Abstract
Objective: This study was designed to assess the pharmacokinetics of single dose of olopatadine hydrochloride 10 mg extended release (ER) tablet of Ranbaxy laboratories limited (two test formulations) with two doses of Allelock® 5 mg immediate release (IR) tablets of Kyowa Hakko Kogyo Co. Ltd. (reference formulation R), in healthy, adult, Indian male subjects under fed condition.
 Methods: Fifteen healthy male volunteers, 26.07±6.62 y in age and 57.17±6.68 kg in body weight, were divided into three groups and received either olopatadine hydrochloride 10 mg ER tablet or two doses of Allelock® 5 mg tablets in each period. Blood samples were taken at predetermined time points and plasma concentrations of olopatadine were monitored by liquid chromatography mass spectrometric (LCMS/MS). Pharmacokinetic (PK) parameters AUC0-t, AUC0-24, AUC0-∞, and Cmax were calculated for olopatadine using WinNonlin. A statistical analysis was performed on PK data using SAS system.
 Results: The ER formulations showed a similar AUC as compared to the IR formulation and there was no statistically significant difference in AUC of test formulation A and B and reference R. The ratios of AUC0-t, AUC0-24 and AUC0-∞ for A/R were 91.08, 94.90 and 91.32 and for B/R were 89.63, 93.95 and 89.63 respectively. The ER formulations reported a higher Cmax value as compared to IR formulation. The ratios of Cmax for A/R and B/R were 151.09 and 167.96 respectively. But these higher Cmax values did not pose any safety issue as there were no serious adverse events reported during the study.
 Conclusion: In conclusion, we can say that though the study drugs did not meet the bioequivalence criteria set by regulatory agencies, but this study gave an insight about PK properties of olopatadine extended release formulation and given an idea about effect of smoking on the PK profile of olopatadine which can be studied in future.
Highlights
Extended release (ER) or modified release (MR) mode of drug administration has certain advantageous impact on the magnitude of the pharmacologic response: (a) it minimizes fluctuation in blood drug concentrations’, (b) it produces a slow input rate which tends to minimize the body's counteraction to the drug's intervening effect on regulated physiological processes; and (c) it provides a continuous mode of drug administration [1]
In relation to area under the curve, the results demonstrated that the ER formulations showed a similar extent of abortion as compared to the reference formulation and there was no statistically significant difference (p
In a comparative bioavailability study conducted to examine the pharmacokinetics of prochlorperazine immediate release tablet and sustained release tablet in healthy, adult, male volunteers, the reported Cmax values for sustained release tablet and immediate release tablet were 297.89 and 218.41 ng/ml respectively [18], the similar pattern is shown in our study where the Cmax values of the sustained release formulations were higher than the immediate release
Summary
Extended release (ER) or modified release (MR) mode of drug administration has certain advantageous impact on the magnitude of the pharmacologic response: (a) it minimizes fluctuation in blood drug concentrations’, (b) it produces a slow input rate which tends to minimize the body's counteraction to the drug's intervening effect on regulated physiological processes; and (c) it provides a continuous mode of drug administration [1]. The studies have confirmed good tolerability and safety of ER formulations similar to the IR formulations [2]. Another undoubted advantage of ER formulation is improved patient compliance. The therapeutic effectiveness of a drug depends upon its bioavailability to elicit the desired pharmacological response. There are many drug-related (physicochemical properties) and host factors (physiological factors like age, blood flow to gastrointestinal tract (GIT), pH, gastric emptying etc.) that influence the rate and absorption of the drugs [7]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
