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Please cite this article in press as K. Ramanji Reddy et al., Formulation and Evaluation of Floating Tablets of
Famciclovir Using Various Hydrophilic and Hydrophobic Polymers, Indo Am. J. P. Sci, 2018; 05(01).
the maximum angle that can be obtained between the mechanically tapped and volume reading were taken
free standing surface of a powder heap and the until little further volume changes is observed.
horizontal.
Angle of repose= tan-¹ (h/r) Tap density = M / Vr
Evaluation of tablets:
The quantitative evaluation and assessment of a 4. Content Uniformity [15]:
tablets chemical, physical and bioavailability The content uniformity test is used to ensure that
properties are important in the design of tablets and every tablet contains the amount of drug substance
to monitor product quality. There are various intended with little variation among tablets within a
standards that have been set in the various batch. Due to increased awareness of physiological
pharmacopoeias regarding the quality of availability, the content uniformity test has been
pharmaceutical tablets. These include the diameter, included in the monographs ofall coated and
size, shape, thickness, weight, hardness, Friability, uncoated tablets and all capsules intended for oral
Buoyancy test and invitro-dissolution characters. administration where the range of size of the dosage
form available include 50mg or smaller sizes.
1. Physical Appearance: Method:
The general appearance of a tablet, its identity and Randomly select 30 tablets. 10 of these assayed
general elegance is essential for consumer individually. The Tablet pass the test if 9 of the 10
acceptance, for control of lot-to-lot uniformity and tablets must contain not less than 85% and not more
tablet-to-tablet uniformity. The control of general than 115% of the labeled drug content and the 10th
appearance involves the measurement of size, shape, tablet may not contain less than 75% and more than
colour, presence or absence of odour, taste etc. 125% of the labeled content. If these conditions are
not met, remaining 20 tablets assayed individually
2. Size & Shape: and none may fall outside of the 85 to 115% range.
It can be dimensionally described & controlled. The
thickness of a tablet is only variables. Tablet Friability [16]:
thickness can be measured by micro-meter or by Friction and shock are the forces that most often
other device. Tablet thickness should be controlled cause tablets to chip, cap or break. The friability test
within a ± 5% variation of standard value. is closely related to tablet hardness and designed to
evaluate the ability of the tablet to withstand abrasion
3. Weight variation test [14]: in packaging, handling and shipping. It is usually
This is an in process quality control test to ensure that measured by the use of the Roche friabilator.
the manufacturers control the variation in the weight Method:
of the compressed tablets, different pharmacopoeia A number of tablets are weighed and placed in the
specify these weight variation tests.. These tests are apparatus where they are exposed to rolling and
primarily based on the comparison of the weight of repeated shocks as they fall 6 inches in each turn
the individual tablets (xi) of a sample of tablets with within the apparatus. After four minutes of this
an upper and lower percentage limit of the observed treatment or 100 revolutions, the tablets are weighed
sample average (x-mean). The USP has provided and the weight compared with the initial weight. The
limits for the average weight of uncoated compressed loss due to abrasion is a measure of the tablet
tablets. These are applicable when the tablet contains friability. The value is expressed as a percentage. A
50mg or more of the drug substance or when the maximum weight loss of not more than 1% of the
latter comprises 50% or more, by weight of the weight of the tablets being tested during the friability
dosage form. test is considered generally acceptable and any
Method: broken or smashed tablets are not picked.
Twenty tablets were weighed individually and the The percentage friability was determined by the
average weight was calculated. The individual tablet formula:
weights are then compared to the average weight. Not
more than two tablets should differ in their average % friability = (W1-W2) / W1 X 100
weight by more than percentages stated in USP. No
tablet must differ by more than double the relevant W1 = Weight of tablets before test
percentage. W2 = Weight of tablets after test
Table 2: Limits for Tablet Weight variation test:
Average weight of tablet % Difference Floating lag time [17]:
(mg) allowed The time between the introductions of the tablet into
130 or less 10 % the medium and its rise to upper one third
From 130 to 324 7.5 % of the dissolution vesselis termed as floating lag time
> 324 5% and the time for which the dosage form floats is term
ed as the floating or flotation time. These tests are us
ually performed in simulated gastric fluid or 0.1N
FORMULATION DEVELOPMENT
Procedures:
The Purpose of key ingredients included in the formulation.
Table 3: Composition of Acyclovir Floating Tablets
Ingredients F1 F2 F3 F4 F5 F6 F7 F8 F9
Famcyclovir 200 mg 200 mg 200 mg 200 mg 200 mg 200 mg 200 mg 200 mg 200 mg
Chitosan 100 mg 200 mg 300 mg --- --- 33.3 mg --- 50 mg 50 mg
Carbopol 934 --- --- --- 200 mg --- 33.3 mg 50 mg --- 50 mg
HPMC K15 M --- --- --- --- 200 mg 33.3 mg 50 mg 50 mg ---
40 mg 40 mg 40 mg 40 mg 40 mg 40 mg 40 mg 40 mg 40 mg
Sodium bi carbonate
Citric acid 5 mg 5 mg 5 mg 5 mg 5 mg 5 mg 5 mg 5 mg 5 mg
Micro Crystalline
245 mg 145 mg 45 mg 145 mg 145 mg 245 mg 245 mg 245 mg 245 mg
Cellulose
Megnesium stearate 10 mg 10 mg 10 mg 10 mg 10 mg 10 mg 10 mg 10 mg 10 mg
Total Weight 600 mg 600 mg 600 mg 600 mg 600 mg 600 mg 600 mg 600 mg 600 mg
1. Drug and polymers pass through 40 # mesh separately and then transfer it to poly bag and mix it for 3
minutes.
