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Non-aqueous liquid composition

A liquid composition, non-aqueous technology, applied in the fields of injections and ophthalmic preparations, can solve problems such as insufficient drug sustained release, and achieve excellent drug sustained release effect

Inactive Publication Date: 2014-10-01
SANTEN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, if the depot preparations disclosed in Patent Documents 1 and 2 are administered on the premise of administration to a living body such as the vitreous body, the sustained release of the drug in the living body is insufficient, and there is a possibility that the drug may swell in the living body.

Method used

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Examples

Experimental program
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Effect test

preparation example 2

[0047] A DOPC formulation containing 0.2% of TA was prepared in the same manner as in Formulation Example 1 except that 20 mg of fludroxycortisol acetate (TA) was used instead of HC.

preparation example 3

[0049] A DOPC formulation containing 0.2% of FA was prepared in the same manner as in Formulation Example 1 except that 20 mg of fluocinolone acetate (FA) was used instead of HC.

[0050] (4) Preparation Example 4

[0051] Add about 200 mg of benzyl alcohol (BzOH) to 50 mg of FA, heat to 60° C. and stir until dissolved (20% FA solution). This 100 mg of 20% FA solution was added to 200 mg of DOPC, and dissolved while heating to 70° C. while stirring. After dissolving, 200 mg of VE was added, heated to 70° C. and stirred until dissolved to prepare a DOPC formulation containing 4% FA.

[0052] (5) Preparation Example 5

[0053] Add 6 mg of fluorouracil (5-FU) to 294 mg of polyethylene glycol (PEG) 400, heat to 70°C and stir until dissolved (2% 5-FU solution). This 50 mg of 2% 5-FU solution was added to 225 mg of DOPC, and dissolved while heating to 70° C. while stirring. After dissolving, 225 mg of VE was added, heated to 70° C. and stirred until dissolved, and a DOPC prepara...

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Abstract

A drug-dissolved non-aqueous liquid composition comprising a drug, dioleylphosphatidylcholine, tocopherol and an organic solvent, wherein the ratio of the blend concentration of dioleylphosphatidylcholine to that of tocopherol falls within the range from 75 / 25 to 25 / 75, the blend concentration of dioleylphosphatidylcholine falls within the range from 15 to 85% (w / w) and the blend concentration of tocopherol falls within the range from 15 to 85% (w / w). The phase of the non-aqueous liquid composition can be changed into a non-lamellar liquid crystal upon the contact with water, a phosphate buffer, a body fluid, a tear fluid or a vitreous fluid.

Description

technical field [0001] The invention relates to a drug-soluble non-aqueous liquid composition containing a drug, dioleoylphosphatidylcholine, tocopherol and an organic solvent, and an injection and an ophthalmic preparation containing the non-aqueous liquid composition. Background technique [0002] Dioleoylphosphatidylcholine (hereinafter, "DOPC") is an amphiphilic substance having a structure in which two oleic acid, glycerol, phosphoric acid, and choline are complexed. As amphiphilic substances, in addition to DOPC, for example, dioleoylphosphatidylglycerol (hereinafter, "DOPG"), dioleoylphosphatidylethanolamine (hereinafter, "DOPE"), phosphatidylcholine (hereinafter, , "PC"), soybean lecithin (hereinafter, "SPC"), glyceryl monooleate (hereinafter, "GMO") and the like. [0003] On the other hand, there is a demand for the development of depot preparations that have the effect of sustaining drug release by staying near the administration site (for example, vitreous body, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/16A61K9/10A61K47/10A61K47/32A61P27/02
CPCA61K9/0048A61K31/513A61K9/0024A61K47/24A61K31/58A61K31/573A61K47/22A61K9/1274A61K9/0051A61P27/02
Inventor 山田和人A·于尔蒂M·比尔梅斯特
Owner SANTEN PHARMA CO LTD
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