Paliperidone gastric retention tablet and preparation method thereof

A technology for paliperidone and gastric retention, which is applied in the field of medicine and can solve problems such as high difficulty, complicated process, and need to improve the sustained release effect

Active Publication Date: 2021-06-11
HONG KONG JOWA & HUAYUAN GRP CHUZHOU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of this application is to provide a Paliperidone Gastric Retentive Tablet and its preparation method, aiming to solve the complex and difficult preparation process of existing paliperidone sustained-release tablets and injections, and the sustained-release effect needs to be improved to a certain extent The problem

Method used

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  • Paliperidone gastric retention tablet and preparation method thereof
  • Paliperidone gastric retention tablet and preparation method thereof
  • Paliperidone gastric retention tablet and preparation method thereof

Examples

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preparation example Construction

[0039] The second aspect of the embodiment of the present application provides a preparation method of paliperidone gastric retention tablets, comprising the following steps:

[0040] S10. Mixing and dissolving the prescribed amount of glyceryl monostearate, lecithin, paliperidone and absolute ethanol to obtain an organic phase;

[0041] S20. After mixing the surfactant with the organic phase, heat and concentrate to obtain paliperidone-solid lipid nanoparticles;

[0042] S30. After mixing the paliperidone-solid lipid nanoparticles with the formulated amount of hydroxypropyl methylcellulose, polyoxyethylene, pregelatinized starch, foaming agent, bleaching aid and flow aid, dry method Tablets are obtained to obtain Paliperidone Gastric Retentive Tablets.

[0043] The preparation method of paliperidone gastric retention tablet provided by the second aspect of the present application, first, mix and dissolve the monostearyl glyceride, lecithin, paliperidone and absolute ethanol ...

Embodiment 1

[0049] Paliperidone-lipid nanoparticles, the preparation of which includes the steps of: mixing a formula amount of glyceryl monostearate, lecithin, paliperidone and absolute ethanol, and maintaining the heating temperature at 40-50°C for dissolution to obtain an organic phase; at a stirring speed of 900-1100r / min, mix and stir the surfactant and the organic phase for 1h, then heat and concentrate, and evaporate the solvent to obtain a translucent nanoemulsion, that is, paliperidone-solid lipid nano Granular colloidal solution, stored at low temperature at 0-4°C, paliperidone-solid lipid nanoparticles can be obtained; pulverized, passed through 80-mesh sieve.

[0050] Using single factor investigation test, using encapsulation efficiency and drug loading as evaluation index, investigating different factors such as paliperidone, monostearyl glyceride, surfactant type, surfactant concentration, etc., to prepare paliperidone- Effect of Lipid Nanoparticles, Again Using Orthogonal ...

Embodiment 2

[0065] Paliperidone gastric retention tablet, its preparation comprises steps:

[0066] ①Mix 21g of glyceryl monostearate, 41g of lecithin, 3g of paliperidone and 2g of absolute ethanol in the prescribed amount, and dissolve at a heating temperature of 40-50°C to obtain an organic phase; stir at 900-1100r / min Mix and stir 2g of 0.4% poloxamer aqueous solution F68 (m / V) aqueous solution with the organic phase for 1 hour, then heat and concentrate, and evaporate the solvent to obtain a translucent nanoemulsion, that is, paliperidone-solid lipid Quality nanoparticle colloid solution, stored at 0-4°C at low temperature, paliperidone-solid lipid nanoparticles can be obtained; pulverize, pass through 80-mesh sieve.

[0067] ②Weigh the prescription amount of HPMC-K15M, polyoxyethylene, pregelatinized starch, sodium bicarbonate, glyceryl monostearate, magnesium stearate, pass through an 80 mesh sieve, and use the paliperidone-solid obtained in step ① The lipid nanoparticles are evenl...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a paliperidone gastric retention tablet and a preparation method thereof. The paliperidone gastric retention tablet is prepared from the following raw material components in parts by weight: 2-3 parts of paliperidone, 10-15 parts of glyceryl monostearate, 20-30 parts of lecithin, 1-2 parts of a surfactant, 10-15 parts of hydroxypropyl methyl cellulose, 10-15 parts of polyoxyethylene, 24-30 parts of a filling agent, 8-12 parts of a foaming agent, 0.5-1 part of a floating aid and 0.1-0.5 part of a flow aid. According to the paliperidone gastric retention tablet, through the synergistic effect of all the components, the medicine floats and is retained in gastric juice, the retention time of the paliperidone medicine in the gastric juice is prolonged, the medicine is slowly released, the release time of the medicine in the digestive tract is prolonged, absorption is enhanced, blood concentration fluctuation is reduced, and therefore the bioavailability is improved.

Description

technical field [0001] The application belongs to the technical field of medicine, and in particular relates to a paliperidone gastric retention tablet and a preparation method thereof. Background technique [0002] Schizophrenia is a psychiatric disease, a persistent, usually chronic, major mental illness, and the most serious of all mental illnesses, characterized by the division of basic personality, thinking, emotion, and behavior, and the separation of mental activities and the environment. It is the most common type of mental illness characterized by incoordination. It usually occurs in young and middle-aged adults, and then affects behavior and emotion. [0003] Paliperidone is an atypical antipsychotic and the main plasma active metabolite of risperidone. It exerts its drug effect mainly by antagonizing 5-HT and dopamine receptors, and has affinity for other 5-HT receptor subtypes. It plays the role of adjuvant therapy and is widely used in the treatment of schizoph...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/14A61K47/24A61K47/38A61K47/32A61K47/10A61K47/12A61K47/44A61K31/519A61P25/18
CPCA61K9/0065A61K9/2013A61K9/2054A61K9/2027A61K9/2059A61K9/2095A61K9/2009A61K9/2031A61K31/519A61P25/18
Inventor 管悦琴罗雪峰李铁程
Owner HONG KONG JOWA & HUAYUAN GRP CHUZHOU PHARMA CO LTD
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