2. Add diluents and other excipients to the above mixture. Finally add the Glidant (Magnesium Stearate) to
the above blend mix it for 2min.
3. Compressed the above lubricated blend by using 10 mm round punches.
Solubility Profile:
Solubility data of Famcyclovir
It is freely soluble in water, soluble in alcohols, and slightly soluble in common organic solvents, such as
acetonitrile and methyl ethyl ketone.
Preparation of Standard stock solutions: Further dilutions were prepared from the same
Famcyclovir equivalent to 100 mg was weighed and solution.
transferred to 100 ml volumetric flask, dissolved in
methanol and the final volume was made upto 100ml Preparation of Standard solutions:
with 0.1N HCL. The resulted solution had the From the stock solution B, further dilution was made
concentration of 1mg/ml (1000μg/ml) which was with 0.1N HCL in 10 ml volumetric flasks to get the
labeled as “stock solution A”. solutions in the range of 2-10 µg/ml concentration
From the stock solution A, 1 ml was pipette out in and absorbance was recorded at 252 nm against
10ml volumetric flask and the final volume was made suitable blank using UV-Spectrophotometer (UV-
upto 10ml with 0.1N HCL.The resulted solution had 1601, Shimadzu, Japan).A calibration curve of
the concentration of 0.1mg/ml (100μg/ml) which was absorbance against concentration was plotted and the
labeled as “stock solution B”. This stock solution B is drug follows the Beer’s & Lambert’s law in the
used as working stock solution for further study. concentration range of 2-10μg/ml. The Regression
equation and correlation coefficient was determined.
0.6
Absorbance
0.4
abs
0.2
Linear (abs)
0
0 2 4 6 8 10 12
-0.2
Concentration
Evaluation of the Prepared Tablets for Physical The results of the tests were tabulated. The drug
Parameters: content of all the formulations was determined and
All formulations were tested for Physical parameters was found to be within the permissible limit. This
like Hardness, thickness, Weight Variation, Friability study indicated that all the prepared formulations
and found to be within the Pharmacopoeial limits. were good.
Parameter F1 F2 F3 F4 F5 F6 F7 F8 F9
Weight 0.600 0.599 0.5998 0.600 0.6 0.599 0.600 0.599 0.600
variation ±0.004 ±0.005 ±0.004 ±0.005 ±0.004 ±0.004 ±0.005 ±0.004 ±0.004
Thickness 5.5 5.6 5.3 5.6 5.5 5.5 5.5 5.5 5.5
(mm) ±0.4 ±0.4 ±0.4 ±0.4 ±0.4 ±0.3 ±0.4 ±0.1 ±0.2
Hardness 8.9 7.4 8.2 6.9 8.4 8.1 8.2 8.3 8.2
(kg/cm2) ±1.4 ±1.2 ±1.2 ±0.9 ±1.9 ±1.7 ±1.5 ±1.6 ±1.4
0.22% 0.26% 0.25% 0.25% 0.25% 0.22% 0.21% 0.21% 0.21%
Friability ±0.2 ±0.23 ±0.19 ±0.26 ±0.22 ±0.1 ±0.4 ±0.5 ±0.7
99.91% 99.84% 99.87% 98.88% 99.88% 99.89% 99.88% 99.68% 99.88%
Assay ±0.2 ±0.4 ±0.3 ±0.2 ±0.3 ±0.2 ±0.2 ±0.2 ±0.2
Floating
lag time
(sec) 34 42 43 51 42 41 36 39 41
Dissolution Profiles
120
F1
100
% Drug release
80 F2
60 F3
40 F4
20 F5
0
F6
0 2 4 6 8 10 12 14 16 18
Time ( Min ) F7
50 %CR
0 Linear (%CR)
0 5 10 15 20 25
TIME
y = -0.1246x + 2.1563
3 FIRST ORDER PLOT R² = 0.8911
HIGUCHI PLOT
y = 24.167x - 0.1394
150
R² = 0.9332
100
% CR
50 %CR
0 Linear (%CR)
-50 0 1 2 3 4 5
SQUARE ROOT OF TIME
1.5
1 log %CR
Linear (log %CR)
0.5
0
0 0.5 1 1.5
LOG TIME
3
cube root of %drug
2 remaining
80
60
F-1 1M
40
F-1 2M
20
F-1 3M
0
0 5 10 15 20
TIME
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