• Title/Summary/Keyword: Meloxicam

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Studies on Microbial Transformation of Meloxicam by Fungi

  • Shyam Prasad, G.;Girisham, S.;Reddy, S.M.
    • Journal of Microbiology and Biotechnology
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    • v.19 no.9
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    • pp.922-931
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    • 2009
  • Screening-scale studies were performed with 26 fungal cultures for their ability to transform the anti-inflammatory drug meloxicam. Among the different fungi screened, a filamentous fungus, Cunninghamella blakesleeana NCIM 687, transformed meloxicam to three metabolites in significant quantities. The transformation of meloxicam was confirmed by high-performance liquid chromatography (HPLC). Based on the liquid chromatography-tandem mass spectrometry (LC-MS/MS) data, two metabolites were predicted to be 5-hydroxymethyl meloxicam and 5-carboxy meloxicam, the major mammalian metabolites reported previously. A new metabolite was produced, which is not detected in mammalian systems. Glucose medium, pH of 6.0, temperature of $27^{\circ}C$, 5-day incubation period, dimethylformamide as solvent, and glucose concentration of 2.0% were found to be suitable for maximum transformation of meloxicam when studied separately. It is concluded that C. blakesleeana can be employed for biotransformation of drugs for production of novel metabolites.

Effect of Ethanolamine Salts and Enhancers on the Percutaneous Absorption of Meloxicam from a Pressure Sensitive Adhesive Matrix

  • Ki, Han-Moe;Cheong, Hyun-Ah;Choi, Hoo-Kyun
    • Journal of Pharmaceutical Investigation
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    • v.37 no.3
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    • pp.173-177
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    • 2007
  • The purpose of this study was to investigate the effect of salt formation on the percutaneous absorption of meloxicam through hairless mouse skin from a pressure sensitive adhesive (PSA) matrix. In addition, the influences of enhancers on the permeation of meloxicam or meloxicam-ethanolamine (MX-EA) salts across the hairless mouse skin were evaluated using a flow-through diffusion cell system. The salt formation of meloxicam resulted in lower permeation rate than the parent drug. $Span^{(R)}$ 80 provided the highest enhancing effect for meloxicam and meloxicam monoethanolamine salt. The maximum amount of the drug that can be loaded without retarding permeation rate was different depending on the compound. No relationship was found between the fluxes of meloxicam or MX-EA salts from saturated solutions and those from PSA matrices containing the same enhancer.

Effects on Nociceptive Neuron Excitability by application of Electroacupuncture and Meloxicam gel in Rat with Inflammation (염증유발 백서에서 전침자극과 Meloxicam gel 적용이 유해성굴곡반사 및 체성감각유발전위에 미치는 효과)

  • Kim, Young-Pil;Lee, Jeong-Woo;Seo, Sam-Ki;Yoon, Se-Won;Yoon, Hee-Jong;Kim, Tae-You
    • Journal of the Korean Academy of Clinical Electrophysiology
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    • v.5 no.1
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    • pp.45-58
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    • 2007
  • This study aims to examine the effects on nociceptive neuron excitability by application of electroacupuncture and Meloxicam gel in rat with inflammation. It used 24 rats for experiment, divided them into control group, electroacupuncture group(EA group), Meloxicam group(ME group), combination of electroacupuncture with Meloxicam group(EA+ME group), caused hyperalgesia by injecting ${\lambda}$-carrageenan into hindpaw and conducted treatment three times for experimental period. Noxious flexion withdrawal reflex(NFR) and somatosensory evoked potential(SEP) were measured immediately after induction, at 24 hours, 48 hours and 72 hours after induction. Change of NFR(reaction time, RMS) showed no significant differences among EA group, Meloxicam group, and EA+Meloxicam group, but all treatment groups showed significant differences compared to control group from 48 hours. In NFR threshold, there were significant differences between EA+Meloxicam and other groups. In SEP amplitude, there were significant differences between EA+Meloxicam and control group from 48 hours. This study showed that EA+Meloxicam gel had an effect on nociceptive neurone excitability. Therefore, it is considered that appropriate combination of anti-inflammatory drug with electroacupuncture for pain control will be very desirable.

