Cetirizine Hydrochloride Microemulsion Preparation And Evaluation Of In Vivo And In Vitro

Objective:In the preparation of cetirizine hydrochloride microemulsion, which is used in localized skin sensitivity treatment, the optimum mixture ratio of surfactant, co-surfactant, oil phase and stabilizers is to be determined along with investigation on various properties including stability and transdermal absorption and so on.Methods:1. Preparation and quality evaluation of cetirizine hydrochloride microemulsion. The optimum composition of blank prescriptions was determined through orthogonal experimental design and ternary phase diagram analysis; the properties of prepared microemulsion for blank prescriptions, such as, appearance, viscosity, diameter and stability, are characterized and investigated.2. Quantification of cetirizine hydrochloride based on HPLC is performed, for which, the reproducibility precision and recovery coefficient are well discussed. The drug content in the prepared cetirizine hydrochloride microemulsion is analyzed.3. Evaluation of the diffusion behaviour of the prepared cetirizine hydrochloride microemulsion. The transdermal absorption of cetirizine hydrochloride microemulsion is measured by HPLC, and the transdermal absorption of the prepared cetirizine hydrochloride microemulsion on rats is characterized.Results:1. Taking the diameter and water-containing capacity as optimization objective, the optimum formulation for preparation of cetirizine hydrochloride microemulsion is, lecithin:1-batanol:oleic acid:water= 13:12:1:16. The prepared microemulsion is yellow pellucid liquid of nice mobility; the PH value is 6-7; the average diameter is(23.22±2.16)nm; the centrifugal creaming stability, long term stability and thermal stability are nice.。2. A linear regression model for cetirizine hydrochloride concentration of the standard solution, denoted by X in, and its HPLC peak, denoted by Y, is obtained: Y=0.0669X-0.0037, r=0.9996, where the linear range is X=0.16-0.78μg/mL. The reproductive experiments show that the peak area RSD is 0.42%, the daily RSD and inter-day RSD are less than 2%, and recover coefficient is 0.78%. The cetirizinehydrochloride content of the prepared microemulsion is measured to be in the range of 95-105%as expected.3. The transdermal absorption of cedrizine hydrochloride microemulsion on rat is characterized by HPLC. The linear regression model tells hat Y=0.08456X+0.00088, r=0.9986, with the linear range as X=0.035-0.620μg/mL. The experiments show that daily RSD is less than 6.9%, the inter-day RSD is less than 8.1%, the recovery coefficient RSD is 2.3%-9.7%and the stability experiment’s RSD is 2.3%-9.7%. Compared with other normal formulations, the cetirizine hydrochloride microemulsion showed big improvement in absorption rate and amount.Conclusions:The cetirizine hydrochloride microemulsion prepared based on the optimum formulation showed good physical and chemical stability, excellent diffusion behavior, and good transdermal absorption.