• Title/Summary/Keyword: Piroxicam

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Complexation of Piroxicam and Tenoxicam with $Hydroxypropyl-{\beta}-cyclodextrin$ (히드록시프로필-베타-시클로덱스트린과 피록시캄 및 테녹시캄 간의 복합체 형성)

  • Kim, Ju-Hyun;Choi, Hoo-Kyun
    • Journal of Pharmaceutical Investigation
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    • v.30 no.1
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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.

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The Solvent-Independent Structure of Piroxicam (피록시캄의 용매 비의존 결정구조)

  • Kim, Bong-Hee;Suh, Il-Hwan;Jhee, Ok-In;Suh, Jong-Myung;Suh, Jung-Jin
    • Journal of Pharmaceutical Investigation
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    • v.18 no.4
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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.

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Spectrophotometric Study of Acidity and Complex Formation of Anti-Inflammatory Drug Piroxicam with Some Transition Metal Ions in Different Methanol/Water Mixtures by Chemometric Methods (Chemometric 방법에 의한 메탄올/물 계에서 전이 금속 이온과 소염제 Piroxicam의 산성도 및 착체 형성에 관한 분광광도법 연구)

  • Ghasemi, Jahan B.;Jalalvand, Alireza
    • Journal of the Korean Chemical Society
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    • v.53 no.6
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    • pp.693-703
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    • 2009
  • The complex formation of anti-inflamatory drug piroxicam (PX, 4-hydroxy-2-methyl-N-2--pridyl-2H-1,2-benzothiazine-3-carboxadiamide-1,1-dioxide) with transition metal ions Co(II), Ni(II), Cu(II) and Zn(II) in methanol(MeOH)/water binary mixtures were studied by spectrophotometric method at 25$^{\circ}C$, constant pH = 5.0 and I = 0.1 M. The computer program SQUAD was used to extract the desired information from the spectral data. The outputs of the fitting processes were stability constants, standard deviations of the estimated stability constants, concentration distribution diagrams and spectral profiles of all species. The sequence of the stability constants of PX complexes with Co(II), Ni(II), Cu(II) and Zn(II) follow the Cu(II) > Co(II) > Ni(II) ${\approx}$ Zn(II) order. This may be due to different geometry tendencies of these metal ions. The acidity constants of the PX were also determined under above condition from its absorption spectra at different pH values. The computer program DATAN was used for determination of acidity constants of PX. The validity of the obtained acidity constants was checked by a well known computer program SPECFIT/32. The effects of the different parameters like solvent nature, cations characteristics on the stability and acidity constants were thoroughly discussed.

CONCENTRATION DEPENDENCES OF GROUND-STATE AND EXCITED-STATE INTRAMOLECULAR PROTON TRANSFER OF PIROXICAM IN METHANOL

  • Cho, Dae-Won;Kang, Seong-Gwan;Kim, Yong-Hee;Yoon, Min-Joong;Kim, Dong-Ho
    • Journal of Photoscience
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    • v.1 no.1
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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.

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Successful Combination Chemotherapy for Nasal Carcinoma in a Dog

  • Kim, Su-Gang;Cho, Seok-Ho;Kim, Keon;Park, Hee-Myung;Park, Sang-Ik;Kim, Tae-Jung;Lee, Chang-Min
    • Journal of Veterinary Clinics
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    • v.36 no.5
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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.

Application of a Cyclooxygenase Inhibitor and Itraconazole for Pulmonary Squamous Cell Carcinoma in a Dog

  • Bae, Seul-gi;Oh, Tae-ho
    • Journal of Veterinary Clinics
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    • v.36 no.2
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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.

Solvent Dependence of Absorption and Fluorescence Spectra of Piroxicam. A Possible Intramolecular Proton Transfer in the Excited State

  • Yoon, Min-Joong;Choi, Hyong-Nae;Kwon, Hwang-Won;Park, Koon-Ha
    • Bulletin of the Korean Chemical Society
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    • v.9 no.3
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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.

Effects on Functional Recovery of Eccentric Exercise-Induced Muscle Damage by Phonophoresis of Piroxicam Gel (피록시캄 겔의 음파영동이 원심성 운동-유발 근 손상의 기능회복에 미치는 효과)

  • Choi, Sug-Ju;Kim, Tae-Youl;Song, Myung-Soo;Kim, Young-Il;Moon, Sung-Ki
    • Journal of the Korean Academy of Clinical Electrophysiology
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    • v.1 no.1
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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.

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