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In vitro and in vivo evaluation of meloxicam capsule

  • Park, Sei-Yeon;Park, Young-Joon;Kang, Dae-Sik;Lee, Ho-Chan;Kang, Heui-Il
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.232.1-232.1
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    • 2003
  • Purpose. To develop a hard gelatine capsule containing meloxicam (Yuhan Meloxam capsule$\^$TM/), in vitro dissolution characteristics and bioavailability in beagle dog were compared with commercial product (Mobic capsule$\^$TM/). Methods. Meloxicam capsule$\^$TM/ was prepared by powder filling method using meloxicam, lactose, magnesium stearate, and others. The release of Meloxicam capsule$\^$TM/ and Mobic capsule$\^$Tm/ were monitored by USP dissolution method under various dissolution donditions - dissolution medium (pH 1.2, 4.0, 6.8 and water). (omitted)

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Anti-Hyperalgesic Effects of Meloxicam Hydrogel via Phonophoresis in Acute Inflammation in Rats; Comparing Systemic and Topical Application

  • Kim, Tae-Youl;Kim, Young-Il;Seo, Sam-Ki;Kim, Soo-Hyeun;Yang, Kyu-Ho;Shin, Sang-Chul
    • Biomolecules & Therapeutics
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    • v.17 no.3
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    • pp.305-310
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    • 2009
  • The aim of this study was to determine if a meloxicam hydrogel could be administered in vivo via phonophoretic transdermal delivery using pulsed ultrasound by examining its anti-hyperalgesic effects in a rat carrageenan inflammation model. Carrageenan (1%) was injected into the plantar surface of the right hindpaw, and meloxicam hydrogel was administered via phonophoretic transdermal delivery. Changes in the mechanical and thermal hyperalgesia, as well as swelling, showed that phonophoretic delivery of meloxicam exhibited significantly better anti-hyperalgesic and anti-inflammatory effects than pulsed ultrasound. Topical and systemic application of meloxicam hydrogel using phonophoresis showed similar anti-hyperalgesic effects. These findings suggest that the transdermal administration of a meloxicam hydrogel using phonophoresis by pulsed ultrasound might be useful for treating acute inflammation.

Preparation and Evaluation of Meloxicam-loaded Poly(D,L-lactic acid) Microspheres (멜록시캄 함유 poly (D,L-lactic acid) 미소립자의 제조 및 평가)

  • Im, Jong-Seob;Oh, Dong-Hoon;Li, Dong-Xun;Sung, Jung-Hoon;Yoo, Bong-Kyu;Kim, Jung-Ae;Woo, Jong-Soo;Lee, Yong-Bok;Kim, Se-Mi;Choi, Han-Gon;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.38 no.1
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    • pp.63-72
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    • 2008
  • Meloxicam-loaded microspheres were prepared with poly(D,L-lactic acid)(PLA) by a solvent-emulsion evaporation method. The morphology, particle size, drug loading capacity, drug entrapment efficiency (EE) and release patterns of drug were investigated in vitro. Various batches of micro spheres with different size and drug content were obtained by changing the ratio of meloxicam to $PLA^{\circ}{\AE}s$ with different molecular weight, PLA concentration in the dispersed phase and stirring rate. Meloxicam crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. Microspheres prepared with smaller molecular weight produced faster drug release rate. The release rate of meloxicam for long-acting injectable delivery system in vitro, which would aid in predicting in vivo release profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres. Blood concentration-time profile of meloxicam after intramuscular injection of meloxicam-loaded microspheres in rabbits showed possibility of long term application of this system in clinical settings.

Skin Permeation Effects of Meloxicam Gel on Ultrasound Parameters by Phonophoresis (초음파의 매개변수에 따른 Meloxicam Gel의 경피투과 촉진효과)

  • Choi, Sug-Ju;Yoon, Se-Won;Jung, Dae-In;Kim, Young-Il;Jeong, Jin-Gyu;Kim, Tae-Youl
    • Journal of the Korean Academy of Clinical Electrophysiology
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    • v.4 no.1
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    • pp.49-61
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    • 2006
  • This study conducted the following experiment to examine and compare transdermal permeation effects according to parameters of ultrasound and physiochemical characteristics of meloxicam. Permeation by ultrasound among these experimental drugs was relatively higher and it was involved in COX-2 inhibition unlike other drugs. Recently use of oral agents has been rapidly increased, but it was not generalized to transdermal agent and this study selected meloxicam that transdermal permeation research using ultrasound was not performed and conducted transdermal permeation experiment with skin of hairless mouse and analyzed permeation with HPLC. It made gel first and analyzed permeation depending on frequency and intensity of ultrasound of meloxicam with the same experimental procedures as the above experiment. The results of this study can be summarized as follows. Transdermal permeation by ultrasound frequency was higher in 1.0 MHz and it was higher as intensity increased. In comparison by parameters of ultrasound, there was similar permeation in $1.0\;W/cm^2$ of continuous mode and $3.0\;W/cm^2$ of pulsed mode and it was effective to high intensity for using pulsed mode. It was found that duty cycle of ultrasound affected transdermal permeation in meloxicam gel used in this experiment and transdermal permeation was higher in used ultrasound as phonophoresis than non-ultrasound for anti-inflammatory effects.

