Formulation and in vitro/in vivo correlation of a drug‐in‐adhesive transdermal patch containing azasetron

Sun, Lixin; Cun, Dongmei; Yuan, Bo; Cui, Hongxia; Xi, Honglei; Mu, Liwei; Chen, Yang; Liu, Chao; Wang, Zhongyan; Fang, Liang

doi:10.1002/jps.23317

Cited by 49 publications

(29 citation statements)

References 20 publications

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“…Blood samples of 7 mL were collected periodically at −1, 0, 1.5, 3,4,6,8,9,10,11,12,13,14,15,16,20,24,30, and 36 h of post-patch-application, and plasma drug concentrations were determined by a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. General adhesion of the patches was analyzed at 2, 4, 6, 8, 10, and 12 h after application.…”

Section: Studies I and Iimentioning

confidence: 99%

“…Traditionally, these methods are used as quality control tools. To date, very few attempts have been made to develop biorelevant IVRT methods and to establish in vitro-in vivo correlation (IVIVC) for transdermal patches (11)(12)(13)(14)(15). The traditional IVIVC methods using PK model and numerical deconvolution (NDC) method have their own limitations such as requirement of intravenous (IV) data, unit impulse response (UIR) values, and errors associated with model building (16).…”

Section: Introductionmentioning

confidence: 99%

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

et al. 2015

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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 (%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.

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Section: Studies I and Iimentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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

et al. 2015

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“…The predicted in vitro skin permeation profiles of FEL-TEA transdermal patches in rabbits were obtained using the following formula as described in a previous study [18].…”

Section: In Vitro/in Vivo Correlationmentioning

confidence: 99%

“…For transdermal delivery, the in vitro property refers to the rate of skin permeation, and the in vivo performance is the drug concentration in plasma. In previous reports, IVIVC has been established for s o m e d r u g s i n t o p i c a l p r e p a r a t i o n s , a n d t h e deconvolution method showed a good prediction performance [18,42,43].…”

Section: Pharmacokinetic Analysismentioning

confidence: 99%

Design and Evaluation of a Novel Felbinac Transdermal Patch: Combining Ion-Pair and Chemical Enhancer Strategy

Liu

Song

et al. 2015

AAPS PharmSciTech

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Abstract. The aim of this study was to design a novel felbinac (FEL) patch with significantly higher (P<0.05) skin permeation amount than the commercial product SELTOUCH® using ion-pair and chemical enhancer strategy, overcoming the disadvantage of the large application area of SELTOUCH®. Six complexes of FEL with organic amines diethylamine (DEA), triethylamine (TEA), N-(2′-hydroxyethanol)-piperdine (HEPP), monoethanolamine (MEtA), diethanolamine (DEtA), and triethanolamine (TEtA) were prepared by ion-pair interaction, and their formation were confirmed by differential scanning calorimetry (DSC), powder X-ray diffraction (pXRD), infared spectroscopy (IR), and proton nuclear magnetic resonance spectroscopy ( 1 H-NMR). Subsequently, the effect of ion-pair complexes and chemical enhancers were investigated through in vitro and in vivo experiments using rabbit abdominal skin. Results showed that FEL-TEA was the most potential candidate both in isopropyl palmitate (IPP) solution and transdermal patches. Combining use of 10% N-dodecylazepan-2-one (Azone), the optimized FEL-TEA patch achieved a flux of 18.29±2.59 μg/cm 2 /h, which was twice the amount of the product SELTOUCH® (J=9.18±1.26 μg/cm 2 /h). Similarly, the area under the concentration curve from time 0 to time t (AUC 0-t ) in FEL-TEA patch group (15.94±3.58 h.μg/mL) was also twice as that in SELTOUCH® group (7.31±1.16 h.μg/mL). Furthermore, the in vitro skin permeation results of FEL-TEA patch was found to have a good correlation with the in vivo absorption results in rabbit. These findings indicated that a combination of ion-pair and chemical enhancer strategy could be useful in developing a novel transdermal patch of FEL.KEY WORDS: chemical enhancer; felbinac-triethylamine (FEL-TEA); in vitro/in vivo correlation (IVIVC); ion-pair; transdermal patch.

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“…DP patches and rabbit abdominal skin were prepared as described in a previous study (5). In vitro permeation experiments were performed using a two-chamber side-byside glass diffusion cell in accordance with the method of Sun et al (5), except that pH 7.4 phosphate buffer solution (PBS) and PEG400 in ratio of 5:1 were used as the receptor solution. Two-milliliter samples were taken at pre-determined time intervals from receptor compartment for analysis and replaced with the same volume of fresh medium to maintain sink conditions.…”

Section: In Vitro Permeation Experimentsmentioning

confidence: 99%

Effect of Backing Films on the Transdermal Delivery of Donepezil from Patches

et al. 2014

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Abstract. The aim of this work was to investigate the effect of backing films on transdermal delivery of donepezil (DP) from patches. Three backing films, Cotran TM 9700, Cotran TM 9701, and Cotran TM 9726 were chosen as backing layers to prepare transdermal patches containing DP. The transdermal penetration and release amount of DP from each patch were evaluated by rabbit abdominal skin in vitro. The partitioning experiments and attentuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy were performed to confirm the existence of interaction between backing films and DP. Results showed that the cumulative release amount of DP from patches with different backing films had the same order of cumulative amount penetrated, i.e. Cotran TM 9701

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Formulation and in vitro/in vivo correlation of a drug‐in‐adhesive transdermal patch containing azasetron

Cited by 49 publications

References 20 publications

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

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

Design and Evaluation of a Novel Felbinac Transdermal Patch: Combining Ion-Pair and Chemical Enhancer Strategy

Effect of Backing Films on the Transdermal Delivery of Donepezil from Patches

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