Abstract: Pharmaceutical compositions comprising nitroxoline lysinate, a preparation method therefor and a use thereof. The pharmaceutical compositions comprise a first layer and a second layer. The first layer comprises, based on the total weight of the first layer, 40%-70% of active pharmaceutical ingredient, 10%-30% of filler, 5%-12% of disintegrant, 0.5%-2% of lubricant, 0.1%-1.5% of glidant and 10%-20% of alkaline substance. The second layer comprises, based on the total weight of the second layer, 40%-70% of active pharmaceutical ingredient, 10%-30% of filler, 10%-35% of sustained-release material, 0.1%-2% of lubricant and 0.1%-2% of glidant. The active pharmaceutical ingredient is selected from one or more of nitroxoline lysinate, nitroxoline lysinate crystalline form and nitroxoline lysinate solvate. The pharmaceutical compositions can achieve the purpose of burst release at an early stage and sustained and slow release at a later stage.

Abstract: A pharmaceutical composition containing a nitroxoline prodrug, and a preparation method and an application therefor. The pharmaceutical composition comprises the following ingredients in parts by weight: 100 parts of active pharmaceutical ingredient, 22.5-320 parts of filler, 0-40 parts of disintegrant, 0-95 parts of binding agent, and 2-30 parts of lubricant; relative to each 100 parts by weight of active pharmaceutical ingredient, the total content of the filler, the disintegrant, and the binding agent is 54-345 parts by weight; the active pharmaceutical ingredient is (S)-(5-nitroxoline-8-yloxy)methyl 1-isopropylpyrrolidine-2-carboxylate. The pharmaceutical composition has good stability, dissolution properties, and pharmacokinetic characteristics.

Abstract: Disclosed are a pharmaceutical composition containing nitroxoline, a nitroxoline tablet, a preparation method therefor, and a use thereof. The pharmaceutical composition comprises an active pharmaceutical ingredient and a pharmaceutically acceptable carrier, the active pharmaceutical ingredient being nitroxoline or a pharmaceutically acceptable salt thereof, and the active pharmaceutical ingredient having a particle size D90 of 10-100 ?m. The pharmaceutical composition containing nitroxoline can be made into a nitroxoline tablet having an appropriate dissolution rate.

Abstract: A pharmaceutical composition containing nitroxoline for the treatment of bladder cancer, a nitroxoline oral solid tablet, a preparation method therefor and use thereof. The pharmaceutical composition comprises nitroxoline, a filler, a disintegrating agent, a binder, and a lubricant. The lubricant is selected from one or two of sodium dodecyl sulfate and sodium stearyl fumarate. The pharmaceutical composition has a moderate dissolution rate, can avoid the burst release phenomenon, is moisture-proof and impermeable, has good stability, is secure and effective, is convenient to take, has strong patient compliance, and meets the requirements of being an oral solid tablet. The preparation method has stable production process, good reproducibility, easy mass production, and good clinical use value and social benefits.

Abstract: The present invention provides a solid pharmaceutical formulation of PARP inhibitors and its use thereof, and more specifically a solid dispersion powder including 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl)piperazine-1-carbonyl)benzyl)quinazoline-2,4(1H,3H)-dione and polymers, wherein the content of polymers is from about 50 wt % to about 80 wt %, and wherein less than 10 wt % of 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl)piperazine-1-carbonyl)benzyl)quinazoline-2,4(1H,3H)-dione is in crystalline form. The present invention also provides a method for preparing the solid dispersion powder, a pharmaceutical composition including the solid dispersion powder and the use of the pharmaceutical composition for treating diseases caused by PARP activity abnormalities.

Abstract: The present invention provides a solid pharmaceutical formulation of PARP inhibitors and its use thereof, and more specifically a solid dispersion powder including 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl)piperazine-1-carbonyl)benzyl)quinazoline-2,4(1H,3H)-dione and polymers, wherein the content of polymers is from about 50 wt % to about 80 wt %, and wherein less than 10 wt % of 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl)piperazine-1-carbonyl)benzyl)quinazoline-2,4(1H,3H)-dione is in crystalline form. The present invention also provides a method for preparing the solid dispersion powder, a pharmaceutical composition including the solid dispersion powder and the use of the pharmaceutical composition for treating diseases caused by PARP activity abnormalities.

Abstract: The present invention provides a solid pharmaceutical formulation of PARP inhibitors and its use thereof, and more specifically a solid dispersion powder including 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl)piperazine-1-carbonyl)benzyl)quinazoline-2,4(1H,3H)-dione and polymers, wherein the content of polymers is from about 50 wt % to about 80 wt %, and wherein less than 10 wt % of 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl)piperazine-1-carbonyl)benzyl)quinazoline-2,4(1H,3H)-dione is in crystalline form. The present invention also provides a method for preparing the solid dispersion powder, a pharmaceutical composition including the solid dispersion powder and the use of the pharmaceutical composition for treating diseases caused by PARP activity abnormalities.

Abstract: The present disclosure is directed to solid forms of the compound of formula (I): to compositions comprising these forms, and to processes for their preparation. The disclosure also relates to methods for the treatment of neurological disorders through the administration of these forms.