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Doxycyline Hyclate lipid gels and preparing method

A technology of doxycycline hydrochloride and body gel, which is applied in the directions of liposome delivery, tetracycline active ingredients, pharmaceutical formulations, etc. The effect of prolonging the action time and improving the antibacterial effect

Inactive Publication Date: 2007-11-14
SHANGHAI NINTH PEOPLES HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, doxycycline hydrochloride preparations mainly include tablets, capsules and powder injections. If local inflammation is treated, especially when treating oral diseases, the anti-inflammatory effect produced locally by oral administration or intramuscular injection is not obvious, and systemic administration Side effects will be greater
Due to the good water solubility of doxycycline hydrochloride, it has poor permeability to skin and mucous membranes when it is prepared into local drug preparations, and the local drug action time is short and the antibacterial effect is not ideal.

Method used

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  • Doxycyline Hyclate lipid gels and preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] 500mg of soybean lecithin and 100mg of cholesterol were co-dissolved in 20ml of ethanol, and formed into a film by rotary evaporation in a water bath at 50°C; Phosphate buffer saline, and this solution is added in the film, oscillates to disperse and stir homogenizes one to two hours, obtain doxycycline hydrochloride liposome, add 0.1wt% sulfurous acid to doxycycline hydrochloride liposome Sodium hydrogen, stored in the refrigerator for later use.

[0033] The average particle size of the obtained doxycycline hydrochloride liposome is between 100-200 mm; the product is applied to the ultrafiltration centrifugation method to determine the encapsulation efficiency of more than 60%.

[0034] Swell 0.6 g of carbopol 934P with distilled water equivalent to 20 times the weight of the carbopol, add triethylamine dropwise to make the pH value about 9, and obtain the carbopol gel matrix, which is stored for later use.

[0035] Mix the doxycycline hydrochloride liposome and the ...

Embodiment 2

[0037] Dissolve 1000 mg of soybean lecithin and 100 mg of cholesterol in 30 ml of ether, and form a film by rotary evaporation in a water bath at 50 ° C. Dissolve 200 mg of doxycycline hydrochloride in 5 mL of phosphoric acid at pH = 7.3 containing 2% poloxamer Add the solution to the membrane, oscillate to disperse and homogenize with stirring for one to two hours to obtain doxycycline hydrochloride liposomes.

[0038] The average particle diameter of the obtained doxycycline hydrochloride liposome is between 100-200nm; the encapsulation efficiency of the product is determined to be over 70% by an ultrafiltration centrifugation method.

[0039] Swell 0.7 g of carbopol 971P with distilled water equivalent to 5 times the weight of the carbopol, add dropwise 1 mol / L sodium hydroxide to make the pH value about 11, and then obtain the carbopol gel matrix, which is stored for later use.

[0040] Mix the doxycycline hydrochloride liposome and the gel base at a ratio of 8:2 to obtain...

Embodiment 3

[0042] Dissolve 1500mg of egg yolk lecithin and 150mg of cholesterol in 20ml of ethanol, dissolve 300mg of doxycycline hydrochloride in 10mL of phosphate buffer containing 5% poloxamer at pH=6, pour the ethanol solution into the buffer solution , and the mixed solution was sheared with a high-speed shear to form colostrum, and the emulsion was evaporated under reduced pressure to obtain a doxycycline hydrochloride liposome suspension.

[0043] The average particle diameter of the obtained doxycycline hydrochloride liposome is within 100nm; the encapsulation efficiency of the product is determined to be 55% by an ultrafiltration centrifugation method.

[0044] Swell 1 g of carbopol 940 with distilled water equivalent to 10 times the weight of the carbopol, add dropwise sodium bicarbonate to make the pH value about 10, and obtain the carbopol gel matrix, which is then placed for later use.

[0045] Mix the doxycycline hydrochloride liposome and the gel base at a ratio of 5:5 to ...

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Abstract

The present invention discloses a doxycycline hydrochloride liposome gel preparation. It is made up by uniformly mixing (by wt%) 20-80% of doxycycline hydrochloride liposome and 80-20% of gel matrix. The invented doxycycline hydrochloride liposome gel preparation can be used as local antibiotic medicine, and can effectively prolong action time of medine and can raise antibacterial effect of medicine.

Description

technical field [0001] The invention relates to a local doxycycline hydrochloride preparation, in particular to a doxycycline hydrochloride liposome gel and a preparation method thereof. Background technique [0002] Doxycycline hydrochloride (doxycycline hydrochloride, doxycycline hydrochloride) is a tetracycline antibiotic. It can be widely used in respiratory, urinary, reproductive system and biliary tract infections, and has certain curative effects on skin and soft tissue infections, sepsis, acne, brucellosis, trachoma, gonorrhea, etc., and can effectively control subgingival plaque in periodontal pockets, Inhibit periodontal disease pathogenic bacteria. At present, doxycycline hydrochloride preparations mainly include tablets, capsules and powder injections. If local inflammation is treated, especially when treating oral diseases, the anti-inflammatory effect produced locally by oral administration or intramuscular injection is not obvious, and systemic administration...

Claims

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Application Information

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IPC IPC(8): A61K31/65A61K9/127A61K9/00A61P31/04A61P1/02A61P17/02A61P11/00A61P13/00A61P15/00
Inventor 金鸿莱芦洁奉建芳胡纯贞肖忠革
Owner SHANGHAI NINTH PEOPLES HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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