Aim: This research was aimed at evaluating the use of Grewia mollis Juss. (Tiliaceae) stem bark gum as a compression coating-agent in a formulation intended to deliver ibuprofen to the colon.Place and Duration of Study: Department of Pharmaceutics and Pharmaceutical Microbiology, Department of Pharmacology and Therapeutics (both in Ahmadu Bello University Zaria) and National Agency for Food and Drug Administration and Control (NAFDAC), Kaduna Laboratory between October 2012 and March 2014.Methods: Ibuprofen core tablets were prepared by the direct compression method and four different compression-coated formulations were produced using powdered and granulated Grewia gum (GG) or hydroxypropyl methyl cellulose (HPMC). The compression-coated tablets were also evaluated for tablet parameters; the in vitro drug release studies were carried out in different simulated gastro-intestinal fluids. An in vivo study was conducted in New Zealand rabbits using the optimized compression-coated tablet and compared with a conventional ibuprofen tablets. The pharmacokinetic parameters were estimated from concentration of ibuprofen in the rabbit plasma using the high performance liquid chromatograph (HPLC).Results: The tablets that were compression-coated with powdered GG showed better ability to offer barrier to drug release and to deliver the drug to the colon than those coated with granulated polymers. The tablets coated with powdered GG coated exhibited greater propensity to deliver ibuprofen to the colon than the other coated tablets. A lower Cmax, longer t1/2 of 8.66 h, longer MRT (7.43 h) and shorter ke (0.08 h-1) revealed that ibuprofen remained in the system for a longer period after oral administration of F2 than when MKT was administered. A high correlation coefficient (0.926) was obtained from the in vitro drug release studies and in vivo studies from F2 indicating that a good relationship was established between both studies.Conclusion: The results of this study have been able to establish that Grewia mollis stem bark gum can be used to effectively deliver ibuprofen to the colon.