Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Solid formulation with improved solubility and stability, and method for producing said formulation

A solid preparation, soluble technology, applied in the field of solid preparations, to achieve the effects of excellent solubility, good stability, and reduced dosage

Inactive Publication Date: 2007-10-03
JAPAN TOBACCO INC
View PDF26 Cites 20 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0137] 2-3. Unresolved issues of MTP inhibitory substances

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Solid formulation with improved solubility and stability, and method for producing said formulation
  • Solid formulation with improved solubility and stability, and method for producing said formulation
  • Solid formulation with improved solubility and stability, and method for producing said formulation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0604] Hereinafter, the present invention is described in detail by way of examples and test examples, but the present invention is not limited to these.

[0605] will contain benzamide derivatives, 2-(2-{3-dimethylcarbamoyl-4-[(4′-trifluoromethyl-biphenyl-2-carbonyl)-amino]-phenyl} -Acetoxymethyl)-2-phenyl-diethyl malonate (hereinafter abbreviated as "MTP inhibitory compound") MTP inhibitory substance was used as a poorly soluble chemical substance in water, and was used in the following examples as active ingredient.

[0606] 1. Granulation,

[0607] (1) Dissolution of chemical substances as active ingredients

[0608] 418.5 g of acetone and 46.5 g of absolute ethanol (% by weight; 9:1) were injected into the propeller mixer, and 30.0 g of the above-mentioned MTP-inhibiting compounds of poorly water-soluble chemicals were added to the obtained acetone / absolute ethanol mixture and mix and fully dissolve.

[0609] (2) Dissolution of polymer substances

[0610] 300.0 g o...

Embodiment 2

[0622] Dissolution test

[0623] Using a 0.1 w / v% degassed sodium lauryl sulfate solution (900 mL, 37° C.), the dissolution test was performed according to the second method (paddle method, 50 rpm) of the Japanese Pharmacopoeia dissolution test method. The tablet (133.00 mg / tablet; containing 5 mg of bulk drug) prepared in Example 1 was put into the test solution as it was. For the reference control, the drug substance that constitutes the crystals is placed into the test solution as it is. Adjust the temperature to 37±0.1°C. The results are shown in Figure 1.

[0624] As shown in Fig. 1, 95.45% of the solid formulation of the present invention was dissolved within 15 minutes, while the reference compound (crystal) was not dissolved even after 60 minutes.

[0625] Considering that it is said that the food at the entrance will reach the small intestine in about 15 minutes to 30 minutes, the solid preparation of the present invention will completely dissolve when the preparat...

Embodiment 3

[0630] Formulations for Stability Testing and Amorphism Confirmation Testing

[0631] Test preparations were prepared in the following manner in order to confirm the stability and amorphousness of the solid preparations of the present invention.

[0632] Meanwhile, it is considered that the main cause affecting stability and crystallinity depends on the combination of the water-soluble polymer substance and the chemical substance poorly soluble in water, and a solid dispersion composed of both of these substances was used as a test preparation. The above MTP inhibitory compounds are used as poorly soluble chemicals in water.

[0633] Test formulations were prepared by adding an appropriate amount of the MTP-inhibiting compound to an appropriate amount of a suitable solvent shown below and additionally gradually adding the polymer substance to be tested, fully dissolving it, and spray-drying it.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

A solid medicinal preparation to which improved solubility has been imparted, while maintaining preparation stability, by taking a formulation contrivance on a sparingly water-soluble chemical substance as an active ingredient for the medicine. The solid preparation comprises a sparingly water-soluble chemical substance as an active ingredient, a water-soluble polymer, and an inorganic porous substance and has improved water solubility. It is characterized in that (1) the sparingly water-soluble chemical substance forms a solid dispersion together with the water-soluble polymer, (2) the water-soluble polymer as a component of the solid dispersion is in the form of fine pieces, and (3) the fine pieces of the water-soluble polymer are held on the surface of the inorganic porous substance in the state of being adsorbed on and / or adherent to the surface. The solid preparation can be produced by dissolving a sparingly water-soluble chemical substance as an active ingredient and a water-soluble polymer in an organic solvent, mixing the resultant solution with an inorganic porous substance with stirring, subsequently granulating the mixture, and then drying the granules.

Description

technical field [0001] The present invention relates to solid formulations with improved solubility and stability and methods of preparing said formulations. [0002] More particularly, the present invention relates to a solid preparation having improved water solubility comprising a chemical substance poorly soluble in water, a water-soluble polymer substance, and an inorganic porous substance as a pharmaceutically active ingredient, and a method for producing the same , characterized by [0003] (1) said poorly soluble chemical substance in water forms a solid dispersion together with said water-soluble polymer substance, [0004] (2) the water-soluble polymer substance forming the solid dispersion is in the form of fine pieces, and [0005] (3) The water-soluble polymer substance is in the form of fine flakes and remains adsorbed and / or attached to the surface of the inorganic porous substance. [0006] The solid preparation of the present invention has excellent solubil...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/02A61K9/14A61K9/20A61K31/225A61K45/00A61K47/04A61K47/30A61K47/32A61K47/36A61K47/38A61K47/42A61P3/04A61P3/06A61P3/10A61P9/10A61P9/12A61P43/00C07C237/30
CPCA61K9/0056A61K9/143A61K9/146A61K9/1635A61K9/1652A61K9/2009A61K9/2027A61K9/2054A61K31/225A61K31/454
Inventor 山根省吾山根博文角南正记
Owner JAPAN TOBACCO INC
Features
  • Generate Ideas
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com