Abstract: The present invention discloses a process for improving the fluidity of palbociclib isethionate and a composition, and belongs to the field of pharmaceutical preparations. The process includes a step of conducting granulation on palbociclib isethionate and pharmaceutically acceptable auxiliary materials to obtain granules with a tap density of 0.55-0.72 g/mL and an angle of repose of less than or equal to 44°. According to the process of the present invention, the palbociclib isethionate composition has good granular fluidity during filling of capsules, and prepared palbociclib isethionate capsules have uniform content, good stability and controllable quality. A preparation method is convenient to operate and easy to understand and adjust, and has good controllability in expanded production.

Abstract: The present invention discloses a composition of palbociclib isethionate and a medicament, and belongs to the technical field of pharmaceutical preparations. The composition includes palbociclib isethionate, a diluent, a disintegrant and a lubricant, as well as optionally a glidant. The palbociclib isethionate in the composition has a release rate of greater than or equal to 60% at a pH of 6.8 at 60 min. According to technical solutions of the present invention, influence of the pH environment in the human body on the release of a palbociclib isethionate medicament is reduced, the restriction that a medicament needs to be taken after a meal is overcome, and the medicament prepared from the composition of palbociclib isethionate can be taken before or after a meal without the restriction of achieving different effects when the medicament is taken before or after a meal.

Abstract: Described herein is N-[4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(R)-[(1-oxo-2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide, including crystalline forms, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the compound, as well as methods of using the compound, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract: The present invention relates to a preparation method for a microneedle patch. Specifically, the present invention provides a preparation method for a microneedle patch, and the method comprises steps: (1) milling a base into a master mold of the microneedle patch; (2) conducting surface treatment on the master mold, to obtain the treated master mold; (3) conducting reverse molding on a surface of the treated master mold, conducting deaeration, curing, and demolding, to obtain the cured daughter mold; and (4) casting the modification solution on the surface of the daughter mold, and then conducting deaeration, drying and curing, to obtain the microneedle patch. The method for preparing the microneedle patch in the present invention can greatly reduce the milling difficulty, and save the milling cost and time. The microneedle molds with different aspect ratios, areas and shapes can also be prepared as required, following with reverse molding to diverse microneedle patches.