• 한국임상약학회지
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• 제19권1호
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• pp.23-31
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• 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
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• 제40권2호
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• pp.79-84
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• 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

• 대한한방부인과학회지
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• 제32권3호
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• pp.1-19
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• 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.

• 대한한방부인과학회지
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• 제31권4호
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• pp.16-38
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• 2018

목 적: 본 연구에서는 고진음자 물 추출물의 골다공증 개선 효과를 난소적출 마우스를 이용하여 risedronate sodium(RES) 2.5 mg/kg 투여군과 비교 평가하였다. 방 법: OVX 35일 후부터 고진음자 물 추출물을 매일 1회씩 35일간 연속 경구 투여하고, 체중, 대퇴골의 중량, 골밀도, 골강도, 무기질 - 칼슘(Ca) 및 무기인(inorganic phosphorus, IP) 함량, 골량 및 구조와 골흡수에 관한 조직병리학적 변화를 혈중 osteocalcin 함량 및 bone specific alkaline phosphatase(BALP) 활성의 변화와 함께 각각 측정하였다. 본 실험에서 고진음자 물 추출물에서의 결과는 RES 경구 투여 OVX 마우스에서의 결과와 비교 평가 하였다. 결 과: OVX대조군에서는 현저한 체중 증가와 함께 대퇴골의 중량, 골밀도, 골강도, 무기질 - Ca 및 IP 함량 감소 및 지주골과 피질골의 현저한 조직병리학적 감소가 함께 확인되었으며, 혈중 osteocalcin 함량의 증가와 함께 혈중 BALP 활성의 감소가 각각 확인되었다. 이에, 전형적인 estrogen 결핍성 골다공증 소견이 OVX 수술에 의해 유발되는 것으로 관찰되었다. 한편 이렇게 OVX에 의해 유발된 estrogen 결핍성 골다공증 소견이 모든 세 용량의 고진음자 물 추출물 500, 250 및 125 mg/kg의 35일에 걸친 연속 경구 투여에 의해 투여 용량 의존적으로 현저히 억제되었고, 특히 고진음자 물 추출물 500 mg/kg은 RES 2.5 mg/kg 투여군과 비교할 만한 골다공증 개선 효과를 나타내었다. 결 론: 이상의 결과에서, 고진음자 물 추출물은 난소적출 마우스에서 투여 용량 의존적으로 유효한 골다공증 개선 효과를 나타내는 것으로 관찰되었다. 따라서 적절한 용량의 고진음자 물 추출물은 새로운 보다 효과적인 estrogen 결핍성 골다공증 개선제로서의 개발 가능성이 매우 높을 것으로 기대된다. 한편 고진음자는 15종의 약제로 구성되어 있으며, 각각의 개별 약제는 수많은 생리활성 물질을 함유하고 있어, 앞으로 생리활성을 나타내는 화학성분의 검색과 함께 다양한 방면으로 기전연구가 추가적으로 수행되어야 할 것으로 판단된다.