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Vol.3 , No. 1, Publication Date: May 9, 2018, Page: 16-21
 in heart was 659.653±200.689 for lipidosome formulation while 586.67±46.635 for reference formulation, the difference was statistically significant, obviously, intake of ligustrazine phosphate in lipidosome formulation achieved more in heart. As for plasma distribution, the Tmax of lipidosome formulation was longer than reference formulation, so ligustrazine phosphate was assimilated slowly in lipidosome formulation. The AUC (0-∞) and Cmax were 784.078±196.337 and 13.103±3.216 in lipidosome formulation, respectively. Brain was distributed more when ligustrazine phosphate was in lipidosome formulation. Undisputedly, this act could contribute to the effective treatment. <i>Conclusion:</i> The ligustrazine phosphate lipidosome formulation improves the ligustrazine phosphate bioavailability and brain targeting.&picture=http://www.aascit.org/aascit/decorators/img/journal/832.jpg)
| [1] | Li Siqi, College of Chinese Medicine, Hebei University, Baoding, Hebei, China. |
| [2] | Yi Xuetao, Qingdao Institute for Food and Drug Control, Qingdao, Shandong, China. |
| [3] | Li Linfeng, College of Chinese Medicine, Hebei University, Baoding, Hebei, China. |
| [4] | Wu Haonan, College of Chinese Medicine, Hebei University, Baoding, Hebei, China. |
| [5] | Li Xuanze, First Hospital Affiliated to Tianjin Medical University, Tianjin, China. |
| [6] | Xin Lili, Qingxian County People's Hospital, Cangzhou, Hebei, China. |
| [7] | Zhang Guowei, College of Chinese Medicine, Hebei University, Baoding, Hebei, China. |
Objective: To research the ligustrazine phosphate Liposome bioavailability and brain targeting by study the pharmacokinetics and tissue distribution of ligustrazine phosphate liposome in Rats. Methods: 48 Rats were intravenous injected ligustrazine phosphateand its ligustrazine phosphate Liposome. The dose level was 50 mg/kg, after the administration, blood was collected at 0.083h, 0.25h, 0.5h, 1h, 2h, 4h, 5h, at terminal time points, heart, liver, spleen, lung, kidney, and brain were excised. All samples were detected with LC/MS/MS method. Pharmacokinetic parameters were calculated with DAS 2.1.1 software using non-compartmental analysis. Results: No significant difference of pharmacokinetics parameters in blood were existed between the reference formulation and lipidosome formulation. The mean AUC 0-∞ (mg/L*min) in heart was 659.653±200.689 for lipidosome formulation while 586.67±46.635 for reference formulation, the difference was statistically significant, obviously, intake of ligustrazine phosphate in lipidosome formulation achieved more in heart. As for plasma distribution, the Tmax of lipidosome formulation was longer than reference formulation, so ligustrazine phosphate was assimilated slowly in lipidosome formulation. The AUC (0-∞) and Cmax were 784.078±196.337 and 13.103±3.216 in lipidosome formulation, respectively. Brain was distributed more when ligustrazine phosphate was in lipidosome formulation. Undisputedly, this act could contribute to the effective treatment. Conclusion: The ligustrazine phosphate lipidosome formulation improves the ligustrazine phosphate bioavailability and brain targeting.
Keywords
Ligustrazine Phosphate, Liposome, Rats, Pharmacokinetics, Tissue Distribution
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