• Journal of Pharmaceutical Investigation
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• v.28 no.4
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• pp.289-294
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• 1998

Bioequivalence of two aceclofenac tablets, the $Airtal^{TM}$ (Daewoong Pharmaceutical Co., Ltd.) and the $Senital^{TM}$ (Hana Pharmaceutical Co., Ltd.), was evaluated according to the guideline of KFDA. Fourteen normal male volunteers (age $20{\sim}29$ years old) were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one tablet containing 100 mg of aceclofenac was orally administered, blood was taken at predetermined time intervals and the concentration of aceclofenac in plasma was determined with an HPLC method using UV detector. The pharmacokinetic parameters ($C_{max}$, $T_{max}$ and $AUC_t$) were calculated and ANOVA was utilized for the statistical analysis of parameters. The results showed that the differences in $C_{max}$, $T_{max}$ and $AUC_t$ between two tablets were 3.69%, 2.44% and 0.51%, respectively. The powers $(1-{\beta})$ for $C_{max}$, $T_{max}$ and $AUC_t$ were 87.85%, 98.70% and more than 99%, respectively. Detectable differences $({\Delta})$ and confidence intervals were all less than ${\pm}20%$. All of these parameters met the criteria of KFDA for bioequivalence, indicating that $Senital^{TM}$ tablet is bioequivalent to $Airtal^{TM}$ tablet.

• Korean Journal of Clinical Pharmacy
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• v.12 no.1
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• pp.22-28
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• 2002

Aceclofenac, 2-[(2',6'-dichlorphenyl)amino]phenylacetoxiacetic acid, is a new nonsteroidal anti-inflammatory drug that belongs to the family of phenylacetic acids. It shows good tolerance and potent analgesic/antiinflammatory properties, and acts on cartilaginous chondriocytes, stimulating their repair mechanism. The purpose of the present study was to evaluate the bioequivalence of two aceclofenac products, $Airtal^{TM}$ tablet (Daewoong Pharmaceutical Co.) and $Acer^{TM}$ capsule (Kyungdong Pharmaceutical Co.), according to the guideliner of Korea Food and Drug Administration (KFDA). The aceclofenac release from the two aceclofenac products in vitro was tested using KP VII Apparatus II method at pH 7.8 dissolution media. Sixteen normal male volunteers, $23.13\pm2.03$ years in age and $66.33\pm7.08$ kg in body weight, were divided into two groups and a randomized $2\times2$ cross-over study was employed. After one tablet or capsule containing 100 mg of aceclofenac was orally administered, blood was taken at predetermined time intervals and the concentrations of aceclofenac in serum were determined using HPLC with UV detector. The dissolution profiles of the two aceclofenac products were very similar at pH 7.8 dissolution media. The pharmacokinetic parameters such as $AUC_t,\;C_{max}\;and\;T_max$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two products were $6.50\%,\;-1.06\%\;and\;11.96\%$ respectively, when calculated against the $Airtal^{TM}$ tablet. The powers $(1-\beta)\;for\;AUC_t,\;C_{max}\;were\;89.82\%\;and\;82.84\%$, respectively. Minimum detectable differences $(\Delta)\;at\;\alpha=0.05\;and\;1-\beta=0.8$ were less than $20\%\;(e.g.,\;17.51\%\;and\;19.30\%\;for\;AUC_t,\;C_{max}$, ). The $90\%$ confidence intervals were within $\pm20\%\;(e.g.,\;-3.73\%\sim16.73\%\;and\;-12.34\%\sim10.22\%\;for\;AUC_t,\;C_{max},\;respectively)$. Two parameters met the criteria of KFDA for bioequivalence, indicating that $Acer^{TM}$ capsule is bioequivalent to $Airtal^{TM}$ tablet.

• Korean Journal of Clinical Pharmacy
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• v.9 no.1
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• pp.44-48
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• 1999

The bioequivalence of two aceclofenac tablets was evaluated in 14 normal volunteers (age $21\sim29$ yrs) following oral administration. The test product was 'Apental tablet' made by Asia Pharmaceutical Co. and the reference was 'Airtal tablet' made by Daewoong Pharmaceutical Co. After one tablet containing 100 mg aceclofenac was administered, blood was taken at predetermined time intervals and the concentration of the drug in plasma was quantitated with an HPLC method. AUC, $C_{max}\;and\;T_{max}$ were calculated and statistically analyzed for the bioequivalence of the two products. The results showed that the differences in AUC, $C_{max}\;and\;T_{max}$ between two products were $4.23\%,\;2.15\%\;and\;0\%$, respectively. The powers for AUC,$\;C_{max}\;and\;T_{max}\;were\;>90\%,\;>90\%\;and\;85.8\%$, respectively. Confidence intervals were within $\pm20\%$ for three parameters. All of these parameters met the criteria of KFDA for bioequivalence, indicating that 'Apental tablet' is bioequivalent to "Airtal tablet".(Kor. J. Clin. Pharm. 1999; 9(1): 44-48)

• Polymer(Korea)
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• v.33 no.6
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• pp.596-601
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• 2009

We prepared nanoparticles containing insoluble aceclofenac by the method of solid dispersions using spray dryer to improve solubility of aceclofenac. We used PVP-K30 as a water soluble carrier for the solid dispersion and poloxamer as a surfactant. Characterization of aceclofenac solid dispersion was performed by SEM, DSC, XRD and FT-IR. The results of SEM, DSC and XRD demonstrated that aceclofenac is amorphous in solid dispersion. The formation of salt by hydrogen bond between aceclofenac and PVP K-30 was confirmed by FT-IR. The dissolution rate measured in intestinal juice showed the method of solid dispersion improved aceclofenac solubility as compared with a conventional drug($Airtal^{(R)}$). In conclusion, the method of solid dispersion using spray dryer would improve solubility of aceclofenac in oral administration.

