• Journal of Pharmaceutical Investigation
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• 제27권3호
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• pp.207-212
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• 1997

The bioequivalence of two nabumetone tablets was evaluated in 16 normal male volunteers $(age\;21{\sim}30\;yrs)$ following oral administration. Test product was 'Nacton tablet' made by Jin Yang Pharmaceutical Co. and reference product was 'Unimeton tablet' made by Dong Kwang Pharmaceutical Co.. After one tablet containing 500 mg of nabumetone was administered, blood was taken at predetermined time intervals and the concentration of 6-methoxy-2-naphthylacetic acid, active metabolite of nabumetone, in plasma was determined with an HPLC method using fluorescence detector. 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 3.66%, 6.87% and 1.85%, respectively. The powers$(1-{\beta})$ for AUC, $C_{max}$ and $T_{max}$ were 91.4%, 88.9% and 81.1%, respectively. Detectable differences$({\Delta})$ and confidence intervals were all less than 20%. All of these parameters met the criteria of FDA for bioequivalence, indicating that "Nacton tablet" is bioequivalent to 'Unimeton tablet'.

• 한국임상약학회지
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• 제10권3호
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• pp.140-144
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• 2000

Reofecoxib는 용량 의존적으로 cyclo-oxygenase-2를 선택적으로 억제한다. 골관절염 환자를 대상으로 하여 이중맹검, 무작위, Western Ontario and McMasters Universi-ties Osteoarthritis Index를 이용하여 평가한 결과, rofecoxib 12.5, 25 mg는 신체적 기능을 크게 향상시키는 것으로 보여졌다. 또한 diclofenac (50 mg, 1일 3회), ibuprofen (800 mg, 1일 3회), nabumetone(1500 mg, 1일 1회)와 유사한 임상효과를 나타내었다. Rofecoxib는 원발성 월경곤란증과 수술 후 치통에 효과적으로 억제하였으며 naproxen sodium과 ibuprofen과 같은 진통 효과를 보였다. Rofecoxib는 안전성 면에서 우수하며 가장 흔한 부작용은 설사, 두통, 오심과 상기도 감염증이다. Rofecoxib 12.5, 25, 50 mg/day를 투여한 골관절염 환자에게서 위장관계 부작용(천공, 궤양, 출혈)은 ibuprofen, diclofenac, nabumetone을 투여한 환자보다 훨씬 낮은 발생빈도를 나타내었다.

• Archives of Pharmacal Research
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• 제18권5호
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• pp.340-345
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• 1995

A nebumetone tablet in development $(Navuton^R)$ was tested for its bioequivalence to the erference tablet $(Uniton^R)$. Seventeen healthy Korean male subjects participated in this study. Each subject received a 1-g dose of nabumetone (2tables each) in an unbalanced, randomized, two-way crossover investigation. Serum concentrations of 6-methoxy-2-na-phthylacetic acid (6-MNA), a major metabolite of nebumetone, were measured over 120 hr interval by a high-performance liquid chromatography. The maximum serum concentration $(C_{max})$ and time to reach the maximum concentration$(T_{max})$ were read directly, but area under the serum concentration time curve from time 0 to 120 hr (AUC) and mean residence time serum curves showed multiple peaks of 6-MNA in most subjects, and the $C_{max}$ and $T_{max}$ were read from the highest serum peaks. calculated bioavailability parameters for test and reference tablets were 148.6 : 1377.9 $\mug \cdot hr/ml$ for AUC; 25.2:23.1 $\mu/ml$ for $C_{max}$; 11.8:16.4 hr for $T_{max}$, and 42.6 : 43.8 hr for MRT, respectively. The paired t-test revealed no significant differences in all the parameters between the two tablets. Analysis ofl variance (ANOVA) revealed no significant differences between groups and formulations in all the parameters ($C_{max}$ and $T_{max}$, AUC and MRT) indicating the crossover design of the experiment was properly performed. But significant differences (p<0.05) between subject/groups and periods were found for all the parameters indicating substantial intersubject and interperiodic variations for these parameters.

