• Journal of Pharmaceutical Investigation
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• 제41권2호
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• pp.117-123
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• 2011

Loxoprofen sodium, a 2-phenylpropionate non-steroidal anti-inflammatory drug (NSAID), has marked analgesic and antipyretic activities and relatively weak gastrointestinal ulcerogenicity. The purpose of the present study was to evaluate the bioequivalence of two loxoprofen sodium tablets, Hana loxoprofen sodium tablet (Hana Pharm. Co., Ltd.) and Dongwha Loxonin$^{(R)}$ tablet (Dongwha Pharm. Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The in vitro release of loxoprofen from the two loxoprofen sodium formulations was tested using KP IX Apparatus II method with various dissolution media. Twenty four healthy Korean male volunteers, $22.83{\pm}1.862$ years in age and $69.92{\pm}9.14$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ crossover study was employed. After a single tablet containing 60 mg as loxoprofen sodium was orally administered, blood samples were taken at predetermined time intervals and the concentrations of loxoprofen in serum were determined using a online column-switching HPLC method with UV/Vis detection. The dissolution profiles of two formulations were similar in all tested dissolution media. The pharmacokinetic parameters such as $AUC^t$, $C_{max}$ and $T_{max}$ were calculated, and computer programs (Equiv Test and K-BE Test 2002) were utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and un-transformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, Dongwha Loxonin$^{(R)}$ tablet, were 2.03, 2.99 and -9.49% for $AUC_t$, $C_{max}$, and $T_{max}$, 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 log0.8 to log1.25 (e.g., log0.9831~log1.0535 and log0.9455~log1.1386 for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Hana loxoprofen sodium tablet was bioequivalent to Dongwha Loxonin$^{(R)}$ tablet.

• 대한정형외과학회지
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• 제54권2호
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• pp.120-126
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• 2019

목적: 내측 개방 근위 경골 절골술 후 통증 조절에서 관절 주위 다중 약물 국소 주사와 내전근관 차단술의 효과를 비교하고자 하였다. 대상 및 방법: 2016년 11월부터 2017년 3월까지 개방형 내측 근위 경골 절골술을 시행한 환자 60명을 대상으로 하여 후향적으로 분석하였다. 전 예에서 척추 마취를 시행하였으며, 수술 직전 선제 약물 투여 후 정맥내 자가 통증 조절 장치를 시행하였다. 30명의 환자(I군)는 관절 주위 다중 약물 국소 주사를 맞았고, 다른 30명의 환자(II군)는 내전근관 차단술을 시행 받았다. 두 그룹에 대해 수술 후 통증 수준, 추가적인 tramadol hydrochloride 주사의 빈도, 자가 통증 조절 장치 사용 총량 및 버튼을 누른 횟수 등을 비교하였다. 결과: 수술 후 2주째까지 시각통증점수(visual analogue scale)는 두 군 간에 유의한 차이를 보이지 않았다. 추가 tramadol hydrochloride 주사의 빈도는 두 군 간에 유의한 차이가 없었다. 자가 통증 조절 장치 버튼을 누르는 횟수와 평균 총 fentanyl 소비량에서도 그룹 간에 유의한 차이가 없었다. 결론: 내측 개방적 근위 경골 절골술을 시행한 환자의 급성기 통증 조절에 있어서 관절 주위 다중 약물 주입 및 내전근관 신경 차단술은 비슷한 효과를 가지는 것으로 생각된다.

• Archives of Pharmacal Research
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• 제19권4호
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• pp.297-301
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• 1996

Plasma profile of niflumic acid following oral administration of talniflumate tablets (Somalgen) was compared to that of niflumic acid tablets in man. Plasma niflumic acid was assayed by HPLC method. Plasma niflumic acid profile from the tainiflumate tablets was similar to that from the niflumic acid tablets resulting in no differences in $AUC, C_max, t_max$ and MRT. It demonstrates that talniflumate is a prodrug of niflumic acid, and undergoes extensive first-pass biotransformation to niflumic acid. However, plasma niflumic acid concentration at 30 min after tainiflumate dosing was significantly (p<0.05) higher than that of niflumic acid dosing. The more potent analgesic activity of talniflumate than niflumic acid might be related to this higher plasma drug concentration at the earlier phase. Considering that tainiflumate is less irritant to gastrointestinal mucosa than niflumic acid, talniflumate seems to be advantageous over niflumic acid in terms of activity and side effects.

