Aim: A newer LC-MS/MS method was developed and validated for the simultaneous quantification of raloxifene (RL) and cladrin (CL). Methodology: Both drugs were resolved in RP-18 (4.6×50mm, 5μ) Xbridge Shield column using acetonitrile and 0.1% aqueous solution of formic acid (FA)(70:30%v/v) as mobile phase by using biological matrices in female Sprague-Dawley rats using-MS/MS. Results: The developed method was found to be linear over the concentration ranges of 1-600ng/ml, and lower limit of quantification was 1ng/ml for RL and CL, respectively. Pharmacokinetic results of RL+CL showed Cmax=4.23±0.61, 26.97±1.14ng/ml, at Tmax(h) 5.5±1.00 and 3.5±1.00, respectively. Conclusion: Pharmacokinetic study results will be useful in the future for the combined delivery of RL and CL for osteoporosis treatment.