• Biomolecules & Therapeutics
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• v.6 no.4
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• pp.423-428
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• 1998

Aceclofenac is an orally effective non-steroidal anti-inflammatory agent of the phenylacetic acid derivative. Bioequivalence study of two aceclofenac preparations, the test drug (Senafe $n_{R}$: Daewon Phar-maceutical Company) and the reference drug (Airta $l_{R}$: Daewoong Pharmaceutical Company), was conducted according to the guidelines of Korea Food and Drug Administration (KFDA). Sixteen healthy male volunteers, 24$\pm$4 years old and 63.9$\pm$6.9 kg of body weight in average, were divided randomly into two groups and administered the drug orally at the dose of 100 mg as aceclofenac in a 2$\times$2 crossover study. Plasma concentrations of aceclofenac were monitored by HPLC method for 12 hr after administration. AU $Co_{-12h}$ (area under the plasma concentration-time curve from initial to 12 hr) was calculated by the linear trapezoidal method. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{msx}$) were compiled directly from the plasma drug concentration-time data. Student's t-test indicated no significant differences between the formulations in these parameters. Analysis of variance (ANOVA) revealed that there are no differences in AU $Co_{12h}$, $C_{max}$ and $T_{max}$ between the formulations. The apparent differences between the formulations were far less than 20% (e.g., 0.25, 0.01 and 7.32 for AU $Co_{-12h}$, $C_{max}$. and $T_{max}$, respectively). Minimum detectable differences (%) between the formulations at $\alpha$=0.05 and 1-$\beta$=0.8 were less than 20% (e.g., 14.65, 12.47 and 15.46 for AU $Co_{-l2h}$, $C_{max}$ and $T_{max}$, respectively). The 90% confidence intervals for these parameters were also within $\pm$ 20% (e.g.,-10.19~10.68, -8.87~8.89 and -3.69~ 18.33 for AU $Co_{-12h}$, $C_{msx}$ and $T_{max}$, respectively). These results satisfy the bioequivalence criteria of KFDA guidelines, indicating that two formulations of aceclofenac are bioequivalent.quivalent.ivalent.ent.t.ent.

• Journal of Pharmaceutical Investigation
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• v.34 no.1
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• pp.49-55
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• 2004

To develop a aceclofenac soft capsule, four preparations with various solubilizers were prepared and their dissolution test was carried out. Among four preparations tested, a preparation with ethanolamine was selected as a formula of aceclofenac soft capsule (Clanza $S^{TM}$), since it showed the fastεst dissolution rate. Bioequivalence of aceclofenac tablet, $Airtal^{TM}$ (Dae-Woong Pharmaceutical Co., Ltd.) and aceclofenac soft capsule, Clanza $S^{TM}$ (Korea United Pharmaceutical Co., Ltd.) was evaluated according to the guideline of KA Fourteen normal male volunteers (age 20 - 25 years old) were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After oral administration of one tablet or capsule containing 100 mg of aceclofenac, blood was taken at predetermined time intervals and the concentration of aceclofenac in plasma was determined with an HPLC method under UV detector The pharmacokinetic parameters ($C_{max}$ and $AUC_t$) were calculated and ANOVA was utilized for the statistical analysis of parameters using logarithmetically transformed $AUC_t$, $C_{max}$ and $T_{max}$. The results showed that the differences in $AUC_t$, $C_{max}$ and $T_{max}$ between Aral tablet and Clanza soft capsule were 2.89%, 0.18% and 43.0%, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(15) (e.g. log(0.81) -log(1.23) ad log(0.89) -log(1.4)) fo $AUC_t$ and $C_{max}$, respectively. Thus, the criteria of the KFDA guidelines for the equivalence was satisfied, indicating that Clanza $S^{TM}$ soft capsule is bioequivalent to$Airtal^{TM}$ tablet.

• Polymer(Korea)
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• v.39 no.1
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• pp.6-12
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• 2015

In order to improve the poor water solubility of aceclofenac, it was loaded into solid Kollidon VA 64 dispersion prepared by spray drying and rotary evaporation methods using different drug and polymer ratios. Morphology and physicochemical behavior of the aceclofenac loaded solid dispersions was analyzed by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), X-ray diffractometry (XRD), and differential scanning calorimetry (DSC). Encapsulation efficiency and dissolution behavior in a simulated intestinal juice of aceclofenac in the solid dispersions was measured using HPLC and the latter was compared with that of the active pharmaceutical ingredient (API) and Airtal$^{(R)}$. It was demonstrated that two methods could significantly improve the dissolution behavior of aceclofenac.