Quality Evaluation And Stability Studies Of Tilmicosin Release-enteric Granules

Tilmicosin, its chemical name is 4A-O-deoxidation(2,6-dideoxy-3-C-methylL-ribose-pyran-hexyl)-20-deoxidation-20-(3,5-dimethyl-1-piperidinyl)-[20(cis:trans)Tylosin. It belongs to fourth generation of macrolide antibiotic,which is belonging to animal-specific. Tilmicosin antibacterial spectrum is more broad than Tylosin, and its resistance is more lower than Tylosin.It has a good supporting effect in the aspects like Porcine reproductive and respiratory syndrome, Swine mycoplasma infections,Pleuropneumoniae, Porcine circovirus and other bacterial diseases. A large number of studies show that Tilmicosin,which is animal-specific antibiotic,has made a significant effect in controling PRRS.Currently,There are injection,solution,soluble powder and premixes for Tilmicosin.Few studies have reported about Tilmicosin release granules.Because there are some limitations still existing in preparation.For example,although the injection of Tilmicosin can reach the target efficacy directly,but it is inconvenient to use in the group,and studies have shown that low-dose injection is also very easy to cause cardiac toxicity in pigs.Therefore,in order to reduce side effects in actual production,the majority proportion is oral drugs.Because Tilmicosin is bitterness,oral administration has seriously affected in palatability,leaded to bad results in using effect.Such as Tilmicosin premixes,Tilmicosin solution,Tilmicosin soluble powder,phosphate Tilmicosin,etc.Therefore,the only way to improve the percentage of oral administration is to improve the bitterness Tilmicosin and increase Tilmicosin palatability.Then new formulations of Tilmicosin coated microcapsules was developed.This research studys quality and stability of Tilmicosin release-enteric granules mainly based on related requirements of "China Veterinary Pharmacopoeia" 2010 edition,veterinary chemicals quality control methods validation technical guidelines, Normalizationprocess technical guidelines veterinary chemicals quality standards established and Veterinary chemical drug stability guidelines.The quality evaluation of Tilmicosin release-enteric granules has mainly evaluated in the projects of traits, appearance, color, identification, size, loss on drying, release, quantity of contents, determination.The results show that the development Tilmicosin release-enteric granules can effectively mask the bitter taste and has a good palatability.And the projects like traits have meet the quality requirements of the Enteric sustained-release preparations.The stability test result of Tilmicosin release-enteric granules show that it will affect to some degree under the bright light, high temperature conditions.And it has no effect under high-humidity conditions.So,Tilmicosin release-enteric granules should be stored in a cool, dark, dry place.It has good stability and no effect under(40 ± 2) ℃, RH(75 ± 5)% conditions,where has placed continuously six months, the indexes of its character,content showed no significant difference, good stability.Placed continuously under the(25± 2)℃, RH(60 ± 10)% condition for 12 months,Tilmicosin release-enteric granule quality indicators are in line with the provisions.It has good stability.It is valid for 3 years.In summary, the quality evaluation methods of Tilmicosin release-enteric granule can effectively to control its quality.Tilmicosin release-enteric granule can completely mask the bitter taste, improve palatability,and has a good stability.It has good slow release enteric effect and can effectively improve the bioavailability of drugs,when used by oral.This study can provide scientific data for the development and application in the field of Tilmicosin release-enteric granule.