Background: Floating drug delivery systems have been reported for different active pharmaceutical ingredients as single-unit tablets with gas-generating agents. In this present research, the formulation of floating multiple-unit minitablets of Nimodipine without using gas-generating agent was attempted with an objective of increased residence time, sustain-release and improved oral bioavailability. Solid dispersion with different ratios (1:0.5, 1:1, 1: 1.5, 1:2, 1:2.5) of drug with the lipophilic carrier such as Compritol ATO 888, Gelucire 43/01, G39/01 and Precirol ATO 05 was formulated using melt granulation technique. The adsorbent Sylysia 350 to lipophilic carrier is maintained at 1:1. The granules were compressed into minitablets weighing 15 mg and were filled into a '0' size capsule.Results: Differential scanning calorimetry study justified no interaction of the drug with excipients. The formulations which exhibited desirable flow property, floating lag time less than 1 min and floating time of 12 h were further characterized for various post-compression parameters. The optimized single-dose (capsule) of floating multiple-unit minitablets of Nimodipine consisting of 60 mg of drug, 120 mg of G43/01 and 120 mg of Sylysia 350 showed an average of floating lag time within 24.48 s, floating time of 14.32 h and sustained-release up to 12 h. Pharmacokinetic study of the optimized formulation (F9) showed nearly 2.5 times increase in area under the curve with increased residence time in comparison to aqueous suspension of Nimodipine. The stability study revealed no significant change in various parameters before and after storage.Conclusion: Hence, gelucire 43/01-based multiple-unit minitablets of Nimodipine can be considered a promising approach for sustaining the drug release with gastric retention for 12 h without using gas-generating agent.

Objective:The present study was to investigate the antiasthmatic potential from the flavonoid fraction of Apium leptophyllum fruit (FFALF) to validate its traditional claim.Materials and Methods:The antiasthmatic activity of FFALF was evaluated by histamine or acetylcholine-induced bronchospasm model in guinea pigs, compound 48/80 induced mast cell degranulation in albino rats and histamine-induced tracheal contraction in guinea pig. The preconvulsion dyspnea time at 0th and 7th day at the dose of 100 and 200 mg/kg in guinea pig's bronchospasm model, the percentage of granulated and degranulated mast cell at the dose of 500, 750, and 1000 μg/ml in rats and tracheal contraction at the dose of 500, 750, and 1000 μg/ml in guinea pig were measured and compared with respective control groups.Results:The treatments of FFALF were significantly (P < 0.001) decreased the histamine/acetylcholine-induced bronchospasm, mast cell degranulation, and histamine-induced tracheal contraction as compared to inducer group. In addition, FFALF showed dose-dependent antiasthmatic activity in all the animals.Conclusion:Hence, this study suggested that the FFALF showed antiasthmatic activity probably by membrane stabilizing property as well as suppressing antibody production and inhibiting of antigen induced by histamine and acetylcholine.

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.

The utility of lipid-based oral formulations has been familiar for many years. There are an enormous variety of polymeric materials used to modify the delivery platform along with enhancement of therapeutic efficacy. Gelucires are a family of lipid-based excipients comprising of glycerides and esters of polyethylene glycol, these two components conferring hydrophobic and hydrophilic properties to the vehicle. Gelucire is used to enhance the drug’s physicochemical properties, as well as controlled release matrices. This review intends to give a critical overview of the published literature on the properties, chemical nature, advantages over other polymers, methods of characterization of gelucire containing formulations, applications and patents containing various grades of gelucires.