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Erythromycin ethylsuccinate gel and preparation method thereof

A technology of erythromycin ethylsuccinate and gel, which is applied in the field of erythromycin ethylsuccinate gel and its preparation, can solve the problems of potential safety hazards such as drug loading, gel matrix and additive irritation, and achieve avoidance of toxic and side effects, Effects of improving drug safety and reducing burden

Active Publication Date: 2018-10-19
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In view of the irritation of the gel matrix and additives in the current erythromycin ethylsuccinate gel, potential safety hazards and small drug loading, it is necessary to develop an erythromycin ethylsuccinate gel with no additives and high drug loading

Method used

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  • Erythromycin ethylsuccinate gel and preparation method thereof
  • Erythromycin ethylsuccinate gel and preparation method thereof
  • Erythromycin ethylsuccinate gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Add 1 g of erythromycin ethylsuccinate powder to 10 g of N,N-dimethylformamide, stir at 5°C to form a suspension, and then stand at constant temperature at 5°C for 60 minutes to form a gel. The powder X-ray diffraction pattern of gained erythromycin ethylsuccinate gel is 4.4,5.1,6.4,9.2,9.4,10.0,11.3,12.6,13.4,14.0,15.4,16.0,17.8,18.2,18.7, There are characteristic diffraction peaks at 18.9, 20.7, 21.2, 21.9, 23.0 and 24.2, and the storage modulus is about (4.8~5.7)×10 5 Pa, the loss modulus is about (2.6~3.6)×10 5 Pa, the length of erythromycin ethylsuccinate fiber is about 600 μm, and the drug loading is 9.09wt%.

Embodiment 2

[0030] Under magnetic stirring at 300 rpm, 5.5 g of erythromycin ethylsuccinate was added to 10 g of ethanol, stirred at 28° C. to form a suspension, and left to stand at a constant temperature of 28° C. for 45 minutes to form a gel. The powder X-ray diffraction pattern of gained ethylsuccinate erythromycin gel is as attached figure 1 , characterized at diffraction angles 2θ of 4.4, 5.1, 6.3, 9.1, 9.3, 10.1, 11.3, 12.7, 13.3, 13.9, 15.5, 16.1, 17.9, 18.2, 18.7, 18.9, 20.7, 21.2, 21.9, 23.0 and 24.1 Diffraction peaks. The rheological curve of gained erythromycin ethylsuccinate gel is as attached figure 2 , the storage modulus is (4.9~6.1)×10 5 Pa, the loss modulus is about (2.8~4.0)×10 5 Pa, erythromycin ethylsuccinate fiber length is about 200μm, as attached image 3 , the drug loading is 35.5wt%.

Embodiment 3

[0032] Under magnetic stirring at 300 rpm, 10 g of erythromycin ethylsuccinate powder was added to 10 g of acetonitrile, stirred at 50° C. to form a suspension, and left to stand at a constant temperature of 50° C. for 30 minutes to form a gel. The powder X-ray diffraction pattern of gained erythromycin ethylsuccinate gel is 4.4,5.1,6.4,9.1,9.3,10.1,11.3,12.6,13.2,13.9,15.4,16.0,17.9,18.2,18.7, There are characteristic diffraction peaks at 18.9, 20.7, 21.2, 21.8, 23.0 and 24.0, and the storage modulus is about (5.4~6.3)×10 5 Pa, the loss modulus is about (3.2~4.1)×10 5 Pa, the length of erythromycin ethylsuccinate fiber is about 800 μm, and the drug loading is 50wt%.

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Abstract

The invention relates to an erythromycin ethylsuccinate gel and a preparation method thereof, and erythromycin ethylsuccinate molecules form a fiber network to wrap a solution to form the gel. The X-ray diffraction pattern of gel powder shows characteristic peaks at the diffraction angle 2theta of 4.4+ / -0.1-degrees, 5.1+ / -0.1-degrees, 6.3+ / -0.1-degrees, 9.1+ / -0.1-degrees, 9.3+ / -0.1-degrees, 10.1+ / -0.1-degrees, 11.3+ / -0.1-degrees, 12.7+ / -0.1-degrees, 13.3+ / -0.1-degrees, 13.9+ / -0.1-degrees, 15.5+ / -0.1-degrees, 16.1+ / -0.1-degrees, 17.9+ / -0.1-degrees, 18.2+ / -0.1-degrees, 18.7+ / -0.1-degrees, 18.9+ / -0.1-degrees, 20.7+ / -0.1-degrees, 21.2+ / -0.1-degrees, 21.9+ / -0.1-degrees, 23.0+ / -0.1 and 24.1+ / -0.1-degrees. The preparation method is simple, and needs no gel matrix, the safety is good; the contentof erythromycin ethylsuccinate in the gel is high, and is in the range of 9 to 50 wt%.

Description

technical field [0001] The invention belongs to the field of pharmaceutical engineering drug gel, and in particular relates to an erythromycin ethylsuccinate gel and a preparation method thereof. Background technique [0002] Erythromycin Ethylsuccinate, Chinese alias erythromycin ethyl succinate, erythromycin succinate, ethyl succinate erythromycin, ethyl succinate erythromycin, CAS number: 1264-62-6, molecular formula C 43 h 75 NO 16 , the structural formula is as follows: [0003] [0004] Erythromycin ethylsuccinate is a macrolide antibiotic, which is erythromycin ethyl succinate (acetylsuccinate of erythromycin). It acts antibacterially by releasing erythromycin through in vivo hydrolysis. Erythromycin ethylsuccinate has a wide antibacterial spectrum, high bioavailability, and less allergic reactions. It is an anti-inflammatory drug widely used in clinical practice. [0005] Gel is a new drug dosage form that has emerged in recent years. Gels are mostly admini...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/7048A61K47/08A61K47/10A61K47/16A61K47/18A61K47/22A61P31/04
CPCA61K9/06A61K31/7048A61K47/08A61K47/10A61K47/16A61K47/18A61K47/22A61P31/04
Inventor 鲍颖苏显栋高振国侯宝红郝红勋尹秋响
Owner TIANJIN UNIV
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