Lurasidone hydrochloride tablets and preparation method thereof

A technology of lurasidone hydrochloride tablet and lurasidone hydrochloride, which is applied in the direction of pharmaceutical formulation, pill delivery, medical preparations of non-active ingredients, etc., can solve the problem that the dissolution rate cannot be prevented, the preparation process is complicated, and the manufacturing process is increased. Cost and other issues, to achieve the effect of improving bioavailability, simple preparation process, and avoiding strict control

Inactive Publication Date: 2021-10-08
北京丰科睿泰医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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 t

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  • Lurasidone hydrochloride tablets and preparation method thereof
  • Lurasidone hydrochloride tablets and preparation method thereof
  • Lurasidone hydrochloride tablets and preparation method thereof

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preparation example Construction

[0034] As discussed in the background technology, lurasidone hydrochloride has low solubility in the acidic environment of the stomach in the prior art, and there are many problems in the way of increasing drug dissolution in the prior art. In view of this, the present invention provides a lurasidone hydrochloride The lurasidone hydrochloride tablet has high solubility at the absorption site, high bioavailability and good stability and a preparation method thereof.

[0035] In a typical embodiment of the present invention, a lurasidone hydrochloride tablet is provided, comprising lurasidone hydrochloride, a filler, a disintegrant, a binder, and a lubricant; the binder is copovidone, Described disintegrating agent is polyvinylpolypyrrolidone; Each component is made up as follows by weight parts:

[0036] Lurasidone hydrochloride: 20-30 parts

[0037] Filling agent: 45~75 parts

[0038] Copovidone: 5-15 parts

[0039] Crospovidone: 1-15 parts

[0040] Lubricant: 0.5 to 2 par...

Embodiment 1

[0060] prescription:

[0061]

[0062]

[0063] Preparation Process:

[0064] (1) Lurasidone hydrochloride raw material medicine is pulverized with a jet mill to obtain lurasidone hydrochloride micropowder, particle size D 90 Control within the range of 15-35μm;

[0065] (2) Add lurasidone hydrochloride micropowder, filler, and crospovidone obtained in step (1) into a fluidized bed for granulation, and add a cohesive compound containing copovidone with a mass concentration of 3.0% dissolved in purified water. agent solution, the temperature of the material during granulation is controlled at 25-35°C, and after granulation is completed, dry until the loss on drying is less than 2.0%;

[0066] (3) After the granules obtained in step (2) are sized by a mobile granulator, a lubricant is added and mixed, and the resulting mixture is compressed in a rotary tablet press to obtain lurasidone hydrochloride tablets;

Embodiment 2

[0068] prescription:

[0069] composition Dosage (g / 1000 tablets) weight percentage (%) lurasidone hydrochloride 40 25.0 Mannitol 86.4 54.0 Copovidone 24 15.0 Crospovidone 8 5.0 Magnesium stearate 1.6 1.0 total 160 100

[0070] Preparation Process:

[0071] (1) Lurasidone hydrochloride raw material medicine is pulverized with a jet mill to obtain lurasidone hydrochloride micropowder, particle size D 90 Control within the range of 15-35μm;

[0072] (2) Add lurasidone hydrochloride micropowder, filler, and crospovidone obtained in step (1) into a fluidized bed for granulation, and add a cohesive compound containing copovidone with a mass concentration of 3.0% dissolved in purified water. agent solution, the temperature of the material during granulation is controlled at 25-35°C, and after granulation is completed, dry until the loss on drying is less than 2.0%;

[0073] (3) After the granules obtained in step (2) are...

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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...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/496A61K47/32A61P25/18
CPCA61K9/2095A61K9/2027A61K31/496A61P25/18
Inventor 兰颐安明榜李铁军陈晓佳王燕
Owner 北京丰科睿泰医药科技有限公司
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