Abstract
Nizatidine is a gastroprotective drug with a short biological half-life and narrow absorption window. This study aimed at developing floating tablets of nizatidine using various HPMC viscosity grades, namely K4M, E4M, K15 and K200M. Directly compressed tablets revealed an excellent uniformity in hardness, thickness and weight and nizatidine was evenly distributed within the matrix floating tablets. Buoyancy study revealed floating lag time as low as 18–38 s, and tablets remain buoyant for upto 24 h. However, the later depended upon viscosity grade of HPMC and that the higher the viscosity, the less was the total floating time. In vitro dissolution indicated viscosity dependent nizatidine release from the floating tablets. HPMC K4M and E4M based floating tablets released almost 100% drug in 12 h, whilst higher viscosity polymers such as K15 and K200M only released 81.88% and 75.81% drug, respectively. The drug release followed non-Fickian diffusion from tablets formulated with K4M, K15 and K200M, whilst super case II transport was observed with E4M based tablets. More interestingly, K4M and E4M polymers have similar viscosity yet exhibited different drug release mechanism. This was attributed to the difference in degree of substitution of methoxyl- and hydroxypropoxyl- groups on polymer backbone.
Highlights
By far the most common route for drug administration is the oral route because of low cost therapy, improved patient compliance and relatively less side effects [1]
We report floating tablets formulated using different viscosity grades of HPMC in order to investigate the effect of polymer viscosity on the dissolution behaviour of nizatidine
To date no published report is available with this particular drug, which focused on comparing dissolution with viscosity of HPMC
Summary
By far the most common route for drug administration is the oral route because of low cost therapy, improved patient compliance and relatively less side effects [1]. Dosage forms delivered orally may exit the stomach early due to faster gastric emptying rates, bioavailability of drugs may compromise because of low residence time [2]. An extended residence of drugs in the stomach is important if their local action is required, or drugs have poor solubility and stability in intestinal fluid, or the absorption of drugs occurs within a narrow region of gastrointestinal tract [3]. To counter these issues, gastroretentive drug delivery systems have been developed to prolong the gastric retention time of drugs [4,5]. The low-density floating systems are advantageous owing to their low cost and easy manufacturing, and have the ability to remain buoyant in gastric media for an extended period of time [9]
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