Comparative in vivo constituents and pharmacokinetic study in rats after oral administration of ultrafine granular powder and traditional decoction slices of Chinese Salvia

Abstract

Salvia miltiorrhiza, one of the most well-known herbal medicines, is commonly used for the treatment of coronary heart diseases in China. Besides traditional decoction slices (TDS), another relatively new product of S. miltiorrhiza, ultrafine granular powder (UGP; D90 < 45 μm), is also increasingly being used. In this paper, a UHPLC-LTQ-Orbitrap MS technique was developed for a metabolite profile study after oral administration of UGP and TDS of S. miltiorrhiza. The results showed that the number of in vivo absorbed compounds from UGP was much greater than that from TDS, and different types of products from S. miltiorrhiza will have different metabolic processes in vivo. Furthermore, a UHPLC-Q-Trap MS/MS method for simultaneously determining four tanshinones (tanshinone IIA, dihydrotanshinone I, tanshinone I and cryptotanshinone) was established and applied to assess the pharmacokinetics of the two types of products. All of the analytes displayed significant higher area under the concentration-time curve and peak concentration after oral administration of UGP than after TDS, indicating that ultrafine powder product could improve the bioavailability and absorption of cryptotanshinon,tanshinone II A,dihydrotanshinonE I and tanshinone I in vivo. The present study provides scientific information for further exploration of the pharmacology of these two types of S. miltiorrhiza and offers a reference for clinical administration of S. miltiorrhiza.

Immunomodulatory effects of a new whole ingredients extract from Astragalus: a combined evaluation on chemistry and pharmacology

“…The chemical integrity of the UFP could be well retained, and presented a high correlation coefficient to that of the herbal decoction pieces [5]. Moreover, the bioavailabilities of the active compounds in UFP were investigated to be higher than those in normal herbal powders because of their quick and completed dissolution from the UFP [6, 7]. The advantages of UFP allows a lower dose unit in a single dosage thus improving the compliance in clinical applications.…”

“…The ultrafine grinding provides UFP nice surface properties such as the higher dispersibility and specific surface area [3], thus presenting better therapeutic efficacy of the herbs [4]. Moreover, UFP retains higher integrity in chemical composition keeping both water-soluble and alcohol-soluble ingredients [5] and improves their dissolution and absorption in gastrointestinal tract [6, 7]. However, the safety problems of UFP have raised attention [8].…”

Salvia miltiorrhiza Bge. (Danshen) in the Treating Non-alcoholic Fatty Liver Disease Based on the Regulator of Metabolic Targets

“…resulting in low bioavailability of tanshinones. Similar to phenolic acids, the ultrafine powder and solid lipid nanoparticles formulations could improve the bioavailability of CT, TSIIA, TI, and TSI by enhancing their stability and permeability (60)(61)(62). On the other hands, components in tanshinone extracts also affected the pharmacokinetics of monomer constituents.…”

Influence Factors of the Pharmacokinetics of Herbal Resourced Compounds in Clinical Practice

“…Different from traditional processing, new methods like ultrafine powders of Chinese herbs (D 90 < 45 μ m) have made great progress in clinical use for their convenience for carrying and oral administration [ 30 ]. As the pulverized herbal medicine owns a relatively larger surface area than traditional applied forms, bioavailability of many constituents in vivo increased [ 30 , 31 ]. Consequently, this feature will help patients in taking lower dosage of herbal medicine in prescriptions and saving cost, which may improve medication compliance to ensure therapeutic effects…”