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Orlistat oral solid preparation and preparation method thereof

A technology for orlistat and solid preparation, which is applied in the field of medicine and achieves the effects of convenient operation, simple preparation process and rapid dissolution

Active Publication Date: 2014-01-15
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This can not only solve the physical problems such as sticking and punching in the production process of the preparation, but also greatly improve the in vitro dissolution rate of the preparation.

Method used

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  • Orlistat oral solid preparation and preparation method thereof
  • Orlistat oral solid preparation and preparation method thereof
  • Orlistat oral solid preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029]

[0030]

[0031] Preparation Process:

[0032] Heat and melt the prescribed amount of copovidone, add orlistat and stir evenly, and extrude the granules with an extruder; mix the granules with the prescribed amount of microcrystalline cellulose, sodium carboxymethyl starch, and magnesium stearate, and press Slices, ready to serve.

Embodiment 2

[0034] Orlistat 1 part

[0035] Copovidone 10 parts

[0036] Lactose 10 parts

[0037] Preparation Process:

[0038] Heating and melting the prescribed amount of copovidone, adding orlistat and stirring evenly, extruding the granules with an extruder; mixing the granules with the prescribed amount of lactose evenly to obtain granules.

Embodiment 3

[0040]

[0041] Preparation Process:

[0042] Heat and melt the prescribed amount of copovidone, add orlistat and stir evenly, extrude the granules with an extruder; mix the granules with the prescribed amount of lactose and magnesium stearate evenly, and fill them into the capsule shell to obtain the product.

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PUM

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Abstract

The invention discloses an orlistat oral solid preparation. The orlistat oral solid preparation is prepared by the steps of melting a low-melting point polymer and orlistat, then extruding out particles by an extruder, and mixing the particles and other accessories. By adopting the preparation disclosed by the invention, adverse factors in a preparation process caused by extremely low melting point of the orlistat are avoided, and the preparation can be made into various pharmaceutically common dosage forms. Moreover, the tablet preparation prepared by the invention is fast in dissolution and has great advantages over the prior art.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an orlistat oral solid preparation and a preparation method thereof. Background technique [0002] Orlistat is a lipase inhibitor, which has activity against various lipases such as lipoprotein lipase, pancreatic triglyceride lipase and fatty acid synthase both in vivo and in vitro, making triglyceride from diet Esters cannot be hydrolyzed into free fatty acids that are easily absorbed, so that they are not absorbed and excreted out of the body to achieve the purpose of weight loss. [0003] The chemical name of orlistat is: N-formyl-L-leucine(s)-1[(2s,3s)3-hexyl-4oxy-2-epoxypropylmethyl]dodecyl ester , also known as tetrahydrolipstatin (THL), is a semi-synthetic lipstatin derivative with the following structural formula: [0004] [0005] Orlistat is a fat-soluble substance. The specification for weight-loss drugs reaches more than 120mg. Its solubility in wate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K47/32A61K47/30A61P3/04
Inventor 郝贵周张元超
Owner SHANDONG NEWTIME PHARMA
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