Abstract
BackgroundFloating 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.ResultsDifferential 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.ConclusionHence, 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.
Highlights
Floating drug delivery systems have been reported for different active pharmaceutical ingredients as single-unit tablets with gas-generating agents
Preparation of floating multiple-unit minitablets (FMM) of Nimodipine Melt granulation technique was adopted for preparing the solid dispersion of Nimodipine and lipophilic carrier such as Compritol ATO 888 (COM), Gelucire 43/01 (G43/01), Gelucire 39/01 (G39/01) and precirol ATO 05 (PRE)
Compatibility studies using differential scanning calorimeter FMM Differential scanning calorimeter (DSC) study revealed that the pure drug Nimodipine showed a sharp endothermic peak at 124.6 °C with a narrow melting range with an onset temperature of 122 °C and end set temperature of 128 °C
Summary
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. Short transit time of drug with the absorption window in the stomach causes the release of drug in the non-absorbing distal segment of GIT leading to poor bioavailability [1, 2] These features are responsible for the design of gastroretentive formulations [3, 4].
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