Orally dispersible tablet
AssigneeTakeda Pharmaceutical Company Limited
InventorsYutaka Tanoue, Tetsuya Matsuura, Yutaka Yamagata, Nacki Nagahara
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Abstract
The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.
Claims79
1-4. (canceled)
A preparation for oral-mucosal absorption, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide in an amount of 0.05-1.0 mg, wherein the AUC ratio of (i) a metabolite of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide to (ii) (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide after administration to a human is not more than about 20, and wherein the metabolite consists of (2S)-2-Hydroxy-N-{2-[(8S)-1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl]ethyl}propanamide.
A preparation for oral-mucosal absorption, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide in an amount of 0.1-0.8 mg, wherein the AUC ratio of (i) a metabolite of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide to (ii) (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide after administration to a human is not more than about 20, and wherein the metabolite consists of (2S)-2-Hydroxy-N-{2-[(8S)-1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl]ethyl}propanamide.
A preparation for oral-mucosal absorption, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide, wherein the AUC ratio of (i) (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide to (ii) a metabolite of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide after administration to a human is not less than about 5-fold than that by oral administration, and wherein the metabolite consists of (2S)-2-Hydroxy-N-{2-[(8S)-1,6,7,8-tetrahydro-2H-indeno [5,4-b]furan-8-yl]ethyl}propanamide.
A preparation for oral-mucosal absorption, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide, wherein the AUC ratio of (i) a metabolite of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide to (ii) (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno [5,4-b]furan-8-yl)ethyl]propionamide after administration to a human is not more than about 20, and wherein the metabolite consists of (2S)-2-Hydroxy-N-{2-[(8S)-1,6,7,8-tetrahydro-2H-indeno [5,4-b]furan-8-yl]ethyl}propanamide.
A preparation for oral-mucosal absorption, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide, wherein the bioavailability of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide is improved not less than about 10-fold than that by oral administration.
A preparation for oral-mucosal absorption, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide, wherein the average Tmax value of the plasma level of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide after administration to a human is not more than about 0.4 hours.
A preparation for oral-mucosal absorption, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide, wherein the coefficient of variation of pharmacokinetic parameters of (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide after administration to a human subject is not more than about 45%, wherein the pharmacokinetic parameters consist of Cmax and AUC.
A preparation for oral-mucosal absorption, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide in amount of 0.05-1.0 mg.
Dependencies are inferred from the claim text.