Obeticholic acid pharmaceutical composition as well as preparation method and application thereof

A technology of obeticholic acid and its composition, which is applied in the field of obeticholic acid pharmaceutical composition and its preparation, can solve the problems of unfavorable large-scale industrial production, unstable preparation process, and low production efficiency, and achieve optimal dissolution rate and Uniformity of quality, shortened production cycle, and easy operation

Pending Publication Date: 2021-11-19
BEIJING SIHUAN PHARMA +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method has defects such as unstable preparation process, low production efficiency, high preparation cost, and being unfavorable for large-scale industrial production.
[0015] Therefore, there is an urgent need to develop a preparation method for obeticholic acid preparations that is easy to operate, has good process stability, and is more cost-effective, and is suitable for large-scale industrial production, and effectively solves the problems of its quality uniformity and dissolution rate of preparations.

Method used

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  • Obeticholic acid pharmaceutical composition as well as preparation method and application thereof
  • Obeticholic acid pharmaceutical composition as well as preparation method and application thereof
  • Obeticholic acid pharmaceutical composition as well as preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0108] Embodiment 1 Preparation of obeticholic acid pharmaceutical composition of the present invention

[0109] The preparation method of obeticholic acid pharmaceutical composition comprises the following steps:

[0110] (1) sending the obeticholic acid crude drug into an ultra-high-speed jet mill for micronization, with a pressure of 0.3Mpa;

[0111] (2) Put obeticholic acid micronized granules, microcrystalline cellulose in granules, and sodium carboxymethyl starch in granules into a ziplock bag and mix for 5 minutes, pass through a vertical granulator equipped with a 1.0mm screen, and then transfer to After mixing in a ziplock bag for 8 minutes, add intragranular magnesium stearate, and mix for 5 minutes to prepare a premix;

[0112] Put the prepared premix into the dry granulator, set the feeding speed: 20rpm, the roller pressure: 25bar, the roller speed: 8rpm, the shear speed: 100rpm, the granulation speed: 100rpm, the screen aperture: 1.0 mm, run with the above par...

Embodiment 2

[0115] Embodiment 2 Preparation of obeticholic acid pharmaceutical composition of the present invention

[0116] The preparation method of obeticholic acid pharmaceutical composition comprises the following steps:

[0117] (1) Send the obeticholic acid crude drug into a jet mill for micronization, with a pressure of 0.5Mpa;

[0118] (2) Put obeticholic acid micronized granules, intragranular microcrystalline cellulose, and intragranular sodium carboxymethyl starch into a 5L mixing hopper, mix at 30rpm for 25min, and pass through a vertical granulator equipped with a 1.2mm screen. , then transferred to the mixing hopper and mixed at the same speed for 10 minutes, then added intragranular magnesium stearate, and mixed for 8 minutes to obtain a premix;

[0119] Put the prepared premix into the dry granulator, set the feeding speed: 20rpm, the roller pressure: 40bar, the roller speed: 8rpm, the shear speed: 100rpm, the granulation speed: 100rpm, the screen aperture: 1.5 mm, ru...

Embodiment 3

[0122] Embodiment 3 Preparation of obeticholic acid pharmaceutical composition of the present invention

[0123] The preparation method of obeticholic acid pharmaceutical composition comprises the following steps:

[0124] (1) Send the obeticholic acid crude drug into a jet mill for micronization, with a pressure of 0.6Mpa;

[0125] (2) Put obeticholic acid micronized granules, microcrystalline cellulose in granules, and sodium carboxymethyl starch in granules into a 50L mixing hopper for mixing, mix at a speed of 25rpm for 60min, and then pass through a vertical mixer equipped with a 1.5mm sieve. The granulator and the granulator are also equipped with rounded granulation knives, set the speed at 300rpm, and then transfer the undersieve to a 50L mixing hopper, and mix at a speed of 45rpm; after 30min, add magnesium stearate in the granule and mix for 20min. Get the premix;

[0126] Put the prepared premix into the dry granulator, set the feeding speed: 60rpm, the roller p...

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Abstract

The invention provides a pharmaceutical composition containing obeticholic acid or a derivative thereof, as well as a preparation method and application thereof. According to the preparation method of the pharmaceutical composition of obeticholic acid or the derivative thereof, the operation step of mixing microcrystalline cellulose in batches for multiple times and multiple steps is omitted, and the dissolution rate and the quality uniformity of the pharmaceutical composition are improved by optimizing the preparation process; and the prepared pharmaceutical composition has the advantages of high product uniformity, low possibility of cracking, high dissolution rate and the like, so that the effectiveness and the safety of the medicine are improved, and the quality problems of preparation friability and the like are effectively solved.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an obeticholic acid pharmaceutical composition, a preparation method thereof and an application thereof. Background technique [0002] Obeticholic acid (6α-ethyl-3α, 7α-dihydroxy-5β-cholan-24-acid, whose structure is shown in formula I) is the natural human bile acid CDCA (chenodeoxycholic acid) Orally active analogue, clinically used for the treatment of primary biliary cholangitis (PSC). [0003] [0004] Obeticholic acid has the characteristics of low solubility and high permeability, and drug dissolution and dissolution are the rate-limiting steps for its in vivo absorption. For this reason, improving drug dissolution rate has become an important means to improve drug bioavailability. Previous studies have used methods such as reducing the particle size of the drug substance and changing the crystal form to improve the dissolution, dissolution rate and bioavailability...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K47/36A61K47/38A61K31/575A61P1/16A61P19/10A61P35/00
CPCA61K9/28A61K9/2095A61K9/2054A61K9/2059A61K31/575A61P1/16A61P19/10A61P35/00
Inventor 刘亚萍李巧霞唐文雅王辉春金振诗邓声菊徐艳君王田园
Owner BEIJING SIHUAN PHARMA
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