Sitagliptin phosphate tablet and preparation method thereof

Abstract

The invention discloses a sitagliptin phosphate tablet and a preparation method thereof, the tablet core of the tablet is composed of the following components by weight: 20-50% of sitagliptin phosphate, 50-80% of a diluent, 3-10% of a disintegrating agent and 1-10% of a lubricant, the particle size distribution of sitagliptin phosphate is 60 [mu] mlt; d901t; D901t; and 120 [mu] m. The preparation method comprises the following steps: (1) adding sitagliptin phosphate, a diluent and a disintegrating agent into a wet granulator for mixing, and then transferring the mixture into a mixer for mixing to obtain a premix; (2) adding a lubricant into the premix, and mixing in a mixer to obtain a total mixture; (3) tabletting the total mixture to obtain a tablet core; and (4) carrying out coating treatment on the tablet core to obtain the sitagliptin phosphate tablet. The preparation process is simple and low in cost, and the prepared sitagliptin phosphate tablet is high in hardness and good in dissolution, has good stability under the conditions of high temperature, high humidity and illumination, and meets actual production and storage requirements.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a sitagliptin phosphate tablet and a preparation method thereof. Background technique [0002] Type 2 diabetes mellitus (T2DM) is a disease that occurs when the body cannot effectively use insulin and the pancreas does not produce enough insulin to control blood sugar levels. Type 2 diabetes (type 2diabetesmellitus, T2DM) accounts for about 6% of the adult population in Western societies, and its pathogenesis is mainly due to three major defects: insulin resistance, decreased insulin secretion, and excessive glucose production in the liver. Type 2 diabetes has become a relatively prevalent disease. Lack of physical exercise in life and uncontrolled diet may increase the risk of diabetes. Over the years, China's population has shown an aging trend, and people's daily life is getting better and better. Nutrient intake is rich, the taste is sweet, and physical exercise is reduced....

AI Technical Summary

Problems solved by technology

[0003] Limitations of current treatments include a range of safety and tolerability issues, limited range and / or durability of effectiveness, and inconvenience associated with administration

Since sitagliptin phosphate is easily decomposed under alkaline environmental conditions, there is a risk of degradation during drug transportation or storage, and its degradation products pose a greater safety hazard

[0006] At present, sitagliptin phosphate preparations adopt wet granulation or dry granulation process, but these two preparation processes are complex and costly, and the solvent introduced in wet granulation will increase the risk of crystallization of active pharmaceutical ingredients, while dry granulation The pellets are prone to sticking to the roller, resulting in problems such as exceeding the standard of the magazine and prolonging the disintegration time

Both patents CN109157522A and CN110559270B adopt the powder direct compression process to prepare sitagliptin phosphate tablets. The direct compression process is simple, but because the sitagliptin phosphate raw material itself has poor fluidity and accounts for a large proportion in the prescription, it is also easy to compress the tablet. Cause sticking and punching, and uneven mixing can easily lead to stratification between different components

In order to solve the problem of poor fluidity and easy sticking of the active component in the preparation process of sitagliptin phosphate tablets, in patent CN202011431091.6, the active component, filler and disintegrant are mixed evenly before adding lubricant Mixing, wherein reducing the content of the active ingredient and using microcrystalline cellulose and calcium sulfate as fillers can improve the problem of poor fluidity and easy sticking of the active ingredient, but the dissolution rate of the prepared tablet is relatively small, and if To prepare tablets containing the same amount of active ingredients, it is necessary to increase the amount of excipients, which increases the cost of materials and affects the metabolism of excipients by the human body after medication

In addition, patent CN112843010A controls the particle size of the active ingredient in sitagliptin phosphate tablets (60μm<D90<300μm, preferably 120μm<D90<300μm, and regulates the particle size by controlling the recrystallization process), reducing the active pharmaceutical ingredient The contact area between materials with poor compatibility can improve the stability of the tablet, but the particle size of the active ingredient in the mixed powder is too large, and the active ingredient in the tablet prepared in different periods is quite different, which is not conducive to the stability of the drug. dissolution

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