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Orlistat oral preparation and preparation method thereof

An orlistat and tablet technology, applied in the field of pharmaceutical preparations, can solve the problems of unimproved dissolution rate of tablets, sticking and punching, etc.

Inactive Publication Date: 2013-07-31
QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the process of spraying the suspension on the surface of the granular excipients, it is impossible for all orlistat raw material surfaces to be covered by the polymer, and a part of orlistat must be attached to the outer surface of the particles. During the tableting process, it will also stick to the punch due to the heat of the punch
[0012] In addition, for the dissolution test of orlistat tablets prepared by the above technology, surfactants were added to the dissolution medium to improve the in vitro dissolution rate. However, there is no surfactant in the human gastrointestinal tract, and the tablets prepared by the above technology The dissolution rate of the

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] 1. Solid Dispersion Preparation

[0034] Orlistat 120g

[0035] Acrylic resin 60g

[0036] Absolute ethanol 600g

[0037] Dissolve the prescribed amount of orlistat and acrylic resin in absolute ethanol, and on the supercritical fluid equipment, pass the supercritical fluid CO2 to quickly depressurize through a nozzle with an aperture of 10 microns, and the decompression time is 10 -5 Second, a solid dispersion of orlistat acrylic resin was prepared by supercritical fluid rapid expansion method, and the D90 of the dispersion was less than 10 μm.

[0038] 2. Preparation of Orlistat Tablets

[0039]

[0040] Mix the solid dispersion with microcrystalline cellulose and crospovidone evenly, add an appropriate amount of pure water, granulate, dry, and pass the dry granules through a 20-mesh sieve, then mix evenly with the prescribed amount of magnesium stearate, and tablet it. have to.

Embodiment 2

[0042] 1. Solid Dispersion Preparation

[0043] Orlistat 120g

[0044]Acrylic resin 360g

[0045] Absolute ethanol 2000g

[0046] Dissolve the prescribed amount of orlistat and acrylic resin in absolute ethanol, and on the supercritical fluid equipment, pass the supercritical fluid CO2 to quickly depressurize through a nozzle with an aperture of 10 microns, and the decompression time is 10 -5 Second, a solid dispersion of orlistat acrylic resin was prepared by supercritical fluid rapid expansion method, and the D90 of the dispersion was less than 10 μm.

[0047] 2. Preparation of Orlistat Tablets

[0048]

[0049] Mix the solid dispersion with microcrystalline cellulose and crospovidone evenly, add an appropriate amount of pure water, granulate, dry, and pass the dry granules through a 20-mesh sieve, then mix evenly with the prescribed amount of magnesium stearate, and tablet it. have to.

Embodiment 3

[0051] 1. Solid Dispersion Preparation

[0052] Orlistat 120g

[0053] Acrylic resin 180g

[0054] Absolute ethanol 1000g

[0055] Dissolve the prescribed amount of orlistat and acrylic resin in absolute ethanol, and on the supercritical fluid equipment, pass the supercritical fluid CO2 to quickly depressurize through a nozzle with an aperture of 10 microns, and the decompression time is 10 -5 Second, a solid dispersion of orlistat acrylic resin was prepared by supercritical fluid rapid expansion method, and the D90 of the dispersion was less than 10 μm.

[0056] 2. Preparation of Orlistat Tablets

[0057]

[0058] Mix the solid dispersion with microcrystalline cellulose and crospovidone evenly, add an appropriate amount of pure water, granulate, dry, and pass the dry granules through a 20-mesh sieve, then mix evenly with the prescribed amount of magnesium stearate, and tablet it. have to.

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Abstract

The invention discloses an orlistat oral preparation and a preparation method thereof. The orlistat oral preparation is an orlistat tablet. The orlistat tablet comprises an orlistat acrylic resin solid dispersion, a disintegrating agent and pharmaceutically acceptable auxiliary materials. The orlistat acrylic resin solid dispersion is prepared by rapid expansion of supercritical solution and has D90 less than 10 microns. The raw materials of the orlistat oral preparation are micronized by a supercritical technology and an inert material layer is coated on the orlistat surface so that the problems of a low dissolution rate of the preparation obtained by the prior art, and sticking in tabletting are solved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an orlistat oral preparation and a preparation method thereof. Background technique [0002] Orlistat is a long-acting and potent specific gastrointestinal lipase inhibitor that inactivates the enzymes by forming a covalent bond with the active serine sites of gastric and pancreatic lipases in the lumen of the stomach and small intestine. Fat in food cannot be decomposed into free fatty acids, so fat cannot be absorbed and utilized, thereby reducing calorie intake and controlling body weight. The drug does not need to be absorbed systemically to exert its efficacy, and is rarely absorbed through the gastrointestinal tract, so its blood concentration is extremely low. There is no accumulation in the body with the therapeutic dose of this product. The metabolic site is in the wall of the gastrointestinal tract, and the elimination half-life is abou...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/14A61K31/365A61K47/32A61P3/04A61P3/06
Inventor 孙勇马宝华徐丽洒徐平袁海成
Owner QINGDAO UNIV
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