Literature review

4. LITERATURE REVIEW
Literature review indicating advancement in sustained release matrix tablets is given
below:
Saptarshi D., et al.28 An attempted was to prepare the Metformin hydrochloride
matrix tablets by taking hydroxyl methyl cellulose polymer (HPMC) as rate regulating factor
for oral sustain release and to estimate drug release parameters as per different release kinetic
models. It is examined that the basic goal of analysis in the improvement of Metformine
hydrochloride release dosage form is to maximize bioavailability; decrease risk of
hospitalization, deliver drug at an available constant rate for approximately 12hrs;
independent of and gastrointestinal pH. The dry granulation method was used to prepare the
tablet as powder expose the poor flowability; less cohesiveness at the time direct compression
and due to moisture sensation and usage to hydrolyte, wet granulation system was not taken
for the present work.
Dhirendra K, et al.13 The present study was to prepare once Stavudine daily
sustained release matrix tablets to extend therapeutic efficacy, decrease frequency of
administration and develop patient compliance. The sustained release tablets were formulated
by direct compression and prepared by taking different drug: polymer ratios, preparations as
F1 to F15. Polymers of Hydrophilic like Hydroxypropyl methylcellulose (HPMC), Carboxy
methyl cellulose (CMC) and starch 1500 were taken. Compatibility of the drug with different
excipients was carried. The prepared tablets were evaluated and done compliance with
pharmacopoeial standards.

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Madhusmruti K, et al23 The main objective of the work was to develop sustain
release matrix formulation of Propanolol hydrochloride and consider the effects of both
hydrophobic and hydrophilic polymer on in-vitro drug release. Matrix tablets were processed
by direct compression method by different concentrations of Ethyl Cellulose (EC) and
Hydroxypropyl methylcellulose (HPMC). Prepared formulations were administer to different
studies like friability, hardness, thickness, weight variation, %drug content, dynamic of
erosion and water uptake etc. Tablets were administered to in-vitro drug release in 0.1N HCl
(pH 1.2) for first 2 hours result by phosphate buffer (pH 6.8) remaining time.
Jayaprakash S., et al.17 The sustained release (SR) tablets of Ambroxol
Hydrochloride were formulated by Wet granulation process. The conclusion of hydrophilic
matrices on the act of Ambroxol hydrochloride using distinct polymers and their
combinations. The formulated tablets were calculated for physical characteristics such as
Thickness, Hardness, Weight Variation, Friability, Content uniformity and in-vitro release
behavior. The drug release from the optimized preparation was shown to follow zero order
kinetics.
Umesh D.S, et al.34 The main objective of the present work was to develop daily
once

sustained

release

tablets

of

Aceclofenac

by

wet

granulation

using

carboxypolymethylene polymer. The drug excipient mixtures were advice to preformulation

studies during the time the tablets were administer to physicochemical studies, stability
studies, in vitro drug release and validation studies.
Raghavendra R.N.G, et al.26 The main objective of the present work was to develop
water soluble Tramadol hydrochloride sustained release matrix tablets using different
polymers viz. Hydroxypropyl methylcellulose (HPMC) and natural gums like carrageenan

