• 한국임상약학회지
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• 제1권1호
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• pp.9-14
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• 1991

Inclusion complexes of piroxicam with $\alpha,\;\beta\;and\;\gamma- cyclodextrins$ were prepared and suspended to enhance the bioavailability of piroxicam. A quantitative analysis was employed HPLC for the determination of piroxicam in the rabbit serum after a single oral dose in suspension of piroxicam and each of inclusion complexes of piroxicam with $\alpha,\;\beta\;and\;\gamma- cyclodextrins$, respectively. The bioavailability and serum level of piroxicam exhibited the highest in piroxicam clathrated $\beta-cyclodextrin$ than both piroxicam and the other complexes administered. and the total area under the curve of serum concentration versus time for their inclusion complexes were larger than that of piroxicam.

• Journal of Pharmaceutical Investigation
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• 제33권2호
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• pp.85-89
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• 2003

Piroxicam-arginine complex was prepared to improve the solubility and dissolution rate of poorly water-soluble piroxicam. Its formation was identified by infrared spectrophotometry, differential thermal analysis and dissolution rate. Piroxicam complex dispersible tablets, commercial $Feldene^{\circledR}$ dispersible tablets and piroxicam physical mixture hard capsules were prepared to compare dissolution rate in water. Dissolved amounts (%) after 15 mins of piroxicam complex dispersible tablets, commercial $Feldene^{\circledR}$ dispersible tablets and piroxicam physical mixture hard capsules were 98%, 48% and 10%, respectively. The solubility of complex in water was significantly higher than that of piroxicam itself. In vivo, pharmacokinetic parameters were obtained after oral administrations of piroxicam complex and physical mixture at a does of 2 mg to New Zealand White Rabbit. The $C_{max}$ of piroxicam complex was similar to that of piroxicam. However, there were much difference between the two formulations with regard to $T_{max}$ and AUC. The $T_{max}$ of piroxicam alone was 4 hours, but that of piroxicam complex was 0.8 hours. In addition, the AUC of piroxicam complex was 1.38 times greater than that of piroxicam alone.

• Biomolecules & Therapeutics
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• 제2권1호
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• pp.71-76
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• 1994

Anti-inflammatory and analgesic activities and skin irritation of piroxicam patch were investigated. Piroxicam patch increased the pain threshold in rat hind paw inflamed by carrageenan and inhibited writhing induced by acetic acid in mice. Piroxicam patch also inhibited the carrageenan-induced edema in rat hind paw as well as the increased vascular permeability induced by histamine in rats. In adjuvant arthritis of rats, piroxicam patch showed anti-inflammatory effects. Skin irritation of piroxicam patch was tested in Newzealand White rabbits and evaluated by Primary Irritation Index of Draize. The results from skin irritation test showed that piroxicam patch seemed practically non-irritating. The result from the present study indicates that piroxicam may be useful without serious side effects as anti-inflammatory analgesics in this patch form.

• 한국임상약학회지
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• 제8권2호
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• pp.95-100
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• 1998

