11 results about "Sitagliptin Phosphate" patented technology

The invention provides a sitagliptin and metformin sustained-release pharmaceutical composition as well as a preparation method and application thereof, and relates to the technical field of sustained-release preparations. The pharmaceutical composition comprises a sustained-release tablet core and a quick-release coating layer, the sustained-release tablet core comprises an active ingredient metformin hydrochloride and a sustained-release framework material hydroxypropyl methylcellulose, and the sustained-release tablet core does not contain microcrystalline cellulose; the quick-release coating layer comprises an active component sitagliptin phosphate; the weight ratio of metformin hydrochloride to hydroxypropyl methylcellulose in the sustained release tablet core is 50: (24-27). The composition utilizes a double-layer structure to realize double-phase release of the medicine; the microcrystalline cellulose is removed, and the specific ratio of the active component to the framework material is limited, so that the moldability and ideal dissolution behavior of the preparation are ensured while the tablet weight is remarkably reduced to improve the swallowing compliance, and the technical problem that the slow-release framework function is difficult to maintain under the condition that the weight of a high-drug-loading-capacity compound preparation is greatly reduced is successfully solved.

The application provides a sitagliptin and metformin hydrochloride sustained-release pharmaceutical composition and a preparation method and application thereof, and relates to the technical field of sustained-release preparations. The pharmaceutical composition comprises a sustained-release tablet core and a quick-release coating layer; the sustained-release tablet core comprises active ingredients metformin hydrochloride and a sustained-release matrix material hydroxypropyl methyl cellulose, and the sustained-release tablet core does not contain microcrystalline cellulose; the quick-release coating layer comprises active ingredients sitagliptin phosphate; the weight ratio of metformin hydrochloride to hydroxypropyl methyl cellulose in the sustained-release tablet core is 50:(24-27). The composition realizes double-phase release of drugs by using a double-layer structure; by removing the microcrystalline cellulose and limiting the specific ratio of active ingredients to the matrix material, the forming property of the preparation and the ideal dissolution behavior are ensured while the tablet weight is significantly reduced to improve the swallowing compliance, and the technical problem that a high drug loading compound preparation is difficult to maintain the function of the sustained-release matrix under a large amount of weight reduction is successfully solved.

The utility model discloses a drying device for preparing sitagliptin phosphate, which belongs to the technical field of medicine production and comprises a base, a drying box is mounted on the base, a conveying belt is arranged in the drying box, a plurality of air holes are formed in the conveying belt, a plurality of rotating rollers are mounted in the conveying belt, and the rotating rollers are arranged on the drying box. The two ends of the rotating roller are connected with the interior of the drying box, and a rotating shaft is installed on the rotating roller at one end in the conveying belt. According to the drying device for sitagliptin phosphate preparation, the conveying belt is driven to rotate, meanwhile, the air bellow installed on the base works, air generated by the air bellow can move upwards through the air blowing opening, the air is heated through the electric heating wire to form hot air, and the hot air moves upwards to penetrate through air holes formed in the conveying belt so as to dry medicine on the conveying belt; and the conveyor belt rotates to move the dried medicines to the discharge port, and then the medicines slide down from the inclined plate, so that the subsequent collection work is facilitated, and the time and energy of workers are saved.

This invention provides a stable sitagliptin phosphate pharmaceutical composition comprising the following components: the active ingredient sitagliptin phosphate, a sulfite stabilizer, a filler, a disintegrant, and a lubricant. By adding a sulfite stabilizer to the sitagliptin phosphate pharmaceutical composition, this invention effectively controls the formation of nitrosamine impurities (NTTP) in the sitagliptin pharmaceutical composition, ensuring the quality stability of the sitagliptin phosphate pharmaceutical composition. The sitagliptin phosphate pharmaceutical composition of this invention has a dissolution effect comparable to a reference. The stable sitagliptin phosphate pharmaceutical composition of this invention is prepared using conventional preparation processes and is suitable for industrial production.

The invention belongs to the technical field of medicines, and relates to a preparation method and application of sitagliptin phosphate resin sustained-release microcapsules. The sitagliptin phosphate resin sustained-release microcapsule is prepared from sitagliptin phosphate, cation exchange resin, an impregnant and a capsule wall material, the sitagliptin phosphate resin sustained-release microcapsule is prepared by the following steps: statically or dynamically loading sitagliptin phosphate and cation exchange resin to obtain sitagliptin phosphate drug resin, impregnating the sitagliptin phosphate drug resin with an impregnant to obtain impregnated drug resin, and coating the impregnated drug resin with a capsule wall material to obtain the sitagliptin phosphate resin sustained-release microcapsule. The weight ratio of the sitagliptin phosphate to the cation exchange resin is (1: 4)-(9: 4); the cation exchange resin is sulfonic acid type strong acid cation exchange resin; the capsule wall material is poly (ammonium methacrylate) or ethyl cellulose; the impregnant is polyethylene glycol. The sitagliptin phosphate resin sustained-release microcapsule disclosed by the invention has a release rate of about 75% in 10h, has an obvious sustained-release effect, and can stabilize the blood concentration level.