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gum (CG) and karaya gum (KG).Changing ratios of drug and polymer like 1:1 and 1:2 are
taken for the study. After arranging the drug :polymer for control the release of drug upto
choose time, the release rates were regulate by combination of two differential rates triple
mixture and controlling material of three differential rate controlling material.
Anton S, et al.7 The main objective was to improve Ondansetron Hydrochloride(5mg)
formulated sustained release matrix tablets apply Hydroxypropyl Methyl Cellulose(HPMC),
polymer and the sustained release management of the tablets was considered. Tablets were
formulated by wet granulation process.
Parasuram R.R, et al.25 The aim of the present project was to arrangement of
Glipizide an oral sustained release matrix tablet and to optimize the drug discharge profile by
considering return surface approach. The tablets were formulated by the wet granulation
process using Eudragit L 100 and HPMC K100 as matrix forming polymers. A central
compound design for 2 factors at 3 levels each was active to systematically optimized drug
release profile. Eudragit L 100 and HPMC K100 are shown as the independent variables. The
dependent variables chosen were % of drug discharged in 2 h (release 12 h).
Kalyani C, et al.18 The aim of the study was to design Zidovudine oral sustained
release matrix tablets using Guar Gum, Ethyl Cellulose and Hydroxypropyl methylcellulose
(HPMC)K 4M, as the holdup polymers and study the effect of different preparation factors
such as polymer distribution, polymer effect and type of filler type on the in-vitro release of
drug. Matrix tablets were by Wet granulation process and formulated tablet were evaluated
%friability, weight variation, thickness, in-vitro dissolution studies and hardness. All the
granules and process showed compliance with pharmacopeial standards. In-vitro release
studies declare that the release rate reduces with increase polymer proportion and
hydrophobic polymers close off the drug release increased than hydrophilic polymers.
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Tapan K.P, et al.33 The aim of the project study was to prepare Metformin HCl an
oral sustained release matrix tablet and to optimize the drug discharge profile by discharge
surface methodology. Tablets were formulated by non-aqueous wet granulation technique
using a matrix forming polymer HPMC K 15M. A central composition arrangement for 2
factors at 3 levels each was active to systematically optimize drug release profile. PVP K 30
(X2) and HPMC K 15M (X1) were using as the independent variables. The dependent
variable selected were % of drug discharged in 1 hr (rel1hr), % of drug release in 8 hr (rel8hr),
and time to 50% drug release (t50%).
Basak S. C, et al.9

Monolithic matrix tablets of Ambroxol Hydrochloride are

prepared as sustained release tablets apply Hydroxypropyl methylcellulose polymer, and the
sustained release matrix tablets consisting 75 mg Ambroxol hydrochloride were improved
taking different drug :polymer of Hydroxy propyl Methyl Cellulose. Tablets were formulated
by direct compression. Preparation was optimized on the base of adequate tablet properties
and in vitro drug release.
Varshosaz J, et al.35 The aim of this project was to improve highly water-soluble
Tramadol HCl matrix sustained release tablets using natural gums Guar [G gum] and
Xanthan [X gum] as nontoxic, cost-effective, easily applicable and advisable hydrophilic
matrix systems corelated with greatly investigated hydrophilic matrices (ie, Carboxymethyl
cellulose [CMC] /Hydroxypropyl methylcellulose [HPMC]) related to hydration rate and invitro drug release rate of the polymers. Tramadol Matrix tablets (dose 100 mg) are produced
by direct compression technique.

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Muhammad K.S, et al.24 The present study was done to investigate the low viscosity
grades of ethyl cellulose (EC) and Hydroxypropyl methylcellulose (HPMC) in approve the
discharge of water insoluble drug, Naproxen from the matrix tablets. Both EC and HPMC
were integrated in the matrix system independently or in combinations by wet granulation
method. In vitro dissolution studies recorded that EC significantly decrease the rate of drug
release correlated to HPMC in 12hr testing time. But, no important difference was examined
in the discharge profiles of matrix tablets formed by higher percentages of EC.
Yeole P.G., et al.36 In the present study, and workout has been made to decrease
frequency of administration, maximize therapeutic efficacy, and develop patient compliance,
by improving Diclofenac sodium sustained release matrix tablets. Diclofenac sodium
Sustained release matrix tablets, were improved by using distinct drug: polymer ratios.
Xanthan gum was used as matrix former, and microcrystalline cellulose as diluents.
Compressed tablets were evaluated for friability, uniformity of weight, thickness, hardness, in
vitro dissolution and content of active ingredient, using swelling index and basket method.
Hosseinali T, et al.16 A sustained release tablet preparation must ideally have a proper
release profile unresponsive to moderate changes in tablet hardness that is commonly close in
preparing. In the study, matrix Aspirin (acetylsalicylic acid) tablets with ethyl cellulose (EC),
Eudragit RL100, Eudragit S100 were formulated by direct compression. The release act were
then studied in two complement series of tablets with hardness variation of three Kp units,
and correlated by non-linear backsliding analysis.
Raghuram R.K, et al.27 The aim of the present study was to improve once-daily
Nicorandil sustained- release matrix tablets, a novel potassium channel opener taken in
cardiovascular diseases. The tablets were formulated by the wet granulation technique. ethyl

