Study Of The Consistency Evaluation Of Loratadine Tablets

Loratadine was a new drug developed by Schering-Plough Corporation.Loratatdine tablet,with Clarityne as trade name,first went on sale in Belgium in the year of 1988.Loratadine,which is used in the treatment of allergic rhinitis,urticaria,pruritus and some other allergic dermatosis,is a new kind of selectivehistamine H1 receptor antagonists with no sedativeeffect.Through a way of technology transfer and with the domestic approval number of H10970410 Shanghai Schering Plough Pharmaceutical has started to mamufacture and sale loratadine tablet which is known as Clarityne with a strength of 10mg since the year of 1997.The formula and preparation technology of Clarityne is the same at home and abroad.Currently 35 pharmaceutical companiesare mamufacturing loratadine tablets,with the same dosage of 10mg.The formula and preparation technology vary from one to another.Thus it’s difficult to evaluate the quality equivalence between innovative and generic drugs.In this essay,based on the work of National Assessment Programs for loratadine preparations,related compounds of loratadine and loratadine preparationswere studied,and a method of the consistency evaluation of disslubility for loratadine tablets was established.1).The high-performance liquid chromatography(HPLC)separation was performed on an Agilent TC-C18 column gradient eluted with a mobile phase consisting of 2%acetic acid as mobile phase A and acetonitrile as mobile phase B.The flow rate was 1.0 mL min-1.The column temperature was at 35℃.Detection wavelength was 276 nm.Five related compounds of loratadine were separated.High performance liquid chromatography-tandem mass spectrometry(LC-MS/MS)was used to study the related compounds in loratadine andits preparations.Multiple reaction monitoring(MRM)mode operating in positive ion was used in MS detection.2).To establish a method of the consistency evaluation of disslubility for loratadine tablets,the dissolution profiles of loratadine tablets in five different medium with different pH value(pH1.2,pH3.0,pH4.0,pH5.0 and pH6.8)were studied.Loratadine tablets named Clarityne from Shanghai Schering Plough Pharmaceutical were used as reference preparations.Preliminary method for evalution of comparability of dissolution profiles in different mediums in vitro between reference and generic loratadine tablets was found.Because the dissolution behavior of loratadine is pH-dependent and loratadine is classified as Biopharmaceutics Classification System(BCS)Ⅱ drug substance,it will be better to carry out the equivalence evaluation both through dissolution profiles in vitro and bioequivalency in vivo.In conclusion,this study can provide scientific reference and guidance for consistency evaluation of generic loratadine oral solid preparations.