablet, one layer is a drug-containing layer, and the other layer is a booster l...

Embodiment 2

[0077] 1) Tablet core prescription, based on 1000 tablets:

[0078] Drug-containing layer:

[0079] Paliperidone 6g

[0080] Sucrose 120g

[0081] 15g pregelatinized starch

[0082] Microcrystalline Cellulose 60g

[0083] Sodium Carboxymethyl Cellulose 45g

[0084] Magnesium Stearate 2g

[0085] Boost layer:

[0086] Hydroxypropyl Methyl Cellulose 28g

[0087] Sodium chloride 46g

[0088] Sucrose 34g

[0089] Polyethylene oxide 50g

[0090] Magnesium Stearate 1g

[0091] 2) Prescription of semi-permeable membrane coating solution

[0092] Cellulose acetate 54g

[0093] Polyethylene glycol 15g

[0094] Ethanol 1000ml

[0095] 3) Prescription of film coating solution

[0096] Gastric coating powder 10g

[0097] water 100ml

[0098] Two, detailed preparation process is the same as embodiment 1

Embodiment 3

[0100] 1. Prescription

[0101] 1) Tablet core prescription, based on 1000 tablets:

[0102] Drug-containing layer:

[0103] Paliperidone 6g

[0104] Sucrose 120g

[0105] 15g pregelatinized starch

[0106] Microcrystalline Cellulose 60g

[0107] Sodium Carboxymethyl Cellulose 45g

[0108] Magnesium Stearate 2g

[0109] Boost layer:

[0110] Hydroxypropyl Methyl Cellulose 28g

[0111] Sodium chloride 46g

[0112] Sucrose 34g

[0113] Polyethylene oxide 50g

[0114] Magnesium Stearate 1g

[0115] 2) Prescription of semi-permeable membrane coating solution

[0116] Cellulose acetate 54g

[0117] Polyethylene glycol 13g

[0118] Ethanol 1000ml

[0119] 3) Prescription of film coating solution

[0120] Gastric coating powder 10g

[0121] water 100ml

[0122] Two, detailed preparation process is the same as embodiment 1

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Abstract

The invention provides a novel paliperidone osmotic pump-type controlled-release tablet, which adopts cellulose acetate and polyethylene glycol as semipermeable membrane film-forming materials, which can overcome the semipermeable membrane aging phenomenon, obtain a stable release rate, and Reduce drug residues. The dronedarone oral osmotic pump preparation provided by the present invention has excellent release performance and high stability, and there is no obvious aging phenomenon after being placed for a long time, which meets the market demand.

Description

technical field [0001] The invention relates to a paliperidone osmotic pump-type controlled-release tablet, which uses cellulose acetate-polyethylene glycol as a semipermeable membrane material and belongs to the field of pharmaceutical preparations. Background technique [0002] Paliperidone is clinically used in the treatment of schizophrenia. The English chemical name of the paliperidone intermediate is 4-(6-fluoro-3a,7a-dihydrobenzo[d]isoxazol-3-yl)-1-(2-(9-hydroxy-2-methyl-4-oxo- 3,4,6,7,8,9-hexahydro-2H-pyrido[1,2-a]pyrimidin-3-yl)ethyl)piperidine 1-oxide, the molecular formula is C 23 h 27 FN 4 o 4 . Developed by Johnson & Johnson in the United States, it was approved for marketing by the FDA in December 2006. Studies have shown that it can effectively delay the relapse rate of schizophrenia, and can be used for acute short-term and long-term maintenance treatment of schizophrenia to relieve symptoms and stabilize patients' condition effectively in long-term use...

Claims

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Application Information

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IPC IPC(8): A61K9/24A61K9/36A61K9/44A61K31/519A61P25/18A61K47/38A61K47/10A61K9/28
CPCA61K9/2866A61K9/2054A61K9/2059A61K9/2072A61K9/2086A61K9/284A61K31/519
Inventor 严洁
Owner TIANJIN HANKANG PHARMA BIOTECH