Lidocaine Transdermal Patch

Pharmacokinetic Modeling and In Vitro–In Vivo Correlation (IVIVC)

Phani Krishna Kondamudi, Phani Prasanth Tirumalasetty, Rajkumar Malayandi, Srinivas Mutalik, Raviraj Pillai

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

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 (%Ctn) was calculated. A suitable polynomial mathematical model was used to establish a correlation between time and %Ctn. Percent in vivo absorbed was calculated by using numerical deconvolution (NDC) and non-compartmental analysis (NCA) methods. Pharmacokinetic (PK) parameters such as AUClast and Cmax were predicted with the established in vitro–in vivo correlation (IVIVC) models. The minimum prediction errors in NDC method for Cmax 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 AUClast 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.

Original languageEnglish
Pages (from-to)588-596
Number of pages9
JournalAAPS PharmSciTech
Volume17
Issue number3
DOIs
Publication statusPublished - 2016

Fingerprint

Transdermal Patch
lidocaine
Lidocaine
pharmacokinetics
Pharmacokinetics
in vivo studies
skin (animal)
volunteers
prediction
Volunteers
methodology
drug delivery systems
Therapeutic Equivalency
Skin
Statistical Models
Drug Delivery Systems
Biological Availability
bioavailability
Theoretical Models
mathematical models

All Science Journal Classification (ASJC) codes

  • Agronomy and Crop Science
  • Pharmaceutical Science
  • Drug Discovery

Cite this

Kondamudi, Phani Krishna ; Tirumalasetty, Phani Prasanth ; Malayandi, Rajkumar ; Mutalik, Srinivas ; Pillai, Raviraj. / Lidocaine Transdermal Patch : Pharmacokinetic Modeling and In Vitro–In Vivo Correlation (IVIVC). In: AAPS PharmSciTech. 2016 ; Vol. 17, No. 3. pp. 588-596.
@article{3ad37b0b9d524a1dbd8773b1d10e71ff,
title = "Lidocaine Transdermal Patch: Pharmacokinetic Modeling and In Vitro–In Vivo Correlation (IVIVC)",
abstract = "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 ({\%}Ctn) was calculated. A suitable polynomial mathematical model was used to establish a correlation between time and {\%}Ctn. Percent in vivo absorbed was calculated by using numerical deconvolution (NDC) and non-compartmental analysis (NCA) methods. Pharmacokinetic (PK) parameters such as AUClast and Cmax were predicted with the established in vitro–in vivo correlation (IVIVC) models. The minimum prediction errors in NDC method for Cmax 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 AUClast 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.",
author = "Kondamudi, {Phani Krishna} and Tirumalasetty, {Phani Prasanth} and Rajkumar Malayandi and Srinivas Mutalik and Raviraj Pillai",
year = "2016",
doi = "10.1208/s12249-015-0390-1",
language = "English",
volume = "17",
pages = "588--596",
journal = "AAPS PharmSciTech",
issn = "1530-9932",
publisher = "American Association of Pharmaceutical Scientists",
number = "3",

}

Lidocaine Transdermal Patch : Pharmacokinetic Modeling and In Vitro–In Vivo Correlation (IVIVC). / Kondamudi, Phani Krishna; Tirumalasetty, Phani Prasanth; Malayandi, Rajkumar; Mutalik, Srinivas; Pillai, Raviraj.

In: AAPS PharmSciTech, Vol. 17, No. 3, 2016, p. 588-596.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Lidocaine Transdermal Patch

T2 - Pharmacokinetic Modeling and In Vitro–In Vivo Correlation (IVIVC)

AU - Kondamudi, Phani Krishna

AU - Tirumalasetty, Phani Prasanth

AU - Malayandi, Rajkumar

AU - Mutalik, Srinivas

AU - Pillai, Raviraj

PY - 2016

Y1 - 2016

N2 - 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 (%Ctn) was calculated. A suitable polynomial mathematical model was used to establish a correlation between time and %Ctn. Percent in vivo absorbed was calculated by using numerical deconvolution (NDC) and non-compartmental analysis (NCA) methods. Pharmacokinetic (PK) parameters such as AUClast and Cmax were predicted with the established in vitro–in vivo correlation (IVIVC) models. The minimum prediction errors in NDC method for Cmax 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 AUClast 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.

AB - 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 (%Ctn) was calculated. A suitable polynomial mathematical model was used to establish a correlation between time and %Ctn. Percent in vivo absorbed was calculated by using numerical deconvolution (NDC) and non-compartmental analysis (NCA) methods. Pharmacokinetic (PK) parameters such as AUClast and Cmax were predicted with the established in vitro–in vivo correlation (IVIVC) models. The minimum prediction errors in NDC method for Cmax 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 AUClast 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.

UR - http://www.scopus.com/inward/record.url?scp=84939445378&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84939445378&partnerID=8YFLogxK

U2 - 10.1208/s12249-015-0390-1

DO - 10.1208/s12249-015-0390-1

M3 - Article

VL - 17

SP - 588

EP - 596

JO - AAPS PharmSciTech

JF - AAPS PharmSciTech

SN - 1530-9932

IS - 3

ER -