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Self-emulsifying formulation of biphenyldicarboxylate and preparation method thereof

A bifendate, self-emulsifying technology, applied in the digestive system, emulsion delivery, active ingredients of heterocyclic compounds, etc., can solve the problems of inconvenient storage and transportation of liquid preparations, phase behavior changes of preparations, drug instability, etc. Achieve the effects of improving bioavailability, small dispersion index, and simple and easy preparation process

Inactive Publication Date: 2009-04-08
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The prepared emulsion is directly filled in capsules, which is prone to adverse phenomena such as drug precipitation and phase behavior changes of preparations during production and storage.
CN 100998561A discloses a bifendate emulsion for intravenous injection, which is a liquid preparation, which is inconvenient to store and transport, and is likely to cause drug instability

Method used

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  • Self-emulsifying formulation of biphenyldicarboxylate and preparation method thereof
  • Self-emulsifying formulation of biphenyldicarboxylate and preparation method thereof
  • Self-emulsifying formulation of biphenyldicarboxylate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Bifendate 1.5g

[0043] Glyceryl Caprylate 45.5g

[0044] Polyoxyethylene castor oil 26.5g

[0045] Polyethylene glycol-12-hydroxy-stearate 26.5g

[0046] Take glyceryl caprate, polyoxyethylene castor oil, polyethylene glycol-12-hydroxyl-stearate (trade name: Solutol 15, the same below), vortex mixing, adding bifendate, and completely dissolving the drug in a 60-degree constant temperature water bath to obtain a bifendate self-emulsifying preparation. Take an appropriate amount of this self-emulsifying liquid preparation, dilute it 100 times with artificial gastric juice, shake gently to form a uniform, stable and blue opalescent emulsion very quickly, the particle diameter of this emulsion is measured to be 178nm, and the polydispersity index is 0.323.

Embodiment 2

[0048] Bifendate 3.0g

[0049] Propylene Glycol Dicaprylate / Dicaprate 35g

[0050] Polyoxyethylene hydrogenated castor oil 30g

[0051] Macrogol-12-hydroxy-stearate 15g

[0052] Ethylene glycol monoethyl ether 17g

[0053] Weigh dicaprylic acid / dicapric propylene glycol ester (trade name: Miglyol 840), polyoxyethylene hydrogenated castor oil, polyethylene glycol-12-hydroxyl-stearate, ethylene glycol monoethyl ether (Transcultol HP, The same below), vortex mixing, adding bifendate, and completely dissolving the drug in a 55-degree constant temperature water bath to obtain a bifendate self-emulsifying preparation. Take an appropriate amount of this self-emulsifying liquid preparation, dilute 100 times with artificial gastric juice, shake gently to form a uniform, stable and blue opalescent emulsion very quickly, the particle diameter of this emulsion is measured to be 153nm, and the polydispersity index is 0.115.

Embodiment 3

[0055] Bifendate 4.0g

[0056] Glyceryl Caprylate 46g

[0057] Polyoxyethylene hydrogenated castor oil 22g

[0058] Macrogol-12-hydroxy-stearate 28g

[0059] Microcrystalline Cellulose 125g

[0060] Weigh caprylic capric acid glyceride, polyoxyethylene hydrogenated castor oil, polyethylene glycol-12-hydroxy-stearate, shake and mix, add bifendate, and dissolve the drug completely in a constant temperature water bath at 50 degrees, The self-emulsifying concentrate of bifendate is obtained, and an appropriate amount of distilled water is added and stirred to form an emulsion. Take microcrystalline cellulose, mix it with the above-mentioned emulsion to make a soft material, extrude the obtained soft material through a 30-mesh sieve to make granules, sieve the 24-mesh sieve, and dry the obtained granules in a drying oven at a constant temperature. The granules are subpackaged to obtain granules. Take an appropriate amount of the self-emulsifying granules, dilute 100 times with...

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Abstract

The invention relates to the field of pharmaceutical preparation, in particular to a bifendate self-emulsifying preparation and a method for preparing the same. The bifendate self-emulsifying preparation is characterized by adopting the mixture of polyethylene glycol-12-hydroxy-stearic acid ester and polyoxyethylene hydrogenated castor oil or the mixture of the polyethylene glycol-12-hydroxy-stearic acid ester and polyoxyethylene castor oil as an emulsifier. The bifendate self-emulsifying preparation is emulsified spontaneously to form micro-emulsion droplets of which the particle diameter is less than 200 nanometers after oral administration, thereby enhancing the solubility and the dissolving speed of the bifendate so as to improve the bioavailability of bifendate. At the same time, the bifendate self-emulsifying preparation prepared by adding a solid adsorption material into a liquid self-emulsifying preparation not only effectively improves the defects of liquid preparations in production, storage, administration and the like, but also significantly improves the stability of drugs with a simple and practicable preparation process.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a bifendate self-emulsifying preparation, a solid self-emulsifying preparation and a preparation method thereof. Background technique [0002] Biphenyl diester, English name: biphenyl dimethyl dicarboxylate, chemical name: 4,4-dimethoxy-5,5,5,6'-dimethoxy-2,2'-dicarboxylic acid methyl ester biphenyl , the molecular formula is: C 20 h 18 o 10 , Molecular weight: 418.3. The structural formula is as follows: [0003] [0004] This product is a white crystalline powder, almost insoluble in water, slightly soluble in methanol and ethanol, easily soluble in chloroform, showing certain fat solubility. Bifendate is an intermediate in the synthesis of schisandrin, and it is the first hepatoprotective drug in my country. A large number of animal experiments and clinical studies have shown that the drug can reduce the structural damage to liver tissue caused by various pa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/36A61P1/16
Inventor 平其能吕文莉王珊宋赟梅
Owner CHINA PHARM UNIV
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