• Journal of Microbiology and Biotechnology
• /
• 제19권9호
• /
• pp.922-931
• /
• 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.

• Journal of Pharmaceutical Investigation
• /
• 제37권3호
• /
• pp.173-177
• /
• 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.

• 대한임상전기생리학회지
• /
• 제5권1호
• /
• pp.45-58
• /
• 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.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
• /
• pp.232.1-232.1
• /
• 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)

• Biomolecules & Therapeutics
• /
• 제17권3호
• /
• pp.305-310
• /
• 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.

• Journal of Pharmaceutical Investigation
• /
• 제38권1호
• /
• pp.63-72
• /
• 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.

• 대한임상전기생리학회지
• /
• 제4권1호
• /
• pp.49-61
• /
• 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.

• Journal of Pharmaceutical Investigation
• /
• 제35권3호
• /
• pp.151-155
• /
• 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.

• Journal of Veterinary Science
• /
• 제24권3호
• /
• pp.43.1-43.8
• /
• 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.

• 한국임상수의학회지
• /
• 제28권3호
• /
• pp.314-317
• /
• 2011

체중이 4.3 kg인 중성화된 16세의 암컷 말티즈견이 약 2주 동안 누런색의 비강과 구강 분비물, 식욕부진과 기면 증상으로 내원하였다. 신체검사에서 구강내 왼쪽 혀 밑 부위에 약 $3{\times}3$ cm 크기의 궤양성 종괴, 심한 치은치주염, 구취, 중등도의 치석, 발열과 아래턱의 연조직 부종을 관찰하였다. 방사선 사진상에서 위턱과 아래턱의 앞 부위에서 골융해 소견을 볼 수 있었다. 총혈액검사와 혈액화학검사에서 혈소판수치, $NH_3$, AST와 ALP의 증가를 관찰할 수 있었으며, 요검사에서 혈뇨와 단백뇨가 나타났다. 조직검사결과 구강 편평 세포암으로 진단되었다. 축주의 거부로 외과적 처치는 실시하지 않았으며, 약물요법으로 carboplatin 주사와 piroxicam 구강내 투여를 병용하였다. 처음 약물투여 후 5일에 지속적인 구토 증상이 나타났으며, 이에 piroxicam을 meloxicam으로 대체하였으며 구토증상은 소실되었다. Meloxicam의 종양에 대한 치료효과에 대한 보고는 흔하지 않지만, 위장관계에 대한 부작용 발생은 piroxicam에 비해 낮음을 알 수 있었다. 이환견은 총 3회의 carboplatin 주사를 실시하였으나, 세 번째 주사 투여 후 5일에 심한 기면증상, 구토와 혈변 증상으로 내원하였고, 검사결과 심한 신기능부전 소견을 보였으며, 축주의 요구에 의해 안락사하였다.