Paper 2
Paper 2
Paper 2
In the present work, floating gastro retentive formulation of Famotidine was formulated to sustained
release of Famotidine above its site of absorption.Famotidine is histamine H2 receptor antagonist in
treating gastric ulcer, duodenal ulcer, Zollinger Ellison syndrome, gastroesophegal reflux disease and
erosive esophagitis. It inhibits acid production by reversibly competing with histamine for binding to
H2 receptors on the basolateral membrane of parietal cells. It competitively inhibits histamine action
at all H2 receptors but their main clinical use is as inhibition of gastric acid secretion. It inhibited
histamine stimulation and gastrin stimulated acid secretion. It decreases both basal and food
stimulated acid secretion by 90% or more, but promote healing of duodenal ulcer. The swelling of
the polymers used (HPMC K15M, Ethyl cellulose, Xanthan Gum) were determined by water uptake
of the tablet. The percent swelling of the tablet was determined for 12 h at different time intervals.
Increase in percent swelling was found with increasing concentration of polymers.
Key words:Famotidine, Zollinger Ellison syndrome, duodenal ulcer, gastrin, histamine.
INTRODUCTION
competing with histamine for binding to H2
Famotidine is histamine H2 receptor antagonist
receptors on the basolateral membrane of
in treating gastric ulcer, duodenal ulcer,
parietal cells. It competitively inhibits
Zollinger Ellison syndrome, gastroesophegal
histamine action at all H2 receptors but their
reflux disease and erosive esophagitis. It
main clinical use is as inhibition of gastric
inhibits acid production by reversibly
acid secretion. It inhibited histamine
Bioavailability 40-45%
Plasma Half Life 2.5h-3.5hrs.
Plasma Protein Binding 15- 20%
Peak Plasma Concentration
1- 3 hours
(Cmax)
Excretion Renal Excretion (65-70%)
Metabolic Excretion ( 30-35%)
Renal Clearance 250-450ml/min
Drug Interaction It does not inhibit hepatic microsomal enzyme CYTP450 system and
hence does not interact with drugs which are substrate for CYTP450
systems like Warfarin, Pheytoin, Quinidine, Caffiene etc. It does not
block androgen receptors and do not causeGynaecomastia and
impotence like Cimetidine.
MATERIAL AND METHODS Dibasic Calcium Phosphate were received as a
gift from Central Drug House, Mumbai.
Famotidine was received as a gift sample from
Povidone and HCl were received as a gift
BelcoPharma, Bahadurgarh, Haryana, India.
sample from Merck SpecialitiesPvt Ltd,
Hypromellose (HPMC), Xanthan Gum, Ethyl
Mumbai. Isopropyl Alcohol was perchased
Cellulose, Microcrystalline Cellulose, and
from Nice Chemicals Pvt Ltd, Cochin.
Talc 3 3 3
Magnesium Stearate 3 3 3
140
120 F3
F4
100 F5
% Swelling
80 F6
F7
60
F8
40 F9
F10
20
F11
0
0 5 10 15
Time (hrs)
120
100 F4
F5
% drug release
80
F6
60 F7
F8
40
F9
20 F10
0
0 5 10 15
Time (hr)
Gastric ulcer, one of the most widespread, is The goals of treating peptic ulcer disease are
believed to be due to an imbalance between to relieve pain, heal the ulcer and prevent ulcer
mucosa is continuously exposed to potentially Various types of treatment are available for
injurious agents such as acid, pepsin, bile the treatment of gastric ulcer Proton pump
gastric ulcer, including enhanced gastric acid used in the management of gastric ulcer,
prostaglandin synthesis and cell proliferation Gastroesophgeal reflux disease. Three types of
growth, diminished gastric blood flow and histamine receptor are known H1, H2, and H3.
gastric motility. Drug treatment of peptic H1 is located in smooth muscles and blood
aggressive factors (acid, pepsin, active glands, heart and uterus. H3 receptors are
oxidants, platelet aggravating factor PAF, located in brain, lungs and spleen.
leukotrienes, endothelins, bile or exogenous Controlled release drug delivery systems are
factors including NSAIDs) or stimulating the developed to modulate the apparent absorption
mucosal defences (mucus, bicarbonate, normal or alter the site of release of drugs, in order to
1. Chien YW. Oral drug delivery and development. 2nd Ed. Bangalore & New
Controlled Drug Delivery. In: Novel 10. Ponchel G, Irache JM. Specific and non-
Marcel Dekker Inc; 1992. P. 43-137 for oral delivery to the gastrointestinal
2. Banker GS, Anderson NR. Tablets: The tract. Adv Drug Deliv Rev. 1998; 34:
Correspondence Address:
PawanJalwal
Department of Pharmaceutical Sciences,
Baba Mastnath University,
Asthal Bohar, Rohtak-124001
E-mail- pawan_jalwal@rediffmail.com
Mobile No. 09812875605