Formulation Development and Evaluation of Enteric Coated Tablets of Rabeprazole Sodium

Abstract

Rabeprazole sodium is highly acid-labile and presents many formulation challenges and to protect it from acidic environment of the stomach an enteric coated tablet formulation is tried in the present study. This study is aimed to develop pharmaceutically equivalent and stable enteric-coated tablets of Rabeprazole sodium comparable to innovator product. Different Formulations of Rabeprazole core tablets were developed using mannitol as diluent and croscarmellose as super disintegrant in different proportions. Further optimized formulation was coated with varying the compositions of sub coating and enteric coating using opadry white and enteric yellow. Compatibility studies were performed for drug, physical mixture tablet which shows no interaction. From the dissolution the formulation F6 shows highest percentage of drug release. The kinetics of drug release for F6 & Innovator followed first order and 'n' value (0.5>n<1) shows that the mechanism may be erosion control rate release. The f1 and f2 were found to be 3.03 and 72.01 respectively for formulation F6 and innovator product. Hence these two products were considered similar and comparable. In the accelerated stability testing carried out at 40°c and 75% RH for three months, no significant change in the physical properties, drug content, and dissolution rate of formulation F6 was observed. From this it can be concluded that formulation F6 developed is found to be an efficient delayed release formulations of Rabeprazole comparable to the innovator product. Thus the study fulfilled the objective of developing efficient Rabeprazole delayed release tablets.

Formulation of Dosage Forms with Proton Pump Inhibitors: State of the Art, Challenges and Future Perspectives

“…As in the case of pellets, the literature provides examples of the manufacturing of an intermediate layer, which separates the enteric coat from the core with the therapeutic substance. HPMC or polyvinyl alcohol dispersions are used for this purpose [ 253 , 254 , 255 , 256 , 257 , 258 , 259 , 260 , 261 ]. The intermediate layer is intended to protect the therapeutic substance sensitive to acidic groups of enteral polymers [ 256 ].…”

Exploring Differences in Pharmacometrics of Rabeprazole between Genders via Population Pharmacokinetic–Pharmacodynamic Modeling

“…PPIs, including rabeprazole, have a common acid-labile, and many of them are formulated into enteric-coated tablets and applied clinically to prevent decomposition in the stomach, while also increasing its absorption in the small intestine [15,16]. Entericcoated tablets consist of a drug-loaded core, which is externally coated in polymers (such as polymethacrylates, cellulose acetate phthalate, and hydroxy propyl methyl cellulose phthalate) that have an anti-dissolving function in the acidic environment of the stomach [17].…”

Application of the New Oroslippery Technology in the Preparation of Enteric Slippery Coated Tablet of Naproxen

“…6) demonstrated a significant acid resistance after 2 h in 0.1 N HCl, followed by a significant reduction in DT and T80% in phosphate buffer pH 6.8 resulting from the effect of CCS as a superdisintergrant which led to fast burst release of naproxen tablet once it is introduced in intestine [17]. For this reason F8 was selected as the optimum formula since it gave the best acid resistance with fast and high % drug release in phosphate buffer pH 6.8.…”

“…This test was performed (according to the USP specification) for the enteric coated slippery tablet in 0.1 N HCl for 2 h, where no sign of disintegration should be observed then followed in phosphate buffer pH 6.8 and record the time for complete disintegration [12,17].…”