Ito Yukako, Ohashi Yoshinori, Shiroyama Keiji, Sugioka Nobuyuki, Takada Kanji
Department of Pharmacokinetics, Kyoto Pharmaceutical University, Kyoto, Japan.
Biol Pharm Bull. 2008 Aug;31(8):1631-3. doi: 10.1248/bpb.31.1631.
The feasibility of self-dissolving micropiles (SDMP) as a percutaneous delivery system of recombinant human growth hormone (rhGH) has been studied in rats using SDMP where dextran was used as a base. After mixing dextran solution with rhGH, SDMPs were prepared by pulling with polypropyrene tips. The mean weight, length and diameter were 0.68+/-0.05 mg, 3.2+/-0.5 mm and 0.6+/-0.2 microm, respectively. To evaluate the bioavailability (BA) of rhGH percutaneously administered by SDMP, an absorption experiment was performed in rats. RhGH SDMPs were inserted into the rats skin, 200 microg kg(-1), and plasma rhGH levels were measured by an ELISA method. Peak plasma rhGH level, 132.8+/-11.8 ng ml(-1), appeared at 0.8+/-0.2 h. By comparing the plasma rhGH levels vs. time profiles after the administration of SDMP and intravenous injection of rhGH solution, 5 microg kg(-1), BA of rhGH from SDMP was calculated to be 87.5%. Theses results may suggest that SDMP can be used as a novel percutaneous drug delivery system.
在大鼠中研究了以葡聚糖为基质的自溶性微针（SDMP）作为重组人生长激素（rhGH）经皮给药系统的可行性。将葡聚糖溶液与rhGH混合后，用聚丙烯尖端拉制成SDMP。其平均重量、长度和直径分别为0.68±0.05mg、3.2±0.5mm和0.6±0.2μm。为评估SDMP经皮给药rhGH的生物利用度（BA），在大鼠中进行了吸收实验。将rhGH SDMP以200μg kg-1的剂量插入大鼠皮肤，并通过ELISA法测量血浆rhGH水平。血浆rhGH峰值水平为132.8±11.8ng ml-1，出现在0.8±0.2小时。通过比较SDMP给药和静脉注射5μg kg-1 rhGH溶液后血浆rhGH水平随时间的变化曲线，计算出SDMP中rhGH的BA为87.5%。这些结果可能表明SDMP可作为一种新型的经皮给药系统。
