Preparation, Characterization Evaluation of Tanshinone IIA Lipid Microspere and Comparative Study of Pharmacokinetics with Sodium Tanshinone IIA Sulfonate Injection

Abstract:

In this study, Tanshinone IIA lipid microspere (Tan-IIA-LM) was successfully prepared by an ultrasonic and high-pressure homogenization method. The particle size, zeta potential, drug entrapment efficiency and morphological properties of Tan-IIA-LM were characterized in detail. A pharmacokinetic comparative study of Tan-IIA-LM with Sodium Tanshinone IIA Silate (STS) injection was developed. A sensitive and specific HPLC method was established to determine the mass concentration of Tan-IIA and STS in rats plasma samples which were compared between Tan-IIA-LM and STS injection after single dose intravenous administration of 18.35μmol/kg and the results were fitted and analyzed by dedicated software. After intravenous administration, the AUC_0- and C_max values of Tan-IIA were 2.14, 2.22 fold higher than STS. The clearance, apparent volume of distribution and mean residence time (MRT) of Tan-IIA were lower (P<0.01) than STS; other pharmacokinetic parameters had no significant deviation (P>0.05). The pharmacokinetic of Tan-IIA, STS have significant differences at the same molar doses and the AUC and C_max values of Tan-IIA were higher compared with STS.

• Periodical: Advanced Materials Research (Volumes 781-784)
• Pages: 1044-1051
• DOI: https://doi.org/10.4028/www.scientific.net/AMR.781-784.1044
• Online since: September 2013
• Authors: Xin Li Liang*, Meng Liang Zhu, Yun Chao Cao, Guo Wei Zhao, Qie Ying Jiang, Li Jun Zhao, Zheng Gen Liao
• Keywords: Lipid Microsphere, Pharmacokinetic, Sodium Tanshinone IIA Sulfonate, Tanshinone IIA

References

[1] T. Chu, Q. Zhang, H. Li, W.C. Ma, N. Zhang, H. Jin and S.J. Mao: International journal of pharmaceutics. Vol. 424 (2012), p.76.

[2] J. Li, P. Liu, J.P. Liu, W.L. Zhang, J.K. Yang and Y.Q. Fan: European Journal of Pharmaceutics and Biopharmaceutics. Vol. 80 (2012), p.426.

[3] T.O. Cheng: Int.J. Cardiol. Vol. 121 (2007), p.9.

[4] National Pharmacopoeia Committee: Pharmacopoeia of People's Republic of China. Part 2. (China Medical Science Press, China, 2005).

[5] X.J. Pu and K.L. Xu.: Clinical Medical Engineering. Vol. 16 (2009), p.154.

[6] E.H. Cao, X.Q. Liu, J.J. Wang and N.F. Xu: Free Radic. Biol. Med. Vol. 20 (1996), p.801.

[7] X. Dong, J. Dong, R. Zhang, L. Fan and G. Wu: Cancer Biother. Radiopharm. Vol, 24 (2009a). p, 681.

[8] G.W. Fan, X.M. Gao, H. Wang, Y. Zhu, J. Zhang, L.M. Hu, Y.F., Su, L.Y. Kang and B.L. Zhang:J. Steroid Biochem. Mol. Biol. Vol. 113 (2009), p.275.

[9] P. N, Chang, J.C. Mao, S.H. Huang, L. Ning, Z.J. Wang, T. On, W., Duan and Y.Z. Zhu: J. Pharmacol. Sci. Vol. 101 (2006), p.245.

[10] D. Sun, M. Shen, W. Li, Y. Zhang, L. Zhao, Z. Zhang, Y. Yuan, H. Wang and F. Cao. Cardiovasc Diabetol. Vol. 10 (2011), p.4.

[11] K. Dong, W. Xu, J. Yang, H. Qiao and L. Wu; Phytother. Res. Vol, 23 (2009b). p, 608.

[12] M. Liu, X. Xia: Chin. Med. Mater. Vol. 33 (2010), p.606.

[13] H. Xiao, M.X. Shong, J. Lai: Chinese Traditional Patent Medicine. Vol. 27 (2005), p.953.

[14] X.J. Zhang, D.K. Wang, J.M. Yao and X. Han: Chinese Journal of Pharmaceutics. Vol, 8(2010), p.117.

[15] F.F. Kong, X. Q Tan, L.J. Guo and M. Q Fu.: China Pharmacy. Vol. 22 (2011), p.3339.

[16] L.H. Li, Z.F. Sun and X.B. Li: Practical Pharmacy and Clinical Remedies. Vo. l13 (2010), p.55.

[17] W. Qu, Q.H. Cheng and B.Q. Zhu: Chin Pharm J. Vol. 36 (2001), p.724.

[18] T.P. Norden, B. Siekmann and S. Lundquist: Eur.J. Pharm Sci. Vol. 13 (2001), p.393.

[19] J. Medina, A. Salvado and A. Pozo: Int.J. Pharm. Vol. 216 (2001), p.1.

[20] T. Yamaguchi and Y Mizushima: Critical Reviews in Therapeutic Drug Carrier Systems. Vol. 11 (1994), p.215.

[21] P. Sharma. M.V.S. Varma., H.P.S. Chawla and R. Panchagnula: IIFarmaco. Vol. 60 (2005), p.874.

[22] B. Liu: New techniques and new dosage forms of drugs (People's Medical Publishing House, China, 2002).