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Solid Preparation Having Improved Light Stability

Abstract: An object of the present invention is to provide a solid preparation comprising a 4,5-epoxymorphinan derivative or a pharmaceutically acceptable acid addition salt thereof, which is stable to light even without light shielding coating. The present invention provides the solid preparation comprising an active ingredient composed of a 4,5-epoxymorphinan derivative as represented below or a pharmaceutically acceptable acid addition salt thereof, and one or more stabilizing agents selected from the group consisting of rc-propyl gallate, sodium hydrogensulfite, dibutylhydroxytoluene, butylhydroxyanisole, tocopherol and D-isoascorbic acid, wherein the amount of the above active ingredient is 0.00001 to 0.01% by weight of the solid preparation, and the amount of the above stabilizing agent is 0.005 to 5% by weight of the solid preparation.

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Patent Information

Application #
Filing Date
28 December 2018
Publication Number
05/2019
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
patent@depenning.com
Parent Application

Applicants

TORAY INDUSTRIES, INC.
1-1, Nihonbashi-Muromachi 2-chome, Chuo-ku, Tokyo 1038666

Inventors

1. TAKAKI, Suguru
c/o Basic Research Center, Toray Industries, Inc., 10-1, Tebiro 6-chome, Kamakura-shi, Kanagawa 2488555
2. MINAKAMI, Satoshi
c/o Basic Research Center, Toray Industries, Inc., 10-1, Tebiro 6-chome, Kamakura-shi, Kanagawa 2488555
3. OHTA, Kotoe
c/o Basic Research Center, Toray Industries, Inc., 10-1, Tebiro 6-chome, Kamakura-shi, Kanagawa 2488555

Specification

WE CLAIM:
1. A solid preparation comprising an active ingredient composed of a
4,5-epoxymorphinan derivative represented by the general formula (I) below or a
pharmaceutically acceptable acid addition salt thereof, and one or more stabilizing
agents selected from the group consisting of /i-propyl gallate, sodium hydrogensulfite,
dibutylhydroxytoluene, butylhydroxyanisole, tocopherol and D-isoascorbic acid,
wherein the amount of the active ingredient is 0.00001 to 0.01% by weight of the solid preparation, and
wherein the amount of the stabilizing agent is 0.005 to 5% by weight of the solid preparation
[wherein R represents cyclopropylmethyl or allyl; R represents hydrogen, hydroxy, acetoxy, or methoxy; R represents hydrogen, hydroxy, acetoxy, or methoxy; A represents -N(R4 )C(=0)- or -N(R4 )C(=0)0-; R4 represents hydrogen or a C1.5 linear or branched alkyl; B represents a C1.3 linear alkylene, -CH=CH-, or -C=C-; R5 represents hydrogen, phenyl, furyl, or thienyl, provided that a hydrogen(s) in the phenyl, the furyl and the thienyl is/are optionally substituted with one or more groups selected from the group consisting of C1.5 alkyl, C1.5 alkoxy, C1.5 alkanoyloxy, hydroxy, fluorine, chlorine, bromine, iodine, amino, nitro, cyano, isothiocyanato, trifluoromethyl, trifluoromefhoxy and methylenedioxy].
2. The solid preparation according to claim 1, wherein the stabilizing agent is ^-propyl gallate.
3. The solid preparation according to claim 1 or 2, which contains sodium

thiosulfate.
4. The solid preparation according to any one of claims 1 to 3, which contains yellow ferric oxide, red feme oxide, or black iron oxide.
5. The solid preparation according to any one of claims 1 to 4, which contains a carbohydrate.
6. The solid preparation according to any one of claims 1 to 5, which is in a dosage form selected from the group consisting of tablet, granule, fine granule, hard capsule, dry syrup, powder, pill and troche.

Documents

Application Documents

# Name Date
1 201847049597.pdf 2018-12-28
2 201847049597-TRANSLATIOIN OF PRIOIRTY DOCUMENTS ETC. [28-12-2018(online)].pdf 2018-12-28
3 201847049597-STATEMENT OF UNDERTAKING (FORM 3) [28-12-2018(online)].pdf 2018-12-28
4 201847049597-PROOF OF RIGHT [28-12-2018(online)].pdf 2018-12-28
5 201847049597-PRIORITY DOCUMENTS [28-12-2018(online)].pdf 2018-12-28
6 201847049597-POWER OF AUTHORITY [28-12-2018(online)].pdf 2018-12-28
7 201847049597-FORM 1 [28-12-2018(online)].pdf 2018-12-28
8 201847049597-DECLARATION OF INVENTORSHIP (FORM 5) [28-12-2018(online)].pdf 2018-12-28
9 201847049597-COMPLETE SPECIFICATION [28-12-2018(online)].pdf 2018-12-28
10 201847049597-CLAIMS UNDER RULE 1 (PROVISIO) OF RULE 20 [28-12-2018(online)].pdf 2018-12-28
11 abstract 201847049597.jpg 2019-01-03
12 Correspondence by Agent_Form1_09-01-2019.pdf 2019-01-09
13 201847049597-FORM 3 [19-03-2019(online)].pdf 2019-03-19
14 201847049597-FORM 18 [11-06-2020(online)].pdf 2020-06-11
15 201847049597-OTHERS [27-04-2021(online)].pdf 2021-04-27
16 201847049597-FORM-26 [27-04-2021(online)].pdf 2021-04-27
17 201847049597-FORM 3 [27-04-2021(online)].pdf 2021-04-27
18 201847049597-FER_SER_REPLY [27-04-2021(online)].pdf 2021-04-27
19 201847049597-CLAIMS [27-04-2021(online)].pdf 2021-04-27
20 201847049597-Correspondence to notify the Controller [09-08-2021(online)].pdf 2021-08-09
21 201847049597-Written submissions and relevant documents [23-08-2021(online)].pdf 2021-08-23
22 201847049597-Retyped Pages under Rule 14(1) [23-08-2021(online)].pdf 2021-08-23
23 201847049597-2. Marked Copy under Rule 14(2) [23-08-2021(online)].pdf 2021-08-23
24 201847049597-RELEVANT DOCUMENTS [03-09-2021(online)].pdf 2021-09-03
25 201847049597-MARKED COPIES OF AMENDEMENTS [03-09-2021(online)].pdf 2021-09-03
26 201847049597-FORM 13 [03-09-2021(online)].pdf 2021-09-03
27 201847049597-AMMENDED DOCUMENTS [03-09-2021(online)].pdf 2021-09-03
28 201847049597-US(14)-HearingNotice-(HearingDate-09-08-2021).pdf 2021-10-17
29 201847049597-FER.pdf 2021-10-17

Search Strategy

1 searchstrategyE_14-12-2020.pdf