Study On Quality Consistence And In Vitro&Vivo Equivalence Of Loratadine Tablet

General Office of the State Council initiate the reformation for drug and medical device registration on August 2015,the key proposal is to improve the efficacy and quality equivalence of generic drug and reference drug equivalence evaluation.The solid dosage form drug listed on National Essential Drug List which approved before Oct2017 should complete GCE work by 2018;Otherwise the license should be withdraw.Loratadine tablets should complete quality and efficacy work by the end of 2018.The product is categorized as long-acting tricyclic antihistamine,which competitively suppresses H1 histamine receptor and therefore its related allergy symptoms.It alleviates relevant symptoms of Allergic Rhinitis,such as sneezing,rhinorrhea,nasal obstruction,and eye itching and ocular burning sensation.Loratadine tablet was originally developed by Schering-Plough(USA),and its launching was approved by FDA in 1993.In 2002,FDA approved the conversion of Loratadine categorization from prescription drug to OTC.Currently available forms in the market include tablets,orally disintegrating tablets,syrups,etc.DMPK and dissolution are the basic two methods utilized to evaluate the efficacy and quality equivalence of generic drug and reference drug equivalence.DMPK indicate the absorption speed and extent for dosage,also as the final acceptance criteria for GCE,but the test cost is the high concern;Dissolution can be used to simulate GI p H value and motion in a certain degree,the advantage is simple?low cost?high efficiency,now the tool has become the most important method to estimate the batch to batch variation and SUPAC.If we can establish correlation between in-vitro and in-vivo,scientist will have ability to predict drug oral absorption leverage dissolution data only.Simulate the stomach composition and p H value at fasting and fed state,performed dissolution curve cover the p H 1.2 to p H6.8.Generic drug got similar dissolution behavior in p H1.2,p H5.0 medium against original drug,appear to have different dissolution curve at other medium.Generally,Non-equivalent will be occur for subsequent BE study,the Formula and process should be totally changed.But based on mechanism of absorption of solid dosage form in physiological?Caco-2 apparent penetration results and PMDA official bio-equivalence data,if the crucial medium of p H1.2,p H5.0 dissolution curve well math that can ensure Bioequivalence for subsequence BE study.This is a randomized,open-label,single-center,single-dose,two-treatment,two-period,two-sequence,replicated crossover study to evaluate relative bioavailability of Xisimin tablet 10 mg with respect to Clarityne tablet 10 mg under fasted condition in healthy subjects.Cmax of test Loratadine and reference Loratadine was 13.11±9.15 ? 12.18±7.04 ng.ml-1,respectively.F(1,18)> 0.0202,P>0.05,t1 =2.033,t2 =2.318;(1-2?)CI 84.9%~121.2%,Statistics results turned out bio-equivalence between these two products.