Claims for Patent: 11,433,076

Summary for Patent: 11,433,076

Title:	Preparation containing tetracyclic compound at high dose
Abstract:	An improved solubility of a pharmaceutical composition or formulation containing a large amount of 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-yl-piperidin-1-yl)-11-oxo-6,11-dihy- dro-5H-benzo[b]carbazole-3-carbonitrile or a salt thereof can be achieved by forming granules of the compound or salt thereof and allowing the granules to be present together with a disintegrating agent.
Inventor(s):	Tomimatsu; Takashi (Tokyo, JP), Okazaki; Kensuke (Tokyo, JP), Ogawa; Yumi (Tokyo, JP), Yamamura; Takahiro (Tokyo, JP)
Assignee:	Chugai Seiyaku Kabushiki Kaisha (Tokyo, JP)
Application Number:	16/508,760
Patent Claims:	1. A pharmaceutical formulation comprising granules containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof: ##STR00004## wherein the granules have a mean particle diameter of 150 .mu.m or more and wherein the granules have a bulk density of 0.5 g/ml or more and a tapping density of 0.6 g/ml or more. 2. The formulation of claim 1, wherein the bulk density is 0.6 g/ml or more and the tapping density is 0.7 g/ml or more. 3. The formulation of claim 1, wherein the upper limit of the bulk density and the tapping density are 1.0 g/ml. 4. The formulation of claim 1, wherein the granules have a mean particle diameter of 200 .mu.m or more. 5. The formulation of claim 1, wherein the upper limit of the mean particle diameter of the granules is 1 mm. 6. The formulation of claim 1, wherein the granules further comprise a disintegrating agent. 7. The formulation of claim 6, wherein the disintegrating agent (ii) is contained in the granules in an amount of 5 wt % or more. 8. The formulation of claim 6, wherein the disintegrating agent (ii) is contained in the granules in an amount of 7.5 wt % or more. 9. The formulation of claim 6, wherein the disintegrating agent is selected from the group consisting of sodium starch glycolate, low-substituted hydroxypropylcellulose, carmellose calcium, sodium hydrogen carbonate, pregelatinized starch, sodium chloride, corn starch, croscarmellose sodium, crystalline cellulose, silicic anhydride and carmellose. 10. The formulation of claim 1, wherein the granules further comprise a solubilizing agent. 11. The formulation of claim 10, wherein the solubilizing agent is sodium lauryl sulfate. 12. The formulation of claim 1, wherein the granules further comprise a binder. 13. The formulation of claim 12, wherein the binder is hydroxypropylcellulose. 14. The formulation of claim 1, wherein the compound is 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-yl-piperidin-1-yl)-11-oxo-6,11-dihy- dro-5H-benzo[b]carbazole-3-carbonitrile hydrochloride. 15. The formulation of claim 1, wherein an amount of the compound in free form per unit formulation is 60 mg to 240 mg. 16. The formulation of claim 15, wherein the amount of the compound in free form per unit formulation is 140 mg to 190 mg.