Claims for Patent: 11,090,386

Summary for Patent: 11,090,386

Title:	Method for suppressing bitterness of quinoline derivative
Abstract:	The present invention provides a method for suppressing bitterness of a quinoline derivative.
Inventor(s):	Kentaro Nagane, Yosuke Ueki, Shusuke Sano, Takahisa Sakaguchi
Assignee:	Eisai R&D Management Co Ltd
Application Number:	US16/038,710
Patent Claims:	1. A method for administering a suspension comprising the compound 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxyamide or a pharmaceutically acceptable salt thereof, and a basic substance, wherein the basic substance is present in an amount effective for suppressing bitterness of the compound or a pharmaceutically acceptable salt thereof the method comprising: 1) suspending a pharmaceutical composition comprising 1 to 24 mg of the 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxyamide or the pharmaceutically acceptable salt thereof, and the basic substance in an aqueous solvent in a vessel; 2) administering the suspension obtained in 1) to a patient from the vessel; 3) rinsing the vessel with an aqueous solvent; and 4) administering the rinsing solution obtained in 3) to the patient; wherein the suppressed bitterness of the suspension comprising 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxyamide or a pharmaceutically acceptable salt thereof and the basic substance is measured relative to a control having the composition of the suspension but without the basic substance; and wherein the weight ratio of the basic substance to 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxyamide or a pharmaceutically acceptable salt thereof is from 0.01:1 to 50:1. 2. The method according to claim 1, wherein 1) comprises: i) pouring the aqueous solvent in the vessel, ii) allowing the vessel to stand; and iii) shaking the vessel. 3. The method according to claim 1, wherein the pharmaceutical composition is suspended in 1 to 10 mL of the aqueous solvent in 1). 4. The method according to claim 3, wherein the pharmaceutical composition is suspended in about 3 mL of the aqueous solvent in 1). 5. The method according to claim 1, wherein the vessel is rinsed with 1 to 10 mL of the aqueous solvent in 3). 6. The method according to claim 5, wherein the vessel is rinsed with about 2 mL of the aqueous solvent in 3). 7. The method according to claim 1, wherein the basic substance is a basic oxide, a basic carbonate, a basic hydroxide, or a sodium salt of a polymer having a carboxyl group. 8. The method according to claim 7, wherein the basic substance is a basic carbonate. 9. The method according to claim 1, wherein the basic substance is calcium carbonate, magnesium carbonate, potassium carbonate, magnesium oxide, magnesium hydroxide, sodium carboxymethyl starch, or croscarmellose sodium. 10. The method according to claim 9, wherein the basic substance is calcium carbonate or magnesium oxide. 11. The method according to claim 9, wherein the basic substance is calcium carbonate.