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Biphenyl diester emulsion and its preparing method

A technology of bifendate emulsion and bifendate, which can be used in pharmaceutical formulations, emulsion delivery, medical preparations of non-active ingredients, etc., can solve problems such as thermodynamic instability, chemical instability, and difficulty in intravenous injection. Achieve the effects of increasing physical stability, simple preparation process, and controllable drug content

Inactive Publication Date: 2007-07-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the emulsion is a thermodynamically unstable system, which is prone to physical instability such as stratification, flocculation, and demulsification, and is inconvenient for storage and transportation.
[0006] CN 03146030.5 discloses a bifendate emulsion, which uses long-chain fatty acid glycerides such as soybean oil and corn oil as the oil phase, and is mainly used for oral administration. Because the solubility of bifendate in long-chain fatty acid glycerides such as soybean oil is less than 0.5mg / ml, and the ideal drug content in the emulsion should reach more than 10mg / 100ml, it is a little bit reluctant to use soybean oil as the oil phase, and when the bifendate content is high, even if a high concentration of oil phase and emulsifier is used , and take a certain pretreatment method to dissolve the drug during the preparation process, and there will be crystallization during the emulsion placement process, and increasing the oil phase content will increase the viscosity of the emulsion, which will bring certain safety issues to clinical applications. The property is also poor, and it is difficult to be used for intravenous injection. In addition, bifendate has certain chemical instability problems in soybean oil.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Biphenyl Diester 100mg

[0062] Soybean Oil 100g

[0063] Caprylic Glyceride 100g

[0064] Phospholipid 40g

[0065] Glycerin 25g

[0066] VE 0.5g

[0067] Water for injection to 1000ml

[0068] Preparation process: the prescription amounts of biphenyl diester, soybean oil, caprylic acid glyceride, phospholipid, and antioxidant are jointly heated to 80 ° C to obtain an oil phase, glycerin is added to 200 ml of water for injection to obtain a water phase, and the oil phase and water are mixed. Add the phases together in a tissue masher and stir at a high speed of 8000 rpm for 3 minutes to obtain white colostrum, and adjust the pH to 6-8. After the emulsion was cooled, water for injection was added to 1000ml, and the emulsion was homogenized under high pressure at 10000psi for 10 cycles. The obtained emulsion has an average emulsion particle size of 150-300 nm, after filtration with a 0.22 μm microporous membrane, it is divided into packages, filled with nitrogen, a...

Embodiment 2

[0070] Biphenyl Diester 300mg

[0071] Caprylic Glyceride 300g

[0072] Phospholipids 20g

[0073] Poloxamer 188 10g

[0074] Glycerin 25g

[0075] VE 0.2g

[0076] Water for injection to 1000ml

[0077] Preparation process: the prescription amounts of biphenyl diester, caprylic acid glyceride, phospholipid and antioxidant are jointly heated to 90 DEG C to obtain an oil phase, glycerol and poloxamer are added to 200ml of water for injection to obtain a water phase, and the oil phase is Together with the water phase, add it to the tissue masher and stir at a high speed of 8000 rpm for 3 minutes to obtain white colostrum, and adjust the pH to 6-8. After the emulsion was cooled, water for injection was added to 1000ml, and the emulsion was homogenized under high pressure at 15000psi and circulated 5 times. The obtained emulsion has an average emulsion particle size of 150-300 nm, after filtration with a 0.22 μm microporous membrane, it is divided into packages, filled with ...

Embodiment 3

[0079] Biphenyl Diester 200mg

[0080] Soybean Oil 20g

[0081] Refined Coconut Oil 180g

[0082] Phospholipids 20g

[0083] Poloxamer 188 10g

[0084] Glycerin 25g

[0085] VE 0.2g

[0086] Water for injection to 1000ml

[0087] The preparation method is the same as that of Example 2.

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Abstract

An emulsion or dried emulsion of biphenyl dimethylesterate and its preparing process which features that the glyceride octocaprate or refined coconut oil is used as its oil phase are disclosed.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a biphenyl diester emulsion and dry milk and a preparation method thereof. Background technique [0002] Bifendate (DDB for short) is an intermediate found in the research on artificial synthesis of Schisandra Propioides. It is a white crystalline powder, insoluble in water, slightly soluble in ethanol, and easily soluble in chloroform. lipophilicity. Its chemical name is 4,4-dimethoxy-5,6,5'6'-dimethyldioxy-2,2'-dicarboxylate biphenyl, molecular formula: C 20 H 18 O 10 The molecular weight is 418.36. [0003] The pharmacological effects of bifendate include: (1) Protect the liver from toxic damage: Experiments have shown that DDB can inhibit CC 14 The resulting lipid peroxidation and covalent bonding of hepatocyte microsomes partially protected the structural and functional integrity of the endoplasmic reticulum membrane of hepatocytes. ②Enhancing the detoxificat...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/36A61K47/34A61K47/24A61P1/16A61K47/10A61K47/14A61K47/26A61K47/32A61K47/36A61K47/38A61K47/40A61K47/44
Inventor 朱家壁薛文静陈志鹏张克军
Owner CHINA PHARM UNIV
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