Cetilistat medicinal composition and preparation method thereof

A technology of new lisstat and its composition, which is applied in the field of drug combination and preparation of new lisstat tablets, can solve the problems such as easy adhesion of the main drug, achieve good dissolution effect, simple preparation process, and increase the effect of impurities

Active Publication Date: 2017-01-11
SHANDONG ACADEMY OF PHARMACEUTICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the report of patent EP1897558, the new lixistat tablet was prepared by fluidized bed granulation method. Due to the small particle size of the drug powder, the main drug is prone to adhesion during the granulation process

Method used

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  • Cetilistat medicinal composition and preparation method thereof
  • Cetilistat medicinal composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] 1) Prescription composition

[0023] prescription composition 500 tablets / g Neolistat 60 polyethylene glycol 6000 24 Mannitol 36 microcrystalline cellulose 7.5 Croscarmellose Sodium 11 Iron oxide yellow 0.2

[0024] Magnesium stearate 2.3

[0025] 2) Preparation method

[0026] Weigh 60g of Neolistat, 24g of polyethylene glycol 6000, mix them evenly, add them into the container, heat and melt at a constant temperature of 70°C, stir evenly, remove the heat, add 12g of mannitol, stir evenly, cool to room temperature, take out, and 30 mesh sieves to obtain the granules containing new lisstat; the new lisstat granules and the remaining mannitol, the microcrystalline cellulose of the prescription amount, croscarmellose sodium, iron oxide yellow, magnesium stearate together After mixing evenly, go directly to the machine to compress the tablet, that is to say.

Embodiment 2

[0028] 1) Prescription composition

[0029] prescription composition 500 tablets / g Neolistat 60 polyethylene glycol 6000 48 Mannitol 30 microcrystalline cellulose 7.5 Croscarmellose Sodium 11 Iron oxide yellow 0.2 Magnesium stearate 2.3

[0030] 2) Preparation method

[0031] Weigh 60g of Neolistat, 48g of polyethylene glycol 6000, mix them evenly, add them into the container, heat and melt at a constant temperature of 65°C, stir evenly, remove the heat, add 15g of mannitol, stir evenly, cool to room temperature, take out, and 30 mesh sieves to obtain the granules containing new lisstat; the new lisstat granules and the remaining mannitol, the microcrystalline cellulose of the prescription amount, croscarmellose sodium, iron oxide yellow, magnesium stearate together After mixing evenly, go directly to the machine to compress the tablet, that is to say.

Embodiment 3

[0033] 1) Prescription composition

[0034] prescription composition 500 tablets / g Neolistat 60 polyethylene glycol 6000 48 Mannitol 30 microcrystalline cellulose 7.5 Crospovidone 8 Iron oxide yellow 0.2 Magnesium stearate 2.3

[0035] 2) Preparation method

[0036] Weigh 60g of Neolistat, 48g of polyethylene glycol 6000, mix them evenly, add them into the container, heat and melt at a constant temperature of 65°C, stir evenly, remove the heat, add 15g of mannitol, stir evenly, cool to room temperature, take out, and 30 mesh sieves to obtain the new lisstat granules; after mixing the new lisstat granules with the remaining mannitol, the prescribed amount of microcrystalline cellulose, cross-linked povidone, yellow iron oxide, and magnesium stearate , directly on the machine to compress the tablet, that is to say.

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Abstract

The invention belongs to the field of medicine compositions for treating obesity and II-type diabetes, and definitely, relates to a medicine composition of cetilistat and a preparation method thereof. A cetilistat tablet prepared from the medicine composition through the preparation method has excellent dissolving-out effect. The preparation method is simple and is suitable for industrial production.

Description

Background technique [0001] New Lisistat, the English name Cetilistat, other Chinese aliases are Xitilista, Celista, and Xitilista, is a long-acting and potent specific gastrointestinal lipase inhibitor, it By interacting with the active serine site of gastric lipase and pancreatic lipase, forming a covalent bond to inactivate the enzyme, the inactivated enzyme cannot hydrolyze the fat in the food into absorbable free fatty acids and monoacylglycerol, so that the fat cannot Absorbed by the body to reduce calorie intake and control weight. The biggest advantage of the drug is that it does not act on the nervous system, does not affect other enzyme activities in the gastrointestinal tract, does not suppress appetite, and does not require dietary restrictions. 24 hours after taking the medicine, the phenomenon of defecation with oil will appear, that is, the undigested fat will be eliminated. [0002] The results of clinical research prove that Neolistat not only has good safet...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/38A61K31/536A61K9/30A61K47/10A61P3/04A61P3/10
Inventor 林振广孔祥雨颜东董世波刘宪华
Owner SHANDONG ACADEMY OF PHARMACEUTICAL SCIENCES
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