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Solid dosage form comprising solid dispersion and method for producing the same

A solid dispersion and solid preparation technology, applied in the field of solid preparations, can solve problems such as lack of solubility and difficult preparations, and achieve the effect of excellent solubility and high solubility

Inactive Publication Date: 2008-02-20
SHIN ETSU CHEM IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the solid dispersion of amorphous nilvadipine described in Journal of the Pharmaceutical Society of Japan (124(1), 19-23(2004) does not seem to have sufficient solubility
In addition, disintegration is inhibited due to the influence of water-soluble polymers, so it is difficult to obtain rapidly dissolving formulations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0083] The present invention is specifically described below by way of examples and comparative examples, however, the present invention is not limited to these examples.

Synthetic example 1～3

[0084] Synthesis Example 1-3 Synthesis of Low Substituted Hydroxypropyl Cellulose Powder

[0085] First, 806g of powdered slurry (750g in anhydrous state) was added to a 10L internal stirring reaction device, 303g of sodium hydroxide aqueous solution (26wt%) was added to the reaction device, and then mixed at 45°C for 30 minutes Produce alkaline cellulose, wherein the weight ratio of sodium hydroxide and anhydrous cellulose is 0.105. Nitrogen purging was then carried out, 123 g of propylene oxide (0.164 parts by weight relative to cellulose) was added to the resultant, and then the mixture was reacted for 1.5 hours in a jacket at a temperature of 60° C., thereby obtaining 1232 g of hydroxypropyl fibers Crude reaction product of a prime with a molar substitution of hydroxypropoxy per anhydroglucose unit of 0.28. The etherification reaction rate was 61.4%.

[0086]Then, 236 g of acetic acid (50 wt %) was added to and mixed in the above-mentioned 10 L internal stirring type r...

Embodiment 1～3 and comparative example 1～3

[0091] By dissolving a predetermined amount (shown in Table 2) of nifedipine and hydroxypropyl methylcellulose (HPMC) (hydroxypropoxyl 8.7wt%, methoxyl 28.8wt%, 6mPa·s) in a solution containing a weight ratio 8:2 mixed solvent of ethanol and water to prepare solid dispersion solution. Then, a mixture of low-substituted hydroxypropyl cellulose (L-HPC), lactose (Pharmatose produced by DMV International) and cornstarch (cornstarch W produced by NIHON SHOKUHIN KAKO) in a predetermined amount (shown in Table 2) was added to the In the fluidized bed granulation equipment (Multiplex MP-01 manufactured by POWREX CORPORATION), the above solid dispersion solution was sprayed onto the above mixture, and the resultant was granulated and dried using 30 mesh (pore: 500 μm) The sieve adjusts the particle size to obtain granular products. The granulation and drying conditions at this time are as follows.

[0092] Inlet air temperature: 60°C,

[0093] Exhaust air temperature: 40°C;

[0094...

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Abstract

Provided are a solid dosage form comprising an enteric solid dispersion that allows a drug in the preparation to be rapidly dissolved without compromising the solubility of the solid dispersion, and a method for producing the same. More specifically, provided is a solid dosage form comprising an enteric solid dispersion comprising a poorly soluble drug, an enteric polymer and a disintegrant, wherein the disintegrant is low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 [mu]m and a specific surface area measured by BET method of at least 1.0 m 2 / g. Moreover, provided is a method for producing a solid dosage form comprising an enteric solid dispersion, the method comprising steps of: spraying an enteric polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a powder of low-substituted hydroxypropylcellulose having an average particle size of 10 to 100 [mu] m and a specific surface area measured by BET method of at least 1.0 m 2 / g and serving as a disintegrant; and granulating the resultant; and drying.

Description

technical field [0001] The invention relates to a solid preparation containing a solid dispersion, which is used to improve the solubility of poorly soluble drugs, and also relates to a preparation method thereof. Specifically, the present invention relates to a solid preparation containing a solid dispersion, which can rapidly disintegrate and allow the drug to dissolve, and also relates to a preparation method thereof. Background technique [0002] Poorly soluble drugs have high crystallinity and very low solubility in water. Therefore, preparations prepared from these drugs have low bioavailability or in vivo absorption, making insufficient drug action a problem. As a technique for solving such problems, solid dispersions have been developed in which poorly soluble drug molecules are dispersed in an amorphous state in a high-molecular-weight carrier such as a cellulose derivative. [0003] Conventional solid dispersions are used in the form of formulations of capsules c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/38A61K9/16
Inventor 星野贵史草木史枝丸山直亮西山裕一福井育生梅泽宏
Owner SHIN ETSU CHEM IND CO LTD
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