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Orlistat tablet and preparation method thereof

A technology of orlistat and tablets, which is applied in the field of pharmaceutical preparations, can solve the problems of orlistat tablets such as poor stability, poor fluidity, and easy sticking and punching, and achieve the effects of good stability, simple preparation process, and convenient operation

Inactive Publication Date: 2013-04-03
QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] In view of the deficiencies in the prior art, the inventors have gone through a lot of experiments and unexpectedly found that the problem of poor stability of orlistat tablets can be solved by preparing the orlistat phospholipid silicon dioxide composition, and it can also improve the stability of orlistat tablets. The in vitro dissolution rate can also overcome the problems of poor fluidity and easy sticking during the preparation of pharmaceutical preparations

Method used

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  • Orlistat tablet and preparation method thereof
  • Orlistat tablet and preparation method thereof
  • Orlistat tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] 1.1 Orlistat phospholipid composition preparation

[0029]

[0030] 1.2 Preparation of Orlistat Tablets

[0031]

[0032] Preparation Process

[0033] (1) Dissolve orlistat and lecithin in ethanol, add silicon dioxide, evaporate the ethanol to dryness under reduced pressure at 30°C, take out the evaporated composition, and pass through a 80-mesh sieve to obtain orlistat phospholipid lipid Body and fully combined with silica, good fluidity;

[0034] (2) Mix the above mixture with microcrystalline cellulose, crospovidone and magnesium stearate evenly, and directly compress into tablets to obtain.

Embodiment 2

[0036] 1.1 Orlistat phospholipid composition preparation

[0037]

[0038] 1.2 Preparation of Orlistat Tablets

[0039]

[0040] Preparation Process

[0041] (1) Dissolve orlistat and lecithin in ethanol, add silicon dioxide, evaporate the ethanol to dryness under reduced pressure at 30°C, take out the evaporated composition, and pass through a 80-mesh sieve to obtain orlistat phospholipid lipid Body and fully combined with silica, good fluidity;

[0042] (2) Mix the above mixture with microcrystalline cellulose, crospovidone and magnesium stearate evenly, and directly compress into tablets to obtain.

Embodiment 3

[0044] 1.1 Orlistat phospholipid composition preparation

[0045]

[0046] 1.2 Preparation of Orlistat Tablets

[0047]

[0048] Preparation Process

[0049] (1) Dissolve orlistat and lecithin in ethanol, add silicon dioxide, evaporate the ethanol to dryness under reduced pressure at 30°C, take out the evaporated composition, and pass through a 80-mesh sieve to obtain orlistat phospholipid lipid Body and fully combined with silica, good fluidity;

[0050] (2) Mix the above mixture with microcrystalline cellulose, crospovidone and magnesium stearate evenly, and directly compress into tablets to obtain.

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Abstract

The invention discloses an orlistat-containing tablet and a preparation method thereof. The orlistat-containing tablet is prepared by directly tabletting a silicon dioxide-containing orlistat phospholipid composition and pharmaceutic adjuvants, wherein the weight ratio of orlistat to phospholipid to silicon dioxide which are contained in the silicon dioxide-containing orlistat phospholipid composition is 1:(0.5-1.5): (0.5-3). The orlistat-containing tablet disclosed by the invention solves the problems of tabletting sticking and poor storage stability of the conventional process of the orlistat and enhances the in-vivo dissolvability of the orlistat.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an orlistat tablet and a preparation method thereof. Background technique [0002] Orlistat is a lipase inhibitor, white to off-white crystalline powder, chemical name: N-formyl-L-leucine (s)-1[(2s,3s)3-hexyl -4 oxy-2-epoxypropylmethyl] dodecyl ester, also known as tetrahydrolipstatin (THL), the structural formula is as follows: [0003] [0004] Orlistat is a fat-soluble substance with low solubility in water at physiological pH. In addition, because orlistat has a low melting point, about 44°C, it will be degraded by hydrolysis or heat, especially when stored in humid air or humid air above 65°C, it is resistant to various in vitro and in vitro The activity of lipases such as lipoprotein lipase, pancreatic triglyceride lipase and fatty acid synthase prevents triglycerides from the diet from being hydrolyzed into easily absorbed free fatty ac...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/365A61K47/24A61K47/04A61P3/06
Inventor 孙勇徐丽洒徐平刘巧囡沈若武
Owner QINGDAO UNIV
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