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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 (52-1 Yada, Suruga-ku, Shizuoka-sh, Shizuoka 26, 〒4228526, JP)
NOGUCHI Shuji (52-1 Yada, Suruga-ku, Shizuoka-sh, Shizuoka 26, 〒4228526, JP)
IWAO Yasunori (52-1 Yada, Suruga-ku, Shizuoka-sh, Shizuoka 26, 〒4228526, JP)
HIRANO Masuharu (Discovery Research Laboratories, 1-22, Hikokawado, Misato-sh, Saitama 05, 〒3410005, JP)
OHTA Takashi (Discovery Research Laboratories, 1-22, Hikokawado, Misato-sh, Saitama 05, 〒3410005, JP)
YAMAKAWA Tomio (Discovery Research Laboratories, 1-22, Hikokawado, Misato-sh, Saitama 05, 〒3410005, JP)
Application Number:
JP2018/043788
Publication Date:
June 06, 2019
Filing Date:
November 28, 2018
Export Citation:
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Assignee:
SHIZUOKA PREFECTURAL UNIVERSITY CORPORATION (52-1, Yada Suruga-ku, Shizuoka-sh, Shizuoka 26, 〒4228526, JP)
NIPPON CHEMIPHAR CO., LTD. (2-3 Iwamotocho 2-chome, Chiyoda-ku Tokyo, 32, 〒1010032, JP)
International Classes:
A61K31/519; A61K9/16; A61K9/20; A61K9/48; A61K47/38; A61P19/06; A61P43/00; C07D513/04
Domestic Patent References:
WO2005121153A12005-12-22
WO2016136727A12016-09-01
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, ISSN: 2189-7026
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, ISSN: 0372-7629
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
Attorney, Agent or Firm:
TANAI Sumio et al. (1-9-2, Marunouchi Chiyoda-k, Tokyo 20, 〒1006620, JP)
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