Hira Naeem a, Mudassar Ashraf b, Aisha Shahzad b
|a||Institute of Pharmacy, Physiology and Pharmacology, University of Agriculture, Faisalabad, Pakistan|
|b||Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, Pakistan|
Published: 20 December 2022
Macrolides are a group of antibiotics produced by Streptomyces bacteria commonly used to treat bacterial infections, including gum infections, gingivitis, and stomach and intestinal ulcers. Roxithromycin is a macrolide antibiotic that effectively targets bacterial cells and inhibits their growth, promoting symptom relief and recovery. Despite this, there is limited research on roxithromycin pharmacokinetics and dosing regimens, particularly in healthy female volunteers from the local population. Thus, this study aimed to investigate roxithromycin's pharmacokinetic parameters and dose regimen in ten healthy female volunteers aged 18 to 30 years. Participants received an oral dose of 300 milligrams of roxithromycin, and blood samples were collected at various intervals for 48 hours. Pharmacokinetic parameters were assessed using two open compartmental models and high-performance liquid chromatography (HPLC). The results showed that the Cmax of roxithromycin was 10.13 ± 0.43 µg/mL, attained at a time to reach tmax of 2.42 ± 0.34 hours. Moreover, the drug exhibited a volume of distribution of 1.38 ± 0.55 L/kg, an elimination half-life of 34.95 ± 22.51 hours, and a total body clearance of 0.04 ± 0.01 L/hr/kg. In accordance with these results, the calculated dosage regimen for 24-hour intervals was 975 milligrams as a priming dose and 372 milligrams as a maintenance dose. In conclusion, this study found that the elimination half-life (t1/2 β) of roxithromycin was higher than literature values, leading to less clearance and ultimately increased Cmax, tmax, and area under the curve (AUC) values of the orally administered drug, indicating the need for dose adjustment in patients.
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Bryant B, Knights K, Rowland A, Darroch S. Pharmacology for health professionals. 5th ed. Amsterdam: Elsevier; 2018. 1025 p.
Shehzad A, Aslam B, Naz U, Ashraf MM, Aslam N, Saleem U, et al. Pharmacokinetics and dosage regimen of moxifloxacin in healthy female volunteers. Lat Am J Pharm. 2017;36(11):2196-202.
Naz U, Ashraf MM, Javed I, Aslam B, Khan JA, Muhammad F, et al. Comparative pharmacokinetics of Cefspan and Ceforal in adult human healthy female subjects. Lat Am J Pharm. 2017;36(4):776-82.
Ashraf MM, Javed I, Aslam B, Khaliq T. Cefixime; disposition kinetics and bioavailability comparison of two formulations of cefixime in healthy adult male subjects. Professional Med J. 2015;22(7):959-65.
Anwar M, Bilal A, Ashraf MM, Ahmed R. Renal clearance and urinary excretion of Cefspan® in healthy male volunteers. Scholar's Adv Anim Vet Res. 2015;2(2):117-22.
Djordjevic S, Drljevic K, Jovanovic B, Kilibarda V. Determination of roxithromycin in human urine by liquid chromatography with photo diode array detection. Med Data. 2011;3(4):345-8.
Kousar S, Naeem H, Alina Z, Riaz L, Bukhari SFR, Naz H, et al. Renal clearance and urinary excretion of roxithromycin in healthy adult female subjects. Cent Euro J Exp Bio. 2017;5(1):77-84.
Illendula S, Singhal NK. A Review: novel analytical method development & validation for the determination of selected anti-cancer & anti-viral drugs. World J Pharm Pharmaceut Sci. 2022;11(7):553-66.
Giguère S, Prescott JF, Dowling PM. Antimicrobial therapy in veterinary medicine. 5th ed. New Jersey: Wiley; 2013. 701 p.
Zafar S, Ali A, Ashraf MM, Khan JA, Aslam B, Naseer RD. Alteration in disposition kinetics of warfarin mediated by caffeine in healthy male albino rabbits. J Anim Plant Sci. 2019;29(2):594-601.
Fassbender M, Lode H, Schiller C, Andro R, Goetschi B, Borner K, et al. Comparative pharmacokinetics of macrolide antibiotics and concentrations achieved in polymorphonuclear leukocytes and saliva. Clin Microbiol Infect. 1996;1(4):235-43. https://doi.org/10.1016/S1198-743X(15)60281-6
Aziz A, Aslam B, Ashraf MM, Naz U, Ashraf N, Raza A. Pharmacokinetic study of glimepiride alone and in combination with atorvastatin in healthy male volunteers. Lat Am J Pharm. 2016;35(10):2331-6.
Britzi M, Berkovitch M, Soback S, Leibovitz A, Segal R, Smagarinsky M, et al. Roxithromycin pharmacokinetics in hospitalized geriatric patients: oral administration of whole versus crushed tablets. Ther Drug Monit. 2015;37(4):512-5. https://doi.org/10.1097/FTD.0000000000000203
Naseer RD, Aslam B, Munir I, Ashraf M, Raza A. Oral pharmacokinetics of rabeprazole in local healthy male volunteers of Pakistan. J Biochem Biotech Biomat. 2016;1(2):21-6.
Finch RG, Greenwood D, Whitley RJ, Norrby R. Antibiotic and chemotherapy: anti-Infective agents and their use in therapy. 9th ed. London: Saunders; 2010. 900 p.
Pankuch GA, Hoellman DB, Lin G, Bajaksouzian S, Jacobs MR, Appelbaum PC. Activity of HMR 3647 compared to those of five agents against Haemophilus influenzae and Moraxella catarrhalis by MIC determination and time-kill assay. Antimicrob Agents Chemother. 1998;42(11):3032-4. https://doi.org/10.1128/AAC.42.11.3032
APO-Roxithromycin. Consumer Medical Information. 2022 [cited 08 August 2022]. Available from: https://media.healthdirect.org.au/medicines/GuildLink_Information/133749/CMI/txcroxit10718.pdf.
Teva. Arrow-Roxithromycin. 2022 [cited 08 August 2022]. Available from: https://www.medsafe.govt.nz/profs/Datasheet/a/Arrowroxithromycintab.pdf.
Sanofi. Australian Product Information. Biaxsig. 2022 [cited 08 August 2022]. Available from: https://secure.guildlink.com.au/gc/ws/sw/pi.cfm?product=swpbiaxs.