Each of the prepared CCTs was composed of a sustained release tablet core and an immediate release coat layer. Amorphous, well-characterized, freeze-dried solid dispersion of lornoxicam with polyvinylpyrrolidone K-30 was employed in the coat layer to attain an initial rapid dissolution of lornoxicam in the stomach, assuring rapid onset of analgesic effect. Compritol ATO 888, a lipophilic matrix-forming material, was included in the core tablets to sustain lornoxicam release. Lactose was also incorporated into these core tablets to ensure complete release of lornoxicam in a time period comparable to the gastrointestinal residence time.
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The use of Central nervous system acting drugs in the management of new degenerative and psychiatric problems cannot be overemphasized. Therefore, the chemical structure of piroxicam can be modified to yield new CNS stimulants and depressants that can be of great benefit to man and animals.
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3-Hydroxy-5-trifluoromethyl-N-(2-(2-thienyl)-2-phenyl-ethenyl)- benzo (b) thiophene-2-carboxamide (L-652,343) is an inhibitor of cyclooxygenase and 5-lipoxygenase in vitro and inhibits the synthesis of the products of both these pathways in whole cells. L-652,343 is an inhibitor of the acute edema induced by carrageenan in vivo and is active topically in suppressing arachidonic acid induced inflammation in the skin. The compound is an effective inhibitor of the chronic inflammation of adjuvant and type II collagen induced polyarthritis. L-652,343 is an extremely potent analgesic in models of yeast and platelet activating factor induced hyperalgesia in rats and phenylbenzoquinone-induced writhing in mice. The fever induced by Brewer's yeast is lowered by L-652,343. The ulcerogenicity and gastric bleeding induced by L-652,343 is extremely low, providing a favorable therapeutic index which is superior to that of indomethacin, piroxicam and phenylbutazone.
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Matrix metalloproteinases (MMPs) play a role in several physiologic and pathologic events. There are some evidence indicating the involvement of MMPs in the pathophysiology of fungal infections.
We found that COX-1 and COX-2 isoforms are expressed in human chondrocytes at rest and in IL-1 stimulated cells, respectively. Antiinflammatory drugs have different capacities to inhibit COX enzyme in human articular chondrocytes.
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Piroxicam was extracted from acid medium into chloroform and isolated on a thin layer of silica gel with the use of the system chloroform - absolute ethanol - benzene - aqueous ammonia (20:15:15:0.5). The intensity of fluorescence of stains was measured densitometrically (an Hg lamp, a filter FL - 39, 330 nm). The limit of detection of the stain is 0.020 microgram/ml of plasma.
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Rates of NSAID discontinuation during the study period were high; only 15 to 20% of those started on a study NSAID were still using the same drug at the end of the 12 month followup period. Using a proportional hazards model to adjust for covariates, the risk of discontinuation did not differ when comparing the agent with the longest duration of use, piroxicam (the referent), to enteric coated aspirin [relative risk (RR) 1.10, 95% confidence interval (CI) 0.93 to 1.30]. Adjusted rates of discontinuation were significantly higher for ibuprofen (RR 1.43, 95% CI 1.22 to 1.69) and for naproxen (RR 1.40, 95% CI 1.19 to 1.65) when compared to piroxicam.
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The consistency of the results provides, in spite of several discussed shortcomings of this pilot study, evidence that in patients with chronic spinal pain syndromes spinal manipulation, if not contraindicated, results in greater improvement than acupuncture and medicine.
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The aim of this work was to develop a proper mathematical model able to describe the kinetics partitioning of a drug between a polar (water buffer) and an apolar (n-octanol) liquid phase. In particular, attention is focussed on sparingly soluble drugs in one or both environments. Basically, we suppose that drug fluxes occurring between the polar and apolar phase depend also on drug solubility, and not only on both the kinetics constants and the instantaneous drug concentration in the two phases. The proposed model adequately describes the drug partitioning of sparingly water soluble drugs (piroxicam and nimesulide) as proven by the comparison of the predicted and experimental data. Moreover, it indicates the unsuitability of a previous approach (Chem. Pharm. Bull. 29 (1961) 2718) in describing the partitioning kinetics unless sink conditions in both phases are attained, this being difficult to achieve when working with sparingly soluble drugs. Consequently, the model represents a simple and reliable tool to study the drug partitioning kinetics.