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A kind of paliperidone tablet and preparation method thereof

A technology for paliperidone and sustained-release tablets, which is applied in the field of medicine and can solve the problems of uneven content of small doses of drugs, changes in paliperidone, and low bioavailability

Active Publication Date: 2021-07-16
沈阳信康药物研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the preparation process of osmotic pumps is complicated, time-consuming, costly, and there is a potential danger of sudden release, which requires strict quality control and process requirements
CN107412180A discloses a paliperidone-coated chip and its preparation method. In the disclosed preparation method, both the tablet core layer and the wrapping layer contain paliperidone. Complexity, high cost, etc., but because paliperidone is a small-dose drug, it will still cause content uniformity problems in scale-up production
This method solves the problem of uneven drug content in small doses
However, the disadvantage of this method is that if the solvent volatilizes and the drug recrystallizes, the original particle size distribution of the Paliperidone bulk drug will be changed, and the crystal form of Paliperidone may be changed, thereby affecting the release of the tablet. behavioral and therapeutic effects
Unable to guarantee complete drug release, low bioavailability

Method used

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  • A kind of paliperidone tablet and preparation method thereof
  • A kind of paliperidone tablet and preparation method thereof
  • A kind of paliperidone tablet and preparation method thereof

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preparation example Construction

[0044] The present invention also provides a preparation method of the paliperidone press-coated sustained-release tablet described in the above technical scheme, comprising the following steps:

[0045] 1) mixing the filler and retarder, and wet granulating the binder solution to obtain the first granular material; mixing the first granular material with paliperidone, lubricant and slow-release material to obtain the mixed material, Compress to obtain the sustained-release portion of the tablet core;

[0046] 2) Mix the filler, blocker and microenvironment regulator, and use the binder solution to wet granulate to obtain the second granular material; mix the second granular material with the lubricant and the slow-release material to obtain the blank slow-release part of the outer layer;

[0047] 3) filling the outer layer of the blank sustained-release part, the tablet core of the sustained-release part and the outer layer of the blank sustained-release part in sequence, an...

Embodiment 1

[0057] Paliperidone Sustained Release Tablets 3mg System (based on 1000 tablets)

[0058] The composition of the prescription is shown in Table 1.

[0059] Table 1 Paliperidone compression-coated sustained-release tablet (3mg) prescription composition table

[0060]

[0061] 1. Tablet core preparation: weigh Eudragit RLPO and microcrystalline cellulose according to the prescription amount, mix them evenly, make a soft material with 3% sodium alginate solution, pass through a 40-mesh sieve, extrude and granulate, and dry at 40°C After 2 hours, pass through a 40-mesh sieve for granulation, add hydroxypropyl cellulose, glyceryl behenate and paliperidone, mix well, and press a 5mm flat punch into a tablet. The tablet hardness is controlled at about 40N, and the mass range is 50±2.25 mg.

[0062] 2. Preparation of the pressing coating layer: Weigh Eudragit RLPO, microcrystalline cellulose and citric acid according to the prescription, mix well, use 3% sodium alginate solution ...

Embodiment 2

[0071] Paliperidone Sustained Release Tablets 6mg System (based on 1000 tablets)

[0072] The composition of the prescription is shown in Table 3.

[0073] Table 3 Paliperidone compression-coated sustained-release tablet (6mg) prescription composition table

[0074]

[0075] 1. Tablet core preparation: Weigh Eudragit RL PO and microcrystalline cellulose according to the prescription amount, mix well, make soft material with 3% sodium alginate solution, pass through a 40-mesh sieve, extrude and granulate, and store at 40°C Dry for 2 hours, pass through a 40-mesh sieve for granulation, add hydroxypropyl cellulose, glyceryl behenate and paliperidone, mix evenly, use a 5mm flat punch to make tablets, the tablet hardness is controlled at about 40N, and the mass range is 50± 2.25 mg.

[0076] 2. Preparation of the pressing coating layer: weigh Eudragit RL PO, microcrystalline cellulose and citric acid according to the prescription amount, mix well, use 3% sodium alginate soluti...

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Abstract

The invention relates to a paliperidone tablet and a preparation method thereof, belonging to the technical field of medicine. The invention provides an oral slow-release tablet capable of sustaining drug release at an increasing rate, which satisfies the need for administration once every 24 hours and improves patient compliance. A microenvironment regulator was added to the blank sustained-release outer layer to ensure that the internal microenvironment of the tablet maintained a relatively stable pH value and achieved complete release without being affected by the pH of the external environment. The tablet of the invention does not contain any harmful organic solvents, breaks through the limitation of the content uniformity of small doses of medicines, and is beneficial to scale-up production; it is mainly used for treating schizophrenia clinically.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a paliperidone press-coated sustained-release tablet and a preparation method thereof. Background technique [0002] Schizophrenia is called "the cancer of the 21st century". The prevalence of schizophrenia in the world has reached 1%, and the incidence and suicide rates are increasing year by year. The treatment process of schizophrenia is relatively slow and easy to relapse, so the prevention and rehabilitation of schizophrenia is an urgent problem to be solved by medical workers. Schizophrenia requires long-term drug treatment, so it is very important to improve patients' medication compliance. According to the results of the first nationwide survey of outpatients with schizophrenia, more than 30% of the patients have compliance problems. In view of this, we urgently need to develop a more suitable sustained-release preparation. Paliperidone, the active metabolite of rispe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/36A61K31/519A61P25/18
CPCA61K9/2054A61K9/2853A61K9/2866A61K31/519A61P25/18
Inventor 黄浩唐星陈淑敏
Owner 沈阳信康药物研究有限公司
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