초록 ▼

The invention relates to a multiparticulate modified release composition that in operation delivers an active ingredient in a pulsed or bimodal manner. The multiparticulate modified release composition comprises an immediate release component and a modified release component; the immediate release c

The invention relates to a multiparticulate modified release composition that in operation delivers an active ingredient in a pulsed or bimodal manner. The multiparticulate modified release composition comprises an immediate release component and a modified release component; the immediate release component comprising a first population of active ingredient containing particles and the modified release component comprising a second population of active ingredient containing particles coated with a controlled release coating; wherein the combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or a bimodal manner. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition. The plasma profile achieved by the multiparticulate modified release composition is advantageous in reducing patient tolerance to the active ingredient and in increasing patient compliance by reducing dosage frequency.

대표청구항 ▼

The invention relates to a multiparticulate modified release composition that in operation delivers an active ingredient in a pulsed or bimodal manner. The multiparticulate modified release composition comprises an immediate release component and a modified release component; the immediate release c

The invention relates to a multiparticulate modified release composition that in operation delivers an active ingredient in a pulsed or bimodal manner. The multiparticulate modified release composition comprises an immediate release component and a modified release component; the immediate release component comprising a first population of active ingredient containing particles and the modified release component comprising a second population of active ingredient containing particles coated with a controlled release coating; wherein the combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or a bimodal manner. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition. The plasma profile achieved by the multiparticulate modified release composition is advantageous in reducing patient tolerance to the active ingredient and in increasing patient compliance by reducing dosage frequency. in the fatty acid or the fatty acid salt or the mixture of a fatty acid and a fatty acid salt is a C5to C24dicarboxylic acid or salt thereof.13. The composition according to claim 4, wherein the fatty acid or the fatty acid salt or the mixture of a fatty acid and a fatty acid salt is selected from the group consisting of glutaric acid, adipic acid, pimelic acid, suberic acid, azelaic acid, sebacic acid, dodecanedioc acid, and tetradecandioic acid, and salts thereof.14. The composition according to claim 1, wherein the fatty acid or the fatty acid salt is a mixture of two or more fatty acids or two or more fatty acid salts.15. The composition according to claim 1, wherein the fatty acid salt is a ammonium, bis(2-hydroxyethyl)ammonium, diethanolammonium, triethanolammonium, sodium, potassium, magnesium or calcium salt.16. The composition according to claim 15, wherein the fatty acid salt is a sodium or potassium salt.17. The composition according to claim 1, wherein 0.05 mg to 20 mg fatty acid or 0.05 mg to 20 mg fatty acid salt or 0.05 mg to 20 mg of a mixture of a fatty acid and fatty acid salt is used per 1 mg pharmaceutically active compound.18. The composition according to claim 17, wherein 0.5 mg to 2 mg fatty acid or 0.5 mg to 2 mg fatty acid salt or 0.5 to 2 mg of a mixture of a fatty acid and fatty acid salt is used per 1 mg pharmaceutically active compound.19. The composition according to claim 2, wherein the orlistat is present in an amount of 10 to 240 mg.20. The composition according to claim 19, wherein the orlistat is present in an amount of 30 to 120 mg.21. The composition according to claim 20, wherein the orlistat is present in an amount of 40, 60, 80, 100, or 120 mg.22. The composition according to claim 20, wherein the orlistat is present in an amount of 60 to 120 mg and the fatty acid or fatty acid salt or a mixture of a fatty acid and a fatty acid salt is present in the amount of 20 mg to 100 mg.23. The composition according to claim 22, wherein the orlistat is present in an amount of 120 mg orlistat and the fatty acid or fatty acid salt or a mixture of a fatty acid and a fatty acid salt is present in the amount of 60 mg.24. The composition according to claim 1 further comprising one or more pharmaceutically acceptable excipients.25. The composition according to claim 24, wherein the one or more pharmaceutically acceptable excipients are selected from the group consisting of mannitol, lactose, HPMC, talcum, sorbitol, polyvinylpyrrolidone, lecithin, trimyristine, polyethylenglycol, sucrose ester, polysorbate, polyoxethylenstearate, and dimethicon.26. The composition according to claim 25, wherein the one or more pharmaceutically acceptable excipients are selected from the group consisting of sucrose ester and lactose.27. The composition according to claim 26, wherein the composition comprises 10-240 mg of orlistat, 0.5-2000 mg of a fatty acid or a fatty acid salt or a mixture of a fatty acid and a fatty acid salt, 5-200 mg of sucrosepalmitate.28. The composition according to claim 27 further comprising 1.5 g lactose.