{"id":201,"date":"2013-01-05T00:00:00","date_gmt":"2013-01-05T00:00:00","guid":{"rendered":"http:\/\/npaa.in\/journal-ijta\/pharmacokinetic-pharmacodynamic-pk-pd-modeling-of-anti-inflammatory-effect-of-meloxicam-a-preferential-cyclooxygenase-2-inhibitor-in-rats\/"},"modified":"2019-09-22T10:28:22","modified_gmt":"2019-09-22T10:28:22","slug":"pharmacokinetic-pharmacodynamic-pk-pd-modeling-of-anti-inflammatory-effect-of-meloxicam-a-preferential-cyclooxygenase-2-inhibitor-in-rats","status":"publish","type":"post","link":"https:\/\/npaa.in\/journal-ijta\/2013\/01\/05\/pharmacokinetic-pharmacodynamic-pk-pd-modeling-of-anti-inflammatory-effect-of-meloxicam-a-preferential-cyclooxygenase-2-inhibitor-in-rats\/","title":{"rendered":"PHARMACOKINETIC\/PHARMACODYNAMIC (PK\/PD) MODELING OF ANTI-INFLAMMATORY EFFECT OF MELOXICAM, A PREFERENTIAL CYCLOOXYGENASE-2 INHIBITOR, IN RATS"},"content":{"rendered":"

Dheeraj Gopu, Harish Kaushik K, Gomathi P<\/p>\n

Objective<\/span>: To establish a suitable Pharmacokinetic \/ Pharmacodynamic (PK\/PD) model for the meloxicams anti-inflammatory activity for predictions<\/span> about efficacy, potency and sensitivity by using a complex indirect response model in the rat, where carrageenin used as a inflammogen.<\/div>\n
Methods: The rats were divided into different<\/span> groups and received 1, 3, 7 and 10 mg\/kg of meloxicam, after sub-plantar injection of carrageenin to the right hind paw. \u00a0The plasma concentrations of meloxicam were determined by RP-HPLC-UV method and pharmacodynamics (paw edema volume) measured by plethesmography.<\/div>\n
PK\/PD model: Before injection of carrageenin, basal inflammatory mediators synthesis (PEI2) is maintained by physiological<\/span> mechanism which is described by a constant rate synthesis (Ksyn) and a first order degradation (Kout). \u00a0Ksyn is computed by equation Ksyn = E0. Kout. After injection of carrageenin, the additional<\/span> inflammatory mediators synthesis is regulated by input rate (IR (t)). This process is governed<\/span> by a first order rate constant (KIN), which can be inhibited by meloxicam. \u00a0<\/div>\n
Results<\/span>: \u00a0The PK parameters showed dose proportionality, with a Vd, 2101, 3761, 4754and 5321 mL\/kg, CL, 774, 1738, 1872 and 1913mL\/hr\/kg<\/span>, Cmax, 175, 290, 544 and 731ng\/mL. Indirect response PD model (inhibitory Emax model), estimated<\/span> KIN 1.24, 1.96, 1.95 and 1.89 1\/hr, Kout 0.012, 0.019, 0.021 and 0.025 1\/hr, Ksyn 0.0032, 0.0039, 0.0038, and 0.0026 h, estimates for IC50 (concentration<\/span> of meloxicam in plasama eliciting half of maximum inhibition of IR(t) or KIN \u00a0were 418.5, 565.91, 832.96 and 1482.7 ng\/mL of group II, group III, group IV and group V respectively.<\/div>\n
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Dheeraj Gopu, Harish Kaushik K, Gomathi P Objective: To establish a suitable Pharmacokinetic \/ Pharmacodynamic (PK\/PD) model for the meloxicams … <\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[10,20],"tags":[],"class_list":["post-201","post","type-post","status-publish","format-standard","hentry","category-10","category-volume-9"],"_links":{"self":[{"href":"https:\/\/npaa.in\/journal-ijta\/wp-json\/wp\/v2\/posts\/201","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/npaa.in\/journal-ijta\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/npaa.in\/journal-ijta\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/npaa.in\/journal-ijta\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/npaa.in\/journal-ijta\/wp-json\/wp\/v2\/comments?post=201"}],"version-history":[{"count":2,"href":"https:\/\/npaa.in\/journal-ijta\/wp-json\/wp\/v2\/posts\/201\/revisions"}],"predecessor-version":[{"id":878,"href":"https:\/\/npaa.in\/journal-ijta\/wp-json\/wp\/v2\/posts\/201\/revisions\/878"}],"wp:attachment":[{"href":"https:\/\/npaa.in\/journal-ijta\/wp-json\/wp\/v2\/media?parent=201"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/npaa.in\/journal-ijta\/wp-json\/wp\/v2\/categories?post=201"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/npaa.in\/journal-ijta\/wp-json\/wp\/v2\/tags?post=201"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}