• Biomolecules & Therapeutics
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• 제15권2호
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• pp.118-122
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• 2007

This study was performed to evaluate the bioequivalency between the Osmetone$^{TM}$ Tablet (Myeongmoon Pharm. Co., Ltd.) as a test formulation and the Relafen$^{TM}$ Tablet (Handok Pharm. Co., Ltd.) as a reference formulation. Twenty-four healthy male volunteers were administered the formulations by the randomized Latin square crossover design, and the plasma samples were determined by a high performance liquid chromatography (HPLC) with Ultra-Violet (UV) detector. AUC$_t$, C$_{max}$ and T$_{max}$ were obtained from the time-plasma concentration curves, and log-transformed AUC$_t$ and C$_{max}$ and log-untransformed T$_{max}$ values for two formulations were compared by statistical tests and analysis of variation. AUC$_t$ was determined to be 897.8${\pm}$431.1 ug.hr/ml for the reference formulation and 902.3${\pm}$408.4 ug.hr/ml for the test formulation. The mean values of C$_{max}$ for the reference and test formulations were 24.2${\pm}$8.9 and 24.0${\pm}$9.5 ug/ml, respectively. The AUC$_t$ and C$_{max}$ ratios of the reference Relafen$^{TM}$ Tablet to the test Osmetone$^{TM}$ Tablet were +5.01% and -0.83%, respectively, showing that the mean differences were satisfied the acceptance criteria within 20%. The results from analysis of variance for logtransformed AUC$_t$ and C$_{max}$ indicated that sequence effects between groups were not exerted and 90% confidence limits of the mean differences for AUC$_t$ and C$_{max}$ were located in ranges from log 0.80 to log 1.25, satisfying the acceptance criteria of the KFDA bioequivalence. The Osmetone$^{TM}$ Tablet as the test formulation was considered to be bioequivalant to the Relafen$^{TM}$ Tablet used as its reference formulation, based on AUC$_t$ and C$_{max}$ values.

• 한국약용작물학회지
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• 제6권3호
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• pp.204-209
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• 1998

오디의 기능성(機能性) 식품개발을 위한 기초연구(基礎硏究)의 일환으로 뽕나무 품종에 따라 9종의 오디를 채취(採取)하여 냉동건조(冷凍乾燥)한 후 각각에 대하여 항염증 및 항산화효과를 검색하였다. 그 결과를 요약하면 다음과 같다. 1. 비스테로이드성 항염증 작용을 검색하기 위하여 cyclooxygenase II의 활성억제도를 측정하였다. 그 결과 신광뽕 > 검설뽕 > 4배성 휘카스 > 2배성 휘카스 >검설뽕 등의 순으로 억제 효과를 나타냈다. 현재 항염증제의 표준물질로 사용되고 있는 nabumetone 10ppm에서 활성억제도(活性抑制度)를 1이라 했을 때, 가장 높은 억제 활성을 나타낸 신광뽕 오디의 경우는 0.55의 활성도를 나타냈다. 2. 최근에 천연물(天然物)로부터 항암작용과 더불어 소염작용을 갖는 물질을 탐색하기 위하여 phosphlipase $A_2$의 활성억제도법을 이용한다. 오디 9품종의 MeOH 추출물 $100{\mu}g/ml$의 농도에서 phospholipase에 대한 억제활성은 신광뽕 > 검설뽕 > 휘카스 > 북산2호의 순으로 억제작용을 나타냈다. 3. 항염증 작용과 항산화 작용은 연관성이 높기 때문에 DPPH법을 이용하여 radical scavengingrate를 측정했다. 그 결과 신광뽕 > 검설뽕 > 휘카스 > 청일뽕의 순으로 항산화작용을 나타냈다. 결론적으로 9종의 오디품종중 항염증제로의 이용가능성이 있는 것은 검설뽕, 휘카스 및 신광뽕이었고, 북산2호와 대도상의 항산화 항염증 효과는 전혀 없었다.

• The Korean Journal of Physiology and Pharmacology
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• 제20권4호
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• pp.379-385
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• 2016

TWIK-related $K^+$ channel-2 (TREK-2) and TWIK-related spinal cord $K^+$ (TRESK) channel are members of two-pore domain $K^+$ channel family. They are well expressed and help to set the resting membrane potential in sensory neurons. Modulation of TREK-2 and TRESK channels are involved in the pathogenesis of pain, and specific activators of TREK-2 and TRESK may be beneficial for the treatment of pain symptoms. However, the effect of commonly used analgesics on TREK-2 and TRESK channels are not known. Here, we investigated the effect of analgesics on TREK-2 and TRESK channels. The effects of analgesics were examined in HEK cells transfected with TREK-2 or TRESK. Amitriptyline, citalopram, escitalopram, and fluoxetine significantly inhibited TREK-2 and TRESK currents in HEK cells (p<0.05, n=10). Acetaminophen, ibuprofen, nabumetone, and bupropion inhibited TRESK, but had no effect on TREK-2. These results show that all analgesics tested in this study inhibit TRESK activity. Further study is needed to identify the mechanisms by which the analgesics modulate TREK-2 and TRESK differently.