Prucalopride succinate tablet composition and preparation method thereof

Abstract

The invention relates to a prucalopride succinate tablet composition and a preparation method thereof, and provides a prucalopride succinate tablet composition which is non-toxic, good in stability, high in uniformity and biological availability, simple in technology and low in cost, and a preparation method of the prucalopride succinate tablet composition.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a tablet composition containing prucalopride succinate and a preparation method thereof. Background technique [0002] Chronic constipation has become a global problem that endangers public health. It is more common in women and the elderly. It not only seriously affects the quality of life of patients, but may also induce other serious diseases, such as anorectal disease, fecal ulcer and hepatic encephalopathy. and increase the risk of cardiovascular events. The treatment of chronic constipation usually uses laxatives, but laxatives are not effective in improving the symptoms of constipation. [0003] Prucalopride succinate is a dihydrobenzofuran drug with the chemical name 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl) -4-piperidinyl]-7-benzofurancarboxamide succinate, a selective, high-affinity serotonin (5-HT4) receptor agonist with prokinetic activity and ineffective in treati...

AI Technical Summary

Problems solved by technology

However, prucalopride succinate tablets are small-scale preparations, and the main ingredient accounts for 0.4-0.8% of the prescription volume. Such a small proportion has brought challenges to industrial production. Generally, powder mixing uniformity problems are prone to occur, which in turn leads to Dosage uniformity problems

[0005] In addition, in the prior art, the patent document CN103070865 discloses a tablet of prucalopride succinate, which contains 5% starch slurry, and uses a wet granulation process, because prucalopride succinate Li and lactose will generate toxic lactose adducts in the presence of water, and the adducts will increase with time. Therefore, the tablet composition disclosed in this patent document has toxic and side effects that threaten human health

[0006] Patent document CN104352465 micronizes prucalopride succinate, controls the particle size distribution of key excipients, controls the mixing method and time, and solves the tablet weight difference caused by material uniformity and particle fluidity through a special granulation process , but this method is complicated in equipment, cumbersome and lengthy, time-consuming and labor-intensive, and is not suitable for industrial production

[0007] Patent document CN104069080 uses mannitol instead of lactose to avoid the production of lactose adducts, and adopts wet granulation to obtain tablets with uniform content. Although the above method has improved toxicity and uniformity, the bioavailability is low and the application effect is low. Difference

[0008] Patent document CN107582535 discloses the tablet of prucalopride succinate, which is sieved by wet granulation or spray drying of ordinary lactose, and selects spherical lactose with an average particle size of 80-100 microns to control Its fluidity, and make the lactose particle size close to the raw material to prevent stratification during the mixing process, thereby improving the compressibility, and solve the problem of uniformity by mixing the raw material with a specific type of auxiliary material. The combination disclosed in this document The raw and auxiliary materials in the product need to be pre-treated to control their shape and size, which also has the problem of complex process and high consumption, and the bioavailability of the tablet is also low.

[0009] Patent document CN107595798 discloses the tablet of prucalopride succinate, but it adds laminin and trehalose and mixes it by wet mixer, which increases the cost and is also relatively toxic

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