Abstract: A new water-soluble form of the calcium blocker nifedipine (NF) with glycyrrhizic acid (GA) (with molecular ratio 1:4) has been obtained by mechanochemical synthesis. Its pharmacological advantages in comparison with nifedipine were determined. An effective dose of nifedipine in complex reduced to 10 times as compared to its therapeutic dose while high antihypertensive activity preservation and pleiotropic antiarhythmic activity enhancement. This new antihypertensive and antiarhythmic agent (complex of NF:GA = 1:4) is chemically stable and safe for parenteral administration.
Reference: Tolstikova T.G., Khvostov M.V., Bryzgalov A.O., Dushkin A.V., Meteleva E.S., Improvement of pharmacological values of the nifedipine by means of mechanochemical complexation with glycyrrhizic acid, Biomeditsinskaya khimiya, 2010, vol:
1. Loftsson Th., Brewster M.E., Mason M. (2004) Amer. J. Drug Deliv., 2(4),266-275.
2. Challa R., Ahuja A., Ali J., Khar R.K. (2005) AAPS Pharm. Sci. Tech., 6(2), article 43.
3. Loftsson Th., Duchene D. (2007) Int. J. Pharm., 329, 1-11.
4. Cilurzo F., Minghetti P., Casiraghi A., Montanari L. (2002) Int. J. Pharm., 242, 313-317. CrossRef
5. Vippagunta S.R., Maul K.A., Tallavajhala S., Grant D.J.W. (2002) Int. J. Pharm., 236, 111-123. CrossRef
6. Portero A., Remuтґan-Lґopez C., Vila-Jato J.L. (1998) Int. J. Pharm., 175, 75-84. CrossRef