Formulation and Characterization of Clarithromycin Floating Tablets by Using Various Polymers
Formulation and Characterization of Clarithromycin Floating Tablets by Using Various Polymers
Formulation and Characterization of Clarithromycin Floating Tablets by Using Various Polymers
9(10), 766-776
RESEARCH ARTICLE
FORMULATION AND CHARACTERIZATION OF CLARITHROMYCIN FLOATING
TABLETS BY USING VARIOUS POLYMERS
Non-Effervescent GFDDS2
The approach involved in the formulation of floating dosage forms is intimate mixing of drug with a gel forming
hydrocolloid, which swells in contact with gastric fluid after oral administration and maintains a relative integrity of
shape and a bulk density of less than one within the outer gelatinous barrier as shown in figure 1a.
Effervescent GFDDS:
The floating drug delivery systems utilize matrices prepared with swellable polymers such as methocel,
polysaccharides, effervescent components like sodium bicarbonate, citric acid and tartaric acid or chambers
containing a liquid that gasifies at body temperature. The optimal stoichiometric ratio of citric acid and sodium
bicarbonate for gas generation is reported to be 0.76:1 carbon dioxide is released, causing the beads to float in the
stomach3 The matrices are fabricated so that upon contact with gastric fluid, carbon dioxide is liberated by the
acidity of gastric contents and is entrapped in the gellyfied hydrocolloid.
Instruments Used
AnalyticalBalance (Shimadzu, Japan.), FTIRSpectrophotometer (Bruker FTIR Germany(AlphaT),
DissolutionApparatus (Electro labTDT-08L), UVSpectrophotometer (U.V 1700 Shimadzu, Japan.),X-
Raydiffractometer (Bruker-AXS- DHR-2 ).
Precompression Studies
Angle of repose
The angle of repose is calculated using the following formula:
Tanθ = h / r Tanθ= Angle of repose
h = Height of the cone, r = Radius of the cone base
Bulk density
The bulk density is calculated using theformula:
Bulk Density = M / Vo
Where, M = weight of sample
Vo = apparent volume of powder
Tapped density
The exploited density is calculated, in gm perL, using the formula:
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Tap= M / V
Where, Tap= Tapped Density
M = Weight of sample
V= Tapped volume of powder
Average Weight
The percent deviation is calculated using the following formula.
% Deviation = (Individual weight – Average weight / Average weight) × 100
Hardness
Hardness of tabletwas determined using Monsanto hardness testerand the average is calculated and presented with
deviation.
Thickness
The mean thickness for core and coated tablets were calculated and presented with a deviation.
Friability
It is measured of mechanical strength of tablets. Roche friabilator was used to determine the friability by following
procedure. Preweighed tablets were placed in the friabilator. The tablets were rotated at 25 rpm for 4 minutes (100
rotations). At the end of the test, the tablets were reweighed andthe tablet weight loss was a measure of friability and
is expressed as a percentage as
% Friability = [( W1-W2) / W1] × 100
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FourierTransformInfrared(FTIR)studies
Compatibility between pure drug and excipient was detected by the FTIR spectrum obtained on the german Bruker
FTIR (Alpha T).The solid powder sample is placed directly on the yellow crystal that is made up of ZnSe. The
spectra were recorded over the wave number of 4000cm-1 to 550cm-1.
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The standard graph of Clarithromycin showed good linearity with R2 of 0.999, which indicates that it obeys “Beer-
Lamberts” law.
The tablet powder mixture was subjected to various pre-formulation parameters. The residual angle value indicates
that the powder mixture has good flow property. The angle of repose values indicates that the powder blend has good
flow properties. The bulk density of all the formulations was found to be in the range of0.43±0.03to 0.58±0.01
(gm/ml) showing that the powder has good flow properties. The tapped density of all the formulations was found to
be in the range of 0.50±0.02to 0.66±0.01showing the powder has good flow properties. The compressibility index of
all the formulations was found to be below 14.96which show that the powder has good flow properties.All the
formulations has shown the hausners ratio ranging between 0.65to 1.17indicating the powder has good flow
properties.
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All the parameters such as weight variation, friability, hardness, thickness, drug content were found to be within
limits.
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Fig: 4:- Dissolution data of Clarithromycin Floating tablets containing all formulations (Chitosan(F1-F3), HPMC
K4M(F4-F6) and Ethyl cellulose(F7-F9)).
The cumulative percent of drug release from various formulations andrelease coefficients values of the various
models for respective formulation wererepresented in tables 8.4 respectively.
Formulation F7 showed good drug releaseand buoyancy time than all other formulations.
The formulation F7 showed aconstant release in a controlled manner with 99.70%. Hence F7 was chosen forkinetics
studies.
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Fig 5:- Zero order release kinetics. Fig 6:- Higuchi release kinetics.
Fig 7:- Kors mayer peppas release kinetics Fig 8:- First order release kinetics.
Optimised formulation F7 was kept for release kinetic studies. From the above graphs it was evident that the
formulation F7 was followed Korsmayer peppas release mechanism.
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There was no disappearance of any characteristics peak in the FTIR spectrum of drug and the polymers used. This
shows that there is no chemical interaction between the drug and the polymers used. The presence of peaks at the
expected range confirms that the materials taken for the study are genuine and there were no possible interactions.
Clarithromycin are also present in the physical mixture, which indicates that there is no interaction between drug and
the polymers, which confirms the stability of the drug.
XRD Studies
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Conclusion:-
The preformulation parameters like angle of repose,bulk density, tapped density, Hausner’s ratio; Carr’s index of
pure drug was evaluated and complied with thepharmacopoeial specifications. The analysis of XRD study shows
that clarithromycin (pure drug) and polymer existed in crystalline in nature. FTIR study shows that there is no
pharmaco-polymer interaction. Gastro retentive floating matrix tablets of Clarithromycin weresuccessfully prepared
with various polymers like Chitosan, HPMC K4Mand Ethyl cellulose.The formulated batch was evaluated for
physio-chemical parameters, floating properties and dissolution profile. From the evaluation results, itwas observed
that the tablets contain the higher viscosity Ethyl cellulose showedlong floating lag time when compared to tablets
prepared with other polymers. The physical properties such as hardness, weight change andfriability mostof the
batches met the pharmacopoeialspecifications. The drug content of all tablets is in the range of 96.35 – 99.80%.In
vitro dissolution studies of all the formulations were carried out in 0.1 N HCL. The tablets containing Ethyl
cellulose (F7) showed satisfactory results with short floating lag time (20 sec) total buoyancy time more than 12 h,
cumulative % drug release (99.70%) and controlled drug release up to 12 h. So F7 was taken for kinetic studies.The
kinetic studies were carried for formulation F7 showed high regressionvalue of 0.992 for Korsmayer peppasrelease
mechanism. Hence it was concluded that formulation C7 chosen as optimumformulation.
Acknowledgement:-
The authors are thankful to Vedprakash Patil College of Pharamcy, Aurangabad (Maharashtra) for the valuable
support and providing facilities to carry out this research work.
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