Abstract
Objectives: We aimed to formulate and optimize bilayer tablets of metoprolol tartrate consisting of both immediate and sustained release layer. Methods: A 23 factorial design was employed in formulating the GFDDS in which parameters, such as amount of HPMC (X1), sodium bicarbonate + citric acid (X2), and crospovidone (X3) were characterized as independent variables, whereas percent metoprolol release at 30 min (Y1), 4 hr (Y2), 8 hr (Y3), floating lag time (Y4), and total floating time (Y5) were considered as dependent variables. Findings: The formulations showed the biphasic release of metoprolol, where the immediate layer was completely disintegrated within 30 min and the release of the sustained layer was extended to 8 hr. Prompt disintegration of the immediate layer was facilitated by the combined effects of sodium starch glycolate and sodium bicarbonate + citric acid, whereas the extended release was assisted by HPMC. Formulations, where HPMC played the major role, were considered the best formulations. A good correlation was displayed between the experimental and predicted values that confirm the practicability of the model. Application/improvements: This study shows the effect of various variables in the release of metoprolol tartrate and formulates the bilayer tablets of metoprolol tartrate for the immediate and sustained drug release.Keywords: Metoprolol, Floating Drug Delivery System, Bilayer, Immediate Release Layer, Sustained Release Layer
Highlights
Among the various routes of drug administration, the oral route of drug administration has gained wide acceptance for decades.[1]
With the aim to develop a formulation that would help to Design and Optimization of Bilayer Floating Gastroretentive Tablets of Metoprolol reach the blood drug therapeutic level in few minutes of drug administration and maintain a steady-state plasma concentration for a long period, a bilayer tablet model was designed that comprise both immediate release and sustained release layers of metoprolol
Metoprolol tartrate was purchased from Shreeji Pharma International, Gujarat, India
Summary
Among the various routes of drug administration, the oral route of drug administration has gained wide acceptance for decades.[1]. To avoid the rapid efflux movement of the gastrointestinal tract, and to improve the solubility and bioavailability of the drug, the gastro-retentive system was designed.[8] Various attempts, such as floating dosage form,[9] mucoadhesive system,[10] high-density system,[11] modified shape system,[12] gastric-emptying delaying device system[13] and co-administration of gastric-emptying delaying drugs[14] have been investigated to retain the dosage form in the stomach and increase the retention time. Among the aforementioned ways of gastric retention, the floating dosage form has been a commonly used system.[14,15] The bulk density of the system would be lesser than the gastric fluid and remain buoyant in the stomach without affecting the gastric emptying rate for a prolonged period releasing the drug at a slow and steady rate.[14] After the release of the drug, the residual system would be emptied into the intestine. The consequence of the system would be the better control of the fluctuations in plasma drug concentration.[15]
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