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Orlistat tablets and preparation method thereof

A technology of orlistat and tablets, which is applied in the field of medicine, can solve the problems of sticky punching, hot punching, etc., and achieve the effects of simple preparation process, improved inhibition, and avoiding unfavorable factors

Active Publication Date: 2010-08-04
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] 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

Method used

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  • Orlistat tablets and preparation method thereof
  • Orlistat tablets and preparation method thereof
  • Orlistat tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1 orlistat tablet

[0046] 1. Orlistat tablet prescription

[0047] 1.1 Inclusion compound formula

[0048] Orlistat 12.4g (0.025mol)

[0049] α-cyclodextrin 24.325g (0.025mol)

[0050] 50% ethanol solution 1500ml

[0051] 1.2 Tablet formulation

[0052] 10 parts of clathrate

[0053] Microcrystalline cellulose 87 parts

[0054] Sodium carboxymethyl starch 2 parts

[0055] 1 part magnesium stearate

[0056] 2. Preparation process

[0057] (1) Dissolve the prescribed amount of α-cyclodextrin in the prescribed amount of 50% ethanol, add the prescribed amount of orlistat, and then heat the mixture. When the orlistat becomes oily, continue heating to 40°C , and then use an ultrasonic homogenizer with a frequency of 20kHz, 60W, and heat preservation and ultrasonication for 46min to prepare a uniformly mixed solution.

[0058] (2) Turn on the freeze dryer to pre-freeze the product, reduce the temperature of the product to about -40°C at 2°C / min, and keep ...

Embodiment 2

[0060] Embodiment 2 orlistat tablet

[0061] 1. Orlistat tablet prescription

[0062] 1.1 Inclusion compound formula

[0063] Orlistat 12.4g (0.025mol)

[0064] γ-cyclodextrin 32.425g (0.025mol)

[0065] water 400ml

[0066] 1.2 Tablet formulation

[0067] 20 parts of clathrate

[0068] Microcrystalline cellulose 55 parts

[0069] Hydroxypropyl cellulose 20 parts

[0070] 3 parts of 2% povidone ethanol solution

[0071] 2 parts magnesium stearate

[0072] 2. Preparation process

[0073] (1) Dissolve the prescribed amount of γ-cyclodextrin in the prescribed amount of water, add the prescribed amount of orlistat, and then heat the mixture. When the orlistat becomes oily, continue heating to 60°C, and then use Stir with an electric mixer for 30 minutes;

[0074] (2) Turn on the freeze dryer to pre-freeze the product, reduce the temperature of the product to about -40°C at 2°C / min, and keep it warm for about 4 hours. After the product is completely frozen, turn on the c...

Embodiment 3

[0076] Embodiment 3 orlistat tablet

[0077] 1. Orlistat tablet prescription

[0078] 1.1 Inclusion compound formula

[0079] Orlistat 12.4g (0.025mol)

[0080] β-cyclodextrin 28.375g (0.025mol)

[0081] water 500ml

[0082] 1.2 Tablet formulation

[0083] 10 parts of clathrate

[0084] Lactose 75 parts

[0085] 10 parts of hydroxypropyl cellulose

[0086] Anhydrous ethanol amount

[0087] Magnesium stearate 5 parts

[0088] 2. Preparation process

[0089] (1) Dissolve the prescribed amount of β-cyclodextrin in the prescribed amount of water, add the prescribed amount of orlistat, and then heat the mixture. When the orlistat becomes oily, continue heating to 50°C, and then use Stir with an electric mixer for 30 min.

[0090] (2) Dry the mixed solution obtained in step (1) by spray drying, wherein the spray drying parameters are: inlet temperature 55°C, outlet temperature 50°C, spray speed 6ml / min, spray pressure 2.5bar. Finally, the dried orlistat cyclodextrin incl...

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PUM

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Abstract

The invention belongs to the technical field of the medicament and in particular relates to tablets comprising orlistat and a preparation method thereof. Orlistat and cyclodextrin which are subjected to enclosing and auxiliary materials acceptable for pharmacy are pressed into the tablets. The tablets solve the sticking problem of carrying out pressing on the orlistat by the conventional process, obviously improve the chemical and physical stability of the orlistat, cover the unpleasant taste of the orlistat, improve the administration compliance of the dysphagia patients, have good dissolution and improve the curative effect of the orlistat.

Description

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

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/365A61K47/48A61P3/04A61K47/61
Inventor 赵志全郝贵周肖月华
Owner LUNAN PHARMA GROUP CORPORATION
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