Abstract
Clinico-pharmacological and pharmacokinetic studies on trans-4- (2-amino-3, 5-dibromobenzylamino) cyclohexanol hydrochloride (NA 872) which is a metabolite of Bromhexine (Bisolvon), an expectorant, were carried out in ten healthy male volunteers.
Seven volunteers were administered orally 5, 10, 20 and 30 mg of NA 872 in each 2 subjects, and three volunteers received three times of 15 mg a day for three days.
The increases of bowel sounds and the slight increases of dermal blood flow were observed in some volunteers after administration of drug. On the other hand, there were no definite changes in heart rate, blood pressure, respiration, GSR, and ECG and laboratory findings.
Analysis of the drug in blood and urine with gas chromatography and pharma cokinetics revealed that NA 872 given orally was well absorbed, and excreted rapidly, and that the majority of main part of the drug was excreted as NA 872 conjugate and a small part was metabolized to NA 873 and dibromoanthranilic acid.
In conclusion, it can be said that blood levels in repeated medication agreed with the estimated values on the basis of single medication, and there was no tendency of accumulation of the drug.
