5 results about "Trelagliptin" patented technology

The invention provides a preparation process of trelagliptin succinate tablets, which comprises the following steps: pretreating trelagliptin succinate and internally added materials in a high-shear wet-process mixing granulator, and then transferring into a fluidized bed to granulate according to optimized parameters. According to the process, various process feasibility problems caused by poor physical properties of raw material medicines are solved in a wet pretreatment mode, and quality risks caused by product crystal transformation are solved in a mannitol addition mode.

The present disclosure discloses a key amino acid-induced new crystal forms of trelagliptin based on protein-drug interaction structure mining and preparation method thereof; the technical solution is to introduce key amino acids into the solvent crystallization system of trelagliptin to induce five new crystal forms of trelagliptin; the preparation method does not require the use of a large amount of organic solvent, and has the characteristics of simplicity, precision and high efficiency, with a strong ability of crystal form regulation, and energy saving, environmental protection, safety, and easy to realize green industrial production.

The application provides a one-pot preparation method of a key intermediate of tigilazone, and belongs to the technical field of medicine manufacturing. 5-amino-3-methyl-1-phenylpyrazole is used as raw material, nitramination and halogenation are carried out, then condensation with Boc-piperazine is carried out, and then deprotection one-pot preparation is carried out. The application not only avoids the explosive system of NaH / DMF in the traditional process, but also avoids the use of reagents such as POCl3, the reaction is mild and environment-friendly, raw materials are easy to obtain, the yield is high, and the method is suitable for industrial production.

The invention discloses a key amino acid induced trelagliptin novel crystal form based on protein-drug interaction structure excavation and a preparation method thereof. According to the technical scheme, key amino acid is introduced into a solvent crystallization system of trelagliptin to induce trelagliptin to generate five new crystal forms; the preparation method does not need to use a large amount of organic solvent, has the characteristics of simplicity, accuracy, high efficiency and the like, has strong crystal form regulation and control capability, is energy-saving, environment-friendly and safe, and is easy to realize green industrial production.

The invention relates to the technical field of medicine component analysis, in particular to an analysis method for determining a thiazolidine impurity in tigliptin hydrobromide, which adopts gas chromatography for detection and comprises the following steps: a chromatographic column takes 5% diphenyl-1% vinylbenzene-94% dimethyl polysiloxane or substances with similar polarity as a stationary liquid; the initial temperature is 50-150 DEG C, the temperature is maintained for 5-15 minutes, then the temperature is increased to 300-360 DEG C at the speed of 10-30 DEG C per minute, and the temperature is maintained for 5-25 minutes; the temperature of a sample inlet is 280-340 DEG C; the temperature of the detector is 305-365 DEG C; the sample injection volume is 1-5 [mu] l; the flow velocity of the carrier gas is 2-5ml per minute; the split ratio is (15: 1)-(25: 1); the tetrahydrothiazole impurity has a basic toxicity warning structure, and the content of the tetrahydrothiazole impurity is directly related to the medication safety of the tigliptin hydrobromide, so that the content of the impurity in the tigliptin hydrobromide can be accurately determined, the level of the harmful impurity in the raw material medicine can be effectively monitored, the medication risk possibly caused by excessive impurity is avoided from a quality control link, and the safety of the quality control link is improved. The medication safety of patients is ensured.