• Korean Journal of Clinical Pharmacy
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• v.10 no.2
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• pp.62-67
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• 2000

Terbinafine has a primary fungicidal action mediated by squalene epoxidase inhibition. Treated fungi accumulate squalene while becoming deficient in ergosterol, an essential component of fungal cell membranes. Bioequivalence of two terbinafine tablets, $Lamisil^{TM}$ (Novartis Korea Ltd., Seoul, Korea) and $Mycosil^{TM}$ (Daewon Pharmaceutical Co., Ltd., Seoul, Korea), was evaluated according to the guidelines of Korea Food and Drug Administration (KFDA). Sixteen normal male volunteers ($20\sim29$ years old) were randomly divided into two groups and a randomized $2\times2$ cross-over study was employed. After oral administration of $Mycosil^{TM}\;or\;Lamisil^{TM}$ (125 mg terbinafine), blood samples were taken at predetermined time intervals and the serum terbinafine concentrations were determined using an HPLC method with UV/VIS detector. The pharmacokinetic parameters $(AUC_t,\;C_{max}\;and\;T_{max})$ were calculated and ANOVA was utilized for the statistical analysis. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two tablets based on the $Lamisil^{TM}$ tablet were $-2.24\%,\;-7.68\%\;and\;2.92\%$, respectively. The powers %(1-\beta)\;for\;AVC_t,\;C_{max}\;and\;T_{max}\;were\;87.11\%,\;95.36\%\;and\;99.99\%$, respectively. Minimum detectable differences $(\Delta)\;and\;90\%$ confidence intervals were all less than $\pm20\%$. All these parameters met the criteria of KFDA for bioequivalence, indicating that $Mycosil^{TM}$ tablet is bioequivalent to $Lamisil^{TM}$ tablet.

• Journal of Pharmaceutical Investigation
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• v.30 no.2
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• pp.133-138
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• 2000

Terbinafine is an orally active antifungal agent as it inhibits the fungal enzyme squalene epoxidase, which is important in the early biosynthetic pathway of ergosterol. This leads to abnormal development of the fungal cell membrane. Bioequivalence of two terbinafine tablets, $Lamisil^{TM}$ (Novartis Korea Ltd.) and $Terbina^{TM}$ (Korean Drug Co., Ltd.), was evaluated according to the guidelines of Korea Food and Drug Administration (KFDA). Sixteen normal male volunteers, $23.56{\pm}1.75$ years old and $65.60{\pm}8.54\;kg$ of body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one tablet containing 125 mg of terbinafine was orally administered, blood was taken at predetermined time intervals and the serum concentrations of terbinafine were determined using an HPLC method with UV detector. The pharmacokinetic parameters $(AUC_t,\;C_{max}\;and\;T_{max})$ were calculated and ANOVA test was utilized for the statistical analysis of parameters. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two tablets based on $Lamisil^{TM}$, tablet were -2.53%, -2.98% and 8.13%, respectively. The powers $(1-{\beta})$ for $AUC_t,\;C_{max}\;and\;T_{max}$ were 85.21%, 98.21% and 93.11%, respectively. Minimum detectable differences $({\Delta})$ at ${\alpha}=0.1\;and\;1-{\beta}=0.8$ were all less than 20%. The 90% confidence intervals were all within ${\pm}20%$. All the parameters above met the criteria of KFDA for bioequivalence, indicating that $Terbina^{TM}$ tablet is bioequivalent to $Lamisil^{TM}$ tablet.