This invention relates to a method for preparing sitagliptin phosphate to extend the lifespan of immobilized transaminases, belonging to the field of pharmaceutical synthesis technology. To address the problem of short lifespan of existing immobilized enzymes, this invention provides a method for preparing sitagliptin phosphate to extend the lifespan of immobilized transaminases. The method includes, in the presence of immobilized transaminases, carrying out an enzymatic reaction of sitagliptin precursor ketone and isopropylamine in a non-water-soluble organic solvent. The reaction is terminated after the raw material conversion rate is detected to be ≥75%, the immobilized transaminases are recovered, the filtrate is washed with water to remove acetone, and an aqueous phosphate solution is added to the filtrate for extraction. The aqueous phase is separated to obtain an aqueous sitagliptin phosphate solution, and the solvent is removed. The organic phase is washed with water and directly reused. This invention can significantly shorten the reaction time, reduce the contact time of the immobilized transaminases in a high-concentration acetone system, and avoid excessive soaking time, thereby extending the overall lifespan of the immobilized transaminases.

The utility model discloses material mixing equipment for preparing sitagliptin phosphate tablets, which comprises a reinforcing bottom plate, a fixing frame body fixedly connected onto the reinforcing bottom plate, a mixing box body fixedly connected onto the fixing frame body, a plurality of fifth reinforcing frames fixedly connected onto the mixing box body, and measurement storage cylinders fixedly connected onto the fifth reinforcing frames. A discharging pipe is fixedly connected to the measuring storage cylinder, a second electric valve is installed on the discharging pipe of the measuring storage cylinder, a weight sensor is installed on the measuring storage cylinder, and a buzzer is installed on the fifth reinforcing frame. The measurement value of the weight sensor is set in advance, then raw materials needing to be mixed are placed in the measurement storage barrel, the weight sensor can detect the raw materials in real time, when the weight of the raw materials reaches a preset threshold value of the weight sensor, the buzzer can be controlled to sound for a period of time, and therefore the use amount of different kinds of raw materials can be controlled, and the mixing efficiency is improved. And the phenomenon of mixing failure caused by a wrong dosage proportion is prevented.

The invention discloses a sitagliptin phosphate pharmaceutical composition as well as a preparation, a preparation method and application thereof. The pharmaceutical composition comprises sitagliptin phosphate, HP-beta-CD and mesoporous silica. According to the invention, a synergistic effect is generated by utilizing a molecular-level clathration effect of HP-beta-CD and a nano-level confinement adsorption effect of mesoporous silica, so that chemical degradation of sitagliptin phosphate, especially generation of a genotoxic impurity NTTP, is remarkably inhibited from molecular and physical double levels, and the stability of a product is greatly improved. Meanwhile, the mesoporous silica effectively solves the technical problems that HP-beta-CD is strong in hygroscopicity and not easy to directly tablet, and the content uniformity of low-dose drugs is fundamentally ensured by forming uniform composite particles. The process is simple, granulation is not needed, the tablet is suitable for industrial production, the prepared tablet is excellent in stability and high in safety, and animal experiments show that the bioavailability of the tablet is superior to that of a commercially available reference preparation.

The invention belongs to the field of pharmaceutical preparations, and particularly relates to sitagliptin phosphate tablets as well as a preparation method and application thereof. According to the specific technical scheme, the sitagliptin phosphate tablet comprises sitagliptin phosphate, a filling agent, a disintegrating agent and a lubricating agent, the filling agent comprises microcrystalline cellulose, and the moisture content of the microcrystalline cellulose is smaller than 5%. When the lubricant is selected, the use of the lubricant sodium stearyl fumarate commonly used in the industry is avoided, so that the generation of impurities is effectively reduced. Meanwhile, the moisture content of microcrystalline cellulose in the filling agent is controlled, and the generation of impurities in the sitagliptin phosphate tablet is further reduced. Finally, the sitagliptin phosphate tablet which is high in purity, low in impurity content and stable in character is provided.

This invention relates to the field of sitagliptin phosphate preparation technology, specifically disclosing a cyclic enzymatic catalytic synthesis process for sitagliptin phosphate. This process uses a diketone compound as a substrate and transaminase as a catalyst, innovatively combining an immobilized enzyme column to achieve a cyclic catalytic reaction. Engineered bacteria are cultured in a fermenter, and after cell disruption, impurity removal, and ultrafiltration concentration, a concentrated transaminase solution is prepared. This solution is then cross-linked with epoxy resin HFA001 to form an immobilized enzyme packing material, which is then packed into an enzyme column. Under optimized reaction conditions, the substrate solution and a catalytic solution containing pyridoxal phosphate are cyclically catalyzed through the enzyme column. The reaction solution is purified through acidification, extraction, washing, vacuum concentration, crystallization, and drying to obtain the sitagliptin product. This invention enables continuous production scale-up of more than 10 batches, with a catalytic yield of 80%-85% and a substrate conversion rate ≥95%, significantly reducing reaction costs and experimental risks, and improving production efficiency and product stability.

The present invention pertains to the technical field of pharmaceuticals and relates to a preparation method for a sitagliptin phosphate resin sustained-release microcapsule and use thereof. The sitagliptin phosphate resin sustained-release microcapsule comprises sitagliptin phosphate, a cation exchange resin, an impregnant, and a capsule material. The sitagliptin phosphate resin sustained-release microcapsule is obtained by performing static or dynamic drug loading of sitagliptin phosphate on the cation exchange resin to obtain a sitagliptin phosphate drug resin, then impregnating the resin with the impregnant to obtain an impregnated drug resin, and then coating the impregnated drug resin with the capsule material. The weight ratio of sitagliptin phosphate to the cation exchange resin is 1:4-9:4. The cation exchange resin is a sulfonic acid-type strongly acidic cation exchange resin. The capsule material is ammonium polymethacrylate or ethyl cellulose. The impregnant is polyethylene glycol. The sitagliptin phosphate resin sustained-release microcapsule of the present invention exhibits a release degree of about 75% at 10 h, indicating a significant sustained-release effect. The microcapsule can stabilize the plasma concentration level.