Unlock instant, AI-driven research and patent intelligence for your innovation.

Paliperidone osmotic pump controlled-release tablet

A technology of paliperidone and osmotic pump, which can be used in medical preparations with non-active ingredients, organic active ingredients, nervous system diseases, etc., and can solve the problems of decreased release performance and aging.

Active Publication Date: 2012-09-19
北京天衡药物研究院南阳天衡制药厂
View PDF2 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Osmotic pump-type controlled-release tablets made of currently commonly used semi-permeable membrane materials, such as cellulose acetate + polyethylene glycol, ethyl cellulose + polyethylene glycol, have good release performance within a period of time just after preparation , but after storage for a period of time, its release performance begins to decline, the longer the storage time, the more obvious the decline, often in the second half of the drug's specified validity period, the release performance declines significantly, the popular saying is aging

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Paliperidone osmotic pump controlled-release tablet
  • Paliperidone osmotic pump controlled-release tablet
  • Paliperidone osmotic pump controlled-release tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] 1. Prescription

[0063] 1. Tablet core prescription (based on 1000 tablets, specification: 6mg):

[0064] Medicinal layer:

[0065]

[0066] Boost layer:

[0067]

[0068] 2. Semipermeable membrane coating liquid prescription

[0069]

[0070] 3. Film coating coating liquid prescription

[0071] Make up

Dosage

Stomach-soluble coating powder

10g

[0072] Water

100ml

[0073] 2. Detailed preparation process

[0074] 1. Paliperidone tablet core preparation process:

[0075] The tablet core is a double-layer tablet, one layer is a drug-containing layer, and the other layer is a booster layer.

[0076] The preparation process is as follows:

[0077] Medicinal layer:

[0078] (1) Paliperidone passes through a 100 mesh sieve, sodium lauryl sulfate is crushed through a 100 mesh sieve, and sucrose is crushed through an 80 mesh sieve;

[0079] (2) Weigh the prescription amount of paliperidone, lactose, sucrose, sodium lauryl sulfate, sodium carboxymethyl cellulose, povidone, and ...

Embodiment 2

[0118] 1. Prescription

[0119] 1. Tablet core prescription: same as Example 1

[0120] 2. Semi-permeable membrane coating liquid prescription:

[0121]

[0122] 3. Film coating coating liquid prescription: same as Example 1

[0123] 2. Detailed preparation process

[0124] 1. Paliperidone tablet core preparation process:

[0125] Same as Example 1

[0126] 2. Preparation process of semipermeable membrane coating liquid

[0127] Weigh the prescription amount of povidone K30 and ethyl cellulose (N-100), add it to ethanol and stir to dissolve it completely, and it is obtained.

[0128] 3. Semi-permeable membrane coating: place the tablet cores in a multifunctional coating machine for coating, and weigh a small amount of tablets regularly to calculate the weight gain of the coating.

[0129] The coating weight gain was 12.0% and 14.0% respectively.

[0130] 4. Heat treatment: same as Example 1

[0131] 5. Laser drilling: same as Example 1

[0132] 6. The preparation process and film coating of the...

Embodiment 3

[0147] 1. Prescription

[0148] 1. Tablet core prescription: same as Example 1

[0149] 2. Semipermeable membrane coating liquid prescription

[0150]

[0151] 3. Film coating coating liquid prescription: same as Example 1

[0152] 2. Detailed preparation process

[0153] 1. Paliperidone tablet core preparation process: same as Example 1

[0154] 2. Preparation process of semipermeable membrane coating liquid

[0155] Weigh the prescription amount of povidone K30 and ethyl cellulose (N-100), add it to ethanol and stir to dissolve it completely.

[0156] 3. Semi-permeable membrane coating: put the tablet core in a multifunctional coating machine for coating, and weigh a small amount of tablets regularly to calculate the coating weight gain.

[0157] The coating weight gain was 15.0% and 18.0% respectively.

[0158] 4. Heat treatment: same as Example 1.

[0159] 5. Laser drilling: same as Example 1.

[0160] 6. The preparation process and film coating of the film coating liquid: the same as in E...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Angleaaaaaaaaaa
Login to View More

Abstract

The invention provides a novel paliperidone osmotic pump controlled-release tablet. Ethyl cellulose and povidone are used as membrane forming materials of a semipermeable membrane, and the asymmetric tablet form is preferably selected, so that the ageing of the semipermeable membrane can be avoided, a stable release speed can be acquired, and the drug residues can be reduced. The invention also provides a method for improving the ageing resistance of the paliperidone osmotic pump controlled-release tablet, wherein the method is characterized in that the ethyl cellulose-povidone are used as the materials of the semipermeable membrane. In addition, the invention also provides applications of the cellulose-povidone composition in preparing the anti-ageing paliperidone osmotic pump controlled-release tablet.

Description

Technical field [0001] The invention relates to a paliperidone osmotic pump type controlled release tablet, which uses ethyl cellulose-povidone as a semi-permeable membrane material and belongs to the field of pharmaceutical preparations. Background technique [0002] Paliperidone is the active metabolite of risperidone and is used to treat schizophrenia. Osmotic pump controlled release tablets have been marketed at home and abroad. [0003] The semipermeable membrane is very important for the control of drug release in oral osmotic pump formulations. Semi-permeable membranes composed of different materials have different water permeability, which is related to the permeability coefficient of the membrane. The most commonly used is cellulose acetate. Others such as ethyl cellulose are also mentioned in the literature. The osmotic pump type controlled release tablet prepared by using currently commonly used semipermeable membrane materials, such as cellulose acetate + polyethylene ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/36A61K31/519A61K47/38A61K47/32A61P25/18
Inventor 孟伟张志永
Owner 北京天衡药物研究院南阳天衡制药厂