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Finely pulverized pharmaceutical composition

A composition and drug technology, applied in the direction of drug combination, powder delivery, pharmaceutical formulation, etc., can solve the problems of foreign matter, inability to prepare drugs, etc., and achieve the effects of increasing blood concentration, high curative effect, and high absorption

Inactive Publication Date: 2012-02-29
MEIJI SEIKA KAISHA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, these milling methods cause problems of drug decomposition by heat generation or foreign matter by scraping the used media by grinding the drug with grinding media.
Therefore, pharmaceuticals cannot be prepared by the above grinding method

Method used

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  • Finely pulverized pharmaceutical composition
  • Finely pulverized pharmaceutical composition
  • Finely pulverized pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0116] Embodiment 1: the grinding of crude drug

[0117] By adding 3.0 kg of 22β-methoxyolean-12-ene-3β, 24(4β)-diol bulk drug (manufacturer: Meiji Seika Kaisha Co., Ltd., cumulative 50% particle size: about 50 μm, cumulative 90% Particle size: about 100 μm), 0.3kg sodium lauryl sulfate and 6.7kg purified water are dispersed in the aqueous solution obtained with the weight ratio of 30:3:67 with high-pressure homogenizer (model: Microfluidizer, manufacturer: Microfluidics) Grinding was performed under the grinding conditions (treatment pressure and number of treatments) shown in Table 1 to obtain a suspension. Regarding the particle diameter of the bulk drug in the suspension, the cumulative 50% particle diameter and the cumulative 90% particle diameter were measured with a particle size distribution measuring device (manufacturer: NIKISSO Co., Ltd., model: Microtruck×100). The results are shown in Table 1.

[0118] [Table 1]

[0119]

Embodiment 2

[0122] Embodiment 2: dissolution test (1)

[0123] Dissolution tests were performed on the suspension prepared in Example 1 (grinding condition 3) and the liquid obtained by suspending the milled drug substance obtained in Comparative Example 1 in water.

[0124]Accurately weigh each suspension in an amount corresponding to 50 mg of 22β-methoxyolean-12-ene-3β,24(4β)-diol drug substance, and pass the dissolution test method detailed in the Japanese Pharmacopoeia - The second method (paddle method) is used to test at a rotational speed of 100 rpm (the rotational speed of the paddle), using 900 mL of 1% polysorbate 80 aqueous solution as the test solution. 15 minutes, 30 minutes, 60 minutes, and 180 minutes after the start of dissolution, 5 mL of the test solution was collected and filtered through a membrane filter with a pore size of 0.2 μm to obtain measurement samples. The samples were analyzed by high performance liquid chromatography (manufacturer: Shimadzu Seisakusho Co...

Embodiment 3

[0128] Example 3: Stability over Time of Milled Drug Substances in Suspension

[0129] The suspension obtained by the grinding of Example 1 (grinding condition 3) was stored in a standing state to confirm whether the particle size of the fine particles of the drug substance in the suspension underwent changes with time. The suspension was stored statically at 5°C, 15°C and 25°C.

[0130] The cumulative 50% particle diameter and the cumulative 90% particle diameter are measured with the same particle size distribution measuring device over time. The results are shown in figure 2 and 3 . Both the cumulative 50% particle size and the cumulative 90% particle size remained unchanged for one month, indicating that secondary aggregation did not occur. That is, it was confirmed that grinding by the method described in this application can allow sodium lauryl sulfate in suspension to suppress secondary aggregation, whereby physicochemically stable drug substance particles can be...

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PUM

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Abstract

Disclosed are a composition containing a poorly soluble medicinal substance and having improved oral absorption, and a method for producing the composition. Specifically disclosed is a finely pulverized composition which contains a poorly soluble medicinal substance such as 22ss-methoxyolean-12-ene-3ss-,24(4ss)-diol and a hydrophilic surfactant. Also specifically disclosed is a method for producing a finely pulverized composition, which is characterized in that a poorly soluble medicinal substance and a hydrophilic surfactant are first dispersed in a solvent, and then pulverized by a high-pressure homogenizer.

Description

technical field [0001] The present invention relates to a finely pulverized composition comprising a sparingly soluble drug and a hydrophilic surfactant. More specifically, the present invention relates to a finely powdered composition comprising a slightly soluble drug 22β-methoxyolean-12-ene-3β,24(4β)-diol and a surfactant, and the finely powdered composition comprises The above ingredients and additional pharmaceutically acceptable polymer compounds. Background technique [0002] 22β-methoxyolean-12-ene-3β,24(4β)-diol is a drug synthesized using soybean sterol B contained in soybean hypocotyls as a raw material, and has been developed mainly as a therapeutic agent for liver diseases Pharmaceutical compounds (see, for example, Patent Document 1). [0003] This compound is unlikely to be soluble in water or an organic solvent, and thus is a slightly soluble compound that cannot be expected to be absorbed into the body of a human or the like without using a special techniq...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/20A61K9/10A61K9/14A61K9/20A61K31/075A61K45/00A61K47/26A61K47/30A61K47/32A61K47/34A61K47/38A61P1/16
CPCA61K9/145A61K9/146A61K31/075A61P1/16A61K9/14A61K9/20A61K47/20
Inventor 近势茂川田大
Owner MEIJI SEIKA KAISHA LTD