Piroxicam-$\beta$-cyclodextrin은 piroxicam을 $\beta$-cyclodextrin으로 포접시킨 비스테로이드성 항염증약물이다. 이러한 포접형 약물은 위장관에서의 흡수속도가 증가하는 것으로 외국자료에서 보고되고 있으며 이는 이 약물의 위장관 내성에 보다 나은 영향을 끼칠 수 있음을 시사하고 있다. 본 연구는 정상성인 한국인을 대상으로 randomized, crossover design에 의해 piroxicam-$\beta-cyclodextrin(Brexin^{(R)})$과 piroxicam 확산정$(Feldene^{(R)})$ 흡수속도를 비교하고자 하였다. 건강한 성인 8명의 피험자를 2군으로 나누어 시험약 또는 대조약을 각각 20 mg씩 20일의 휴약 기간을 두고 이중 맹검으로 교차 투여하였다. 시험약 또는 대조약의 투여 후 24시간 동안 일정 간격으로 채혈하여 HPLC 방법으로 혈장 내 piroxicam 농도를 측정하였다. $AUC_{0-24}\;({\mu}g/mL)$는 piroxicam-$\beta$-cyclodextrin군에서 $56.1\pm4.9$, piroxicam군에서 $57.3\pm5.6$으로 통계적인 유의성이 없었으나, 투여 후 0.5시간에서의 혈중농도는 piroxicam-$\beta$-cyclodextrin군 $2.9\pm0.4\;{\mu}g/mL$, piroxicam군 $1.6\pm0.3\;{\mu}g/mL$으로 통계적인 유의성을 보였다(p<0.05). 또한 최고혈중농도는 piroxicam-$\beta$-cyclodextrin$(4.3\pm0.5\;{\mu} g/mL)\;piroxicam(3.5\pm0.3\l{\mu}g/mL)$,으로 유의성이 있었으며(p<0.05), 흡수 속도상수는 piroxicam-$\beta$-cyclodextrin$(3.00\pm0.49\;h^{-1}), \;piroxicam(1.80\pm0.21\;h^{-1})$이었다(p<0.1). 이상의 결과에서, piroxicam-$\beta$-cyclodextrin정은 piroxicam 확산정과 비교하여 흡수되는 정도는 서로 비슷하지만 흡수 초기의 혈장농도 및 흡수속도상수에서 보다 빠른 약동학적 특성을 나타내었다.

• Archives of Pharmacal Research
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• 제9권1호
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• pp.55-61
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• 1986

To increase the dissolution rate of piroxicam, chitin and chitosan which are widely occurring biodegradable natural materials were used as drug carriers. The ground mixtures of piroxicam with chitin or chitosan were prepared by grinding in a ball mill. The dissolution rates of piroxicam from the ground mixtures were enhanced markedly than that from the physical mixtures or from intact piroxicam. The X-ray diffraction peaks disappeared in the ground mixture indicating the production of the amorphous form. The comparison of infrared spectra of the physical mixture and the ground minture showed an interaction such as association between the functional groups of piroxicam and chitin or chitosan in the molecular level. The weight losses in TGA curves shoed all the same patterns. However, in the ground mixture by DTA curve, the undothermic peak due to the fusion of piroxicam was disappeared indicating the different thermal property.

• 약학회지
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• 제44권3호
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• pp.245-250
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• 2000

Because nonsteroidal anti-inflammatory drugs are reported to cause fluid retention and hypertension by inhibition of prostaglandin synthesis, the effects of piroxicam on pharmacodynamics and pharmacokinetics of nifedipine were studied in male spontaneously hypertensive rats. They received nifedipine (0.5 mg/kg) alone or combined with piroxicam (5 mg/kg) intravenously. Plasma levels norepinephrine, an index of sympathetic stimulation, were measured prior to each treatment and 5 min after drug administration. Changes in blood pressure were examined serially and blood samples for analysis of nifedipine were also taken for 6 hr following drug administration. Plasma nifedipine concentration were assayed by HPLC and pharmacokinetic parameters were calculated. Blood pressure was reduced (p<0.01), but plasma norepinephrine level was increased (p<0.05) by nifedipine administration. Anti-hypertensive effect of nifedipine was potentiated (p<0.05) by piroxicam coadministration, but effect of nifedipine on plasma norepinephrine level was not affected. In case of rats received nifedipine and piroxicam, plasma nifedipine concentrations were higher (p<0.05) than those from rats received nifedipine alone at 2,3,4,5 and 6 hours following drug administration. The area under the plasma concentration vs. time curve was increased (p<0.05), while the elimination rate constant was decreased (p<0.01) by piroxicam coadministration. No significant differences were observed in the plasma clearance, apparent volume of distribution and elimination half-life. Thus, piroxicam not only potentiated antihypertensive effect of nifedipine, but also altered nifedipine pharmacokinetics in the rats. It is concluded that the potentiation of nifedipine antihypertensive effect might correlate with the increment of its plasma concentration by piroxicam coadministration.

