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ABSTRACT
The study was undertaken with an aim to formulate develop and evaluation of a novel twice daily core cup of
Metformin hydrochloride(Antidiabetic drug) tablets using different grades and weight of H PMC polymers as
release retarding agent. Granules were evaluated for tests Bulk density, tapped density, Hausner ratio before
being punched as tablets. Tablets were tested for weight variation, thickness, hardness and friability as per
official procedure. F-2 was found to be 73.90. From the above results and discussion it is concluded that
formulation of Cup core tablet of containing Metformin hydrochlor ide HPMC K 4M & 215: 230 (in mg) can be
taken as an ideal or optimized formulation of sustained release tablets for 12hour release as it fulfills all the
requirements for sustained release tablet and our study encourages for the further clinical trials on this
formulation. The core in cup tablets of Metformin hydrochloride were prepared by wet granulation method, they
were evaluated for weight variation, friability, hardness, and thickness for all batches (F1 – F9). No significant
difference was observed in the weight of individual tablets from the average weight. The weight variation tests
were performed according to the procedure given in the pharmacopoeia. In a weight variation test,
pharmacopoeial limit of tablet for percentage deviation is 5%. The avera ge percentage deviation of all tablet
formulation was found to be within the pharmacopoeial limit and hence all formulation passed the test for
uniformity of weight.
Keywords: Metformin, HPMC, Diabetes.
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delivery system for administration of various undesirable toxicity and poor efficiency. 8 The
drugs. 6,7 The attractiveness of these dosage forms is maintenance of concentration of drug in plasma
due to awareness to toxicity and ineffectiveness of within therapeutic index is very critical for
drugs when administered by oral conventional effective treatment. 9 These factors as well as
method in the form of tablets and capsules. Usually factors such as repetitive dosing and unpredictable
conventional dosage form produces wide range of absorption lead to the concept of oral Sustained
fluctuation in drug concentration in the release drug delivery systems. 10, 11
bloodstream and tissues with consequent
METHODOLOGY
Methods of preparation of cup core tablets
TABLE NO: 1 MATERIAL USED IN FORMULATION
S.NO MATERIALS USED GRADE COMPANY
1 Metformin hydrochloride Essel fine chem, Mumbai
3 Hydroxy propyl methyl cellulose (Hpmc k15M) LR Essel fine chem, Mumbai
4 Hydroxy propyl methyl cellulose(Hpmc k100M) LR Essel fine chem, Mumbai
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Preparation of cup granules time. The dried granules were passed through sieve
no. 22 to form granules of uniform size.
The core tablets were compression coated with
different weight ratios (w/w) of HPMCK4M, Compression of Cup core Tablets
HPMCK15M, HPMC K100 M mixtures. Weighed
Rapid release core tablets composed of the active
quantities of Metformin hydrochloride, SSG,
ingredient were manually placed in the centre of
Microcrystalline cellulose, Talc, Magnesium
9mm die cavity on a punching machine (IP
Stearate, were mixed with each other according to
machineries’ pvt.ltd, Ahmadabad), before the
the geometric method. For each formulation
addition of the cup material and the machine was
(TABLE NO: 2) and granules are prepared by
run until the lower punch moved down slightly.
adding 5%Starch paste. The granules were dried in
Weighed quantity of the blend for the cup was
a Hot air oven (B.T.I. Instruments) for sufficient
manually poured into the die cavity using a spatula,
and finally compressed.
