Lidocaine Transdermal Patch: Pharmacokinetic Modeling and In Vitro-In Vivo Correlation (IVIVC).

Autor: Kondamudi PK; Centre of Excellence- Bio Studies, Hyderabad, Telangana, India.; Integrated Product Development Organisation, IPDO- Innovation Plaza, Dr. Reddy's Laboratories, Bachupally, R R District, Hyderabad, 500090, India., Tirumalasetty PP; Formulations R & D, Softgel, Topical, Transdermal and Respiratory (STaR) Vertical, Hyderabad, India.; Integrated Product Development Organisation, IPDO- Innovation Plaza, Dr. Reddy's Laboratories, Bachupally, R R District, Hyderabad, 500090, India., Malayandi R; Centre of Excellence- Bio Studies, Hyderabad, Telangana, India.; Integrated Product Development Organisation, IPDO- Innovation Plaza, Dr. Reddy's Laboratories, Bachupally, R R District, Hyderabad, 500090, India., Mutalik S; Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal, 576104, Karnataka, India., Pillai R; Softgel-Transdermal/Topical-Respiratory (STaR) Product Development, Dr.Reddy's Laboratories, Hyderabad, 500090, Andhra Pradesh, India. ravip@drreddys.com.; Integrated Product Development Organisation, IPDO- Innovation Plaza, Dr. Reddy's Laboratories, Bachupally, R R District, Hyderabad, 500090, India. ravip@drreddys.com.
Jazyk: angličtina
Zdroj: AAPS PharmSciTech [AAPS PharmSciTech] 2016 Jun; Vol. 17 (3), pp. 588-96. Date of Electronic Publication: 2015 Aug 18.
DOI: 10.1208/s12249-015-0390-1
Abstrakt: The present study aims to develop the correlation between in vitro and in vivo skin permeation of lidocaine in its transdermal patch. In order to minimize the run-to-run variability during in vitro skin permeation studies, release normalized cumulative percent (%Ct n) was calculated. A suitable polynomial mathematical model was used to establish a correlation between time and %Ct n. Percent in vivo absorbed was calculated by using numerical deconvolution (NDC) and non-compartmental analysis (NCA) methods. Pharmacokinetic (PK) parameters such as AUC last and C max were predicted with the established in vitro-in vivo correlation (IVIVC) models. The minimum prediction errors in NDC method for C max were found to be -30.9 and -25.4% for studies I (in vivo study in human volunteers with one batch of Lidoderm patch; internal validation) and II (in vivo study in human volunteers with another batch of Lidoderm patch; external validation), respectively, whereas minimum prediction errors in NCA method were relatively low (3.9 and 0.03% for studies I and II, respectively) compared to those in NDC method. The prediction errors for AUC last were found to be less than 2% for both methods and studies. The established method in this study could be a potential approach for predicting the bioavailability and/or bioequivalence for transdermal drug delivery systems.
Databáze: MEDLINE
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