Der Pharmacia Lettre
Abstract
Author(s): Ankalu Dasa*, Nandhakumar Sathyamoorthyb, Devalarao Garikapatia
The challenge up-front in formulating an efficient oral dosage form for a proton pump inhibitor like pantoprazole is
delivering the acid liable drug unaffected to the intestinal milieu, for which enteric coating possibly will be a most
plausible solution. Sureteric is a specially blended optimized aqueous coating combination of polyvinyl acetate
phthalate, which exhibits a number of properties desirable for an enteric film formation. The present study aimed at
formulation of enteric coated tablets of pantoprazole and to assess the influence of appropriate additives on the
performance of the final product. The influence of different diluents, disintegrants and binders upon the
precompression characters and physico-chemical properties of the tablets were studied and an optimized
formulation with passable quality was selected for enteric coating. The optimized core formulation was then shroud
around in a seal coat using 12% HPMC dispersion in order to increase the mechanical integrity and avoid any
possible interaction between the drug and the enteric polymer. The seal coating was followed by enteric coating by
the application of sureteric at different theoretical weight gains. The enteric coated tablets were evaluated for
disintegration time, acid uptake and drug release. Formulation F19 coated up to 10% weight gain, disintegrated
rapidly with in 8 min and showed <2.5% of acid uptake. The sureteric coating could resist the drug release in 0.1N
HCl up to 2h but propelled the release of about 84% of drug within 30 min in the intestinal pH. Results of the
stability tests were satisfactory with the dissolution rate and assays well within acceptable limits. The
gastrointestinal behaviour of enteric tablets performed in rabbits using a fluoroscopic material revealed that the
tablets remained intact in the stomach and then dissolved on reaching the small intestine. Thus the study ascertained
the influence of additives on the effectiveness of the end formulations and also the suitability of the sureteric
aqueous dispersion successful development of delayed release, dosage forms for proton pump inhibitors.
