Korean Journal of Clinical Pharmacy (한국임상약학회지)

Korean College Of Clinical Pharmacy (한국임상약학회)
권호 표지

Pharmacokinetic Comparison of Actonel and Risenel Tablet Containing Risedronate sodium in Healthy Volunteers

건강한 지원자에 있어서 리세드로네이트 35 mg 함유 악토넬정과 리세넬정의 약물 동력학적 비교

  • Received : 2009.02.12
  • Accepted : 2009.05.11
  • Published : 2009.06.30
Download PDF
⟨ Previous Next ⟩

Abstract

The aim of this study was to evaluate the pharmacokinetic parameters of two risedronate preparations. The clinical assessment was conducted on 46 healthy volunteers who received one tablet (Risedronate sodium 35 mg/tablet) in the fasting state, in a randomized balanced $2{\times}2$ cross-over study design. After dosing of one tablet containing 35 mg risedronate sodium, blood samples were collected serially for a period of 48 hours. Plasma was analyzed for risedronate by using LC/MS/MS assay method. The analysis system was validated in specificity, accuracy, precision, and linearity. $AUC_t$, (the area under the plasma concentration-time curve from the zero-time to 48 hr) was calculated through the trapezoidal rule. $C_{max}$ (maximum plasma drug concentration) were compiled from the plasma risedronate concentration-time data of each volunteer. No significant sequence effect was found for the pharmacokinetic parameters indicating that the cross-over design was properly performed. The 90 % - Confidence intervals of the $AUC_t$ ratio and the $C_{max}$ were from log 0.8752 to log 1.1888 and log 0.8457 to log 1.1478, respectively. These values were within the acceptable intervals between 0.80 and 1.25. Therefore, this study demonstrated that no statistically significant difference was identified with respect to the rate and extent of absorption.

Keywords

References

  1. Shin DH. Bisphosphonate 제제의 득과 실. J Korean Acad Fam Med. 2006; 27(11): Suppl. November. 355-360.
  2. Dunn CJ, Goa KL. Risedronate: a review of its pharmacolo gical properties and clinical use in resorptive bone disease. Drugs 2001; 61(5): 685-712. https://doi.org/10.2165/00003495-200161050-00013
  3. Mortensen L, Charles P, Bekker PJ, et al. Risedronate increases bone mass in an early postmenopausal population: two years of treatment plus one year of follow-up. J Clin Endocrinol Metab. 1998; 83(2): 396-402. https://doi.org/10.1210/jc.83.2.396
  4. Bekker P, Licata A, Harris S. Risedronate dose response in prevention of early postmenopausal bone loss. J Bone Miner Res. 1996; 11(3): S347.
  5. Singer FR, Clemens TL, Eusebio RA, et al. Risedronate, a highly effective oral agent in the treatment of patients with severe Paget''s disease. J Clin Endocrinol Metab. 1998; 83(6): 1906-1910. https://doi.org/10.1210/jc.83.6.1906
  6. Delmas PD, Balena R, Confravreux E. Bisphosphonate risedronate prevents bone loss in women with artificial menopause due to chemotherapy of breast cancer: a double-blind, placebo-controlled study. J Clin Oncol 1997; 15(3): 955-962. https://doi.org/10.1200/JCO.1997.15.3.955
  7. Reid D, Cohen S, Pack S, et al. Risedronate reduces the incidence of vertebral fractures in patients on chronic corticosteroid therapy. Arthritis Rheum. 1998; 41(1): S136.
  8. Fogelman I, Smith L, Mazess R, et al. Absorption of oral diphosphonate in normal subjects. Clin Endocrinol. 1986; 24(1): 57-62. https://doi.org/10.1111/j.1365-2265.1986.tb03254.x
  9. Mitchell DY, Eusebio RA, Dunlap LE, et al. Risedronate Gastrointestinal Absorption is independent of site and Rate of Administration. Pharm Res. 1998; 15(2): 228-232. https://doi.org/10.1023/A:1011910517200
  10. Mitchell DY, Heise MA, Pallone KA, et al. The effect of dosing regimen on the pharmacokinetics of risedronate. Br J Clin Pharmacol. 1999; 48(4): 536-542.
  11. Lin J. Bisphosphonates: a review of their pharmacokinetic properties. Bone 1996; 18(2): 75-85. https://doi.org/10.1016/8756-3282(95)00445-9
  12. Mitchell DY, Eusebio RA, Dunlap LE. Bioavailability administration of immediate-release and delayed-release risedronate formulations upon oral administration to healthy male subjects in fasted and fed state. Pharm Res 1996; 13: S-609.
  13. Mitchell DY, Eusebio RA, Sacco-Gibson NA, et al. Doseproportional pharmacokinetics of risedronate on singledose oral administration to healthy volunteers. J Clin Pharmacol. 2000; 40(3): 258-265. https://doi.org/10.1177/00912700022008928
  14. Zhu LS, Lapko VN, Lee JW, et al. A general approach for the quantitative analysis of bisphosphonates in human serum and urine by high-performance liquid chromatography/ tandem mass spectrometry. Rapid Commun Mass Spectrom. 2006; 20(3): 421-426.
  15. Mitchell DY, Eusebio RA, Pallone KA, et al. Single dose 27 Necciari J, Kiefer G, Maillard D. Pharmacokinetics of linearity of risedronate following oral administration of 2.5, (4-chlorophenyl) thiomethylene bisphosphonic acid after 5, or 30 mg to healthy volunteers. Pharm Res 1997; 14: S-609.