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2,2',6,6'-tetraisopropyl-4,4'-biphenol lipid microsphere preparations and preparation methods therefor

a technology of tetraisopropyl and lipid microspheres, which is applied in the field of pharmaceutical preparations, can solve the problems of difficult water dissolution of tetraisopropyl-4,4'-biphenol, limited clinical application, and affect the efficacy, so as to improve the therapeutic effect of the drug and improve the absorption

Inactive Publication Date: 2014-12-18
XIAN LIBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention encapsulates biphenol within lipid microspheres to increase its solubility in water, allow for higher drug loading, and increase stability. These microspheres are non-toxic, non-immunogenic, and reduce drug irritation and side effects. The invention also extends the drug's shelf life, improves solubility, and ensures safety. Additionally, the method of administration switches from oral to intravenous injection, improving drug absorption and increasing therapeutic effect. The preparation process is simple and cost-effective for mass production.

Problems solved by technology

However, biphenol is a highly lipid soluble compound that is difficult to dissolve in water.
Studies have shown that it is difficult to achieve a desired effect by using surfactants such as cyclodextrin, Tween 80, Vc or DMSO to assist or increase its dissolution and, thereby, its efficacy is affected and its clinical application becomes limited.

Method used

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  • 2,2',6,6'-tetraisopropyl-4,4'-biphenol lipid microsphere preparations and preparation methods therefor

Examples

Experimental program
Comparison scheme
Effect test

example 1

1% Biphenol Lipid Microsphere Preparation

[0046]

Drugs and ExcipientsAmount (g)Biphenol10.0Soybean oil (Injection-grade)100Egg lecithin12Vitamin E10Glycerin25EDTA5Injection-grade waterMake up to 1000 ml

Preparation Method

[0047]1) 12 g of egg lecithin was completely dissolved in 100 g of injection-grade oil under a nitrogen atmosphere and in a 70° C. water bath. 10 g of biphenol and 10 g of vitamin E were then added and nitrogen gas was fed in for protection before being dissolved, with heat and stirring, to obtain an oil phase.

[0048]2) 20 g of glycerin and 5 g of EDTA were dissolved, with stirring, in the injection-grade water to obtained an aqueous phase.

[0049]3) The oil phase was added slowly to the aqueous phase while sheared under nitrogen (10000 r, 5 min) to obtain a preliminary emulsion which was then adjusted to around pH 8.0 with sodium hydroxide.

[0050]4) The preliminary emulsion was homogenized with a high-pressure homogenizer and filtered with a microporous membrane filter be...

example 2

0.1% Biphenol Lipid Microsphere Preparation

[0051]

Drugs and ExcipientsAmount (g)Biphenol1.0Sea buckthorn oil (Injection-100grade)Hydrogenated Lecithin12Ascorbic acid10Glycerin25EDTA5Injection-grade waterMake up to 1000 ml

Preparation Method

[0052]1) 12 g of hydrogenated lecithin was completely dissolved in 100 g of injection-grade oil under a nitrogen atmosphere and in a 70° C. water bath. 1 g of biphenol was then added and nitrogen gas was fed in for protection before being dissolved, with heat and stirring, to obtain an oil phase.

[0053]2) 25 g of glycerin, 10 g ascorbic acid and 5 g of EDTA were dissolved, with stirring, in the injection-grade water to obtain the aqueous phase.

[0054]3) The oil phase was added slowly to the aqueous phase while sheared under nitrogen (10000 r, 5 min) to obtain a preliminary emulsion which was then adjusted to around pH 8.0 with sodium hydroxide.

[0055]4) The preliminary emulsion was homogenized with a high-pressure homogenizer and filtered with a microp...

example 3

3% Biphenol Lipid Microsphere Preparation

[0056]

Drugs and ExcipientsAmount (g)Biphenol30Injection-grade Medium-chain100triglyceride oilSoy lecithin12Sodium bisulfite10Glycerin25EDTA5Injection-grade waterMake up to 1000 ml

Preparation Method

[0057]1) 12 g of soy lecithin was completely dissolved in 100 g of injection-grade oil under a nitrogen atmosphere and in a 70° C. water bath. 30 g of biphenol was then added and nitrogen gas was fed in for protection before being dissolved, with heat and stirring, to obtain an oil phase.

[0058]2) 25 g of glycerin, 10 g of sodium bisulfite and 5 g of EDTA were dissolved, with stirring, in the injection-grade water to obtained an aqueous phase.

[0059]3) The oil phase was added slowly to the aqueous phase while sheared under nitrogen (10000 r, 5 min) to obtain a preliminary emulsion which was then adjusted to around pH 8.0 with sodium hydroxide.

[0060]4) The preliminary emulsion was homogenized with a high-pressure homogenizer and filtered with a micropo...

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Abstract

This invention relates to a 2,2′,6,6′-tetraisopropyl-4,4′-biphenol lipid microsphere preparation having 2,2′,6,6′-tetraisopropyl-4,4′-biphenol as its active ingredient and formed into said lipid microsphere preparation with common medically used injection-grade oil, emulsifier, and injection-grade water.

Description

FIELD OF THE INVENTION[0001]This invention relates to 2,2′,6,6′-tetraisopropyl-4,4′-biphenol lipid microsphere preparations and the preparation methods therefor, in the field of pharmaceutical preparations.BACKGROUND OF THE INVENTION[0002]2,2′,6,6′-tetraisopropyl-4,4′-biphenol (hereinafter referred to as biphenol) is an anti-epileptic compound newly developed (Chinese patent CN 101804043A, Uses of biphenol and its derivatives in drugs for the treatment of epilepsy) for treating many epileptic symptoms such as generalized tonic-clonic seizures (grand mal), absence seizures (petit mal), simple partial seizures, complex partial seizures (psychomotor seizures), autonomic seizures (periodic seizures) and others. Experimental studies have shown that biphenol has a strong affinity towards GABA receptors and is a GABA agonist, while it is an antagonist for NMDA receptors for regulating the Ca2+ influx in Ca2+ channels. Biphenol also offers protection against the excitotoxic effect induced b...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/16A61K31/05
CPCA61K31/05A61K9/16A61K9/0019A61K47/44A61K47/12A61K47/24A61K9/1075A61P25/08A61K9/5015A61K9/5089A61K47/02A61K47/10A61K47/22
Inventor WANG, RUTAOCHEN, TAOGUO, SHUPANHU, HUIJINGAN, LONGWANG, WEIJIAO
Owner XIAN LIBANG PHARMA
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