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W/o/w emulsion composition

A composition and emulsion technology, which is applied in the direction of drug combination, active ingredient of heterocyclic compounds, emulsion delivery, etc., can solve problems such as difficult injection of W/O/W emulsion, difficult emulsification of W/O droplets, increase in viscosity of injection, etc.

Inactive Publication Date: 2009-09-30
OTSUKA PHARM FAB INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In this method, water-soluble polymers are added to the internal aqueous phase to form complexes with ionic drugs; however, W / O / W emulsions containing water-soluble polymers are difficult to use as injections
This is because water-soluble polymers cause an increase in the viscosity of injections, making it difficult to emulsify W / O droplets, and because of the nature of polymer compounds, water-soluble polymers remain in the carrier without leakage, and there is a possibility of long-term remain in the body over time

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-13

[0073] Preparation of W / O / W Emulsion Composition

[0074] Using epirubicin hydrochloride as a drug ingredient and each compound shown in Table 1 as described below as a complex forming ingredient, a compound containing 0.1w / v% epirubicin hydrochloride dissolved in water for injection, 1w / v% Aqueous solution of complex forming component, 4.75w / v% glucose and 0.014M citric acid for internal aqueous phase.

[0075] Polyglyceryl-condensed-ricinoleate (PGCR) (i.e., lipophilic surfactant) was dissolved in ethyl ester of iodinated poppy seed oil fatty acid (trade name: Lipiodol (Guerbet)) ( That is, in the oily component), 5.5 mL of an oily phase having a PGCR concentration of 10 w / v% was prepared. Then, 1 mL of the above-mentioned aqueous solution for the inner aqueous phase was added thereto, and stirred at 25000 rpm for 10 minutes with a Polytron homogenizer (manufactured by Kinematica) under nitrogen flow and heating at 50°C. Thus, an emulsion was prepared.

[0076]Simultane...

Embodiment 14-20

[0086] Preparation of W / O / W Emulsion Composition

[0087] Using doxorubicin hydrochloride as a drug ingredient and each compound as shown in Table 2 below as a complex-forming ingredient, W / O / W emulsion compositions were prepared by the production methods used in Examples 1-13.

[0088] Determination of Water Phase Leakage Ratio

[0089] The aqueous phase leakage ratio (%) was determined by the method used in Examples 1-13.

[0090] Table 2

[0091] Pharmaceutical ingredients: Adriamycin hydrochloride

[0092]

[0093]

Embodiment 21

[0095] Preparation of W / O / W Emulsion Composition

[0096] W / O / W emulsion compositions were prepared by the production methods used in Examples 1-13 using bupivacaine hydrochloride as a drug ingredient and each compound as shown in Table 3 below as a complex-forming ingredient.

[0097] Determination of Water Phase Leakage Ratio

[0098] The aqueous phase leakage ratio (%) was determined by the method used in Examples 1-13. Drug concentrations were calculated from absorbance.

[0099] table 3

[0100] Drug ingredient: bupivacaine hydrochloride

[0101]

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Abstract

The present invention provides a W / O / W multiple emulsion composition composed of an internal aqueous phase, an oil phase, and an external aqueous phase, the internal aqueous phase containing an ionic physiologically active substance and a physiologically acceptable compound having a molecular weight of 1,000 or less and generating a polyvalent counterion with two or more valencies for the ionic physiologically active substance. The W / O / W emulsion composition of the present invention not only can stably encapsulate a useful substance in its internal aqueous phase at a high encapsulation ratio, but also has high safety.

Description

technical field [0001] The present invention relates to W / O / W emulsion compositions. Background technique [0002] W / O / W emulsions, which are liquid microcapsules, have as an external phase an aqueous phase in which water-in-oil (W / O) droplets are dispersed. [0003] W / O / W emulsions have various applications in food, medicine, cosmetics, etc. by encapsulating useful substances inside W / O droplets. W / O / W emulsions can also be used as intermediates in the production process. To make full use of W / O / W emulsions in these applications, it is important to be able to effectively suppress the leakage of useful substances from W / O droplets and control the release rate of useful substances. [0004] The encapsulation efficiency of useful substances in W / O / W emulsions greatly depends on the concentration balance of dissolved useful substances between the inner and outer aqueous phases. Generally, as the concentration of the useful substance in the inner aqueous phase increases, the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/113A61K8/04A61K8/30A61K31/135A61K31/138A61K31/196A61K31/352A61K31/375A61K31/401A61K31/4365A61K31/445A61K31/502A61K31/55A61K31/554A61K31/704A61K47/02A61K47/12A61K47/18A61K47/26
CPCA61K31/138A61K31/704A61K47/12A61K31/502A61K31/554A61K31/4365A61K31/135A61K31/445A61K9/113A61K31/352A61K31/375A61K31/401A61K31/196A61K31/55A61K8/066A61P35/00A61K47/24
Inventor 寺尾敏光今川昂柳卫宏宣江里口正纯
Owner OTSUKA PHARM FAB INC
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