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Method for preparing sulfonamide compound liposome and its formulation

A compound and sulfonamide technology, applied in the field of medicine, can solve the problem that sulfonamide drugs are not easily encapsulated into liposomes, and achieve the effects of high encapsulation efficiency and uniform particle size

Inactive Publication Date: 2005-03-16
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] For sulfonamides, currently they are mainly solutions and solid preparations, mainly solid preparations, and there are no literature reports on liposomes (using sulfanilamide or sulfanilamide and liposomes as search terms through Medline), and it is speculated that the reason may be sulfa drugs Less easily incorporated into liposomes

Method used

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  • Method for preparing sulfonamide compound liposome and its formulation
  • Method for preparing sulfonamide compound liposome and its formulation
  • Method for preparing sulfonamide compound liposome and its formulation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: the preparation of indapamide liposome injection

[0035] 1. Add an appropriate amount of indapamide to an appropriate amount of anhydrous pyridine at a certain temperature to dissolve, add an excess of lauroyl chloride under magnetic stirring, and after a certain period of reaction, add a certain concentration of hot acid water to react the excess lauroyl chloride. Add a strong base to dissolve it, then use an acid to precipitate it once, collect the precipitate, dissolve the precipitate with a certain solvent, and separate lauroyl indapamide by silica gel column chromatography.

[0036] The reaction equation is as follows:

[0037]

[0038] 2. Dissolve a certain amount of lauryl indapamide, phospholipids, cholesterol, and vitamin E with 2ml of ethanol.

[0039] 3. Pour the above solution into a 60°C solution containing 0.2% Ca under magnetic stirring. 2+ in isotonic buffer solution.

[0040] 4. Ethanol was evaporated under reduced pressure.

[004...

Embodiment 2

[0043] Embodiment 2: the preparation of sulfisoxazole liposome gel.

[0044] 1. Dissolve sulfisoxazole in anhydrous pyridine at a certain temperature to dissolve, add excess acetic anhydride under magnetic stirring, after a certain period of reaction, add acid water at a certain temperature to react the excess anhydride, add a strong base to make it Dissolve, then use acid to precipitate once, collect the precipitate, dissolve the precipitate with a certain solvent, and obtain N-acetylsulfaisoxazole with relatively high purity after proper separation.

[0045] The reaction equation is as follows:

[0046]

[0047]2. Dissolve N-acetylsulfisoxazole, phospholipids, cholesterol and vitamin E acetate in absolute ethanol or 95% ethanol and mix well.

[0048] 3. Pour the mixed solution into a 0.5% Ba 2+ in normal saline

[0049] 4. Ethanol was evaporated under reduced pressure.

[0050] 5. Remove Ba by dialysis or adding appropriate amount of EDTA-Na 2+

[0051] 6. Add 1% Ca...

Embodiment 3

[0052] Example 3: Preparation of long-circulating liposome sulfamethazine lyophilized liposome powder injection

[0053] 1. Dissolve sulfamethazine in anhydrous pyridine at a certain temperature, add excess benzoyl bromide under magnetic stirring, after reacting for a certain period of time, add acid water at a certain temperature to react excess acid anhydride, add strong base to make Dissolve it, and then use acid to precipitate it once, collect the precipitate, dissolve the precipitate with a certain solvent, and obtain N-acetylsulfaisoxazole with relatively high purity after proper separation. Modified in the following way

[0054]

[0055] 2. After the modified drug is properly separated, it can be dissolved in ethanol:ether (v / v, 8:2) with soybean lecithin, appropriate amount of DMPE-PEG20000, cholesterol, and propyl gallate

[0056] 3. Inject the solution containing 0.3% Mg 2+ Acetic acid-sodium acetate buffered saline solution (adjusted isotonic with NaCl) at pH 6...

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Abstract

Disclosed is a method for preparing sulfonamide compound liposome and its formulation, wherein the preparation comprises the steps of, (1) if sulfonamide has free ammonia, subjecting the sulfonamide molecule to modification, if sulfonamide has no free ammonia, proceeding no modification and entering the next step, (2) dissolving the sulfonamide compound and right amount of phosphatide, cholesterin, anti-oxidant and other liposolubility substances into alcohols, ethers or mixture of alcohol and ether, (3) injecting the solution into 25-65 deg. C 0.2%-0.6% diatomic and tervalency metallic ion solution under magnetic stirring, (4) decompressing for removing alcohol and ether, squeezing through microporous filtering film, (5) charging a definite quantity of EDTA-Na into the liposome by dialysis, removing free diatomic and tervalency metallic ions to obtain other preparations.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to a preparation method of sulfonamide compound liposome and its preparation. Background technique: [0002] Sulfonamide compounds are a large class of compounds, which are the first antibacterial drugs developed in the 1930s, and also the first chemically synthesized drugs that are systematically used in clinical prevention and treatment of bacterial infections. After years of clinical application, it has been proved that it is a kind of broad-spectrum antibacterial drug and antihypertensive drug, which can effectively treat epidemic encephalomyelitis, respiratory tract infection, urinary tract infection, typhoid fever, plague, intestinal infection, local soft tissue or sore surface infection, eye infection and moderate to mild high blood pressure. [0003] For sulfonamides, currently they are mainly solutions and solid preparations, mainly solid preparations, and there are no l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/06A61K9/08A61K9/12A61K9/127A61K9/14A61K31/63A61P31/04C07C311/39
Inventor 邓英杰索绪斌郝爱军
Owner SHENYANG PHARMA UNIVERSITY
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