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Oil-in-water nano-emulsion capable of obviously improving bioavailability of insoluble medicament and preparation method for oil-in-water nano-emulsion

A technology of insoluble drugs and oil-in-water type, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as increasing the bioavailability of insoluble drugs

Active Publication Date: 2016-10-26
CHONGQING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, only the literature of our research team has reported that the simultaneous use of two techniques can increase the bioavailability of poorly soluble drugs: Literature (Luo Jianchun, et al. Curcumin hydroxypropyl-β-cyclodextrin phospholipid complex in rats In Vivo Pharmacokinetics Research. Chinese Materia Medica. 2015, 38(3):572-5) Simultaneous use of cyclodextrin inclusion complex technology and phospholipid complex technology can improve the bioavailability of poorly soluble drugs, although cyclodextrin inclusion complex technology Fine inclusion complex technology or phospholipid complex technology or nanoemulsion technology can increase the bioavailability of poorly soluble drugs, but there is no preparation of cyclodextrin inclusion complex, phospholipid complex and nanoemulsion technologies at the same time. Any report of an oil-in-water nanoemulsion of a poorly soluble drug-phospholipid complex

Method used

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  • Oil-in-water nano-emulsion capable of obviously improving bioavailability of insoluble medicament and preparation method for oil-in-water nano-emulsion
  • Oil-in-water nano-emulsion capable of obviously improving bioavailability of insoluble medicament and preparation method for oil-in-water nano-emulsion
  • Oil-in-water nano-emulsion capable of obviously improving bioavailability of insoluble medicament and preparation method for oil-in-water nano-emulsion

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The weight ratio of each component contained in the insoluble drug cyclodextrin phospholipid complex formula is: 0.7 parts of evodiamine, 23.1 parts of soybean lecithin, 47.6 parts of α-cyclodextrin, and the oil-in-water nanoemulsion formula contains The weight ratio of each component is: 8.3 parts of evodiamine cyclodextrin phospholipid complex, 18.9 parts of ethyl oleate, 21.9 parts of polyoxyethylene (40) hydrogenated castor oil, 15.5 parts of ethanol, and 26.4 parts of distilled water.

[0029] The preparation method comprises the following steps: (1) Preparation of insoluble drug cyclodextrin phospholipid complex: take prescription amount of evodiamine, soybean lecithin, α-cyclodextrin, place in a round bottom flask, add ethanol, Magnetic stirring in a water bath at 40°C for 2 hours, and then rotary evaporation to remove the organic solvent to obtain the evodiamine cyclodextrin phospholipid complex; (2) Preparation of oil-in-water nanoemulsion: take the ethyl oleate...

Embodiment 2

[0031] The weight ratio of each component contained in the insoluble drug cyclodextrin phospholipid complex formula is: 1.5 parts of curcumin and evodiamine (0.5 part of curcumin and 1 part of evodiamine), 27.7 parts of brain lecithin, β-cyclodextrin 30.4 parts of essence, the weight ratio of each component contained in the oil-in-water nanoemulsion formula is: compound curcumin / Evodia rutaecarpa reduced cyclodextrin phospholipid complex 10.2 parts, glyceryl monostearate 16.9 parts, monostearic acid 31.9 parts of propylene glycol, 17.2 parts of polyethylene glycol 400, and 28.5 parts of distilled water.

[0032] The preparation method includes the following steps: (1) Preparation of insoluble drug cyclodextrin phospholipid complex: take curcumin, evodiamine, brain lecithin, and β-cyclodextrin in the prescribed amount, place them in a round bottom flask, add In dichloromethane, stir magnetically in a water bath at 50°C for 3 hours and then remove the organic solvent by rotary e...

Embodiment 3

[0034] The weight ratio of each component contained in the insoluble drug cyclodextrin phospholipid complex formula is: cyclovir buxin D 1.2 parts, glycerophospholipid 3.4 parts, hydroxypropyl-α-cyclodextrin 6.4 parts, oil-in-water The weight ratio of each component contained in the type nanoemulsion formula is: 8.9 parts of Cyclovir buxus D cyclodextrin phospholipid complex, 11.9 parts of glyceryl monocaprylate, 25.7 parts of polyoxyethylene (40) hydrogenated castor oil, glycerin 25.7 parts of alcohol, 35.6 parts of distilled water.

[0035] The preparation method comprises the following steps: (1) Preparation of insoluble drug cyclodextrin phospholipid complex: take prescription amount of cyclovirbuxine D, glycerol lecithin, hydroxypropyl-alpha-cyclodextrin, and place in round bottom Add ethanol to the flask, stir magnetically in a water bath at 45°C for 4 hours, and then remove the organic solvent by rotary evaporation to obtain cyclovirbuxusin D cyclodextrin phospholipid c...

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Abstract

The invention belongs to the field of medicinal preparation, and relates to oil-in-water nano-emulsion capable of obviously improving the bioavailability of an insoluble medicament and a preparation method for the oil-in-water nano-emulsion. According to the prepared oil-in-water nano-emulsion, the water solubility of the medicament can be achieved, absorption of the medicament can be promoted, and the bioavailability of the medicament can be improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an oil-in-water nanoemulsion for increasing the bioavailability of insoluble drugs and a preparation method thereof. Background technique [0002] Drugs are used clinically in a certain dosage form, and appropriate preparations are selected according to the needs of patients. Therefore, preclinical research on pharmaceutical preparations is of great significance to the clinical application of drugs. Most drugs have remarkable therapeutic effects, but due to their strong fat solubility and poor water solubility, their oral absorption is poor and their bioavailability is low, which limits the clinical application of drugs to a certain extent, such as evodiamine, curcumin, cyclovirbuxine D, Carmustine and others. Therefore, it is necessary to prepare the drug into a certain pharmaceutical preparation, improve the water solubility of the drug, promote the oral absorption of ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/48A61K47/24A61K45/00A61K31/57A61K31/12A61K31/519A61K31/4375A61K31/4409A61K31/496A61K31/4965A61K31/58A61K31/4525A61K31/352A61K31/05A61K31/357
CPCA61K9/1075A61K31/05A61K31/12A61K31/352A61K31/357A61K31/4375A61K31/4409A61K31/4525A61K31/496A61K31/4965A61K31/519A61K31/57A61K31/58A61K45/00A61K47/24
Inventor 张景勍雷婷婷赵华蒋心惠陈静张雪
Owner CHONGQING MEDICAL UNIVERSITY
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