Physicochemical and biological studies of a new erythromycin derivate - erythromycin folate

Authors

  • PK MANNA Department of Pharmacy, Annamalai University, Annamalai Nagar, Tamil Nadu 608002, India
  • V KUMARAN Department of Pharmacy, Annamalai University, Annamalai Nagar, Tamil Nadu 608002, India
  • GP MOHANTA Department of Pharmacy, Annamalai University, Annamalai Nagar, Tamil Nadu 608002, India

Keywords:

Erythromycin folate, In vitro antimicrobial activity, In vivo serum concentration, pharmacokinetic parameters

Abstract

A new derivative of erythromycin, Erythromycin folate was prepared and its physicochemical andbiological properties were evaluated. The derivative has good solubility in methanol, ethanol and propyleneglycol. The partition coefficient values of 1.12 and 1.10 in chloroform/water and octanol/water systemsrespectively indicate that the derivative will probably distribute well in vivo. The in vitro potency ofthe derivative, 716 μg/mg, is higher than the existing derivatives like erythromycin estolate, erythromycinstearate, erythromycin ethyl succinate, erythromycin gluceptate, and erythromycin lactobionate. The invitro Minimum Inhibitory Concentrations are less for the derivative than the base against Klebsiellapneumonia, Pseudomonas aeruginasa, Bacillus pumilis and Escherichia coli. The in vivo pharmacokineticparameters of the derivative in rabbits are as follows: the elimination half life, t½ is 117.45 min for thederivative while it is 150.45 min for erythromycin base the reference standard. The volume of distributionVd is 177.56% and 352.20% for the derivative and erythromycin base respectively. The results of thepresent investigations indicate that erythromycin folate has a high potential for possible clinical application.

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Published

2004-12-20

How to Cite

1.
MANNA P, KUMARAN V, MOHANTA G. Physicochemical and biological studies of a new erythromycin derivate - erythromycin folate. Ars Pharm [Internet]. 2004 Dec. 20 [cited 2024 May 21];46(1):57-72. Available from: https://revistaseug.ugr.es/index.php/ars/article/view/5064

Issue

Vol. 46 No. 1 (2005)

Section

Original Articles

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