Emulsion injection containing dexibuprofen and preparation method of emulsion injection

A technology of Dexibuprofen and injectable milk, which is applied in the field of medicine and can solve the problems of poor water solubility of Dexibuprofen

Inactive Publication Date: 2015-04-29
BIOCHEM ENG COLLEGE OF BEIJING UNION UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, due to the extremely poor water solubility of Dexibuprofen, and according to the clinical needs of many patients who are not easy to take orally, the Dexibuprofen injection emulsion prepared by advanced preparation technology is what many doctors and patients are looking forward to

Method used

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  • Emulsion injection containing dexibuprofen and preparation method of emulsion injection
  • Emulsion injection containing dexibuprofen and preparation method of emulsion injection
  • Emulsion injection containing dexibuprofen and preparation method of emulsion injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] A Dexibuprofen injection emulsion is characterized in that 150g of Dexibuprofen, 500g of soybean oil, 50g of phospholipid, 10g of oleic acid, 10g of poloxamer and 100g of glycerol are included in the injection emulsion.

[0054] Its preparation method is:

[0055] (1) Take glycerin, add water for injection, dissolve it, make glycerin aqueous solution, keep it at 50-60°C, use it as the water phase, and set aside;

[0056] (2) Weigh phospholipids, poloxamers and soybean oil, mix them, stir and dissolve them at 50-70°C, and use them as the oil phase;

[0057] (3) Take oleic acid and dextrobuprofen and add to the oil phase, stir, mix well, and set aside;

[0058] (4) Add (3) to (1) and mix while cutting, and high-speed shearing to form uniform colostrum;

[0059](5) Dilute the obtained colostrum to 5000ml, and adjust the pH value to 4.0-9.0. After mixing evenly, pass through a homogenizer at 900bar for 6 times to obtain lipids with uniform particle size and an average par...

Embodiment 2

[0062] A Dexibuprofen injection emulsion is characterized in that 150g of Dexibuprofen, 1000g of soybean oil, 60g of phospholipid, 25g of oleic acid, 30g of poloxamer and 112.5g of glycerol are contained in the injection emulsion.

[0063] Its preparation method is:

[0064] (1) Take glycerin, add water for injection, dissolve it, make glycerin aqueous solution, keep it at 50-60°C, use it as the water phase, and set aside;

[0065] (2) Weigh phospholipids, poloxamers and soybean oil, mix them, stir and dissolve them at 50-70°C, and use them as the oil phase;

[0066] (3) Take oleic acid and dextrobuprofen and add to the oil phase, stir, mix well, and set aside;

[0067] (4) Add (1) to (3) and mix while shearing, and high-speed shearing to form uniform colostrum;

[0068] (5) Dilute the obtained colostrum to 5000ml, and adjust the pH value to 4.0-9.0. After mixing evenly, pass through a homogenizer at 900bar for 6 times to obtain lipids with uniform particle size and an avera...

Embodiment 3

[0071] A Dexibuprofen injection emulsion is characterized in that 250g of Dexibuprofen, 1000g of soybean oil, 60g of phospholipid, 25g of oleic acid, 30g of poloxamer and 112.5g of glycerol are included in the injection emulsion.

[0072] Its preparation method is:

[0073] (1) Take glycerin, add water for injection, dissolve it, make glycerin aqueous solution, keep it at 50-60°C, use it as the water phase, and set aside;

[0074] (2) Weigh phospholipids, poloxamers and soybean oil, mix them, stir and dissolve them at 50-70°C, and use them as the oil phase;

[0075] (3) Take oleic acid and dextrobuprofen and add to the oil phase, stir, mix well, and set aside;

[0076] (4) (1) and (3) are mixed, and the homogenizer is sheared at high speed to form uniform colostrum;

[0077] (5) Dilute the obtained colostrum to 5000ml, and adjust the pH value to 4.0-9.0. After mixing evenly, pass through a homogenizer at 900bar for 6 times to obtain lipids with uniform particle size and an a...

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Abstract

The invention belongs to the field of medical technology, and discloses emulsion injection taking dexibuprofen as a raw material and a preparation method of the emulsion injection. The emulsion injection is characterized in that each 1 L of the emulsion injection comprises the following components by mass: 30 to 100 g of dexibuprofen, 100 to 250 g of soybean oil, 9 to 24 g of phospholipid, 2 to 6 g of oleinic acid, 1 to 16 g of poloxamer, 20 to 25 g of glycerol, pH adjusting ingredients, and the balance of water for injection. The emulsion injection adopts the emulsification technology, and takes an oil-water surface as a film to carry medicine, so as to solve the problem that as dexibuprofen is difficult to dissolve in water, and improve the drug loading capacity; compared with other preparations, the emulsion injection is lower in adverse reaction and toxic side effects, higher in bioavailability, lower in preparation cost, and more convenient to use by patients.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an injection emulsion whose raw material is Dexibuprofen and a preparation method thereof. Background technique [0002] Mixed ibuprofen is composed of equal amounts of ibuprofen and ibuprofen. It has been used clinically as an anti-inflammatory and analgesic for 30 years and is considered to be the safest non-steroidal anti-inflammatory drug (NSAID) ), and is an over-the-counter drug. However, mixed ibuprofen still has a variety of side effects including gastrointestinal toxicity, water and sodium retention, decreased renal perfusion, and allergic reactions, with an incidence rate of 15% to 30%. For the development of safer NSAIDs, two drugs have been proposed: cyclooxygenase-2 (Cyclooxygenase-2, COX-2) inhibitors and pure steric counterparts of NSAIDs, especially Dexibuprofen. In 1996, Dexibuprofen began to be widely used in the treatment of rheumatoid arthritis ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/192A61P29/00
Inventor 权奇哲闫海军朴成熙李军业
Owner BIOCHEM ENG COLLEGE OF BEIJING UNION UNIV
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