Objective : The purpose of this study is to search for more effective administraion route of herbal medicine. Methods : Pharmacokinetic issues with the methods in experimental papers, which deal with finding the effectiveness of two or more administration routes of herbal medicine, searched from KERIS, KSI, KISTI and KTKP, have been analyzed by, first, categorizing the papers and comparing the validity of administration routes. Results and Conclusions : 1. Upon comparing in total of 24 papers on the basis of each administration route, per oral(PO)-herbal acupuncture(HA) was most superior in terms of number in that there were 13 cases and PO-per rectal(PR) was next superior in that there were 5 cases. PO-per dermal(PD)-inhalation therapy(IT), PO-IT and PO-PR-HA had 3, 2 and 1 cases respectively. 2. Out of the total 24 papers which compares different administration routes, 16 of them were pharmacokinetically appropriate, whereas, the remaining 8 were pharmacokinetically inappropriate. 3. Comparisons were made between PO-HA, PO-PR, PO-IT, PO-PD-IT and PO-PR-HA routes. However, none of them was not particularly effective regardless of the administered medicine or target organ. 4. No route was particularly effective against a particular drug target as a result of comparing damaged liver, asthma, endometriosis and anti-inflammation. 5. In the case of Injinhotang in medicine comparison, HA tended to be more associated with hepatotoxicity over PO. However, Cordyceps Militaris Mycelia, Gagamsohaphyangwon and Hongdeungtang showed no prominent effective administration route.