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In vitro-in vivo correlation study for the dermatopharmacokinetics of terbinafine hydrochloride topical cream.
Drug Dev Ind Pharm. 2013 Sep; 39(9):1372-7.DD

Abstract

BACKGROUND

To investigate the relationship between dermatopharmacokinetic (DPK) tape stripping from in vitro and in vivo using 1% terbinafine hydrochloride topical cream as the model formulation.

METHODOLOGY

In vitro and in vivo tape strippings were conducted on separated pig ear skin used as a biological membrane for franz diffusion cell testing and the non-hairy skin area at the ventral forearms of healthy volunteers, respectively. Terbinafine (1%) topical cream was applied to the skin for 0.5, 2, and 4 h. The drug profiles of terbinafine across the stratum corneum were determined immediately (time 0 h), and at 0.5, 1, 2, and 4 h after removing the formulation. The amounts of terbinafine were analyzed by a validated high-performance liquid chromatography-ultraviolet method. The area under the curve (AUC) and the maximum amounts of terbinafine absorption (Q(max)) were obtained from pharmacokinetic software. Partition coefficient (K(SC/veh)) and diffusion parameter (D/L²) were derived from the Fick's second law equation. During the schedule time of 8 h, the deviations of in vitro and in vivo data were 6.61 and 30.46% for AUC and Q(max), respectively. There was insignificant difference of the K(SC/veh) and the D/L² between excised pig ear and human skin. In addition, K(SC/veh) and D/L² at T(max) of 2 h were used to predict the AUC presented the value of 4.7481 %h whereas the true value calculated from pharmacokinetic software provided the value of 5.9311 %h differing from each other in approximate of 20%.

CONCLUSIONS

In vitro tape stripping using the separated pig ear skin as a viable membrane of the franz diffusion cell testing demonstrates the potential to represent in vivo tape stripping in human for topical bioavailability/bioequivalence study of terbinafine hydrochloride 1% topical cream.

Authors+Show Affiliations

Department of Pharmacy, Mahidol University, Bangkok, Thailand. pyksk2001@yahoo.com.sgNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23057672

Citation

Saeheng, Suwadee, et al. "In Vitro-in Vivo Correlation Study for the Dermatopharmacokinetics of Terbinafine Hydrochloride Topical Cream." Drug Development and Industrial Pharmacy, vol. 39, no. 9, 2013, pp. 1372-7.
Saeheng S, Nosoongnoen W, Varothai S, et al. In vitro-in vivo correlation study for the dermatopharmacokinetics of terbinafine hydrochloride topical cream. Drug Dev Ind Pharm. 2013;39(9):1372-7.
Saeheng, S., Nosoongnoen, W., Varothai, S., & Sathirakul, K. (2013). In vitro-in vivo correlation study for the dermatopharmacokinetics of terbinafine hydrochloride topical cream. Drug Development and Industrial Pharmacy, 39(9), 1372-7. https://doi.org/10.3109/03639045.2012.718786
Saeheng S, et al. In Vitro-in Vivo Correlation Study for the Dermatopharmacokinetics of Terbinafine Hydrochloride Topical Cream. Drug Dev Ind Pharm. 2013;39(9):1372-7. PubMed PMID: 23057672.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vitro-in vivo correlation study for the dermatopharmacokinetics of terbinafine hydrochloride topical cream. AU - Saeheng,Suwadee, AU - Nosoongnoen,Wichit, AU - Varothai,Supenya, AU - Sathirakul,Korbtham, Y1 - 2012/10/12/ PY - 2012/10/13/entrez PY - 2012/10/13/pubmed PY - 2013/12/16/medline SP - 1372 EP - 7 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 39 IS - 9 N2 - BACKGROUND: To investigate the relationship between dermatopharmacokinetic (DPK) tape stripping from in vitro and in vivo using 1% terbinafine hydrochloride topical cream as the model formulation. METHODOLOGY: In vitro and in vivo tape strippings were conducted on separated pig ear skin used as a biological membrane for franz diffusion cell testing and the non-hairy skin area at the ventral forearms of healthy volunteers, respectively. Terbinafine (1%) topical cream was applied to the skin for 0.5, 2, and 4 h. The drug profiles of terbinafine across the stratum corneum were determined immediately (time 0 h), and at 0.5, 1, 2, and 4 h after removing the formulation. The amounts of terbinafine were analyzed by a validated high-performance liquid chromatography-ultraviolet method. The area under the curve (AUC) and the maximum amounts of terbinafine absorption (Q(max)) were obtained from pharmacokinetic software. Partition coefficient (K(SC/veh)) and diffusion parameter (D/L²) were derived from the Fick's second law equation. During the schedule time of 8 h, the deviations of in vitro and in vivo data were 6.61 and 30.46% for AUC and Q(max), respectively. There was insignificant difference of the K(SC/veh) and the D/L² between excised pig ear and human skin. In addition, K(SC/veh) and D/L² at T(max) of 2 h were used to predict the AUC presented the value of 4.7481 %h whereas the true value calculated from pharmacokinetic software provided the value of 5.9311 %h differing from each other in approximate of 20%. CONCLUSIONS: In vitro tape stripping using the separated pig ear skin as a viable membrane of the franz diffusion cell testing demonstrates the potential to represent in vivo tape stripping in human for topical bioavailability/bioequivalence study of terbinafine hydrochloride 1% topical cream. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/23057672/In_vitro_in_vivo_correlation_study_for_the_dermatopharmacokinetics_of_terbinafine_hydrochloride_topical_cream_ L2 - https://www.tandfonline.com/doi/full/10.3109/03639045.2012.718786 DB - PRIME DP - Unbound Medicine ER -