• Journal of Pharmaceutical Investigation
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• 제37권1호
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• pp.1-5
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• 2007

Solid dispersions of piroxicam were prepared by melting method using poloxamer as a carrier. The results of DSC and XRD studies showed that the amorphous farm of piroxicam coexisted with the crystalline form in the solid dispersions. However, the ratio of crystalline form of piroxicam in the solid dispersion prepared by melting method decreased in comparison with the same ratio of the solid dispersion prepared by solvent method. As the ratio of poloxamer in the solid dispersion increased, the ratio of the amorphous form of piroxicam in the solid dispersion increased. The dissolution rate of piroxicam from the solid dispersions was significantly higher than that from piroxicam powder. In comparison to the solid dispersion prepared by solvent method, the dissolution rate of piroxicam from the solid dispersion prepared by melting method was higher. As the ratio of poloxamer in the solid dispersion prepared by melting method increased, the initial dissolution rate decreased, however, the total amount dissolved at the end of the study increased.

• Archives of Pharmacal Research
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• 제28권2호
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• pp.243-248
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• 2005

To improve the skin permeability of piroxicam, a new oil-in-water microemulsion containing $0.5\%$ piroxicam was developed. Among various oils investigated for their suitability as an oil phase for the microemulsion system, oleic acid showed both excellent solubility and skin permeation enhancing effect for piroxicam. Microemulsion existence ranges were identified through the construction of the pseudo-ternary phase diagram. The effect of the content of oleic acid and the ratio of the surfactant/cosurfactant on skin permeation of piroxicam were evaluated with excised rat skins. The optimum formulation with the highest skin permeation rate ($47.14\;{\mu}g/cm^2/h$) consisted of $0.5\%$ piroxicam, $10\%$ oleic acid, $60\%$ Labrasol/ethanol (1:5) and water.

• Journal of Yeungnam Medical Science
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• 제8권1호
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• pp.215-219
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• 1991

저자들은 54세 여자에서 piroxicam 복용 후 일광노출부위에 광과민성 피부염이 발생한예를 경험하고 광검사 및 광첩포검사 결과 광알레르기성 피부염으로 사료되는 예를 문헌고찰과 함께 보고하는 바이다.

• 대한한방부인과학회지
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• 제28권1호
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• pp.13-28
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• 2015

Objectives: To observe the in vitro anti-inflammatory effects of Hyunbulikyung-tang aqueous extracts (HBLKT) and the possible synergic combination effects with a nonsteroidal anti-inflammatory drug, piroxicam. Methods: Anti-inflammatory effects of HBLKT (yield=16.17%) were observed on LPS activated raw 264.7 cells based on $ED_{50}$ to cell viability, NO, $PGE_2$, $TNF-{\alpha}$, $IL-1{\beta}$ and IL-6 productions as compared with piroxicam, in the present study. In addition, the combination effects of HBLKT with piroxicam were observed after treatment of HBLKT 1/4 $ED_{50}$ + piroxicam 1/4 $ED_{50}$, 1/8 $ED_{50}$, 1/16 $ED_{50}$, 1/32 $ED_{50}$ and 1/64 $ED_{50}$ concentrations, respectively. Results: Significant (p<0.01 or p<0.05) increases of cell viabilities and decreases of NO, $PGE_2$, $TNF-{\alpha}$, $IL-1{\beta}$ and IL-6 cytokine releases were detected in HBLKT 1/4 $ED_{50}$ + piroxicam 1/4 $ED_{50}$, 1/8 $ED_{50}$, 1/16 $ED_{50}$ and 1/32 $ED_{50}$ concentration co-treatment as compared with each of single 1/4 $ED_{50}$ concentration of piroxicam and HBLKT treatments, respectively. Although significant (p<0.01 or p<0.05) increases of cell viabilities and decreases of NO, $PGE_2$, $TNF-{\alpha}$, $IL-1{\beta}$ and IL-6 cytokine releases were also demonstrated in piroxicam 1/64 $ED_{50}$ + HBLKT 1/4 $ED_{50}$ co-treatment as compared with LPS control, no significant changes were detected as compared with each of single 1/4 $ED_{50}$ concentration of piroxicam and HBLKT treatments, in this experiment. Conclusions: Hyunbulikyung-tang showed cell protective and anti-inflammatory effects against LPS activated raw 264.7 cells. It, therefore, expected that HBLKT will be showed favorable effects to relieve dysmenorrhea related to over expressed inflammatory cytokines, and it also expected that the clinical dosages of piroxicam can be reduced as 1/8 levels as combination with HBLKT.