International Journal of Pharmacy Research and Technology

2012, Volume 2, Issue 2, 29-32.

ISSN 2250 – 0944 (Online)
ISSN 2250 – 1150 (Print)
Research Article

Glipizide Loaded Gastro Retentive Floating Tablets: Formulation and in vitro Evaluation

Shah Zeel*1, Seth A.K.1, Sailor Girish1, Shah Chainesh1, Dhamat Khushal1, Bhalala Chirag1,
Vegada Rajnikant1,Ramani Vinod2.
1
Sumandeep Vidyapeeth, Piparia, vadoadara. Gujarat.
2
C.K.Pithawalla Institute of Pharmaceutical Science and Research, Surat. Gujarat.
*Corresponding Author Email: shahzeel86@yahoo.com
Received: 27/04/2012, Revised: 04/06/2012, Accepted: 15/06/2012
ASTRACT
The objective of this research was to formulate and evaluate hydro dynamically balanced controlled drug delivery system of
Glipizide. Initially, considering buoyancy as the main criteria, blank tablets were compressed for different formulae with
various polymers like Carbopol-940p, HPMC, Citric acid and sodium bi carbonate. The formula selected for design had a
combination of Glipizide, Carbopol-940p, HPMC, Citric acid. The tablets were prepared by direct compression method and
evaluated for Glipizide content, in vitro release profile and buoyancy. The dissolution study was carried out in simulated
gastric fluid using USP dissolution test apparatus employing paddle stirrer. Duration of buoyancy was observed
simultaneously when the dissolution has carried out. The Glipizide content of F9 batch 97.87±0.16% and in-vitro release was
found to be in the range of 98.85% and from the above result it was concluded F9 was the optimized formulation. This
indicates the suitability of the technique chosen for the present dosage form.

Keywords: Gastro retentive, floating tablet, Glipizide.

INTRODUCTION pancreatic beta cells to release insulin, reduces glucose

Oral route of administration is the most important and
convenient route for drug delivery. The benefits of long-
term delivery technology have not been fully realized for
dosage forms designed for oral administration. This is
mainly due to the fact that the extent of drug absorption
from gastro intestinal tract is determined by GI physiology;
irrespective of the control release properties of the device
prolonged gastric retention improves bioavailability.
Although differential absorption from various regions of GI
has been known for decades, only recently drug delivery
systems have been designed to target drugs to differential
regions of GIT. These include gastro retentive systems,
delayed release systems and colon targeting.[1,2] Floating
dosage form is also known as hydro dynamically balanced
system (HBS). It is an oral dosage form (capsule or tablet)
that is designed to prolong the residence time of the dosage
form within the GI tract. This not only prolongs GI
residence time but also does so in an area of the GI tract
that would maximize drug reaching its absorption site in
solution and hence ready for absorption. Drug dissolution
and release from the capsule retained in stomach fluids
occur at the stomach, under fairly controlled condition. The
retentive characteristics of the dosage form in gastric
content are most significant for drugs. [3]
1. Insoluble in intestinal fluid.
2. That acts locally.
3. That exhibits site-specific absorption.
Gastric retention systems are important for drugs that
are degraded in the intestine, drugs with local action in the
stomach, drugs with poor solubility in intestine due to
alkaline pH, drugs with rapid absorption from
gastrointestinal tract to produce transient peaks in serum
drug levels. Glipizide is a second generation sulphonyl urea
used in the treatment of type II diabetes mellitus. From
gastrointestinal tract to produce transient peaks in serum
drug levels. It lowers blood glucose by stimulating
output from the liver and increase insulin sensitivity at
peripheral stage sites. 90% extended release and half life is
Half-life – 3.4 ± 0.7 h. [4,5]
MATERIALS AND METHODS:
Glipizide was procured from Alembic Pharmaceutical
Ltd; Carbopol 940P was produced from Ranikem Ltd,
Mumbai, India. Hydroxy propyl methyl cellulose (HPMC)
was procured from CDH, New Delhi India. Sodium
bicarbonate and Citric acid were produced from Loba
chemie, Mumbai India. Magnesium Stearate, Poly vinyl
pyrollidine K 30 (PVP K-30) and Micro crystalline
cellulose (MCC) were obtained from CDH, New Delhi.
Drug polymer interaction study by IR [5]
Glipizide discs were prepared by pressing the
Glipizide with potassium bromide and the spectra between
4000-1cm –400-1cm was obtained under the operational
conditions. The absorption maxima in spectrum obtained
with the substance being examined.
Preparation of Glipizide Floating Tablets:
Nine formulations of varying constituents were prepared.
The formula had a combination of Glipizide, Carbopol-
940p, HPMC, Citric acid. The tablets were prepared by
direct compression method. Nine floating matrix
formulations of Glipizide with the help of gas forming
agent were prepared. HPMC 5cps and Carbopol 940P were
to triturated and passed through sieve to formulate the
Matrix system. Incorporation of sodium bicarbonate into
above matrix and directly compressed which was resulted
in the tablet floating over simulated gastric fluid for
sustained release.
Characteristics Glipizide Floating tablets
Tablet Size: [5,6,7]

