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Delamanid quick-release preparation and preparation method thereof

A technology for immediate-release preparations and lubricants, which is applied in the directions of pill delivery, pharmaceutical formulations, and medical preparations with inactive ingredients, etc., can solve problems such as poor in vitro dissolution of delamanid, and achieve improved in vitro and in vivo performance and low energy consumption. , the effect of simple preparation process

Inactive Publication Date: 2019-05-10
REYOUNG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In view of the deficiencies in the prior art, the object of the present invention is to provide a delamanid immediate-release preparation, which solves the problem of poor dissolution of delamanid in vitro, improves its bioavailability in vivo, and improves the therapeutic effect; At the same time, the present invention also provides its preparation method, which is simple, low energy consumption, no solvent residue, no other impurities will be introduced in the whole process, and it is easy to realize continuous production

Method used

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  • Delamanid quick-release preparation and preparation method thereof
  • Delamanid quick-release preparation and preparation method thereof
  • Delamanid quick-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] A delamanid immediate-release preparation made of the following components in mass percent:

[0033]

[0034] Preparation:

[0035] (1) After delamanid, xylitol and hypromellose phthalate are passed through an 80 mesh sieve respectively, they are mixed with a three-dimensional mixer to obtain a physical mixture;

[0036] (2) Preheat the hot-melt extruder for 30 minutes, set the hot-melt extrusion temperature to 175°C, and set the screw speed to 45r / min. After the temperature reaches the set temperature, add the physical mixture evenly into the hot-melt extruder In the stuffing hopper, it is melted by the screw of the hot-melt extruder, mixed, extruded, and strip-shaped solids are extruded;

[0037] (3) After the strip solid is cooled, it is pulverized into particles with a pulverizer, and the particles pass through a 40-mesh sieve to obtain a Dramani solid dispersion;

[0038] (4) Mix the Delamani solid dispersion with lactose, microcrystalline cellulose, croscarme...

Embodiment 2

[0043] A delamanid immediate-release preparation made of the following components in mass percent:

[0044]

[0045] Preparation:

[0046] (1) After delamanid, xylitol and hypromellose phthalate are passed through an 80 mesh sieve respectively, they are mixed with a three-dimensional mixer to obtain a physical mixture;

[0047] (2) Preheat the hot-melt extruder for 30 minutes, set the hot-melt extrusion temperature to 185°C, and set the screw speed to 50r / min. After the temperature reaches the set temperature, add the physical mixture evenly into the hot-melt extruder In the stuffing hopper, it is melted by the screw of the hot-melt extruder, mixed, extruded, and strip-shaped solids are extruded;

[0048] (3) After the strip solid is cooled, it is pulverized into particles with a pulverizer, and the particles pass through a 40-mesh sieve to obtain a Dramani solid dispersion;

[0049] (4) Mix the Delamani solid dispersion with lactose, microcrystalline cellulose, croscarme...

Embodiment 3

[0052] A delamanid immediate-release preparation made of the following components in mass percent:

[0053]

[0054]

[0055] Preparation:

[0056] (1) Pass through an 80-mesh sieve respectively after delamani, xylitol and hypromellose acetate phthalate are mixed with a three-dimensional mixer to obtain a physical mixture;

[0057](2) Preheat the hot-melt extruder for 30 minutes, set the hot-melt extrusion temperature to 175°C, and set the screw speed to 45r / min. After the temperature reaches the set temperature, add the physical mixture evenly into the hot-melt extruder In the stuffing hopper, it is melted by the screw of the hot-melt extruder, mixed, extruded, and strip-shaped solids are extruded;

[0058] (3) After the strip solid is cooled, it is pulverized into particles with a pulverizer, and the particles pass through a 40-mesh sieve to obtain a Dramani solid dispersion;

[0059] (4) Mix the Delamani solid dispersion with lactose, microcrystalline cellulose, cro...

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Abstract

The invention belongs to the field of pharmacy, in particular to a Delamanid quick-release preparation and a preparation method thereof. The Delamanid quick-release preparation takes hydroxypropyl methylcellulose acetate phthalate or hypromellose phthalate as a dispersed carrier material, functional auxiliary materials such as sugar alcohols are added as plasticizers, the materials and Delamanid active pharmaceutical ingredients are subjected to high-temperature extrusion through a hot melt extruder, then cooled and crushed into powder, then the powder is fully mixed with a filler, a disintegrating agent and a lubricant, tabletting is conducted directly, and the preparation is obtained. The problem that Delamanid is poor in in vitro dissolution is solved, the in vivo bioavailability is improved, and the therapeutic effect is ultimately improved; the preparation method is simple, energy consumption is small, no residual solvents exist, other impurities cannot be introduced in the wholeprocess, and continuous production is easy to achieve.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a delamani quick-release preparation and a preparation method thereof. Background technique [0002] Delamanid is a nitro-dihydro-imidazole-oxazole derivative that can selectively inhibit mycobacterium tuberculosis cell wall components, thereby exhibiting antibacterial activity against mycobacteria, but delamanid is a water difficult Soluble crystalline drug with low solubility and low bioavailability. Commonly used methods to improve the bioavailability of poorly soluble drugs include nanocrystallization, micronization technology and solid dispersion technology. After the drug is micronized, its surface free energy increases, and there will be a tendency to agglomerate, which reduces the micronization effect to a certain extent. At present, insoluble drugs are prepared into solid dispersions by using highly water-soluble carrier materials, so as to achieve the purpose of im...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/454A61K47/26A61P31/06
Inventor 苗得足胡清文李相林曾丽丽
Owner REYOUNG PHARMA
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