首页> 外文期刊>Journal of bone and mineral research: the official journal of the American Society for Bone and Mineral Research >Development of a novel transdermal patch of alendronate, a nitrogen-containing bisphosphonate, for the treatment of osteoporosis.
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Development of a novel transdermal patch of alendronate, a nitrogen-containing bisphosphonate, for the treatment of osteoporosis.

机译:阿仑膦酸盐(一种含氮的双膦酸盐)新型透皮贴剂的开发,用于治疗骨质疏松症。

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摘要

Bisphosphonates are widely used for the treatment and prevention of bone diseases, including Paget disease, hypercalcemia of malignancy, and postmenopausal osteoporosis. In this study, we developed a novel transdermal patch of alendronate, a nitrogen-containing bisphosphonate, for the treatment of bone diseases. The maximum permeation fluxes of alendronate through rat and human skin after application of this patch were 1.9 and 0.3 microg/cm(2) per hour, respectively. The bioavailability (BA) of alendronate in rats was approximately 8.3% after the application of alendronate patch and approximately 1.7% after oral administration. These results indicated that the transdermal permeation of alendronate using this patch system was sufficient for the treatment of bone diseases. The plasma calcium level was effectively reduced after application of the alendronate patch in 1alpha-hydroxyvitamin D(3) -induced hypercalcemia model rats. The alendronate patch also effectively suppressed the decrease in bone mass in model rats with osteoporosis. Modest alendronate-induced erythema of rat skin was observed after application of the alendronate patch. Incorporation of butylhydroxytoluene in the alendronate patch almost completely suppressed this alendronate-induced skin damage while maintaining the transdermal permeation and pharmacologic effects of alendronate. These findings indicate that our novel transdermal delivery system for alendronate is a promising approach to improve compliance and quality of life of patients in the treatment of bone diseases.
机译:双膦酸盐广泛用于治疗和预防骨骼疾病,包括Paget病,恶性血钙过多和绝经后骨质疏松症。在这项研究中,我们开发了一种新型的阿仑膦酸盐透皮贴剂(一种含氮的双膦酸盐),用于治疗骨疾病。应用此贴剂后,阿仑膦酸盐通过大鼠和人类皮肤的最大渗透通量分别为每小时1.9和0.3 microg / cm(2)。阿仑膦酸盐贴剂施用后在大鼠中的生物利用度(BA)约为8.3%,口服后约为1.7%。这些结果表明,使用该贴剂系统的阿仑膦酸盐透皮渗透足以治疗骨疾病。在1alpha-羟基维生素D(3)诱导的高钙血症模型大鼠中应用阿仑膦酸盐贴剂后,血浆钙水平有效降低。阿仑膦酸盐贴剂还有效地抑制了骨质疏松模型大鼠的骨量减少。应用阿仑膦酸盐贴剂后,观察到适度的阿仑膦酸盐诱发的大鼠皮肤红斑。在阿仑膦酸盐贴剂中掺入丁基羟基甲苯几乎完全抑制了阿仑膦酸盐引起的皮肤损害,同时保持了阿仑膦酸盐的透皮渗​​透和药理作用。这些发现表明,我们新颖的阿仑膦酸盐透皮给药系统是一种有前途的方法,可以改善治疗骨病患者的依从性和生活质量。

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