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Thickness of the tablet was measured by using Vernier
caliper in mm.
Hardness test: [5,6]
Hardness test was carried out by using Monsanto
hardness tester.
Friability test: [5,6,8]
Friability of the tablets was tested using Roche
friabilator. Loss of less than 1% in weight is considered to
be acceptable. The weight of 10 tablets was noted initially
(W1) and placed in the friabilator for 100 RPM/ 4min. The
tablets were reweighed and noted as (W2). The difference in
the weight is noted and expressed as percentage.
(W − W )
Friability = × 100
W
Weight variation test: [6,9]
Twenty tablets were selected at random and the
average weight was determined. Not more than two of the
individual weights deviate from the average weight by
more than the percentage shown in table and none deviates
by more than twice the percentage.

Table 1 Formulation Of Floating Matrix Tablets of Glipizide

Ingredients F1 F2 F3 F4 F5 F6 F7 F8 F9
Glipizide 10 10 10 10 10 10 10 10 10
HPMC 5cps 30 40 50 -- -- -- 50 50 50
Carbopol 940 -- -- -- 30 40 50 10 20 30
Sodium Bicarbonate 20 20 20 20 20 20 20 20 20
Citric Acid 5 5 5 5 5 5 5 5 5
PVP-K 30 5 5 5 5 5 5 5 5 5
MCC 175 165 155 175 165 155 145 135 125
Magnesium Stearate 5 5 5 5 5 5 5 5 5
All quantity is in milligram
the drug release data into zero order, first order and higuchi
Buoyancy determination [10, 11] Model.
In practice floating time and buoyancy lag time was
determined by using beaker containing 100 ml of 0.1N RESULTS AND DISCUSSION
HCl, maintained at 37ºC. The time required for the tablet to The major IR peaks observed in GLIPIZIDE were 1640
rise to the surface of the medium was determined as (CONH stretching), 1370 (SO2NH Stretching), 1142 (cyclo
Buoyancy Lag time and the duration of which the tablet hexyl stretching) the crystal behaviors was not observed in
floats on the surface of the medium was noted as the the physical mixture which can be confirmed by the FTIR
Buoyancy floating time. study. In FTIR study of drug and polymer which show all
prominent peaks. The preliminary identification tests were
Drug content [10,11] also carried out according to USP which complies with the
Drug content of the tablets were determined by using same.
UV visible spectrophotometer.10 tablets were taken and
powdered. The tablet powder equivalent 100 mg of
Glipizide was accurately weighted and transferred to 100
ml volumetric flask and the volume was made up to 100 ml
with 0.1N HCL of pH1.2, 1ml of the aliquot was further
diluted to 100 ml with 0.1N Hcl pH1.2. The absorbance
was measured at 318.5nm.