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A Novel Drug Delivery System Design for Meloxicam

  • Kim, Hyun-Jo;Lee, Il-Kyu
    • Journal of Pharmaceutical Investigation
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    • v.35 no.3
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    • pp.151-155
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    • 2005
  • A drug delivery system(DDS) for practically insoluble meloxicam was developed and evaluated by dissolution study. A novel DDS is two layered system, where the first layer is consisted of gas-forming agent for an immediate release and the second layer is composed of metolose SR(HPMC) for sustained release. This bilayered tablets were manufactured by using manual single punch machine. The results of dissolution study showed an initial burst release followed by sustained release for the experimental period time. From a pharmaceutical point of view, the designed DDS for meloxicam would be informative system in terms of poorly soluble analgesic medicines.

Effects on hematology and blood biochemistry profile of intramuscular meloxicam injection in Brahminy kite and Barn owl

  • Ratiwan Sitdhibutr;Raveewan Ploypan;Sirawit Subaneg;Chaiyan Kasorndorkbua
    • Journal of Veterinary Science
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    • v.24 no.3
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    • pp.43.1-43.8
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    • 2023
  • Background: Meloxicam is used widely for exotic animal analgesia, but its toxicity in common raptor species in Thailand is unclear. Objectives: This study evaluated the single-dose effect of intramuscular meloxicam in common raptor species in Thailand for short-term and long-term periods. Methods: Twenty-two raptors were administered a single 1 mg/kg dose of meloxicam individually via intramuscular injection. The following were evaluated: clinical appearance, body weight, body condition score, body temperature, fecal appearance, complete blood cell count, and biochemistry panel before (day 0) and after the injection (1, 7, and 30 days). The collected samples were categorized into three groups: Brahminy kite (Haliastur indus) (n = 10), adult Barn owl (Tyto javanica) (n = 4), and juvenile Barn owl (n = 8). Results: None of the raptors in the study groups showed any abnormalities. The hematological profiles were significantly different in the short-term period (day 1 and day 7). The creatinine, aspartate aminotransferase, and creatinine kinase increased in several groups. On the other hand, the packed cell volume decreased in the Brahminy kite and juvenile Barn owl groups. According to the findings, an intramuscular injection of 1 mg/kg meloxicam affected the blood biochemistry panel of the muscle, but the affected raptors recovered within one week. Conclusions: An intramuscular injection of meloxicam at a single 1 mg/kg dose in Brahminy kites and Barn owls was not associated with the morbidity, hepatotoxicity, gastrointestinal toxicity, and nephrotoxicity in the short- and long-term periods.

Combined Therapy with Carboplatin and Meloxicam for Oral Squamous Cell Carcinoma in a Dog (구강 편평 세포암 이환견에서 Carboplatin과 Meloxicam의 병용투여 증례)

  • Jang, Hwan-Soo;Kim, Jun-Il;Kim, Jae-Hoon;Jang, Kwang-Ho
    • Journal of Veterinary Clinics
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    • v.28 no.3
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    • pp.314-317
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    • 2011
  • A 16-year-old, spayed female, Maltese dog weighing 4.3 kg was presented with a 2-week history of yellowish nose-and oral-discharge, anorexia and lethargy. In physical examination, indefinite ulcerative mass about $3{\times}3$ cm in size in the left sublingual region, severe gingivoperiodontitis, halitosis, moderate dental calculus, fever and swelling of mandible soft tissue were noted. In radiographic view, periodontitis and bone lysis findings on the left rostral part of maxilla and mandible were observed. In complete blood count and blood chemistry test, thrombocytosis, increased levels of serum $NH_3$, AST and ALP were obtained. Urinalysis revealed hematuria and proteinuria. In histological examination, squamous cell carcinoma was diagnosed. No surgery was performed, but combined treatment with carboplatin and piroxicam was initiated. Five days after initiation of medication, because of insistent vomiting, piroxicam was substituted to meloxicam. Although the therapeutic efficacy of meloxicam could not be known; administration of meloxicam might be less potential to gastrointestinal side-effects than piroxicam. The dog totally received 3 times of carboplatin infusion. Five days after third infusion of carboplatin, the dog was hospitalized with severe lethargy, vomiting and bloody diarrhea. In examination, severe renal failure signs were noted, and the dog was euthanized.