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Preparation method of kitasamycin microcapsules

A kitasamycin and microcapsule technology, applied in the field of microcapsules, can solve problems such as poor stability and reduced biological activity, and achieve the effects of good stability, low cost and improved bioavailability

Inactive Publication Date: 2018-10-23
QINGDAO BRIGHT MOON SEAWEED GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The poor stability of kitasamycin to gastric acid leads to a large amount of direct oral drug degradation resulting in reduced biological activity, so it is necessary to improve the kitasamycin manufacturing process to increase the bioavailability of kitasamycin

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0022] The preparation method of kitasarmycin microcapsules of the present invention comprises the following steps:

[0023] (1) Stir and mix liquid oil and lipophilic emulsifier evenly to obtain the first mixed solution, add kitasarmycin solution to the first mixed solution and stir and mix evenly to obtain colostrum; The element is wrapped inside, the liquid oil is an oily substance, and kitamycin is a water-soluble active substance, thus forming a water-in-oil colostrum;

[0024] (2) Stir and mix the sodium alginate solution and the hydrophilic emulsifier evenly to obtain the second mixed solution, add colostrum into the second mixed solution and stir and mix evenly to obtain a composite emulsion; in the composite emulsion, the sodium alginate solution The colostrum is wrapped inside, that is, sodium alginate wraps liquid oil, and liquid oil wraps kitamycin, thus forming water-in-oil-in-water microcapsules;

[0025] (3) Drop the composite emulsion into calcium chloride sol...

Embodiment 1

[0038] (1) Mix 30ml of liquid paraffin oil with 10ml of sorbitan trioleate, and stir for 2 minutes at 1000rpm on a high-speed dispersing homogenizer to obtain the first mixed solution;

[0039] Add 10ml of kitasarmycin solution with a mass concentration of 10g / L to the first mixed solution, stir at 9500rpm for 6min on a high-speed dispersing homogenizer and mix evenly to obtain colostrum;

[0040] (2) Mix 50ml of sodium alginate solution with a mass concentration of 10g / L and a viscosity of 300cps with 3ml of polysorbate-80, stir on a high-speed dispersing homogenizer at 1000rpm for 2min and mix evenly to obtain the second mixed solution;

[0041]Mix according to the volume ratio of colostrum: the second mixed solution is 1:20, and stir and disperse for 3 minutes at a speed of 2000 rpm on a high-speed dispersing homogenizer to obtain a composite emulsion;

[0042] (3) Take out the compound emulsion with a 10ml syringe, set the advance speed of the syringe pump to 3ml / min, drop...

Embodiment 2

[0050] (1) Mix 30ml of liquid paraffin oil with 10ml of sorbitan trioleate, and stir for 2 minutes at 1000rpm on a high-speed dispersing homogenizer to obtain the first mixed solution;

[0051] Add 15ml of kitasarmycin solution with a mass concentration of 10g / L to the first mixed solution, and stir at 9500rpm for 6min on a high-speed dispersing homogenizer to mix evenly to obtain colostrum;

[0052] (2) Mix 80ml of sodium alginate solution with a mass concentration of 10g / L and a viscosity of 300cps with 4ml of polysorbate-80, stir on a high-speed dispersing homogenizer at 1000rpm for 2min and mix evenly to obtain the second mixed solution;

[0053] Mix according to the volume ratio of colostrum: the second mixed solution is 1:10, and stir and disperse for 3 minutes at a speed of 2000 rpm on a high-speed dispersing homogenizer to obtain a composite emulsion;

[0054] (3) Take out the compound emulsion with a 10ml syringe, set the advancing speed of the syringe pump to 3ml / min...

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Abstract

The invention discloses a preparation method of kitasamycin microcapsules. The method includes the steps of firstly, evenly stirring and mixing liquid grease and an oleophylic emulsifier to obtain first mixed liquid, adding a kitasamycin solution into the first mixed liquid, and evenly stirring and mixing to obtain a primary emulsion; secondly, evenly stirring and mixing a sodium alginate solutionand a hydrophilic emulsifier to obtain second mixed liquid, adding the primary emulsion into the second mixed liquid, and evenly stirring and mixing to obtain a compound emulsion; thirdly, dropwise adding the compound emulsion into a calcium chloride solution to perform calcification, and filtering to obtain the kitasamycin microcapsules. The method has the advantages that a water-oil-water emulsification method is used to wrap kitasamycin inside sodium alginate, calcium alginate is formed through the calcification reaction to tightly wrap the emulsification system inside, the kitasamycin ishigh in encapsulation rate, and good stability is achieved; the kitasamycin microcapsules can increase the bioavailability of the kitasamycin, and the kitasamycin is not released in the stomach, doesnot irritate the stomach and is only released and absorbed in the intestinal tract.

Description

technical field [0001] The invention relates to the technical field of microcapsules, in particular to a method for preparing kitasamycin microcapsules. Background technique [0002] Kitamycin is a multi-component macrolide antibiotic produced by Streptomyces. Macrolide antibiotics are weakly basic and lipophilic antibiotics with multiple internal aliphatic ring structures. Similar to mycin, it has a strong inhibitory effect on Gram-positive bacteria (such as Staphylococcus, Streptococcus pyogenes, Streptococcus viridans, Streptococcus pneumoniae, Bacillus tetanus, Bacillus diphtheria, etc.), and has a strong inhibitory effect on Gram-negative bacteria , such as Neisseria gonorrhoeae, pertussis and other Gram-negative bacteria also have a certain inhibitory effect, have inhibitory effects on mycoplasma, leptospira, rickettsia, and are effective against most Staphylococcus aureus resistant to penicillin and erythromycin. Compared with other types of antibiotics such as tetra...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/36A61K31/7048A61P31/04A61P11/00A61P1/16A61P11/14A61P11/04A61P15/00
CPCA61K9/5036A61K31/7048A61P1/16A61P11/00A61P11/04A61P11/14A61P15/00A61P31/04
Inventor 张梦雪张德蒙王发合秦益民逄锦龙张健石少娟
Owner QINGDAO BRIGHT MOON SEAWEED GROUP
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