Preparation method of low melting point drug solid dispersion

A technology of solid dispersion and low melting point, which can be applied to medical preparations containing non-active ingredients, medical preparations containing active ingredients, and drug delivery, etc. Bioavailability, environmental friendliness, effect of reducing operation steps

Inactive Publication Date: 2011-02-02
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the usual solid dispersion preparation technology, povidone (PVP), PEG, F-68, etc. are commonly used as carrier materials for immediate release preparations, but these excipients are cohesive, and when they exist in large amounts, they are difficult to make due to the impact of disintegration immediate release tablet

Method used

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  • Preparation method of low melting point drug solid dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] α-Asarone 30g

[0025] Low-substituted hydroxypropyl cellulose (LH-21) 236.4g

[0026] Sodium carboxymethyl starch 24g

[0027] Talc powder 3g

[0028] Magnesium Stearate 1.5g

[0029] Micronized silica gel 0.6g

[0030] Sodium Lauryl Sulfate 4.5g

[0031] Prepare the raw material α-asarone and each auxiliary material according to the above prescription and pass through an 80-mesh sieve, mix evenly, seal, keep the temperature at 65°C for 1.5h, cool to room temperature, and obtain a solid dispersion, lightly crush and pass through a 40-mesh sieve Sieve, and compress into 1000 tablets according to the weight of each tablet of 0.3g, to obtain immediate-release α-asarone tablets.

Embodiment 2

[0033] Ibuprofen 100g

[0034] Microcrystalline Cellulose (PH101) 135.5g

[0035] Sodium carboxymethyl starch 12g

[0036] Talc powder 1.5g

[0037] Magnesium stearate 0.7g

[0038] Micronized silica gel 0.3g

[0039] The raw material ibuprofen and various auxiliary materials were prepared according to the above prescription and passed through an 80 mesh sieve, mixed evenly, sealed, kept at a constant temperature of 85°C for 2 hours, cooled to room temperature to obtain a solid dispersion, lightly crushed, passed through a 40 mesh sieve, and Press each tablet weight 0.25g and press into 1000, obtain quick-release ibuprofen tablet.

Embodiment 3

[0041] Paeonol 40g

[0042] Low-substituted hydroxypropyl cellulose (LH-21) 229.4g

[0043] Sodium carboxymethyl starch 24g

[0044] Talc powder 3g

[0045] Magnesium Stearate 1.5g

[0046] Micronized silica gel 0.6g

[0047] Sodium Lauryl Sulfate 1.5g

[0048] Prepare the raw materials and various auxiliary materials according to the above prescription and pass through a 80-mesh sieve, mix evenly, seal, keep the temperature at 60°C for 1.5h, cool to room temperature, and after obtaining a solid dispersion, lightly press and crush, pass through a 40-mesh sieve, and press Each tablet weighing 0.3 g was pressed into 1000 tablets to obtain immediate-release paeonol tablets.

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Abstract

The invention belongs to the pharmaceutical field and relates to a preparation method of a low melting point drug solid dispersion. The preparation method comprises the following steps: crushing pharmaceutical raw materials and auxiliary materials, passing through a 60-120-mesh sieve, then uniformly mixing, sealing, placing at the constant temperature of 45-140 DEG C for 0.5-4h, cooling to room temperature and obtaining the solid dispersion, wherein the pharmaceutical raw materials are insoluble drugs with the melting points in the range of 45-130 DEG C; and the auxiliary materials comprise a filling agent, a disintegrant, a dry adhesive, a lubricating agent, a glidant and a surfactant. The preparation method has the following advantages: simple operation, low equipment requirements and no solvent residue; the prepared solid dispersion is easy to crush and can be prepared into quick-release tablets, capsules, power or slow-release tablets; a quick-release preparation prepared through the preparation method has high drug loading, fast drug dissolution speed and high dissolution rate; and the prepared slow-release tablets have good uniformity and stable drug release.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a method for preparing a drug with poor solubility and low melting point (45-130° C.) into a solid dispersion and an oral quick-release or sustained-release solid preparation thereof. Background technique [0002] For drugs with poor solubility, when they are prepared into oral solid preparations by ordinary methods, there are problems such as low dissolution rate and poor absorption after taking, which will affect the drug efficacy and therapeutic effect. In response to this situation, people invented the solid dispersion preparation technology, which highly disperses the drug in the carrier material to make an oral solid preparation, thereby improving the dissolution rate and bioavailability of the drug. But the method (melt method, solvent method, melt-solvent method, spray drying method, grinding method, hot-melt extrusion method etc.) of the method (melt method, solvent m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K47/38A61K47/40A61K45/00A61K47/34A61K47/44A61K9/00A61K47/32A61K47/10
Inventor 赵会英董达文
Owner BEIJING UNIV OF CHEM TECH
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