• Polymer(Korea)
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• v.33 no.3
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• pp.237-242
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• 2009

This study examined the transdermal delivery of alendronate across hairless mouse skin. The effects of iontophoresis, perforation with a microneedle, and a combination of a microneedle pretreatment and iontophoresis were evaluated in vitro test. Hydrogel patches were polymerized by UN polymerization to supply a hydrogel patch to the iontophoretic transdermal drug delivery system. The alendronate content in the iontophoretic delivery patch was $5.0\;mg/cm^3$. The amounts of alendronate that permeated across the hairless mouse skin when current densities of 0.25 and $0.50\;mA/cm^2$ were supplied to the iontophoretic alendronate patch were $0.80{\pm}0.03$ and $2.00{\pm}0.02{\mu}g$, respectively. After pretreatment with a microneedle, the amounts of alendronate that permeated across the hairless mouse skin increased to $70.65{\pm}0.37$ and $162.23{\pm}0.40{\mu}g$, respectively. The biocompatibility of the iontophoretic alendronate patch was examined according to the international standardization organization 10993.

• The Journal of Korean Academy of Prosthodontics
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• v.51 no.3
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• pp.175-182
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• 2013

Purpose: The purpose of this study was to investigate the effect of different administration duration of alendronate on initial wound healing and new bone formation of extraction socket in rats. Materials and methods: Fifteen male Sprague-Dawley rats (body weight 130-140 g, 4 weeks old, male) were divided into control group (no alendronate administration) and experimental group (alendronate administration). Experimental group was subdivided into 1 week administrated group, 2 week administrated group, 4 week administrated group and 6 week administrated group according to duration of administration. For the experimental groups, during the designated time period (at the time of extraction, 1 week before extraction, 3 week before extraction and 5 week before extraction) till 1 week after extraction, rats were subcutaneously injected with Alendronate at the dose of 1.0 mg/Kg three times a week. Each specimen from 6 week experimental group and control group were used for microarray analysis, and other specimens were used for histological analysis. The rate of new bone formation within the extraction site and bone loss activity was analyzed using TRAP staining. Statistical analysis was performed using Kruskal Wallis test. (${\alpha}=.05$) Results: After one week from the time of extraction, the rate of new bone formation within extraction site for the control group ($16.77%{\pm}1.36%$) compared to the 4 week experimental group ($14.99%{\pm}6.26%$) was lower. However, no statistically significant difference was found. Increase in the number of inactive lacuna (empty lacuna) and decrease in the number of TRAP positive cell were identified with increased duration of administration. There was no significant difference. Conclusion: The results of this study showed as the duration of Alendronate administration increased the rate of new bone formation decreased with loss of bone activity and reduced number of osteoclast.

• Korean Journal of Clinical Pharmacy
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• v.18 no.2
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• pp.114-119
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• 2008

Alendronate is a bisphosphonate that selectively inhibits osteoclast-mediated bone resorption. Dosing convenience is an important element for the enhancement of patient compliance and the effective management of osteoporosis. The purpose of this study was to compare the effectiveness and compliance among alendronate pharmaceutical products (oral once-weekly alendronate 70 mg, daily alendronate 10 mg, and once-weekly alendronate 70 mg with Vitamin $D_3$ 2800 IU) in terms of the change in bone mineral density (BMD), biochemical markers, and compliance estimates. A retrospective chart review was conducted in patients with osteoporosis who received alendronate 70 mg (Group 1), alendronate 10 mg (Group 2), or alendronate 70 mg with Vitamin D3 2800 IU (Group 3) at the endocrinology department of a hospital in Korea from Jan. 1, 1998 to Mar. 31, 2008. The primary endpoints were the increases in spine antero-posterior BMD T-score and femur trochanter BMD T-score, and the compliance of alendronate products. Secondary endpoints included changes in bone turnover-related biochemical markers including bone-specific alkaline phosphatase, urinary N-terminal telopeptides (NTX) and osteocalcin, and in serum vitamin $D_3$ concentration. There was no statistical difference in the BMD increase among the three alendronate products; spine BMD T-score increased by $0.49{\pm}0.52$, $0.39{\pm}0.48$ and $0.50{\pm}0.41$, and femur trochanter BMD T-score by $0.29{\pm}0.42$, $0.21{\pm}0.53$ and $0.24{\pm}0.22$ in Group 1, 2 and 3, respectively. With respect to the increases in femur trochanter BMD T-score and the decreases in NTX and osteocalcin, 70 mg once-weekly group was remarkably superior to 10 mg daily group (p < 0.05) The compliance of 70 mg once-weekly group was significantly higher than that of 10 mg daily treatment group (p < 0.001). In conclusion, all three alendronate treatment groups were equivalent in effectiveness, and the compliance of 70 mg once-weekly group was better than that of 10 mg daily treatment group.

• Journal of Pharmaceutical Investigation
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• v.36 no.2
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• pp.137-142
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• 2006

A bioequivalence of Daewoong $Alendronate^{TM}$ (Daewoong Pharmaceutical Co., Ltd., Korea) and $Fosamax^{TM}$ tablets (MSD Korea) was evaluated according to the guideline of Korea Food and Drug Administration (KFDA). A single 70 mg dose of sodium alendronate of each medicine was administered orally to 56 healthy male volunteers. This study was performed in a $2\;{\time}\;2$ crossover design. Concentrations of alendronate in the urine were monitored by a high-performance liquid chromatography (HPLC). $A_{et}$ (cumulative urinary excreted amount from time 0 to last sampling interval) was calculated by the accumulation of the urinary excreted alendronate. $U_{max}$ (maximum urinary excretion rate) and $T_{max}$ (time to reach $U_{max}$) were compiled from the urinary excretion rate - time data. Analysis of variance was performed using logarithmically transformed $A_{et}$ and $U_{max}$. No significant sequence effect was found for all of the bioavailability parameters. The 90% confidence intervals of the $A_{et}$ and $U_{max}$ for Daewoong $Alendronate^{TM}/Fosamax^{TM}$ were 0.89-1.12 and 0.82-1.02, respectively. This study demonstrated the bioequivalence of Daewoong $Alendronate^{TM}$ and $Fosamax^{TM}$ with respect to the rate and extent of absorption.