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Orlistat oral emulsion and preparation method thereof

An orlistat and emulsion technology, applied in the field of medicine, can solve the problems of complex components, accelerated consumption, etc., and achieve the effects of high bioavailability, improved compliance, and simple preparation method

Active Publication Date: 2018-10-23
ZHONGSHAN WANHAN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the invention has many functions such as reducing the absorption of fat and calories in food, accelerating the consumption of stubborn brown adipose tissue accumulated in the body, supplementing the micronutrients lost in the weight loss process, and reducing blood lipid and cholesterol, its composition is complex and contains relatively high content of surfactant
[0006] There are few reports about orlistat oral emulsion at present, so it is necessary to develop a kind of bioavailability high, stable quality orlistat oral emulsion

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1, a kind of orlistat oral emulsion

[0035]

[0036] Preparation:

[0037] S1 Heat and dissolve orlistat in a hot water bath at 43°C, add Tween-80, heat and stir evenly, and control the temperature at 43°C to obtain an oil phase;

[0038] S2 Add purified water into a high-speed homogeneous mixer, add tragacanth gum, set the temperature at 45°C to heat and swell, stir evenly, add xylitol and potassium sorbate, heat, stir to dissolve, and control the temperature at 45°C to obtain an aqueous phase;

[0039] S3 Turn on the high-speed homogeneous mixer, add the oil phase obtained in step S1 to the aqueous phase obtained in step S2, stir while adding, complete the addition, homogenize, the homogenization speed is 3000r / min, and the homogenization time is 5min to obtain a homogeneous emulsion ;

[0040] S4 The jacket of the high-speed homogenizer passes cold water to cool down, and when the temperature of the homogeneous emulsion obtained in step S3 drops belo...

Embodiment 2

[0042] Embodiment 2, a kind of orlistat oral emulsion

[0043]

[0044]

[0045] Preparation:

[0046] S1 Heat and dissolve orlistat in a hot water bath at 43°C, add Tween-80, heat and stir evenly, and control the temperature at 42°C to obtain an oil phase;

[0047] S2 Add purified water into a high-speed homogeneous mixer, add tragacanth gum, set the temperature at 45°C to heat and swell, stir evenly, add xylitol and potassium sorbate, heat, stir to dissolve, and control the temperature at 44°C to obtain an aqueous phase;

[0048] S3 Turn on the high-speed homogeneous mixer, add the oil phase obtained in step S1 to the aqueous phase obtained in step S2, stir while adding, complete the addition, homogenize, the homogenization speed is 3000r / min, and the homogenization time is 5min to obtain a homogeneous emulsion ;

[0049] S4 The jacket of the high-speed homogenizer passes cold water to cool down, and when the temperature of the homogeneous emulsion obtained in step S...

Embodiment 3

[0051] Embodiment 3, a kind of orlistat oral emulsion

[0052]

[0053]

[0054] Preparation:

[0055]S1 Heat and dissolve orlistat in a hot water bath at 43°C, add Tween-80, heat and stir evenly, and control the temperature at 44°C to obtain an oil phase;

[0056] S2 Add purified water into a high-speed homogeneous mixer, add tragacanth gum, set the temperature at 45°C to heat and swell, stir evenly, add xylitol and potassium sorbate, heat, stir to dissolve, and control the temperature at 46°C to obtain an aqueous phase;

[0057] S3 Turn on the high-speed homogeneous mixer, add the oil phase obtained in step S1 to the aqueous phase obtained in step S2, stir while adding, complete the addition, homogenize, the homogenization speed is 3000r / min, and the homogenization time is 5min to obtain a homogeneous emulsion ;

[0058] S4 The jacket of the high-speed homogenizer passes cold water to cool down, and when the temperature of the homogeneous emulsion obtained in step S3...

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Abstract

The invention belongs to the technical field of medicine, and in particular, relates to an orlistat oral emulsion and a preparation method thereof. The orlistat oral emulsion provided by the inventionincludes the following components by the mass percentage: 2-2.6% of orlistat, 0.32-0.38% of an emulsifier, 6-9% of a flavoring agent, 0.7-1.2% of a suspending aid, 0.08-0.12% of potassium sorbate, 0.08-0.12% of an essence, and 86.58-90.82% of purified water. In the orlistat oral emulsion provided by the invention, orlistat is dispersed in water in a form of extremely fine emulsion particles and is released immediately after oral administration, and the orlistat oral emulsion has fast absorption and release by oral administration and high bioavailability. In addition, the quality of the orlistat oral emulsion provided by the invention meets the standard requirements, and the quality is stable.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an orlistat oral emulsion and a preparation method thereof. Background technique [0002] Orlistat (orlistat) is a lipase inhibitor weight-loss drug developed by Roche Pharmaceuticals. The trade name is Xenical. It was first launched in Europe and the United States in the late 1990s. FDA-approved switch to over-the-counter drug. Its chemical name is N-formyl-L-leucine(s)-1[(2s,3s)3-hexyl-4oxy-2-epoxypropylmethyl]dodecyl ester, also known as tetrahydro Tetrahydrolipstatin (Tetrahydrolipstatin, THL), is a semi-synthetic lipstatin derivative, its chemical structure is shown in the following formula: [0003] [0004] Orlistat is available in capsules and tablets of its Ⅱ crystal form. It is also the only chemical weight-loss drug at home and abroad that does not affect appetite and does not act on the central nervous system. It has superior safety characteristics. ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/365A61K47/36A61P3/04
CPCA61K9/0053A61K9/107A61K31/365A61K47/36A61P3/04
Inventor 郑明泽杜志博彭韪
Owner ZHONGSHAN WANHAN PHARM CO LTD
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