Abstract
Objective: In this present research, formulation of floating multiple unit minitablets of metoprolol succinate without using gas generating agent was attempted with an objective of increased residence time, sustained release, and improved oral bioavailability.
 Methods: Solid dispersions were prepared with lipophilic carriers such as compritol ATO888, Gelucire 43/01, Gelucire 39/01, and precirol ATO 05 was formulated using fusion technique. Neusillin US2 was used as an adsorbent. The solid dispersions were compressed into minitablets, weighing 20 mg, and then filled into ‘0’ size capsule.
 Results: Formulation F9, F10, F14, and F15 showed instantaneous floating lag time, i.e., 0 min, floating time more than 12 h, and sustained release up to 12 h. Pharmacokinetic study of the optimized formulation (F9) showed 2.46 times increase in area under the curve with increased residence time.
 Conclusion: Hence gelucire 43/01 based floating multiple unit minitablets of metoprolol succinate can be considered a promising approach.
Highlights
For a long time, oral controlled release (CR) formulations are popularly used for controlling the release of drugs
Fourier transform infrared spectroscopy (FT-IR) study for the pure drug metoprolol succinate showed absorption bands at 3181 cm-1 assigned to the NH group, absorption bands at 3040 cm-1 assigned to OH group, and absorption bands at
Floating minitablets prepared with compritol ATO 888 and Precirol ATO 05 did not exhibit floating, whereas gelucire 43/01 and 39/01 floating minitablets without gas generating agent exhibited desirable floating and sustain release characteristics
Summary
Oral controlled release (CR) formulations are popularly used for controlling the release of drugs. Short transit time of drug with absorption window in the stomach causes drug release in the non-absorbing distal segment of GIT, leading to poor bioavailability [1] These features are responsible for the design of gastro retentive formulations [2, 3]. Metoprolol succinate has a short half-life (3-4 h), and absorption window in the upper GI tract favors developing a sustained release and floating drug delivery system, respectively [11, 12]. It exhibits a high solubility at gastric pH 1.2. In the present research work, it is planned to use hydrophobic carriers to formulate floating multiple unit minitablets of metoprolol succinate to achieve floating with sustain release for 12 h
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