Kumari et al Journal of Drug Delivery & Therapeutics. 2019; 9(4-s):315-321
ISSN: 2250-1177 [315] CODEN (USA): JDDTAO
Available online on 15.08.2019 at http://jddtonline.info
Journal of Drug Delivery and Therapeutics
Open Access to Pharmaceutical and Medical Research
© 2011-18, publisher and licensee JDDT, This is an Open Access article which permits unrestricted
non-commercial use, provided the original work is properly cited
Open Access Research Article
Formulation Development & Evaluation of Buffered Tablet of Proton Pump
Inhibitors Drug Rabeprazole Sodium
Mamta Kumari*, Dr. Nishi Prakash Jain
*Sagar Institute of Research & Technology- Pharmacy, Bhopal, Madhya Pradesh 462041
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
Article Info: Received 08 June 2019; Review Completed 22 July 2019; Accepted 26 July 2019; Available online 15 August 2019
Cite this article as:
Kumari M, Jain NP, Formulation Development & Evaluation of Buffered Tablet of Proton Pump Inhibitors Drug
Rabeprazole Sodium , Journal of Drug Delivery and Therapeutics. 2019; 9(4-s):315-321
http://dx.doi.org/10.22270/jddt.v9i4-s.3324
*Address for Correspondence:
Miss Mamta Kumari, Sagar Institute of Research & Technology, Pharmacy, Bhopal, Madhya Pradesh 462041
INTRODUCTION
Rabeprazole sodium drug is a sodium salt of 2-((4-(3-
methoxypropoxy)-3-methylpyridin-2-yl) methylsulfinyl)-1H-
benzo[d]imidazole belongs to a class of proton pump
inhibitors. It suppress gastric acid secretion by specifically
inhibiting the H
+
/K
+
- ATPase enzyme system at the secretory
surface of the gastric parietal cell
1
. Peptic ulcer disease
comprises a group of chronic ulcerative conditions that
primarily affect the gastric mucosa and proximal duodenum.
The drug like H2 blockers cimetidine, ranitidine and
famotidine reduce the amount of acid produced by stomach.
But Proton Pump Inhibitors (PPIs) are a group of drugs
whose main action is pronounced and long-lasting reduction
of gastric acid production. These drugs are metabolized in
the parietal cells to active sulfonamide metabolites that
inactivate the sulfhydryl group of the proton pump, thus
reducing the hydrogen ion secretion
2,3
. Most of the PPIs are
formulated in an enteric-coated solid dosage form (either a
delayed-release capsule or tablet) or as an intravenous
solution. There are some problems associated with enteric-
coated preparations as dissolution of the enteric coating is
pH-dependent and gastric empting time. pH profile of the
gastrointestinal tract in an individual is variable at different
times and is dependent on numerous physiological factors
(e.g., the fed or fasted state), variable dissolution times for
the enteric coat and variable pharmacokinetic profiles of
individuals may affects
4-6
. The acid-labile drugs for oral
administration may also be protected from gastric acidity by
neutralizing the pH of the gastric fluid. So the current
frontier in PPI therapy is immediate-release tablet combined
with buffering agents which prevent degradation of drug by
neutralizing the pH of stomach before absorption and
protect the drug from low pH. Such dosage forms are known
as buffered tablet and such tablet is advantageously devoid
of any enteric coating or delayed or sustained-release
delivery
7,8
.
MATERIAL AND METHOD
Material
Rabeprazole sodium was obtained as gift sample from Cadila
Healthcare Ltd., Ahmedabad. All chemicals were used of
pharmaceutical grade obtained as gift sample from apex
pharmaceutical, Chennai.