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A kind of omeprazole nanoemulsion and preparation method thereof

An omeprazole and nanoemulsion technology, which is applied in the field of omeprazole nanoemulsion and its preparation, can solve the problems of low bioavailability, poor water solubility, inconvenient storage and the like, and achieves simple preparation process, moderate price and easy operation. Effect

Active Publication Date: 2016-04-06
TIANJIN ZHONGSHENG TIAOZHAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Omeprazole sodium powder injection commonly used in veterinary clinics is not easy to store and must be used up in a short time after dilution; omeprazole tablets or microcapsules can only be administered orally, and cannot overcome the first-pass effect of the liver
Due to the poor water solubility of omeprazole (slightly soluble in water), it is difficult to be effectively transported to the lesion or into cells, its aqueous solution is unstable, and it decomposes quickly under acidic conditions, and its sodium salt is expensive, Poor stability, which in turn leads to low bioavailability, frequent medication times, affects animal welfare and production performance, and greatly limits its clinical application in veterinary medicine

Method used

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  • A kind of omeprazole nanoemulsion and preparation method thereof
  • A kind of omeprazole nanoemulsion and preparation method thereof
  • A kind of omeprazole nanoemulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] A kind of omeprazole nanoemulsion, is made up of following raw material:

[0043] Omeprazole API 5g

[0044] 160g soybean oil

[0045] Tween-80250g

[0046] 1,2 propylene glycol 110g

[0047] Water for injection 475g

[0048] Total 1000g

[0049] The preparation method of above-mentioned omeprazole nanoemulsion is as follows:

[0050] (1) At room temperature, weigh the omeprazole raw material according to the formula ratio and dissolve it in 1,2 propylene glycol, then add Tween-80 and soybean oil in the formula amount, mix well and set aside;

[0051] (2) Use the formulated amount of water for injection as the water phase. Slowly add water for injection into the system at room temperature while stirring continuously until a clear and transparent liquid is formed, that is, the particle size is 10-100 nanometers, and the appearance is clear and uniform. Omeprazole nanoemulsion.

Embodiment 2

[0053] A kind of omeprazole nanoemulsion, is made up of following raw material:

[0054] Omeprazole API 10g

[0055] Ethyl oleate 200g

[0056] Castor oil polyoxyethylene ether (EL-40) 170g

[0057] PEG-400185g

[0058] Water for injection 435g

[0059] Total 1000g

[0060] The preparation method of above-mentioned omeprazole nanoemulsion is as follows:

[0061] (1) At room temperature, weigh the omeprazole raw material according to the formula ratio and dissolve it in PEG-400 first, then add castor oil polyoxyethylene ether (EL-40) and ethyl oleate in the formula amount, mix uniform spare;

[0062] (2) Use the water for injection of the formula amount as the water phase, slowly add the above water for injection into the system at room temperature, and keep stirring until a clear and transparent liquid is formed, that is, the particle size is 10-100 nanometers, and the appearance is clear. Uniform omeprazole nanoemulsion.

Embodiment 3

[0064] A kind of omeprazole nanoemulsion, is made up of following raw material:

[0065] Omeprazole API 1g

[0066] Isopropyl myristate (IPM) 240g

[0067] Polyoxyethylene ether hydrogenated castor oil (RH-40) 280g

[0068] PEG-600135g

[0069] Water for injection 344g

[0070] Total 1000g

[0071] The preparation method of above-mentioned omeprazole nanoemulsion is as follows:

[0072] (1) At room temperature, weigh the omeprazole raw material according to the formula ratio, dissolve it in PEG-600 first, and add the formula amount of polyoxyethylene ether hydrogenated castor oil (RH-40) and isopropyl myristate (IPM), mix well and set aside;

[0073] (2) Use the formulated amount of water for injection as the water phase. Slowly add the above-mentioned water for injection into the system at room temperature while stirring continuously until a clear and transparent liquid is formed, that is, to obtain a particle size of 10-100 nanometers and a clear appearance. Uniform o...

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Abstract

The invention provides an omeprazole nano emulsion and a preparation method thereof. The emulsion is respectively prepared from the following components by weight percent: 0.1-1% of omeprazole, 16-30% of surfactant, 0.15-20% of cosurfactant, 2-25% of oil and 34-50% of water for injection. The omeprazole nano emulsion is good in thermodynamic stability, good in storage stability, and free of layering after being placed for a long period of time, and can be subjected to oral medication and intramuscular injection; a stable emulsion state can be completely recovered by placement and sufficient oscillation after heating to 80 DEG C; especially, the omeprazole can be well prevented from being destroyed by gastric acid after a nano emulsion matrix is orally taken, and the first-pass effect of the liver can be overcome. Therefore, the omeprazole nano emulsion is simple in preparation method, and applicable to the requirements of large-scale industrial production.

Description

technical field [0001] The invention relates to an omeprazole pharmaceutical preparation and a preparation method thereof, in particular to an omeprazole nanoemulsion and a preparation method thereof. Background technique [0002] Omeprazole (Omeprazole), the first proton pump inhibitor (PPI) developed by Astra Company in Sweden, can inhibit the secretion of gastric acid and is mainly used for the treatment of peptic ulcer and digestive system dysfunction diseases related to gastric acid. It has the advantages of high curative effect, short course of treatment, good tolerance and low recurrence rate. Its mechanism of action is: Omeprazole acts on the H of the parietal cells on the gastric mucosa. + K + —ATPase, while H + K + —ATPase is involved in the last link of gastric acid secretion, so omeprazole can inhibit gastric acid secretion caused by all stimulants. The U.S. FDA approved Merial Limited's omeprazole oral paste as early as 2003, and the trade name is GASTROGAR...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/4439A61P1/04
Inventor 焦晓军程雪娇王建焦伟丽季坤王勇余贵菊朱士江甄盼盼王猛姜淋洁李丽琴
Owner TIANJIN ZHONGSHENG TIAOZHAN BIOTECH
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