Empagliflozin metformin sustained release preparation and preparation method thereof

Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to an empagliflozin metformin sustained release preparation and a preparation method thereof. An empagliflozin pellet core is a quick release part, a metformin hydrochloride pellet core is a sustained release part, the two pellet cores are coated with isolation layers respectively, and then the two drug-loaded pellets are mixed and filled into capsules. The invention further discloses the preparation method of the empagliflozin metformin sustained release preparation. The preparation method comprises the steps that (1), the metformin hydrochloride pellet core is prepared through an extrusion and spheronization process; (2), the empagliflozin quick release pellet core is prepared through the extrusion and spheronization process; (3), the two drug-loaded pellet cores are coated with the isolation layers respectively; and (4), the two drug-loaded pellets are filled into the capsules according to a certain proportion. The preparation process is good in stability, simple, high in production efficiency and suitable for industrial mass production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an empagliflozin metformin sustained-release preparation and a preparation method thereof. Background technique [0002] Empagliflozin, a sodium glucose cotransporter 2 (SGLT-2) inhibitor, is the main transporter that reabsorbs glucose from the glomerular filtrate into the blood circulation, by reducing renal glucose reabsorption , lower the renal glucose threshold, and promote the excretion of glucose from the urine. Empagliflozin is a white to pale yellow non-hygroscopic powder. Very slightly soluble in water, slightly soluble in methanol, ethanol and acetonitrile, soluble in 50% acetonitrile / water, almost insoluble in toluene. Its chemical name is (1S)-1,5-anhydro-1-(4-chloro-3-{4-[(3S)-tetrahydrofuran-3-oxyl]benzyl}phenyl]-D-glucitol, The structural formula is as follows: [0003] [0004] Metformin hydrochloride is used for patients with type II ...

AI Technical Summary

Problems solved by technology

The technological process is complex, and due to the need to use a double-layer tablet press for tablet compression, the requirements for the fluidity and compressibility of the granules are relatively high

Since the tablet core is a double-layer tablet, there will be cracks at the junction of the double-layer tablet during the coating process, which requires slow coating, and the setting requirements for the coating process and parameters are relatively high, resulting in an increase in the overall production cost

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