Study Of Azithromycin In Situ Gel For Ophthalmic

In situ gel for ophthalmic that is used at non-physiological state for the free flow of liquid,after administration of physiological conditions of the eyes turn to gel,that can be extended the residence time of drug in eyes,thereby enhancing bioavailability.In this paper,azithromycin(AZM) as a model drug.The temperature-sensitive polymers Poloxamer 407 and bioadhesion polymers polycarbophil,as the matrix gel.In the prefomulation research,the first established HPLC method to determination azithromycin,by method of study to prove that for the HPLC determination of azithromycin with good reproducibility,high accuracy,the systemadaptable,and easy to use.Secondly,the stability test of azithromycin in acid, alkali,light,heat,oxidative damage conditions was enforced, the results indicated that the stability of azithromycin in the acid and thermal is poor.In addition,the solubility of azithromycin increased with the pH value decreased. Azithromycin solution in different pH value thermal stability was measured.Azithromycin in pH6.0-6.5 the degradation rate constant is smaller,the most stable pH value is 6.3Part in the prescription process to the physical conditions of polymer materials and non-physiological conditions, mobility and ability to gel as an index prescription were screened for the appropriate amount of polymer materials. Combined with the physical and chemical properties of azithromycin options some cosolvent,buffer right,osmotic pressure regulator,metal ion chelating agent.Through the antimicrobial effectiveness testing to choose the amount of the preservative.Finalization,the prescription of temperature-sensitive in situ gel of azithromycin for ophthalmic is a 1%azithromycin,17%poloxamer407,0.2% polycarbophil,0.2%citric acid,sodium citrate 0.445% benzalkonium chloride 0.005%,0.14%NaC1,0.1%EDTA-2Na. Preparation for the temperature-sensitive in situ gel of azithromycin for ophthalmic that is a gel-type temperature and viscosity of the study results show that it can meet in non-physiological state for the free flow of the liquid.After administration,turn to gel in physiological conditions. Temperature-sensitive in situ gel of azithromycin for ophthalmic that slowed the in vitro drug release,gel temperature about 35℃.The research component of quality control,combined with general ophthalmic preparations quality requirements and in situ gel characteristics,the establishment of a trait, identification,pH,osmotic pressure,visible particles,gel temperature,related substance,the release degree,the assay etc.Finally,we conduct a preliminary stability study.We use the classical constant temperature method,accelerate test and long-term stability test to forecast stability of temperature-sensitive in situ gel of azithromycin for ophthalmic.The results show that the shelf life can be achieved 2 years in the range of 2 -8℃.