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Indissolvable drug oral sustained-release composition and preparation method thereof

A technology for sustained-release compositions and insoluble drugs, applied in the field of medicine, can solve the problems of inability to obtain satisfactory sustained and controlled-release formulation development prescription process, incomplete dissolution, too fast dissolution, etc., and achieve stable and effective localized release effect and complete release. Effect

Active Publication Date: 2020-10-02
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] In the course of the research, the inventor found that the physical mixing of insoluble drugs and sustained-release materials, or further granulation, and then tablet compression, is prone to the problem of excessive dissolution or incomplete final dissolution, and cannot obtain satisfactory sustained-release formulation development. Prescription process

Method used

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  • Indissolvable drug oral sustained-release composition and preparation method thereof
  • Indissolvable drug oral sustained-release composition and preparation method thereof
  • Indissolvable drug oral sustained-release composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～4

[0057] The used prescription of embodiment 1~4 and consumption ratio are as shown in table 1 below, and the material total amount of every batch is 500g (excluding solvent weight):

[0058] Table 1

[0059]

[0060] *Solvents will be removed by drying during processing.

[0061] Embodiment 1~4 preparation process steps:

[0062] 1) Dissolve Eudragit S 100 in an appropriate amount of ethanol (95%); add Apremilast, talcum powder and triethyl citrate into an appropriate amount of ethanol (95%), and homogenize with a homogenizer for about 10 minutes. Then pour it into the Eudragit S 100 solution, and use a stirrer to continuously stir the suspension during the granulation process;

[0063] 2) Spray the suspension in step 1) on the microcrystalline cellulose through WBF-2G fluidized bed top spray granulation, and control the atomization pressure at 0.5-2.0bar during the process (adjust 0.5bar every 10min to the maximum value) ) and spray speed 5 ~ 15g / min (up to 5g / min every ...

Embodiment 5～8

[0067] The prescriptions and dosage ratios used in Examples 5 to 8 are shown in Table 2 below, wherein the particle size distribution d90 of the bulk drug used in Apremilast is 7.4 microns, and the total amount of materials in each batch is 500g (excluding solvent weight).

[0068] Table 2

[0069]

[0070]

[0071] *Based on weight of solid matter in Eudragit aqueous dispersion.

[0072] **The amount of purified water includes the amount of water in the Eudragit water dispersion and the amount of added water. The purified water will be dried and removed during processing. In the prescription, other components except the liquid strong adsorption carrier and the binder are prepared into a suspension with the solvent, and the amount of the solvent used is that the solid content of the suspension is about 20% to 25%.

[0073] Embodiment 5~8 preparation process steps:

[0074] 1) Add anti-sticking agent, plasticizer, surfactant, and main ingredient to a certain amount of s...

Embodiment 9

[0079] The prescription and dosage ratio used in embodiment 9 are shown in the following table 3, wherein the particle size distribution d90 of the crude drug used in apremilast is 15 microns, and the total amount of material in each batch is 500g (excluding solvent weight).

[0080] table 3

[0081]

[0082] *In the prescription, other components except liquid strong adsorption carrier and adhesive are prepared into a suspension with the solvent. The amount of solvent used is that the solid content of the suspension is 25.4%, and the purified water will be dried during processing remove.

[0083] Embodiment 9 preparation process steps:

[0084] 1) Slowly pour the enteric-coated material Eudragit L100 into water and stir for 5-10 minutes. After the enteric-coated material is completely wetted, slowly add sodium hydroxide powder or solution and keep stirring, and finally continue stirring for 30 minutes. Then add raw material drug, plasticizer and anti-adhesive agent, con...

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Abstract

The invention discloses an indissolvable drug oral sustained-release composition, which is especially suitable for low-dose indissolvable drugs. The indissolvable drug oral sustained-release composition comprises sustained-release particles and a gel skeleton, wherein the sustained-release particles comprise an indissolvable drug, an enteric material and a liquid strong adsorption carrier; the gelskeleton comprises a hydrophilic gel skeleton material; and the sustained-release particles are obtained by preparing a suspension from the indissolvable drug and the enteric material and then spraying the suspension onto the liquid strong adsorption carrier. The sustained-release particles are partially wrapped by the gel skeleton to form a multi-sustained-release system technology, the releasetime is prolonged, the preparation process is simple, the efficiency is high, the drug mixing is uniform, and the content loss is less.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an oral sustained-release composition, in particular to an oral sustained-release composition of low-dose insoluble drugs and a preparation method thereof. Background technique [0002] In the field of pharmaceuticals, many drugs have been developed as sustained-release, multi-stage release controlled-release preparations in order to stabilize the blood concentration, reduce the number of medications, increase the compliance of patients taking medication, improve medication safety, curative effect and reduce side effects, etc. Highly active drugs are used in low doses in clinical practice and show good therapeutic effects, but sometimes they also cause toxic and side effects due to high and low blood drug levels and fluctuations. Therefore, there is a large proportion of low-dose highly active drugs that need to be developed into slow-release and controlled-release preparatio...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/26A61K31/454A61K31/4035A61K31/519A61K31/4545A61K47/36A61K47/38A61K47/32
CPCA61K9/2095A61K9/2077A61K9/2054A61K9/205A61K9/2027A61K31/454A61K31/4035A61K31/519A61K31/4545A61K9/2031A61K9/2059A61K9/2009A61K9/2013A61K9/1652A61K9/1635
Inventor 刘锋谭晓峰梁文伟周伟杰黄俊龙
Owner AC PHARMA CO LTD
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