• Archives of Pharmacal Research
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• 제26권7호
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• pp.540-544
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• 2003

Morphine, an analgesic with significant abuse potential, is considered addictive because of drug craving and psychological dependence. It is reported that repeated treatment of morphine can produce conditioned place preference (CPP) showing a reinforcing effect in mice. CPP is a useful method for the screening of morphine-induced psychological dependence. In the present study, we investigated the effect of the methanolic extract of Coptis japonica (MCJ) on morphine-induced CPP in mice. Furthermore, we examined c-fos expression in the parietal cortex, piriform cortex, striatum, nucleus accumbens, and hippocampus of the morphine-induced CPP mouse brain. Treatment of MCJ 100 mg/kg inhibited morphine-induced CPP. Expression of c-fos was increased in the cortex, striatum, nucleus accumbens, and hippocampus of the morphine-induced CPP mouse brain. These increases of expression were inhibited by treatment with MCJ 100 mg/kg, compared to the morphine control group. Taken together, these results suggest that MCJ inhibits morphine-induced CPP through the regulation of c-fos expression in the mouse brain.

• Archives of Pharmacal Research
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• 제20권5호
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• pp.414-419
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• 1997

Gastrointestinal irritation is the most frequent adverse effect in patients chronically taking nonsteroidal antiinflammatory drugs (NSAIDs) for the treatment of arthritic conditions. Gastroprotective effect of DA-9601, a new antiulcer agent from Artemisiae Herba extract, against NSAID was evaluated in a rat model of arthritis that is similar in many aspects to human rheumatoid arthritis. Daily oral dosing of naproxen (30 mg/kg), one of the most commonly used NSAID, induced apparent gastric lesions as well as a significant decrease in mucosal prostagiandin $E_2;(PGE_2)$ and prostagiandin F_${1{\alpha}}$$(PGF_{1{\alpha}})$ levels. Coadministration of DA-9601 prevents naproxen-induced mucosal injury and depletion of prostaglandins, in a dose-related manner. DA-9601 did not alter the antiinflammatory or analgesic effect of naproxen. The present results suggest that DA-9601 may be useful as a mucoprotectant against NSAIDs in clinical practice.

• Biomolecules & Therapeutics
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• 제16권2호
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• pp.113-117
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• 2008

Morphine is a potent analgesic with significant abuse potential, because of drug craving and psychological dependence. It is reported that repeated treatment of morphine can produce conditioned place preference (CPP) showing a reinforcing effect in mice. Previously, we have reported the inhibitory effect of the methanolic extract of Coptis japonica (MCJ) on morphine-induced CPP in mice. The present study was employed whether p-CREB expression is involved in the inhibitory effect of MCJ on the morphine-induced CPP in the mouse hippocampus. Repeated administration of MCJ 100 mg/kg inhibited morphine-induced CPP. Expression of p-CREB was increased in the dentate gyrus of the hippocampus that had undergone morphineinduced CPP. This increase of expression was significantly inhibited by administration of MCJ 100 mg/kg, compared to the morphine control group. Taken together, these results suggest that MCJ inhibits morphine-induced CPP through the regulation of p-CREB expression in the mouse dentate gyrus of the hippocampus.

• Journal of Dental Anesthesia and Pain Medicine
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• 제15권1호
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• pp.1-4
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• 2015

In pediatric dentistry, chloral hydrate is habitually selected for sedation of uncooperative children. Although chloral hydrate has been used for decades, various adverse effects are reported and necessity for new alternative drugs has increased. Dexmedetomidine was approved by FDA for sedation at intensive care units (ICU) in 1999. Compared to conventional sedative drugs, dexmedetomidine has not only analgesic and sedative effects but also it barely suppresses the respiratory system. Due to these characteristics, dexmedetomidine is known as safe sedative drug for children and elderly patients. Furthermore, approved by KFDA in 2010 in Korea, the frequency of sedation using dexmedetomidine is increasing. However, due to its intravenous administration method, it was difficult to apply in pediatric dentistry. Recently, intranasal administration method was introduced which might be a new possible alternative of oral sedation. In this study, we compare the mechanisms, pros and cons of chloral hydrate and dexmedetomidine, introducing new possibilities.

