Title:
SOLID DISPERSION
Document Type and Number:
WIPO Patent Application WO/2019/107412
Kind Code:
A1
Abstract:
The present invention pertains to a solid dispersion containing a compound represented by general formula (I) (wherein R1 represents an unsubstituted phenyl group or a phenyl group substituted with a substituent; the substituent represents an alkyl group comprising 1–8 carbon atoms, an alkyl group comprising 1–8 carbon atoms substituted with a halogen atom, an alkoxy group comprising 1–8 carbon atoms, an alkoxy carbonyl group comprising 2–8 carbon atoms, a formyl group, a carboxyl group, a halogen atom, a phenyl group, or a phenoxy group; R2 represents a cyano group or a nitro group; R3 represents a hydroxy group; X represents an oxygen atom or -S(O)n-; n represents an integer in a range of 0–2; and Y represents an oxygen atom or a sulfur atom), or a pharmaceutically acceptable salt thereof, and a hypromellose derivative.
Inventors:
ITAI SHIGERU (JP)
NOGUCHI SHUJI (JP)
IWAO YASUNORI (JP)
HIRANO MASUHARU (JP)
OHTA TAKASHI (JP)
YAMAKAWA TOMIO (JP)
NOGUCHI SHUJI (JP)
IWAO YASUNORI (JP)
HIRANO MASUHARU (JP)
OHTA TAKASHI (JP)
YAMAKAWA TOMIO (JP)
Application Number:
PCT/JP2018/043788
Publication Date:
June 06, 2019
Filing Date:
November 28, 2018
Export Citation:
Assignee:
SHIZUOKA PREFECTURAL UNIV CORPORATION (JP)
NIPPON CHEMIPHAR CO (JP)
NIPPON CHEMIPHAR CO (JP)
International Classes:
A61K31/519; A61K9/16; A61K9/20; A61K9/48; A61K47/38; A61P19/06; A61P43/00; C07D513/04
Domestic Patent References:
| WO2005121153A1 | 2005-12-22 | |||
| WO2016136727A1 | 2016-09-01 | |||
| WO2005121153A1 | 2005-12-22 |
Foreign References:
| JP2017227807A | 2017-12-28 | |||
| JP3938938B2 | 2007-06-27 | |||
| JPS5944514B2 | 1984-10-30 |
Other References:
UEDA, HIROSHI: "Importance of solid physical property evaluation in formulation development of amorphous drug", FARUMASHIA, vol. 52, no. 5, 2016, pages 392 - 396, XP009520816, ISSN: 2189-7026, DOI: 10.14894/faruawpsj.52.5_392
TANNO, FUMIE: "Evaluation of Characteristics of Hypromellose Acetate Succinate (HPMCAS) as a Carrier for Solid Dispersion: from Study to Improve In Vitro Dissolution of Poorly Water Soluble Drugs", THE ARCHIVES OF PRACTICAL PHARMACY, vol. 73, no. 4, 2013, pages 214 - 222, XP009520813, ISSN: 0372-7629, DOI: 10.14843/jpstj.73.214
CURATOLO, W. ET AL.: "Utility of hydroxypropylmethylcellulose acetate succinate (HPMCAS) for initiation and maintenance of drug supersaturation in the GI milieu", PHARM. RES., vol. 26, no. 6, 2009, pages 1419 - 1431, XP019686188
FRIESEN, D. T. ET AL.: "Hydroxypropyl methylcellulose acetate succinate-based spray- dried dispersions: an overview", MOL. PHARM., vol. 5, no. 6, 2008, pages 1003 - 1019, XP055056966
SUN, D. D. ET AL.: "Probing the mechanisms of drug release from amorphous solid dispersions in medium-soluble and medium-insoluble carriers", J. CONTROL. RELEASE, vol. 211, 2015, pages 85 - 93, XP029205133
"Evaluation of the physical properties of poorly water-soluble drugs and new development of formulation designs", 2010, CMC PUBLISHING, pages: 141 - 150
See also references of EP 3718548A4
TANNO, FUMIE: "Evaluation of Characteristics of Hypromellose Acetate Succinate (HPMCAS) as a Carrier for Solid Dispersion: from Study to Improve In Vitro Dissolution of Poorly Water Soluble Drugs", THE ARCHIVES OF PRACTICAL PHARMACY, vol. 73, no. 4, 2013, pages 214 - 222, XP009520813, ISSN: 0372-7629, DOI: 10.14843/jpstj.73.214
CURATOLO, W. ET AL.: "Utility of hydroxypropylmethylcellulose acetate succinate (HPMCAS) for initiation and maintenance of drug supersaturation in the GI milieu", PHARM. RES., vol. 26, no. 6, 2009, pages 1419 - 1431, XP019686188
FRIESEN, D. T. ET AL.: "Hydroxypropyl methylcellulose acetate succinate-based spray- dried dispersions: an overview", MOL. PHARM., vol. 5, no. 6, 2008, pages 1003 - 1019, XP055056966
SUN, D. D. ET AL.: "Probing the mechanisms of drug release from amorphous solid dispersions in medium-soluble and medium-insoluble carriers", J. CONTROL. RELEASE, vol. 211, 2015, pages 85 - 93, XP029205133
"Evaluation of the physical properties of poorly water-soluble drugs and new development of formulation designs", 2010, CMC PUBLISHING, pages: 141 - 150
See also references of EP 3718548A4
Attorney, Agent or Firm:
TANAI Sumio et al. (JP)
Download PDF: