Core-shell tablets designed for modified and sequential release of ibuprofen and rabeprazole

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Pharmacokinetics

Background:

• Non-steroidal anti-inflammatory drugs like ibuprofen (IBU) can cause gastrointestinal (GI) side effects.
• Rabeprazole (RAB) is a proton pump inhibitor often co-administered with NSAIDs.
• Developing combined dosage forms for sequential drug release is a key challenge in pharmaceutical research.

Purpose of the Study:

• To develop and characterize core-shell tablets for sequential release of rabeprazole (RAB) and ibuprofen (IBU).
• To achieve pharmacokinetic profiles comparable to individual drug formulations.
• To reduce potential gastrointestinal side effects associated with ibuprofen.

Main Methods:

• Core-shell tablets were fabricated using a wet granulation method.
• Formulations were optimized through comparative evaluation of trial batches.
• Physicochemical properties, storage stability, and in vivo pharmacokinetics in beagle dogs were assessed.

Main Results:

• The core-shell tablets demonstrated immediate release of RAB (99.5% in 1 hour at pH 1.2) and delayed release of IBU (88% in buffer stage).
• In vivo studies in beagle dogs showed comparable or improved plasma concentrations (Cmax) for both RAB and IBU versus single-drug tablets.
• The developed tablets exhibited good long-term and accelerated storage stability.

Conclusions:

• The core-shell tablet design is a viable strategy for co-administering RAB and IBU with sequential release.
• This approach can potentially mitigate GI complications associated with ibuprofen therapy.
• The formulation holds promise for managing inflammatory conditions while enhancing patient compliance.