Design And Evaluation Of Sustained Release

Gastroretentive Drug Delivery System .

Presented By
Arvind S. Bagde

Guide Co-Guide
Mr. Kamlesh .J .Wadher Mr. B. K. Shrikhande
(M. Pharm.) (M. Pharm.)

SMT.KISHORITAI BHOYAR COLLEGE OF

PHARMACY, KAMPTEE
Rashtrasant Tukadoji Maharaj Nagpur University,Nagpur
1
INTRODUCTION

Gastroretentive Drug Delivery System:

 After oral administration, such dosage form would be retained in the
stomach and release the drug there in a controlled and prolonged
manner, so that the drug could be supplied continuously to its
absorption sites in the upper gastrointestinal tract.

 Gastroretentive dosage form can remain in the gastric region for

several hours and hence significantly prolong the gastric residence
time of drugs.

2
A. Floating drug delivery systems
(a) Non-effervescent systems
 Colloidal gel barrier system
 Microporous compartment system
 Alginate beads
 Hollow microspheres / Microballons

(b) Gas-generating (Effervescent) systems

B. Expandable systems

C. Bio/Muco-adhesive systems

D. High-density systems
3
 Sustained drug delivery/reduced frequency
of dosing
 Targeted therapy for local ailments in the
upper GIT
 Reduced fluctuations of drug concentration
 Improved selectivity in receptor activation
 Enhanced bioavailability
 Extended time over critical(effective)concentration
 Minimized adverse activity at the colon
 Site specific drug delivery
4
 FACTORS CONTROLLING GASTRIC
RETENTION OF DOSAGE FORMS
The gastric retention time (GRT) of dosage forms is
controlled by several factors such as

 Density and size of the dosage form

 Food intake
 Nature of the food
 Posture
 Age
 Sex
 Sleep
 Disease state of the individual (e.g.,gastrointestinal
diseases and diabetes) and
5
 Metformin is an anti- hyperglycemic agent, which improves glucose
tolerance in type II diabetes.

 It has been reported that the absolute bioavailability of Metformin

when given orally is 50–60%.

 Biological half-life of Metformin is 1.5–1.6 h and the main site of

its absorption is proximal small intestines.

 A system when administered would remain buoyant on the gastric

fluids for a prolonged period of time and the drug would be available
in the dissolved form at the main site of its absorption i.e., proximal
small intestines . This would lead to improvement in the
bioavailability of the drug.

6
 To formulate and evaluate sustain release gastroretentive dosage
form of metformin HCL

7
PLAN OF WORK :

 Selection of drug
Criteria for selection of drug is based on narrow absorption window
in G I tract, primarily absorbed from stomach and upper part of Gi
tract, drugs that act locally in the stomach ,drugs that degrade in the
colon .

 Selection of polymer
 Formulation of dosage form
 Evaluation of dosage form

Weight variation
Hardness
Drug content
In vitro dissolution study
8
Drug name : Metformin Hydrochloride
Molecular formula :C14H11N5HCl
Structure:

IUPAC Name : 1,1 dimethyl biguanide

Colour :White
Appearance :Crystalline powder, Hygroscopic
Melting Point :221-2250c
Solubility:
Freely soluble in water
Slightly soluble in ethanol(95%)
Practically insoluble in acetone, chloroform, dichloromethane and
ether
9
 HPMC K100 M

 HPMC k4M

 Carbopol 943 p

 Hydroxyethyl cellulose 250HHX

 sodium carboxymethyl cellulose (NaCMC, 450 cps and

2500 cps)

10
Composition of floating tablets of Metformin Hcl.
Ingredients (mg/tablet):

Formula Drug HPM Carbo Citric Sodium PVP Magnesi Talc

tion (metfor C pol acid bicarbon k-30 um
min) K100 934P ate Stearate
M
F1 500 100 - 15 50 75 5 5

F2 500 150 - 15 50 75 5 5

F3 500 - 100 15 50 75 5 5

F4 500 - 150 15 50 75 5 5

F5 500 75 75 15 50 75 5 5

11
Formulation containing:

HPMC K100M,
HPMC K15M,
carbopol 934P

was consider as the best product with respect to in

vitro drug release for 24 hours release action, total
floating time and improved bioavailability and site‐
specific action.

12
THANK YOU

13