• SAIYED ZEYAUL ABRAR HUSAIN Department of Pharmaceutical Medicine, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India 110062
  • ARSHAD KHUROO Ranbaxy Research Laboratories, Gurgaon, India 122015
  • AMIT MARWAH Ranbaxy Research Laboratories, Gurgaon, India 122015
  • DIVYA VOHORA Department of Pharmaceutical Medicine, Faculty of Pharmacy, Jamia Hamdard, New Delhi, India 110062



Olopatadine, Antihistaminic, Antiallergic, Pharmacokinetic, Bioavailability, Extended-release, Smoking


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.


Download data is not yet available.


1. Hoffman A. Pharmacodynamic aspects of sustained release preparations. Ad Drug Delivery Rev 1998;33:185-99.
2. Talan DA, Naber KG, Palou J, Elkharrat D. Extended-release ciprofloxacin (Cipro XR) for treatment of urinary tract infections. Int J Antimicrob Agents 2004;23:54-66.
3. Pullar T, Birtwell AJ, Wiles PG, Hay A, Feely MP. Use of a pharmacologic indicator to compare compliance with tablets prescribed to be taken once, twice, or three times daily. Clin Pharmacol Ther 1998;44:540-5.
4. Eisen SA, Miller DK, Woodward RS, Spitznagel E, Przybeck TR. The effect of prescribed daily dose frequency on patient medication compliance. Arch Intern Med 1990;150:1881-4.
5. Brun J. Patient compliance with once-daily and twice-daily oral formulations of 5 isosorbide mononitrate: a comparative study. J Int Med Res 1994;22:266-72.
6. Claxton AJ, Cramer J, Pierce C. A systematic review of the associations between dose regimens and medication compliance. Clin Ther 2001;23:1296-310.
7. Shargel L, Wu Pong S, Yu A. Applied biopharmaceutics and pharmacokinetics. (6th Ed.). The McGraw Hill Companies Inc. USA; 2010.
8. Ohmori K, Hayashi K, Kaise T, Ohshima E, Kobayashi S, Yamazaki T, et al. Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Japan J Pharmacol 2000;88:379-97.
9. Kaliner MA, Oppernheimer J, Farrar JR. Comprehensive review of olopatadine: the molecule and its clinical entities. Allergy Asthma Proc 2010;31:112-9.
10. Guidance for industry: Bioavailability and bioequivalence studies for orally administered drug products--general considerations. U. S. department of health and human services, food and drug administration (FDA), centre for drug evaluation and research (CDER); 2003.
11. Guidelines for bioavailability and bioequivalence studies. Central drugs standard control organization (CDSCO), Ministry of health and family welfare, Government of India, New Delhi; 2005.
12. USFDA Code of Federal Regulation. 21 CFR 320. Vol. 5; 2012. Available from: [Last accessed on 10 Aug 2020]
13. Ethical guidelines for biomedical research on human participants. Indian council for medical research (ICMR), Government of India, New Delhi; 2006.
14. Declaration of Helsinki. 59th World medical association (WMA) general assembly, Seoul; 2008.
15. Guidance for industry: Bioanalytical method validation. US department of health and human services, food and drug administration (FDA), center for drug evaluation and research (CDER); 2001.
16. Beaulieu AD, Peloso PM, Haraoui B, Bensen W, Thomson G, Wade J, et al. Once-daily, controlled-release tramadol and sustained-release diclofenac relieve chronic pain due to osteoarthritis: a randomized controlled trial. Pain Res Manag 2008;3:103-10.
17. Duchier J, Iannascoli F, Safar M. Antihypertensive effect of sustained-release isosorbide dinitrate for isolated systolic systemic hypertension in the elderly. Am J Cardiol 1987;60:99–102.
18. Venkatesh DN, Sankar S, Meyyanathan SN, Muralidharan S, Shanmugam R, Elango K, et al. Bioavailability studies on developed prochloperazine maleate sustained release tablets by HPLC. J Bioanal Biomed 2009;1:54-7.
19. Meyer RJ, Hussain AS. Awareness topic: mitigating the risk of ethanol induced dose dumping from oral sustained/controlled dosage forms, FDA’s ACPS meeting; 2005.
20. Hendeles L, Weinberger M, Milavetz G, Hill M 3rd, Vaughan L. Food-induced dose-dumping from a once-a-day theophylline product as a cause of theophylline toxicity. Chest 1995;57:758-65.
21. Wonnemann M, Schug B, Anschütz M, Brendel E, De Nucci G, Blume H. Comparison of two marketed nifedipine modified release formulations: An exploratory clinical food interaction study. Clin Ther 2008;30:48-58.
22. Kroon LA. Drug interactions with smoking. Am J Health Syst Pharm 2007;64:1917-21.
23. Guideline on the investigation of bioequivalence. Committee for medicinal products for human use (CHMP), European medicines agency (EMA), London; 2010.
24. Guidance document: Conduct and analysis of comparative bioavailability studies. Therapeutic products directorate (TPD), Health Canada; 2012.
25. World Health Organization (WHO) Technical report series, no. 937. WHO expert committee on specifications for pharmaceutical preparations, WHO, Geneva, Switzerland; 2006.



How to Cite

HUSAIN, S. Z. A., A. KHUROO, A. MARWAH, and D. VOHORA. “PHARMACOKINETIC STUDY OF OLOPATADINE 10 MG EXTENDED RELEASE TABLET IN COMPARISON WITH OLOPATADINE 5 MG IMMEDIATE RELEASE TABLET IN INDIAN POPULATION”. International Journal of Current Pharmaceutical Research, vol. 13, no. 1, Jan. 2021, pp. 70-74, doi:10.22159/ijcpr.2021v13i1.40820.



Original Article(s)