Lurasidone hydrochloride tablets and preparation method thereof

Abstract

The invention belongs to the technical field of pharmaceutical preparations and particularly relates to lurasidone hydrochloride tablets and a preparation method thereof. The tablets take lurasidone hydrochloride as an active component and consist of the lurasidone hydrochloride, a filling agent, copovidone, cross-linked povidone and a lubricant. According to the lurasidone hydrochloride tablets and the preparation method thereof, based on physicochemical property characteristics of the lurasidone hydrochloride, the hydrogen bond association effect between the copovidone and the cross-linked povidone and the lurasidone hydrochloride is utilized, the recrystallization rate of the medicine is inhibited, the dissolution rate of the medicine is improved, and the bioavailability of the medicine is guaranteed. Simultaneously, the invention further discloses a preparation process of the lurasidone hydrochloride tablets. The preparation process is simple, has good reproducibility and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a lurasidone hydrochloride tablet and a preparation method thereof. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Lurasidone hydrochloride (Lurasidone HCI) belongs to the category of atypical antipsychotic drugs, and is a dual-action atypical antipsychotic drug developed by Japan's Sumitomo Pharmaceutical Company. It has both 5-HT2A receptors and dopamine D2 receptors High affinity. On October 28, 2010, the FDA approved the marketing application of lurasidone hydrochloride tablets in the United States for the first-line treatment of patients with schizop...

AI Technical Summary

Problems solved by technology

[0006] Patent CN 102048734 B discloses the prescription and preparation process of the commercially available Lurasidone Hydrochloride Tablets. The raw material is micronized to control the average particle size below 4 μm, and pregelatinized starch with a specific pregelatinization rate range is used. One-step granulation, but the in vitro dissolution rate of the drug fluctuates greatly due to the influence of the gelatinization rate of pregelatinized starch, which requires high quality excipients, which is not conducive to production control, and because the particle size of the raw material drug is very low, the crushing process is more demanding. High, low yield, high energy consumption, further increase the manufacturing cost

Patent CN 105395493 B discloses a lurasidone hydrochloride tablet and its preparation method. The solid dispersion technology is used to disperse lurasidone hydrochloride in the matrix material in an amorphous manner to increase the dissolution rate of lurasidone hydrochloride. Guarantee the bioavailability in vivo, but the drug in the tablet is dispersed in an amorphous form, and there is a problem of poor stability caused by crystallization. At the same time, it is difficult to achieve large-scale production by using a hot-melt extruder, which requires high energy consumption and requires equipment. higher

Patent CN 104248769 A discloses a pharmaceutical composition of lurasidone hydrochloride, which uses cyclodextrin inclusion technology to increase drug solubility, but the yield of cyclodextrin inclusion is not high, the preparation process is complicated, and the production cost is high, and There is also a tendency for the dissolution rate of lurasidone HCl to decrease during long-term storage

Patent CN104971046A discloses an immediate-release granule of lurasidone hydrochloride containing an insoluble drug, which contains lurasidone hydrochloride and poloxamer in a weight ratio of 1:0.25 to 1:1. Solubilization effect to improve the solubility of lurasidone hydrochloride, but, on the one hand, the addition of surfactant can not prevent the trend of dissolution rate decline in the long-term storage process, and at the same time, due to the addition of a large amount of surfactant poloxamer, it is easy to cause Reversal of the water-oil environment of the gastrointestinal mucosa, causing adverse reactions such as nausea and vomiting

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