Rifaximin-containing in-situ gel for breast injection and preparation method of rifaximin-containing in-situ gel

An in-situ gel, rifaximin technology, applied in the directions of medical preparations containing active ingredients, medical preparations with non-active ingredients, pharmaceutical formulas, etc. Gel application, long residence time and other problems, to achieve the effect of strong adhesion, reducing bacterial resistance and slowing gel corrosion

Active Publication Date: 2016-01-13
NANJING DEPOT VETERINARY PHARMA R&D CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thermosensitive in situ gel (thermosensitive insitugel) has the advantages of convenient use, good biocompatibility, low irritation, strong affinity for mucosal tissue, long residence time, and good rheological characteristics in vitro. It is widely used in pharmaceutical preparations and is In recent years, research hotspots in the field of sustained and controlled release preparations. Although temperature-sensitive in-situ gels have excellent sustained-release effects, it is difficult to maintain them for 40 to 70 days, especially when the main ingredients are dissolved in water. shortened, limiting the application of thermosensitive in situ gel in the field of prevention and treatment of mastitis in dairy cows

Method used

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  • Rifaximin-containing in-situ gel for breast injection and preparation method of rifaximin-containing in-situ gel
  • Rifaximin-containing in-situ gel for breast injection and preparation method of rifaximin-containing in-situ gel
  • Rifaximin-containing in-situ gel for breast injection and preparation method of rifaximin-containing in-situ gel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1: in vitro antibacterial test

[0033] (1) Test material

[0034] Drugs: rifaximin, neomycin sulfate, lysozyme, neohouttuydin sodium

[0035] Bacterial strains: clinically isolated drug-resistant strains of Staphylococcus aureus, Escherichia coli and Streptococcus agalactiae, common agar medium (self-made), common broth medium (self-made).

[0036] (2) Test method

[0037] 2% rifaximin solution and 0.2% neohouttuydin sodium solution were prepared with DMSO as solvent, and 2% neomycin sulfate solution was prepared with water for injection as solvent.

[0038] Inoculate the suspension of Staphylococcus aureus, Escherichia coli and Streptococcus on the agar medium, place it in a 37°C incubator and cultivate it for 24-48h, pick the grown colony and place it in a medium containing 2 mL of sterilized common broth medium In the test tube, dilute it properly with sterilized physiological saline to a bacterial content of 1.5×10 8 individual / mL. For aseptic opera...

Embodiment 2

[0045] Cyclodextrin inclusion complex of rifaximin

[0046] prescription

[0047] Rifaximin 100g

[0048] Ethyl-β-cyclodextrin 190g

[0049] 50% ethanol aqueous solution 1800mL.

[0050] Preparation method: (a), rifaximin is ultrafinely pulverized, and 90% of the particle size is controlled within 5 μm, and there must be no particles with a particle size larger than 10 μm; (b), 100 g of rifaximin and 190 g of ethyl- Put β-cyclodextrin into a grinder, add 900mL of 50% ethanol aqueous solution, and grind for 30 minutes; (c), add the remaining 900mL of 50% ethanol aqueous solution, stir for 4 hours, spray dry, and pass through a 300-mesh sieve to obtain rifaxime A cyclodextrin inclusion compound is disclosed, the particle size of the cyclodextrin inclusion compound is below 50 μm, and rifaximin exists in the form of inclusion compound in the cyclodextrin inclusion compound.

Embodiment 3

[0052] Rifaximin-Neomycin Sulfate Cyclodextrin Inclusion Complex

[0053] prescription

[0054]

[0055]

[0056] Preparation method: (a), rifaximin is ultrafinely pulverized, and 90% of the particle size is controlled within 5 μm, and there must be no particles with a particle size larger than 10 μm; (b), 100 g of rifaximin, 100 g of neosulfate Put mymycin and 400g of 2,6-diethyl-β-cyclodextrin into a grinder, add 2000mL of 50% ethanol aqueous solution, and grind for 30 minutes; (c), add the remaining 2000mL of 50% ethanol aqueous solution, stir for 5h, and spray dry through a 300-mesh sieve to obtain the rifaximin-neomycin sulfate cyclodextrin inclusion compound, the particle size of the cyclodextrin inclusion compound is below 50 μm, and the rifaximin and neomycin sulfate in the cyclodextrin inclusion compound Elements exist in the form of inclusion complexes.

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Abstract

The invention discloses rifaximin-containing in-situ gel for breast injection. The rifaximin-containing in-situ gel comprises the following components in percentage by mass: 0.1-15% of an active drug component existing in a dispersed way, 0.25-20% of an active drug component existing in an inclusion compound form, 12-30% of poloxamer 407, 0.01-11% of poloxamer 188, 0.01-10% of a polymer drag reduction agent, 0.001-3% of a bacterial inhibitor, a pH regulator for regulating the pH value to 5.5-7.5 and the balance of injection water. The invention also discloses a preparation method of the rifaximin-containing in-situ gel for breast injection. Water is used as a solvent, so that the rifaximin-containing in-situ gel is good in biocompatibility, little in irritation and high in safety, exists in a liquid state under a storage condition, is completely formed within 4-15 seconds after being injected to the breast because of thermal stimulation inside the breast and can be used for effectively treating, preventing and controlling mastitis of milk cows within the whole dry cow period; and in addition, the sustained-release effect is remarkable, and the in-vitro drug release time is long and reaches up to 48 days.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations for animals, and relates to a rifaximin-containing in situ gel for breast injection and a preparation method thereof, in particular to a rifaximin-containing breast injection gel with a suitable phase transition temperature Bit gel and its preparation method. Background technique [0002] Dairy cow mastitis is a common and frequently-occurring disease in dairy farming. It is mainly induced by Staphylococcus aureus, Streptococcus, Escherichia coli, Bacillus cereus, Actinomyces pyogenes, Pseudomonas aeruginosa, and Klebsiella. The incidence of dairy cow mastitis in my country is higher than the world average level, which has seriously restricted the development of dairy cattle breeding industry. In the prevention and treatment of dairy cow mastitis, the treatment of the dry period is an important link in the control of herd mastitis. At this time, the cows are in the weaning period, which...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/437A61K47/48A61K31/7036A61P15/14A61P31/04A61K31/185
Inventor 余祖功郭凡溪
Owner NANJING DEPOT VETERINARY PHARMA R&D CO LTD
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