PubMed:23293945 JSONTXT

{"project":"Allie","denotations":[{"id":"SS1_23293945_7_0","span":{"begin":858,"end":896},"obj":"expanded"},{"id":"SS2_23293945_7_0","span":{"begin":898,"end":902},"obj":"abbr"},{"id":"SS1_23293945_7_1","span":{"begin":1008,"end":1023},"obj":"expanded"},{"id":"SS2_23293945_7_1","span":{"begin":1025,"end":1027},"obj":"abbr"}],"relations":[{"id":"AE1_23293945_7_0","pred":"abbreviatedTo","subj":"SS1_23293945_7_0","obj":"SS2_23293945_7_0"},{"id":"AE1_23293945_7_1","pred":"abbreviatedTo","subj":"SS1_23293945_7_1","obj":"SS2_23293945_7_1"}],"text":"Benzathine penicillin G: a model for long-term pharmacokinetic comparison of parenteral long-acting formulations.\nWHAT IS KNOWN AND OBJECTIVE:   Long-acting intramuscular penicillin G injection is an important product for the management of some severe infections. However, testing the bioequivalence of such long-acting formulations is difficult. Our aim was to undertake such a test using a generic formulation containing 1 200 000 IU of benzathine penicillin G powder and an innovator's product (Retarpen(®) 1·2 million units; Sandoz, Switzerland).\nMETHODS:   In an open, double-blind, randomized, two-periods, two-group crossover study, 12 healthy male volunteers received both formulations of benzathine penicillin G on two different days with a 5-month washout period between the doses and a sampling period of over 500 h. A simple, sensitive and rapid high-performance liquid chromatography (HPLC)-UV method was developed and validated for determination of penicillin G plasma concentrations and other pharmacokinetic (PK) parameters.\nRESULTS AND DISCUSSION:   The analytical method used produced linear responses within a wide analyte concentration range with average within-run and between-run variations of below 15% with acceptable recovery, accuracy and sensitivity. The primary PK parameters we used were maximum plasma concentration (Cmax ), time to reach the maximal concentration (Tmax ) and the area under the plasma concentration vs. time curve from time zero to the last sampling time (AUC0→t ) using a standard non-compartmental approach. Based on these parameters, the two formulations were bioequivalent.\nWHAT IS NEW AND CONCLUSION:   We illustrate the bioequivalence testing of a very long-acting product. The data indicate that the generic test formulation and the branded reference formulation were bioequivalent in fasting healthy Iranian male volunteers."}