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cellulose(EC) Ethanolic solutions, Eudragit RL-100, Eudragit RS-100, and poly vinyl
pyrrolidone are taken as granulating agents on with hydrophilic matrix substances like
sodium carboxy methyl cellulose, Hydroxy propyl Methyl Cellulose(HPMC), and sodium
alginate.
Chandria M., et al.11 The present investigation attempt has been made maximize
therapeutic efficacy , decrease frequency of control and develop patient Compliance, by
improving Zidovudine sustained release matrix tablets, Were developed by using drug
polymer ratio kollidon SR, HPMC k15M, HPMC K100M as matrix former, all lubricated
formulation were compressed by direct compression and wet granulation method.
Krishnaiah Y.S.R., et al.21 The aim of the present project is to carry out
pharmacokinetic evaluation of oral controlled release formulation (guar gum-based three
layer matrix tablets) containing highly soluble Metoprolol tartrate as a model drug. Six
healthy volunteers taken in the study, and a two way crossover design was ensue. The plasma
content of Metoprolol tartrate was approximated by HPLC reverse-phase. The
pharmacokinetic parameters were estimated from the plasma concentration of metoprolol
tartrate vs time data.
Suvakanta D., et al.31 In this paper were reviewed mathematical models used to
determine the kinetic of drug release from drug delivery system the quantitative analysis of
the values are obtained in dissolution/ release rate is easier when mathematical formula used
to describe the process. The mathematical modeling can optimize to design therapeutic
design of therapeutic device to yield information on the various efficacy of various release
models.

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Ganesan V., et al.,

15

The main aim of the present project was to improve matrix

tablets of guar gum for oral controlled release of Ambroxol hydrochloride. Present to the
theoretical release profile estimation, a twice daily sustained release preparation must release
19.6 mg of Ambroxol hydrochloride in 1 hr like conventional tablets, and 5.2 mg per hour
upto 12 hours. Ambroxol hydrochloride matrix tablets containing either 30%wt/wt of low
viscosity (F-III), 25% wt/wt medium viscosity (F-VI) or 20 %wt/wt high viscosity (F-IX)
guar gum showed sustained release.
Keny R.V., et al.19 The present work was aimed to improve once daily minocycline
hydrochloride extended release matrix tablets, using HPMC either alone or in combination
with ethyl cellulose as the matrix substance in different concentrations. The prepared tablets
were also correlated with a marketed substance. The results of the dissolution study show that
preparations FC-IV, FC-V, FC-VI, gives maximum drug release upto 24 hr. Drug release
from matrix caused by synthesis of two mechanisms diffusion of tablet matrix and erosion of
tablet surface which was returned from Highuchis model and Erosion plot.
Tabandeh H., et al.32 A sustained release tablet preparation must excellently have a
proper release profile unresponsive to moderate correction in tablet hardness that is
commonly encountered in preparation. In the study, matrix Aspirin (acetylsalicylic acid)
tablets with ethyl cellulose (EC), Eudragit RL100, Eudragit S100 were processed by direct
compression. The release act were then examined in two correlative series of tablets with
hardness change of three Kp units, and correlated by non-linear backsliding analysis.
Sasidhar R.L.C, et al.30 In the present aim work an attempt has been done to reduced
frequency of administration, maximize therapeutic efficacy and develop patient compliance
by improving Losartan Potassium controlled release matrix tablets. Losartan Potassium was

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prepared by using poly (ethylene oxides) {Polyox WSR 303} as oral controlled release
matrix tablets. The investigation of this study was to access of polymer type and level if
fillers namely microcrystalline cellulose, [soluble filler] lactose and [insoluble fillers]
anhydrous dibasic calcium phosphate on the mechanism and release rate of matrix tablets
from Losartan Potassium.