• Journal of Korean Neurosurgical Society
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• 제56권5호
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• pp.448-450
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• 2014

Nefopam, a centrally acting analgesic, has been used to control postoperative pain. Reported adverse effects are anticholinergic, cardiovascular or neuropsychiatric. Neurologic adverse reactions to nefopam are confusion, hallucinations, delirium and convulsions. There are several reports about fatal convulsive seizures, presumably related to nefopam. A 71-year-old man was admitted for surgery for a lumbar spinal stenosis. He was administered intravenous analgesics : ketorolac, tramadol, orphenadrine citrate and nefopam HCl. His back pain was so severe that he hardly slept for several days; he even needed morphine and pethidine. At 4 days of administration of intravenous analgesics, the patient suddenly started generalized tonic-clonic seizures for 15 seconds, and subsequently, status epilepticus; these were not responsive to phenytoin and midazolam. After 3 days of barbiturate coma therapy the seizures were controlled. Convulsive seizures related to nefopam appear as focal, generalized, myoclonic types, or status epilepticus, and are not dose-related manifestations. In our case, the possibility of convulsions caused by other drugs or the misuse of drugs was considered. However, we first identified the introduced drugs and excluded the possibility of an accidental misuse of other drugs. Physicians should be aware of the possible occurrence of unpredictable and serious convulsions when using nefopam.

• Journal of Pharmaceutical Investigation
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• 제39권1호
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• pp.43-49
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• 2009

Aspirin or acetylsalicylic acid, a member of the salicylate family, is frequently used as an analgesic, antipyretic, anti-inflammatory and antiplatelet drug. Because aspirin is chemically unstable in water and heat for tablet formulation, additives including lubricants are used in preparing aspirin tablets, using a dry-granulation process. Aspirin tablets are produced by a number of manufacturers which usually use their own unique combination of additives during the manufacturing process. In this study, we employed an NMR based metabolomics technique to identify the manufacturers of various aspirin tablets. Aspirin tablets from six different companies were analyzed by 1H 400 MHz NMR. The acquired data was then integrated and processed by principal component analysis (PCA). Based on the NMR data, we were able to identify peaks corresponding to acetylsalicylic acid in all of the six samples, whereas different NMR patterns were found in the aromatic and aliphatic regions depending on the unique additive used. These observations led to the conclusion that the differences in the NMR patterns among the different aspirin tablets were due to the presence of additives.

• The Korean Journal of Pain
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• 제11권2호
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• pp.258-262
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• 1998

Background: In view of the safety and effectiveness of butorphanol as a postoperative analgesic, we designed to compare its activity and side effects with those of ketoprofen, when administered intramuscularly. Methods: Ninety four patients, scheduled for elective total abdominal hysterectomy, received either ketoprofen 100 mg (ketoprofen group) or butorphanol 2 mg (butorphanol group) intramuscularly after surgery. For the first six hours after injection of butorphanol or ketoprofen, the patients were asked to reevaluate the intensity of pain, using numeric rating scale (NRS) and pain score. If the pain score was above 2, supplemental ketoprofen was administered IM. Incidence of side effects were also checked. Results: Butorphanol group showed lower NRS and pain score for the first four hours compared to ketoprofen group, but the incidence of drowsiness was higher in butorphanol group. There were no significant difference in the incidence of other side effects such as nausea and dizziness. In both group, there were neither respiratory depression nor pruritus. Conclusions: Butorphanol gave better relief of postoperative pain compared to ketoprofen. Butorphanol might be a useful drug for postoperative analgesia after hysterectomy with minor side effects.