Comparative Pharmacokinetics and Bioavailability of Epimedin C in Rat after Intramuscular Administration of Epimedin C, a Combination of Four Flavonoid Glycosides and Purified Herba Epimedii Extract

Abstract

Chuan-Ke-Zhi (CKZ), a purified Herba Epimedii extract, is a potent Chinese medicine preparation whose main bioactive components are a class of flavonoid glycosides such as epimedins A, B, and C and icariin. And epimedin C is far more abundant than other flavones in this extract. This study aims to investigate the pharmacokinetic and bioavailability of epimedin C and what effects, if any, other ingredients in CKZ have on its pharmacokinetics. Epimedin C, CKZ, and a combination of epimedins A, B, and C and icariin were, respectively, administrated to rats, and then the pharmacokinetic parameters of epimedin C in the three groups were calculated and compared. The result indicated that CLZ, MRT0–∞, and AUC0–∞ of epimedin C were significantly different among the three groups (P < 0.05), and compared with the epimedin C group, the absorption of epimedin C significantly increased in the CKZ group. Furthermore, in this study the absolute bioavailability of epimedin C was also investigated by comparing intramuscular and intravenous administration of epimedin C. As a result, epimedin C could be quickly absorbed with extremely high absolute bioavailability after intramuscular administration.

Comparative Effectiveness and Safety of Seven Qi-Tonifying Chinese Medicine Injections for AECOPD Patients: A Systematic Review and Network Meta-Analysis

“…Regarding the administration ways, intravenous mode was the preferred mode of administration (6 studies), followed by intermuscular administration (1 study). Different ways of administration may lead to difference in their bioavailability [ 19 ]. In order to get better effect, physicians should adjust the administration strategies timely according to individualized treatment.…”

“…According to TCM theory, the pathological basis of AECOPD is “exterior excess and interior deficiency.” Qi deficiency runs through the process of AECOPD development, which means qi-tonifying strategy is one of the most important treatment options for AECOPD [ 17 ]. Coupled with the high bioavailability of injections [ 18 , 19 ], multiple qi-tonifying injections were widely used. However, some existing evidence demonstrated that different types of qi-tonifying injections varied in their mechanism of action and clinical efficacy [ 20 – 22 ].…”

Study of Absorption Characteristics of the Total Saponins from Radix Ilicis Pubescentis in an In Situ Single-Pass Intestinal Perfusion (SPIP) Rat Model by Using Ultra Performance Liquid Chromatography (UPLC)

“…Numerous studies have proven that administration of a natural material in a TCM extract formulation results in higher plasma concentration and oral bioavailability than when administered as a monomer [ 11 , 25 , 26 , 27 , 28 , 29 ]. Consequently, this feature of TCMs can explain why some categories of ingredients, such as flavonoids or pentacyclic triterpenoid saponins, have good efficacy and broad clinical applications despite unsatisfactory pharmaceutical properties, i.e., poor solubility, poor stability, and inappropriate lipid solubility.…”

Evidence Construction of Chuankezhi Injection Against Chronic Obstructive Pulmonary Disease: A Systematic Review and Network Pharmacology

“…and Morinda officinalis F.C.How. 10 These medicines are originated from the Shen Nong Ben Cao Jing, in which Epimedium sagittatum (Sieb. et Zucc.)…”