• Journal of Pharmaceutical Investigation
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• 제30권1호
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• pp.33-37
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• 2000

One of the methods to increase the solubility of a drug is to use complexation with a cyclodextrin. Due to the hydrophobic nature of the interior cavity of the cyclodextrin, it has been known that undissociated lipophilic drugs can be included within the cyclodextrin by hydrophobic interaction. Recently, inclusion of hydrophilic or dissociated form of a drug has been investigated. In this study, the synergism of pH and complexation with $hydroxypropy-{\beta}-cyclodextrin\;(HP\;{\beta}\;CD)$ to increase the solubility of two oxicam derivatives was investigated. In addition, the effect of partition coefficient of dissociated and undissociated form of the drug on the extent of complexation with HP ${\beta}$ CD was studied. The solubility was measured by equilibrium solubility method. The solubility of tenoxicam and piroxicam increased exponentially with an increase in solution pH above the pKa of the drug in the presence and absence of HP ${\beta}$ CD. The solubility of the drugs increased linearly as a function of HP ${\beta}CD$ concentration at fixed pH. Although the stability constant of ionized species is less than that of the unionized species, the concentration of the ionized drug complex is greater than that of the unionized drug complex due to higher concentration of ionized species at pH 7.3.

• Journal of Pharmaceutical Investigation
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• 제18권4호
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• pp.209-215
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• 1988

The three-dimensional structures of piroxicam crystallized from two different solvents, toluene and toluene/hexane mixture respectively, are proved identical: $C_{15}H_{13}N_3O_4S,\;M\;=\;331.35$, monoclinic, a = 7.128(1), b = 15.146(2), c = 13.956(2) ${\AA},\;{\beta}=\;97.33(1)^{\circ},\;V\;=\;1494.37{\AA}^{3},\;Dx\;=\;1.472\;g/cm^{3},\;Z\;=\;4,\;space\;group\;P2_{1}/c,\;Mo\;K{\alpha}(\lambda=\;0.71073\;{\AA})$, F(000) = 688, T = 295 K, R = 0.0611 for 1993 unique observed reflections. The thiazine ring exhibits a half chair conformation. An amide group is involved in an intramolecular hydrogen bond to the hydroxy group, O(17)-H(17)${\cdots}O(15){\AA}$. The molecule is planar within 2 ${\AA}$ with the interplanar angle $127.9(4)^{\circ}$ between pyridine and benzene rings. A molecular chain parallel to [011] is formed by two intermolecular hydrogen bonds N(16)-H(6)${\cdots}O(11)$ and C(6)-H(6)${\cdots}O(11)$, and the molecular chains are held together by van der Waals forces.

• 대한화학회지
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• 제53권6호
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• pp.693-703
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• 2009

소염제 piroxicam (PX, 4-hydroxy-2-methyl-N-2-pridyl-2H-1, 2-benzothiazine-3-carboxadiamide-1,1-dioxide)의 착물형성을 전이금속이온, Co(II), Ni(II), Cu(II), Zn(II)과 함께 메탄올(MeOH)/물 이성분 혼합물에서 25$^{\circ}C$, 일정한 pH=5.0와 I=0.1 M에서 분광광도법으로 연구하였다. 컴퓨터 프로그램 SQUAD를 스팩트라 데이터로부터 원하는 정보를 얻는데 사용하였다. Fitting 과정의 output은 안정도 상수, 평가한 안정도 상수의 표준편차, 농도분포 다아그램, 모든 종의 스팩트럼 프로파일이다. Co(II), Ni(II), Cu(II), Zn(II)의 PX 착체의 안정도 순서는 Cu(II) > Co(II) > Ni(II) ${\approx}$ Zn(II) 순서이다. 이것은 이들 금속이 온들이 기하학적 경향이 다른 이유일 것이다. PX의 산성도 상수는 다른 pH 값에서 흡수 스펙트럼으로 부터 위의 조건에서 역시 결정하였다. 컴퓨터 프로그램 DATAN을 PX의 산성도 상수의 결정하는 데 사용하였다. 산성도 상수의 validity는 잘 알려진 컴퓨터 프로그램 SPECFIT/32을 사용하였다. 안정 및 산성도 상수의 용매성질, 음이온과 같은 다른 인자의 효과에 관하여 자세하게 논의하였다.

