Abstract
Purpose : To compare oral bioavailability and pharmacokinetic parameters of different lornoxicam formulations and to assess similarity in plasma level profiles by statistical techniques. Methods : An open-label, two-period crossover trial was followed in 24 healthy Pakistani volunteers (22 males, 2 females). Each participant received a single dose of lornoxicam controlled release (CR) microparticles and two doses (morning and evening) of conventional lornoxicam immediate release (IR) tablet formulation. The microparticles were prepared by spray drying method. The formulations were administered again in an alternate manner after a washout period of one week. Pharmacokinetic parameters were determined by Kinetica 4.0 software using plasma concentration-time data. Moreover, data were statistically analyzed at 90 % confidence interval (CI) and Schuirmann’s two one-sided t-test procedure. Results : Peak plasma concentration (C max ) was 20.2 % lower for CR formulation compared to IR formulation (270.90 ng/ml vs 339.44 ng/ml, respectively) while time taken to attain C max (t max ) was 5.25 and 2.08 h, respectively. Area under the plasma drug level versus time (AUC) curve was comparable for both CR and IR formulations. The 90 % confidence interval (CI) values computed for C max , AUC 0-24 , and AUC 0- , after log transformation, were 87.21, 108.51 and 102.74 %, respectively, and were within predefined bioequivalence range (80 - 125 %). Conclusion : The findings suggest that CR formulation of lornoxicam did not change the overall pharmacokinetic properties of lornoxicam in terms of extent and rate of lornoxicam absorption. Keywords : Analgesic, Microparticles, Controlled release, Lornoxicam, NSAIDs, Pharmacokinetics
Highlights
Lornoxicam is a short-acting non-steroidal antiinflammatory drug (NSAID) which belongs to the oxicam group
The microparticles were ellipsoidal in shape with surface morphology clearly showing presence of drug particles (Figure 1)
The incorporation efficiency increased from 56.48 % ± 2.21 to 83.04 % ± 1.22 with the increase in the polymer contents
Summary
Lornoxicam is a short-acting non-steroidal antiinflammatory drug (NSAID) which belongs to the oxicam group. It decreases prostaglandin production by reducing cyclo-oxygenase (COX) activity. It is successfully being used in clinical settings for alleviating the symptoms of rheumatoid arthritis, osteoarthritis, acute sciatica and ankylosing spondylitis. Patient compliance to prescribed regimen of NSAIDs in chronic disorders (rheumatoid arthritis & ankylosing spondylitis) is generally poor [4]. The reasons for low compliance of NSAIDs include temporary relief of symptoms and gastric irritation associated with frequent intake of NSAIDs. Substantial variation in compliance has been observed in patients taking NSAIDs resulting in poor drug efficacy and safety [5]
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