Different Effects of Traditional Chinese Medicines Containing Similar Herbal Constituents on Prednisolone Pharmacokinetics

1. MASATO HOMMA^1,*,
2. KITARO OKA¹,
3. KEN IKESHIMA¹,
4. NORIYUKI TAKAHASHI^1,2,
5. TOMOYUKI NIITSUMA^1,3,
6. TOSHIAKI FUKUDA^1,3,
7. HISAO ITOH^1,3

Article first published online: 12 APR 2011

DOI: 10.1111/j.2042-7158.1995.tb05861.x

Abstract

Three major traditional Chinese medicines (TCM), Sho-saiko-To, Saiboku-To, and Sairei-To, consist of similar herbal prescriptions containing glycyrrhizin, which is a strong inhibitor of 11β-hydroxysteroid dehydrogenase. We performed cross-over open trials in healthy subjects to clarify prednisolone pharmacokinetics on co-administration of these preparations.

All subjects received a single oral dose of 10 mg prednisolone before oral treatment with one of the test preparations. After a 2-week wash-out interval, they received one of the test preparations for three days at daily doses of 7·5 or 9·0 g. On the third study day, 10 mg prednisolone was administered orally in combination with the test preparation. Area under the curves (AUC) of prednisolone before and after the treatment decreased from 0·94 to 0·78 mg h L⁻¹ (P < 0·05) in the Sho-saiko-To group, increased from 0·92 to 1.06 mg h L⁻¹ (P < 0·01) in the Saiboku-To group, and did not change in the Sairei-To group. AUC ratios of prednisone and prednisolone, which reflect the 11β-hydroxysteroid dehydrogenase activity, increased in the Sho-saiko-To group (P < 0·01), decreased in the Saiboku-To group (P < 0·01), and did not change in the Sairei-To group after the treatments. Similar results were observed in ratios of endogenous cortisone to cortisol.

Because of the equal glycyrrhizin content in all three preparations, it was unexpected that the 11β-hydroxysteroid dehydrogenase effect was different amongst the three groups. These observations suggest that some unknown metabolic enzyme modifiers, promoters or inhibitors, may be involved in these traditional treatments.