Formulation Development & Evaluation of Buffered Tablet of Proton Pump Inhibitors Drug Rabeprazole Sodium

Abstract

The aim of present study was to prepare buffered tablets of acid labile drug, Rabeprazole sodium for oral administration using buffering agents to protect a drug from gastric fluid. Rabeprazole belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but suppress gastric acid secretion by inhibiting the gastric H+, K+ATPase at the secretory surface of the gastric parietal cell. Rabeprazole blocks the final step of gastric acid secretion. The tablets were prepared by direct compression and wet granulation method. The formulations contain water soluble buffers such as sodium bicarbonate and trisodium phosphate as well as water insoluble buffers as magnesium oxide, magnesium hydroxide and calcium carbonate and crospovidone as superdisintegrant. Preformulation studies like angle of repose, bulk density, tapped density, Carr’s index, hausner’s ratios, DSC and drug/excipient compatibility study were conducted and evaluated for hardness, friability, weight variation, drug content, disintegration and in-vitro dissolution. In the present study, pH of F6 batch was found to be optimum and disintegration time is 42 sec. The drug release was found to show maximum drug release in case of F6 with 99.3% in 60 minutes. In case of stability studies study of the optimized batch, all the results were found to be satisfactory and within limits. There were no significant changes after the period of 1 month study.
 Keywords: Rabeprazole sodium, Proton-pump inhibitors, Buffered tablet, Superdisintegrants, Buffering agents

Quality by Design Applied Development of Immediate-Release Rabeprazole Sodium Dry-Coated Tablet

“…Each mixture was stored in a stability chamber for 4 weeks at room temperature of 25 ± 2 °C/ 60 ± 5% RH and under acceleration conditions of 40 ± 2 °C/ 75 ± 5% RH. After 4 weeks, 1–3 mg of each mixture was heated from 25–330 °C at 10 °C/min and DSC was used to monitor changes in the endothermic and exothermic peaks [ 32 ]. If none were detected, an additional impurity test was performed to confirm compatibility.…”

“…Rabeprazole sodium was mixed at a 1:1 ratio (w/w) with the following excipients: mannitol, lactose, dicalcium phosphate dihydrate, microcrystalline cellulose, pregelatinized starch, precipitated calcium carbonate, sodium starch glycolate, crospovidone, sodium croscarmellose, sodium stearyl fumarate, magnesium stearate, povidone K, hydroxypropyl methylcellulose, hydroxypropyl cellulose, calcium hydroxide, and sodium hydroxide. Each mixture was stored in a stability chamber for 4 weeks at room temperature of 25 ± 2 °C/ 60 ± 5% RH and under acceleration conditions of 40 ± 2 °C/ 75 ± 5% RH .. After 4 weeks, 1-3 mg of each mixture was heated from 25-330 °C at 10 °C/min and DSC was used to monitor changes in the endothermic and exothermic peaks [32]. If none were detected, an additional impurity test was performed to confirm compatibility.…”

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].…”