Effects of Borneol on the Release of Compound Danshen Colon-Specific Osmotic Pump Capsule In Vitro and Pharmacokinetics
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Research Article Effects of Borneol on the Release of Compound Danshen Colon-Specific Osmotic Pump Capsule In Vitro and Pharmacokinetics Study in Beagle Dogs Liangyu Shao,1,2,3 Chaojie Sun,1,2,3 Wenjie Lu,4 Jiayi Chen,5 Dan Su,6 Song Gao,1,2,3 Shengqi Chen,1,2,3 Wenyou Fang,1,2,3 Yu Liu,1,2,3 Bin Wang,1,2,3,8 and Rongfeng Hu1,2,3,7,8
Received 26 May 2020; accepted 7 October 2020 Abstract. Borneol can enhance the bioavailability of several other drugs by opening the bloodbrain 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 R1 (R1), ginsenoside Rg1 (Rg1), and ginsenoside Re (Re) from CDCOPC, while it slightly impacted ginsenoside Rb1 (Rb1) 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).
Liangyu Shao and Chaojie Sun contributed equally to this work. Bin Wang and Rongfeng Hu were considered as co-corresponding authors 1
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. 2 Anhui Province Key Laboratory of Pharmaceutical Technology and Application, Anhui University of Traditional Chinese Medicine, Hefei, 230038, Anhui, People’s Republic of China. 3 Anhui Province Key Laboratory of R&D of Chinese Medicine, Anhui University of Traditional Chinese Medicine, Hefei, 230038, Anhui, People’s Republic of China. 4 School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, Jiangsu, China. 5 Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John’s University, New York, New York 11439, USA. 6 Depart
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