FACTORS INFLUENCING DELAYED RELEASE FOLLOWED BY RAPID PULSE RELEASE OF DRUGS FROM COMPRESSION COATED TABLETS FOR COLON TARGETING
Keywords:
LBG, CMLBG, Osmogen, Rat cecal content, In vitro dissolutionAbstract
Objective: This work was undertaken to develop colon targeted tablets that can minimize premature release of ibuprofen (IBP) and metronidazole (MNZ) in a lag period of 7h during which the tablets are likely to remain in the upper gastro-intestinal tract, and produce rapid pulse release within 1-5 h after the lag period when the tablets could be located in the colon with or without intervention of colonic microflora.
Methods: Core tablets of ibuprofen and metronidazole containing different amounts of tri-sodium citrate (TSC) as osmogen were compression coated with locust bean gum (LBG) and carboxymethyl LBG (CMLBG). In vitro drug release studies were performed in a dynamic pH shift condition with or without rat cecal matters. The release of the drugs were also monitored at different hydrodynamic conditions.
Results: In vitro release studies revealed that increase in the amount of TSC, decrease in coat-weight and change in hydrodynamic conditions influenced the drug release considerably. While LBG coated tablets under the stated conditions failed to provide complete release of the drugs in 12 h, CMLBG coated tablets produced complete release rapidly in the post lag period minimizing the release in the initial 7 h. Presence of rat cecal matter in dissolution medium further accentuated the release of the drugs from CMLBG compression coated tablets in the post lag period.
Conclusion: The study revealed that tablets containing appropriate amount of osmogen in the core and compression coated with suitable amount of CMLBG may be suitable for colon targeting of drugs even in the absence of colonic microflora.
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