In vitro Dissolution of Fabricated Tablets [5,6,12]

Tablet’s dissolution was assessed using standard USP Figure 1: IR Spectroscopy of Glipizide
Dissolution apparatus equipment in 900 ml of 0.1N HCL of
pH1.2. The stirring speed of 100 rpm for the basket was
used. The Glipizide tablets were subjected to dissolution
testing in 900 ml dissolution medium. Three tablets were
taken in each batch and a temperature of 37 ºC was
maintained throughout the experiment. Dissolution studies
were carried out for 24 h. 5ml of the Aliquot was taken at
intervals of 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 20 and 24 h.
After collecting the sample, the dissolution medium was
replenished with the same volume of fresh medium, and the
sample was filtered 1ml of the filtrate was diluted to 10ml Figure 2: IR spectroscopy of drug and polymers
with the phosphate buffer and analyzed spectrometrically at
318.5nm. Table 2 IR Peaks and Identified Group
S.No Peaks (cm-1) Groups
Release Kinetic Study 1 1640 CONH Stretching
The rate and mechanism of release of Glipizide through the 2 1370 SO2NH Stretching
prepared Floating matrix tablets were analyzed by fitting 3 1142 Cyclo hexyl stretching

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Table 3 Physical Characteristics, Buoyancy and Floating Time of Glipizide Floating Tablets (F1-F9)
Weight Floating
Batch Thickness Friability Hardness Drug Buoyancy Lag
Variation Duration
No (mm) (%) (kg/cm2) Content Time (sec)
(mg±SD) (hrs)
F1 3.4±0.12 0.47 5.5±0.34 202±2.99 93.76±019 45 16
F2 3.2±0.21 0.68 5.2±0.73 205±1.98 98.16±0.27 60 20
F3 3.4±0.53 0.47 5.4±1.92 202.5±3.7 92.48±0.76 50 22
F4 3.2±0.16 0.46 5.3±0.34 198±6.5 97.28±0.33 65 18
F5 3.3±0.42 0.72 5.6±0.28 204±1.3 91.48±0.26 70 19
F6 3.1±0.53 0.74 5.5±0.37 199±6.59 95.67±0.17 90 21
F7 3.3±0.24 0.63 5.4±0.89 204±1.6 93.87±0.32 45 22
F8 3.2±0.16 0.83 5.3±0.42 194±3.06 90.08±0.89 50 24
F9 3.4±0.29 0.45 5.8±0.56 207±3.9 97.87±0.16 55 24

The physical properties of the tablets (F1 – F9) obtained by CONCLUSION

compressing the blend using Cadmach eight punches tablet
machine. The physical properties of Glipizide (F1 – F9)
such as tablet size, hardness, friability and weight variation
were determined and results of the formulations (F1 – F9)
found to be within the limits specified in Pharmacopoeia.
Buoyancy and floating time of Glipizide Floating Tablets
(F1 – F9) Buoyancy lag time and duration of floating were
determined using USP dissolution test apparatus in 0.1N
HCl Maintained at 37ºC. Buoyancy lag time of F1- F9 was
in the range of 45-90secs.
In the context of developing a gastro-retentive dosage
form of Glipizde, an effervescent-based floating drug
delivery was tried. The present study was carried out to
develop the floating drug delivery with controlled-release
of glipizde using HPMC and carbopol polymer as a matrix.
The present investigation of a tablet form of a gastric
floating controlled drug delivery of glipizde using a
polymer and alkalising agent proved to be an ideal
formulation as it released the drug in a controlled fashion
for extended periods of time so the incomplete absorbance
of drug can be avoided. Hardness, friability and drug
content were in the normal range.
A formulation F9 containing 50mg HPMC and 30mg
carbopol was prepared by a direct compression method; the
total floating time of this formulation was less than 24 hrs
and the drug release was in a controlled fashion (96.62% in
24hrs). It can be concluded that lesser floating lag time and
prolonged floating duration can be achieved. It was also
observed that formulations containing HPMC K100M
retarded the release of drug as the polymer swelling.

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