Literature review indicating work carried out on selected drug, Metaprolol succinate is
given below:
Sandeep.g et al

29

, formulate and characterize extended release matrix tablets of

metaprolol succinate using hydrophilic polymers like hydroxypropyl methyl cellulose

(HPMC K100M), hydroxyl propyl cellulose (HPC), ethyl cellulose, carbopol 934 ans
magnesium stearate, and these selected matrices were directly compressed into tablet. The
physical parameters of the granules and tablets were studied.
Deshmukh .V. N et al,14 designed and evaluate metoprolol succinate using natural
hydrophilic gums such as xanthan gum and karaya gum as a release modifier as oral
sustained drug delivery system for. Matrix tablets were formulted by wet granulation
technique and were evaluated for hardness, content uniformity, thickness, and weight
variation, friability, swelling index, stereo photography and invitro dissolution. The
kinetic analysis display that the optimized preparation as per ICH guidelines follow
zero order kinetic with release exponent (n)0.7656 and having good stability. The
matrix preparation containing 38.4 and 9.6 of Karaya gum and Xanthan gum
respectively display metotprolol succinate sustained release by the diffusion mechanism.

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Gothi G.D., et al. (2010)15 In the present study and an attempt was done to decrease
the frequency of dose administration, to eradicate nocturnal heart attack and to develop the
patient compliance by improving metoprolol succinate extended release (ER) matrix tablet.
The conclusion of absorption of hydrophilic (Xanthan gum, hydroxypropyl methylcellulose
[HPMC K 100 M]) on the release rate of metoprolol succinate was examined.
Rajesh z.Mujoriya et al The preparation of Amlodipine Besilate and ER Metoprolol
Succinate and were prepared by using different polymer (Methocel, HPMC, Carbapol) with
different diluents (Croscarmalose Sodium, Cellulose Phosphate, MCC, Starch,) and then
evaluated. Thus it can be achieve that a stable bilayer tablet of Amlodipine besilate and ER
Metoprolol succinate and can be formulate by using carbomer and HPMC K 15 M as a
polymer. It was shown ER Metoprolol succinate that the in vitro drug release was best done
by first order (r2 =0. 9994), as the plots display the highest linearity, show zero-order (r2 =
0.9471), followed by Higuchis equation (r2= 0.9974).
V. N. Deshmukh*, S. P. Singh, D. M. Sakarkar The aim of this study was to
prepare and evaluate Metoprolol succinate oral sustained drug delivery system using natural
hydrophilic gums such as xanthan gum and karaya gum as a release alterer. Nine batches
were formulated by using xanthan gum (XG) and karaya gum (KG) in concentration of 15%,
20% and 25% individually and in combination of 2:8. Matrix tablets were formulated by wet
granulation technique and were evaluated for weight variation, thickness, friability, hardness,
content uniformity, in vitro dissolution, stereo photography and swelling index,.
Ajay L. Barhate, Santosh N. Shinde This work aims at investigating different types
and levels of hydrophilic matrixing agents,including sodium alginate (Alg), and
Hydroxypropyl methyl cellulose K15M (HPMC K15M) in an attempt to prepare 50 mg

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Metoprolol Succinate controlled-release matrix tablets. The tablets were prepared by wet
granulation. The Influence of three granulating fluid, Dichloromethane (DCM), isopropyl
alcohol (IPA), vizacetone & were also studied with a view to develop and design slow release
preparation of Metoprolol succinate.
M. V. V Nageswara; Rao, G. Chandra Sekhara, Narla Santosh Kumar Reddy,
The objective of the present study was to prepare the sustained release matrix tablets
Metoprolol Succinate for production efficient and cost saving procedure. Among different
tablet preparation procedure, direct compression is the cost saving procedure and simplest.
Different trials were preparation and evaluated using different concentrations of directly
compressible grade and Kollidon SR controlled release polymer to match the reference
product dissolution profile. Dissolution studies were conducted using USP recommended
conditions.

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