• Korean Journal of Clinical Pharmacy
• /
• v.19 no.1
• /
• pp.23-31
• /
• 2009

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.

• Journal of Pharmaceutical Investigation
• /
• v.40 no.2
• /
• pp.79-84
• /
• 2010

Osteoporosis was traditionally defined by the occurrence of nontraumatic fractures, especially of the spine, in the setting of low bone mass. Bisphosphonates are an important group of therapeutic agents for the management of osteoporosis, as they inhibit bone resorption and increase bone density, thereby potentially decreasing fracture risk. Risedronate sodium is a bisphosphonate class used by oral formulation. In this study, risedronate was transdermally delivered by iontophoresis. Effects of polarity, pH, current density, and drug concentration were studied using a side-by-side diffusion cell including the hairless mice skin. In addition we studied effect of enhancers. The flux was evaluated by HPLC/UV system. The amount of transported drug under iontophoretic delivery was approximately 186 fold higher than that under passive delivery. Flux was proportional to the increase of drug concentration and current density. The flux was observed about 0.68mg/$cm^2$ when the amout of Propyleneglycol monolaurate (PGML) used 1% as enhancer. Results indicated that iontophoresis is an effective method for transdermal administration of risedronate sodium

• The Journal of Korean Obstetrics and Gynecology
• /
• v.32 no.3
• /
• pp.1-19
• /
• 2019

Objectives: To select the optimal ranges showing obvious synergic anti-osteoporotic potential after adjust mixed formula consisted of Morindae Radix (MR) and Cistanchis Herba (CH) as compared with those of each single formula or risedronate sodium (RES) using bilateral ovariectomized (OVX) female mice. Methods: Fourteen groups, total eight sham or 104 OVX mice were selected based on the body weights at 34 days after OVX surgery. After that, 9 types mixed compositions, single formula of MR and CH, and RES were orally administered for 35 days. And we measured changes in body weight and gain, femur weight, bone mineral density (BMD), bone strength (failure load) and mineral content - calcium (Ca) and inorganic phosphorus (IP), osteocalcin contents and bone specific alkaline phosphatase (bALP) activities of all mice. Results: The OVX-induced estrogen-deficient osteoporotic signs were significantly inhibited by 35 days of continuous oral treatment of all treated mice as compared with OVX control mice. Especially, MR:CH 1:3 and 1:1 mixed formula treated mice showed significantly more favorable inhibitory activities against estrogen-deficient osteoporosis symptoms as compared to those of each single formula of MR and CH. Although RES also ameliorated the decreases of the femur BMD, strength and trabecular bone architectures through the inhibited the increases of bone turnover, but they did not critically influenced on the bone formations. Conclusions: The results suggest that MR:CH 1:3 mixed formula showed somewhat lower anti-resorptive effects as compared to those of RES, but they also showed bone formation effects. therefore, it is expected that MR:CH 1:3 mixture will be promising as a potent protective agents for relieving the osteoporosis in menopausal women.

• The Journal of Korean Obstetrics and Gynecology
• /
• v.31 no.4
• /
• pp.16-38
• /
• 2018

Objectives: The objective of this in vivo study is to observe the anti-osteoporotic activities of Gojineumja aqueous extracts (GJEJ) on the ovariectomized (OVX) mice as compared to those of risedronate sodium (RES). Methods: Thirty five days after bilateral OVX, GJEJ was orally administered, for 35 days once a day and then the changes on the body weight and gain during experimental periods, femur weights, bone mineral density (BMD), bone strength (failure load), mineral contents - calcium (Ca) and inorganic phosphorus (IP), histological profiles and histomorphometrical analyses at sacrifice were conducted with serum biochemistry - osteocalcin contents and bone specific alkaline phosphatase (BALP) activities. And the results of GJEJ were compared with RES orally administered OVX mice. Results: As a result of OVX, noticeable increase of body weight and gains and serum osteocalcin levels, decrease of serum BALP activities, femur weights, femur Ca and IP contents, BMD and strength were observed as compared to those of sham control mice, respectively. Also, the decrease of all histomorphometrical indices indicating the bone mass and structure, and the increase of indices about resorption were also detected in the femur of OVX control. However, these estrogen-deficient osteoporotic signs were significantly and dose-dependently inhibited by 35 days of continuous oral treatment of GJEJ, at dose levels of 500, 250 and 125 mg/kg, respectively. Especially, GJEJ 500 mg/kg showed favorable inhibitory activities against estrogen-deficient osteoporosis symptoms induced by OVX as comparable to those of RES 2.5 mg/kg. Conclusions: The results in this study suggest that oral administrations of GJEJ have clear dose-dependent favorable anti-osteoporotic activities in OVX mice.