Klemsdal T O, Gjesdal K, Bredesen J E
Oslo University Hospital Ullevål, Department of Cardiology, Norway.
Eur J Clin Pharmacol. 1992;43(6):625-8. doi: 10.1007/BF02284961.
19 healthy volunteers wore a nitroglycerin patch releasing 10 mg per 24 h for 2 h. Subsequently, the skin area surrounding the patch was exposed to 15 min of local heating with an infrared bulb (Group A, n = 10), or local cooling with an ice-pack (Group B, n = 9). The patch was protected by an insulating shield (Styrofoam). After 10 min of heating, the median (Walsh) plasma nitroglycerin level increased from 3.1 to 7.6 nmol.l-1. Body temperature remained constant. After 15 min of cooling the median plasma level had dropped from 2.1 to 1.4 nmol.l-1. The results demonstrate that changes in skin temperature may cause extensive short-term changes in the bioavailability of nitroglycerin. Presumably, a subcutaneous or cutaneous reservoir builds up during transdermal treatment, and changes in regional cutaneous blood flow affect the rate of drainage from the reservoir into the systemic circulation.
19名健康志愿者佩戴每24小时释放10毫克硝酸甘油的贴片2小时。随后,贴片周围的皮肤区域用红外灯进行15分钟的局部加热(A组,n = 10),或用冰袋进行局部冷却(B组,n = 9)。贴片用隔热罩(泡沫聚苯乙烯)保护。加热10分钟后,(沃尔什)血浆硝酸甘油水平中位数从3.1纳摩尔/升升至7.6纳摩尔/升。体温保持恒定。冷却15分钟后,血浆水平中位数从2.1纳摩尔/升降至1.4纳摩尔/升。结果表明,皮肤温度变化可能导致硝酸甘油生物利用度出现广泛的短期变化。据推测,经皮治疗期间会形成皮下或皮肤贮库,局部皮肤血流的变化会影响贮库向体循环引流的速度。