Baldwin J R, Carrano R A, Imondi A R
J Pharm Sci. 1984 Jul;73(7):1002-4. doi: 10.1002/jps.2600730739.
Studies to determine the extent of local tissue penetration of topically applied trolamine [14C]salicylate were conducted in domestic pigs. The preparation was applied onto a 100-cm2 shaved area of skin overlying the biceps femoris at a concentration of 0.7 mg of salicylate/cm2 to closely approximate the actual use in humans. At least 82% of the topically applied trolamine salicylate was absorbed over a 2-h period. Based on blood and muscle salicylate levels, a localization of the absorbed drug occurred in muscle underlying the treated area within 120 min. Muscle from the treated area had a concentration of salicylate that was 13 times that of blood and 49 times that of muscle taken from untreated areas. Blood samples taken from the treated area at 10, 20, and 30 min showed that salicylate levels ranged from 15.8 to 5.3 micrograms/g. Less than 0.5% of the applied drug was excreted in the urine during the 2-h period.
在家猪身上进行了研究，以确定局部应用的三乙醇胺[¹⁴C]水杨酸盐在局部组织中的渗透程度。将该制剂以0.7mg水杨酸盐/cm²的浓度涂抹在覆盖股二头肌的100cm²剃毛皮肤上，以紧密模拟人类的实际使用情况。在2小时内，至少82%的局部应用三乙醇胺水杨酸盐被吸收。根据血液和肌肉中的水杨酸盐水平，吸收的药物在120分钟内在治疗区域下方的肌肉中发生定位。治疗区域的肌肉中水杨酸盐浓度是血液的13倍，是未治疗区域肌肉的49倍。在10、20和30分钟时从治疗区域采集的血样显示，水杨酸盐水平在15.8至5.3微克/克之间。在2小时内，少于0.5%的应用药物从尿液中排出。
