Miska W, Geiger R, Schill W B
Dept. of Dermatology and Andrology, University Giessen, Germany.
Agents Actions Suppl. 1992;38 ( Pt 2):136-43.
Porcine pancreatic kallikrein (PPK), the main component of Padutin (Bayropharm, FRG), is used since 1974 for the treatment of some forms of idiopathic infertility in man. During kallikrein therapy the number of spermatozoa increases, and qualitative and quantitative sperm motility is improved. In order to investigate the intestinal absorption of PPK in man a clinical study with 7 healthy volunteers was performed. 4500 KE (corresp. to 2.8 mg PPK) and 600 KE (corresp. to 0.38 mg PPK) of kallikrein respectively was orally administered in one dosis. Serum and urine samples were collected several times within 24 hours. Seminal plasma was collected 4-5 days before and 8 hours after treatment with kallikrein. Absorbed PPK was determined using a highly sensitive bioluminescence-enhanced enzyme immunoassay (1) and a newly developed light measuring equipment (MTP reader) (3). The limit of detection was 1 pg/ml in serum corresponding to 6 amol PPK per assay. For both groups (600 KE and 4500 KE) absorption of PPK in serum was found. Maximum absorption was observed between 4 and 12 h and between 2 and 6h, respectively, after oral application of kallikrein. Renal excretion plays no important role in the elimination of PPK from serum. In gel filtration experiments with blood samples of volunteers in which absorbed PPK was detected, one peak of immunochemically active material corresponding to a molecular mass of 82 kDa was found. According to our results, kallikrein is absorbed in unaltered form by the intestine.(ABSTRACT TRUNCATED AT 250 WORDS)
猪胰激肽释放酶(PPK)是Padutin(德国拜耳制药公司生产)的主要成分,自1974年以来一直用于治疗人类某些形式的特发性不孕症。在激肽释放酶治疗期间,精子数量增加,精子的质和量的活力都得到改善。为了研究PPK在人体中的肠道吸收情况,对7名健康志愿者进行了一项临床研究。分别一次性口服给予4500激肽释放酶单位(相当于2.8毫克PPK)和600激肽释放酶单位(相当于0.38毫克PPK)。在24小时内多次采集血清和尿液样本。在激肽释放酶治疗前4 - 5天和治疗后8小时采集精浆样本。使用高灵敏度的生物发光增强酶免疫测定法(1)和新开发的光测量设备(MTP读数仪)(3)测定吸收的PPK。血清中的检测限为1皮克/毫升,每次测定相当于6阿托摩尔PPK。在两组(600激肽释放酶单位和4500激肽释放酶单位)中均发现血清中有PPK吸收。口服激肽释放酶后,分别在4至12小时和2至6小时观察到最大吸收。肾脏排泄在血清中PPK的消除过程中不起重要作用。在对检测到吸收有PPK的志愿者血样进行的凝胶过滤实验中,发现了一个免疫化学活性物质峰,其分子量对应于82千道尔顿。根据我们的结果,激肽释放酶以未改变的形式被肠道吸收。(摘要截短至250字)