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Sravanthi T et al, ICJPIR 2016, 3(2), 119-128
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Sravanthi T et al, ICJPIR 2016, 3(2), 119-128
2 1hr 48.73 31.41 14.16 11.84 8.76 8.06 11.56 7.22 5.96
3 2hr 68.18 38.63 20.89 15.07 11.77 9.46 13.04 9.46 7.57
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4 3hr 103,24 55.04 26.99 20.96 13.95 11.84 16.19 12.90 9.25
5 4hr 103.42 69.06 30.29 24.19 15.42 14.16 18.16 14.93 12.55
6 5hr 87.29 36.53 28.11 18.30 17.17 21.73 17.17 14.37
7 6hr 91.67 51.39 32.88 20.05 20.19 26.99 19.91 16.47
8 7hr 107.28 59.24 35.76 25.10 22.43 29.87 21.38 20.12
9 8hr 69.34 37.72 29.44 2.82 33.51 23.55 21.10
10 9hr 74.67 41.93 33.51 28.25 35.76 27.27 23.48
11 10hr 85.71 45.22 37.30 30.78 38.21 29.44 25.59
12 11hr 99.74 55.32 38.42 34.28 42.14 32.60 27.62
13 12hr 99.04 61.28 42.21 36.46 48.17 36.46 30.29
350
Time
300 (f1)%0f d.r
(f2)%of d.r
250
%of drug release
(f3)of d.r
200 (f4)of d.r
50 (f8)of d.r
y = 0.0814x - 0.0416
R² = 0.984 (f9)of d.r
0
Linear (Time)
0 5 10 15
Time hr Linear ((f1)%0f d.r)
Figure 1
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Sravanthi T et al, ICJPIR 2016, 3(2), 119-128
60 (f3)of d.r
Linear ((f3)of d.r)
40
Linear ((f3)of d.r)
20
0
0 5 10 15
Time
Figure: 2
DISCUSSION drug release 48.1712% in 12hours (TABLE NO:
12). In case of Tablets F8 containing drug.
Standard calibration curve of Metformin
HPMCK100M (in mg) 215: 200. The release
hydrochloride was prepared in phosphate buffer
profile was showing drug release 36.46138% in 12
medium 6.8pH.Correlation coefficient values
hours (TABLE NO: 13). In case of tablets F9,
indicate the linear correlation between
containing drug. HPMCK100M (in mg) 215:230.
concentration and absorbance and following
The release profile was showing drug release
lamberts beers law. The release of Metformin
30.29099% in 12hours (TABLE NO: 16, with very
hydrochloride from sustained release tablet of
slower release than all formulations).
various formulations varied according to the ratio
and degree of the polymer.
In case of tablets of F1 containing drug & SUMMARY AND CONCLUSION
HPMCK4M (quantity in mg). 215: 170. The release
The study was undertaken with an aim to
profile was showing the release 103.4241% in
formulate develop and evaluation of a novel twice
4hours (TABLE NO: 6). In case of tablets of F2
daily core cup of Metformin
containing drug and HPMC K4M (in mg).
hydrochloride(Antidiabetic drug) tablets using
215:200 it was showing 107.2806% release in 7
different grades and weight of Hpmc polymers as
hours (TABLE NO: 7). In case of tablets of F3
release retarding agent. Granules were evaluated
containing drug polymer (HPMCK4M in mg) 215:
for tests Bulk density, tapped density, Hausner ratio
230: but it was showing 99.7429% up to 12 hour
before being punched as tablets. Tablets were
(TABLE NO: 8). In case of tablets F4 containing
tested for weight variation, thickness, hardness and
drug and HPMC K15M (in mg) 215:170 the release
friability as per official procedure. F-2 was found
profile was showing drug release61.28316 % 0nly
to be 73.90. From the above results and discussion
up to 12hours(TABLE NO: 9). In case of tablets of
it is concluded that formulation of Cup core tablet
F5 containing drug and HPMC K15M (in mg)
of containing Metformin hydrochloride HPMC K
215:200.But it also showing the drug release
4M & 215: 230 (in mg) can be taken as an ideal or
42.2116% in12hours (TABLE NO: 10). In case of
optimized formulation of sustained release tablets
tablets of F6 containing drug and HPMC K 15M (in
for 12hour release as it fulfills all the requirements
Mg) 215: 230. It was seen the release of drug
for sustained release tablet and our study
shown 36.46138% in 12hours (TABLE NO: 11). In
encourages for the further clinical trials on this
case of tablets F7, containing drug. HPMCK100M
formulation.
(in mg) 215:170 the release profile was showing
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BIBLIOGRAPHY
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