Key Laboratory of Xin' an Medicine Ministry of Education, Anhui Province Key Laboratory of Chinese Medicinal Formula, Anhui University of Traditional Chinese Medicine, Hefei, 230038, Anhui, People's Republic of China.
Anhui Province Key Laboratory of Pharmaceutical Technology and Application, Anhui University of Traditional Chinese Medicine, Hefei, 230038, Anhui, People's Republic of China.
AAPS PharmSciTech. 2020 Nov 10;21(8):316. doi: 10.1208/s12249-020-01840-8.
Borneol can enhance the bioavailability of several other drugs by opening the blood-brain barrier and inhibiting P-glycoprotein (P-gp) efflux. However, whether borneol will impact the bioavailability and the mechanism of compound Danshen colon-specific osmotic pump capsule (CDCOPC) remains unclear. This study aimed to determine the effects of borneol on the in vitro release and in vivo pharmacokinetic characteristics of CDCOPC. Besides, the in vitro release behavior of CDCOPC was further assessed by chromatographic fingerprints. The in vitro release studies showed that borneol followed the zero-order release and hardly impacted the in vitro release of Salvia miltiorrhiza and Panax notoginseng in CDCOPC. Moreover, as revealed from the similarity results of fingerprints, the in vitro release of different components of CDCOPC was almost simultaneous. Compared with the commercially available tablets, the pharmacokinetics studies suggested that both CDCOPCs containing and lacking borneol could significantly prolong the retention time of these effective components; their average relative bioavailability values increased to 448.70% and 350.97%, respectively. Notably, borneol significantly improved the relative bioavailability of some components of CDCOPC, such as salvianolic acid B (SAB), tanshinone IIA (Tan IIA), notoginsenoside R (R), ginsenoside Rg (Rg), and ginsenoside Re (Re) from CDCOPC, while it slightly impacted ginsenoside Rb (Rb) and ginsenoside Rd (Rd). Summarily, borneol is capable of improving the bioavailability of some effective components in CDCOPC, which is critical to design with CDCOPC for enhanced bioavailability. This study could also help reveal the composition principle of the compound Danshen formula (CDF).
龙脑可以通过打开血脑屏障和抑制 P 糖蛋白（P-gp）外排来提高几种其他药物的生物利用度。然而，龙脑是否会影响化合物丹参结肠靶向渗透泵胶囊（CDCOPC）的生物利用度和机制尚不清楚。本研究旨在确定龙脑对 CDCOPC 的体外释放和体内药代动力学特征的影响。此外，还通过色谱指纹图谱进一步评估了 CDCOPC 的体外释放行为。体外释放研究表明，龙脑遵循零级释放，几乎不会影响 CDCOPC 中丹参和三七的体外释放。此外，从指纹图谱的相似度结果可知，CDCOPC 不同成分的体外释放几乎是同时的。与市售片剂相比，药代动力学研究表明，含有和不含龙脑的 CDCOPC 都能显著延长这些有效成分的滞留时间；它们的平均相对生物利用度值分别增加到 448.70%和 350.97%。值得注意的是，龙脑显著提高了 CDCOPC 中一些成分的相对生物利用度，如丹酚酸 B（SAB）、丹参酮 IIA（Tan IIA）、三七皂苷 R（R）、人参皂苷 Rg（Rg）和人参皂苷 Re（Re），而对人参皂苷 Rb（Rb）和人参皂苷 Rd（Rd）的影响较小。总之，龙脑能够提高 CDCOPC 中一些有效成分的生物利用度，这对于设计具有增强生物利用度的 CDCOPC 至关重要。本研究还有助于揭示复方丹参配方（CDF）的组成原理。