• Journal of Pharmaceutical Investigation
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• 제16권3호
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• pp.132-133
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• 1986

• Journal of Photoscience
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• 제1권1호
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• pp.15-23
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• 1994

The absorption and fluorescence spectral properties of piroxicam (PRX) in the hydrogenbonding solvents show the most sensitive dependence on the concentration ranging from 8 x 10$^{_5}$ to 2 x10$^{_5}$ M. These are attributed to both the solvent-mediated ground-state intermolecular proton transfer (GSIerPT) leading to formation of the ground state anion and the excited-state intmmolecular proton transfer (ESIraPT). The concentration dependences of the time-resolved emission kinetics at both room temperature and 77 K have also been investigated. It is shown that in the excited state, the ESIraPT of PRX is the dominant process to form a keto tautomer at the high concentration, whereas at the low concentration the excited-state conformational change of the anion is an additional process leading to formation of a zwitterion. The ESI~PT of PRX in the hydrogenbonding solvent is coupled with the ultrafast excited-state solvent reorganization.

• 한국임상수의학회지
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• 제36권5호
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• pp.274-277
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• 2019

A Miniature Schnauzer presented with bilateral mucopurulent nasal discharge and sneezing. Computed tomography of the skull revealed exudates in the nasal cavity and frontal gyrus. Nasal swab cytology showed features of an epithelial-origin tumor. Histopathologic evaluation of the biopsy specimen revealed irregular proliferation of epithelial cells and necrotized tissue. Positive immunohistochemical staining confirmed the epithelial origin of the cells. The dog was diagnosed with nasal carcinoma and was treated with a chemotherapy protocol of carboplatin and piroxicam. This report confirms the effectiveness of combination chemotherapy only without radiotherapy in a dog with nasal carcinoma and provides a guideline for providing alternative treatment.

• 한국임상수의학회지
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• 제36권2호
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• pp.109-111
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• 2019

A dog with anorexia, cough, and regurgitation was referred to clinic. Diagnostic imaging revealed a solitary mass involving the right cranial and middle lung lobes, compression of the cranial vena cava, and deviation of the heart and mediastinum toward the left side because the mass. The mass was diagnosed as a squamous cell carcinoma via fine needle aspiration. Ten days later, the tumor was larger and the clinical signs were more severe. A combination of piroxicam and itraconazole was administered to control the mass. Two weeks after initiating this treatment, the tumor size decreased and the clinical signs improved significantly.

• Bulletin of the Korean Chemical Society
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• 제9권3호
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• pp.171-175
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• 1988

The spectral properties of piroxicam in different solvents are similar to those of its skeletal precursor, HMBDC. The maximum absorption and emission wavelengths strongly depend on the hydrogen bonding ability of the solvent, and it is shown that intramolecular hydrogen bonding between the -OH and the ortho carbonyl group of the parent benzothiazine ring plays an important role in the solvent-dependence of their spectroscopic properties. The fluorescence spectra in aprotic nonpolar solvent exhibit abnormally large Stokes-shifted (${\sim}9,000cm^{-1}$) emission bands in contrast to the spectra in water. In ethanol, dual emission bands with two different fractional components of lifetimes have been observed. These results suggest that the abnormally red-shifted emission is attributed to the proton transferred form of an intramolecularly hydrogen-bonded closed conformer.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.221.1-221.1
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• 2002

• 대한임상전기생리학회지
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• 제1권1호
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• pp.17-29
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• 2003

This study was investigated the effects on functional recovery of eccentric exercise-induced muscle damage by phonophoresis transdermal permeation of piroxicam gel and observed the change of amplitude at muscle action potential. Through eccentric exercise-induced muscle damage, performed healthy men and women take eccentric resistance exercise and measured action, potentials. The subjects were divided into three groups of four men each 24 hour, 48 hour, 72 hour. The results of this were as follows: 1. Change of maximal action potential at maximal voluntary contraction : The phonophoresis group was increase more than control group and gel group. 2. Change of average action potential at maximal voluntary contraction : The gel group was increase more than control group and phonophoresis group. 3. Change of maximal action potential at pain subthreshold voluntary contraction : The phonophoresis group was increase more significantly than control group and gel group. 4. Change of average action potential at pain subthreshold voluntary contraction : The phonophoresis group was increase more significantly than control group and gel group. In conclusion, the change of muscle action potential amplitude by eccentric exercise-induced muscle damage showed that the phonophoresis by pulsed ultrasound of piroxicam gel was improved the recovery of muscle function.