Cetilistat tablets and preparation method thereof

A kind of Lisi, a certain amount of technology, applied in the direction of pharmaceutical formula, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2016-04-20
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The object of the present invention is to provide a kind of cetiristat tablet and its preparation method that can effectively solve the dissolution problem of the main drug without affecting the stability of the main drug

Method used

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  • Cetilistat tablets and preparation method thereof
  • Cetilistat tablets and preparation method thereof
  • Cetilistat tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: the preparation of west for Li Sita tablet

[0023] Prescription composition:

[0024] name

weight ratio / %

cetiristat

10

PEG4000

5

2 --> PEG6000

5

Mannitol

35

Microcrystalline Cellulose PH101

34

Hypromellose

5

Low-substituted hydroxypropyl cellulose

5

Magnesium stearate

1

[0025] Preparation Process:

[0026] (1) Dissolve cetiristat in an appropriate amount of absolute ethanol, put PEG4000 and PEG6000 in a 50°C water bath to completely melt, add cetiristat ethanol solution and stir for 1 hour, and remove ethanol by rotary evaporation or drying under reduced pressure , transferred to -20°C for solidification for 12 hours, taken out and placed in a vacuum desiccator to balance for 24 hours, ground into fine powder, and passed through an 80-mesh sieve to obtain a solid dispersion of cetiristat;

[0027] (2) Weigh a certain amount of cetiristat solid d...

Embodiment 2

[0028] Embodiment 2: the preparation of west for Li Sita tablet

[0029] Prescription composition:

[0030]

[0031]

[0032] Preparation Process:

[0033] (1) Dissolve cetilistat in an appropriate amount of absolute ethanol, put PEG5000 and PVPK30 in a 50°C water bath to completely melt, add cetilistat ethanol solution and stir for 2 hours, then remove ethanol by rotary evaporation or drying under reduced pressure , transferred to -20°C for solidification for 12 hours, taken out and placed in a vacuum desiccator to balance for 24 hours, ground into fine powder, and passed through an 80-mesh sieve to obtain a solid dispersion of cetiristat;

[0034] (2) Weigh a certain amount of cetiristat solid dispersion and lactose, microcrystalline cellulose PH101, high-substituted hydroxypropyl cellulose and low-substituted hydroxypropyl cellulose, and adopt 20% ethanol aqueous solution to granulate, 24 mesh Granulate, dry at 50°C to 1-3%, granulate with 24 mesh, add stearic acid ...

Embodiment 3

[0035] Embodiment 3: the preparation of west for Li Sita tablet

[0036] Prescription composition:

[0037] name

weight ratio / %

cetiristat

10

PEG4500

12

PVP K90

8

Sorbitol

30

Microcrystalline Cellulose PH101

29

3 --> Hypromellose

5

Crospovidone

5

Magnesium stearate

1

[0038] Preparation Process:

[0039] (1) Dissolve cetilistat in an appropriate amount of absolute ethanol, put PEG4500 and PVPK90 in a 50°C water bath to completely melt, add cetilistat ethanol solution and stir for 1.5h, then remove by rotary evaporation or drying under reduced pressure Ethanol, transferred to -20°C for solidification for 12 hours, taken out and placed in a vacuum desiccator to balance for 24 hours, ground finely, and passed through a 80-mesh sieve to obtain a solid dispersion of cetiristat;

[0040] (2) Take a certain amount of cetiristat solid dispersion and sorbitol, microcrystalline ...

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PUM

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Abstract

The invention belongs to the field of medicinal preparations and relates to cetilistat tablets, in particular to cetilistat tablets capable of effectively increasing the active ingredient dissolution rate and a preparation method thereof. The preparation method includes the steps that an active ingredient and a polymer support are prepared into solid dispersion, and the cetilistat tablets are obtained through wet or dry granulation, wherein the solid dispersion can be blended with accessory materials including a filling agent, a binding agent, a disintegrating agent and a lubricating agent. The cetilistat tablets are high in active ingredient dissolution rate, good in technological reproducibility and suitable for industrial production and provide a research basis for other cetilistat preparations.

Description

technical field [0001] The invention relates to a pharmaceutical composition for treating obesity, in particular to a tablet containing cetiristat. The cetiristat tablet can effectively improve the dissolution of a main drug and belongs to the field of pharmaceutical preparations. Background technique [0002] With the development of social economy and the improvement of people's living standards, the number of obese people is increasing day by day. According to the statistical analysis data of the Organization for Economic Co-operation and Development (OECD), in 2008, the number of obese adults in the world's seven major pharmaceutical markets was about 125 million. According to statistics, my country's current obese population is nearly 83 million. In the past ten years, the detection rate of childhood obesity has increased by an average of about 9% per year, which means that the number of obese children in my country will double in ten years. Obesity has become a major...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/30A61K31/536A61K47/10A61K47/32A61P3/04
CPCA61K9/2054A61K9/282A61K31/536
Inventor 冯思欣马莉
Owner BEIJING VENTUREPHARM BIOTECH
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