7.litreture

Chapter.3 Review Of Literature

NIMS Institute Of Pharmacy, NIMS University Jaipur Page 44

3. REVIEW OF LITERATURE

A Arunachalam et al (2010) developed Metoprolol Succinate and Telmisartan combination

in a single dosage form. it enhanced the patient compliance and prolong cardiovascular

system, Various polymers, such as hydroxy propyl methylcellulose K4M (HPMC- K4M),

hydroxy propyl methylcellulose K100M (HPMC- K100M), MCCpH102, Lactose DCL 11,

Bronopol, were studied. The HPMC- K4M was found to be best in controlling the release. In-

vitro dissolu-tion studies were carried out for all the bi-layered tablets developed using USP

dissolution apparatus type 2 (paddle).

Atul Kuksal et al (2006) prepared and characterized extended-release matrix tablets of

zidovudine using hydrophilic Eudragit RLPO and RSPO alone or their combination with

hydrophobic ethyl cellulose. Release kinetics was evaluated by using United States

Pharmacopeia (USP)-22 type I dissolution apparatus. Scanning electron microscopy was used

to visualize the effect of dissolution medium on matrix tablet surface. Furthermore, the in

vitro and in vivo newly formulated sustained-release zidovudine tablets were compared with

conventional marketed tablet (Zidovir, Cipla Ltd, Mumbai, India). The in-vitro drug release

study revealed that either Eudragit preparation was able to sustain the drug release only for 6

hours (94.3% ± 4.5% release). Combining Eudragit with ethyl cellulose sustained the drug

release for 12 hours (88.1% ± 4.1% release).

B. S. Sudha et al (2010) evaluated hydrogenated cottonseed oil (HCSO) as a Extended

release matrix for a freely soluble drug, tramadol. Hydrophobic matrix tablets of tramadol,

was evaluated by compression of physical mixture of drug and wax, dispersion of drug in

HCSO by hot fusion or solubilisation techniques. The method of preparation of tablet had a

significant effect on drug release with higher release observed from direct compression

matrices and slower release from matrix prepared by dispersion (hot-fused matrices).

Durgacharan A et al (2008) evaluated Glyceryl monostearate and Stearic acid in formulation

of extended release dosage form of water soluble drugs. It was decided to study the effect of

these waxes at different drug: wax ratios, on the release profile of drug from matrix

formulations prepared using Glyceryl monostearate, Stearic acid and both waxes in

combination. The Extended release matrices of Verapamil HCl were prepared by melt

granulation technique in different drug: wax ratios. Drug release was studied by using USP

apparatus-I with pH 1.2 for one hour and pH 6.8 for seven hours. The drug release profile



3compared with marketed formulation and specifications given in USP for extended release

Verapamil HCl tablets.

Frank w. et al (1994) characterized the release of drug from a wax matrix tablet under

relatively mild agitation conditions. It was found that phenylpropanolamine hydrochloride

was released from a typical wax matrix by a diffusion mechanism. After an initial rapid

release of drug from the tablet, the amount dissolved was proportional to the square root of

time. The advance of the solvent front into the tablet matrix was also proportional to the

square root of time. Compression force was not a major factor affecting drug release. Data on

drug release from a single tablet face compared to release from a totally exposed tablet

indicated that drug release is proportional to the total surface area.

Gbolahan Samuel et al (2007) studied the solubility of ibuprofen in Witepsol H15, a semi-

solid wax matrix. Higuchi release rates and Hyper DSC (high speed differential scanning

calorimetry ); solubility values of 15–20%, 18.6% and 12.7% w/w resulted from the three

techniques, respectively. Microscopy was useful in additionally examining crystal size, shape

and homogeneity. Release rate experiments showed that release from these formulations

followed Higuchi kinetics with an inflection in release rate constant at the drug loading

corresponding to drug solubility. Hyper DSC not only measured solubility but also

determined the melting point of the formulation. The results from these three techniques

correlated well, suggesting that the simpler techniques of microscopy or Hyper DSC are

appropriate to determine the solubility in semi-solid pharmaceutical formulations.

Hadi Mehrgan et al (2005) studied effects of various hydrophilic (HPMC and Carbopol 971)

and plastic (Ethylcellulose and Eudragit RL100) polymers on the release profile of diltiazem

HCl from matrix tablets were evaluated in-vitro. For this purpose, tablets containing 60 mg of

diltiazem HCl along with various amounts of the aforementioned polymers were prepared

using the wet granulation technique. The results showed that all the polymers used in this

study could slow down the release of diltiazem HCl from the matrices prepared. This effect,

except for HPMC, generally increased proportionately with the amount of polymer. HPMC

imparted the best control over drug release and could sustain it for approximately 6 h. All the

matrices prepared had a burst release initially; however, it was minimum with HPMC-

containing formulations. Fitting of release data to different kinetic models showed that

HPMC-matrices conformed best to Hixson-Crowell model, 4 ethylcellulose-matrices to

Higuchi and both Eudragit RL100 and Carbopol 971-formulations to either of Hixson-

Crowell, Higuchi and first-order kinetics.



Hamdy Abdelkader et al (2007) investigated different types and levels of hydrophilic

matrixing agents, including methylcellulose (MC), sodium alginate (Alg), and sodium

carboxymethylcellulose (CMC), in an attempt to formulate controlled-release matrix tablets

containing 25 mg baclofen. The tablets were prepared by wet granulation. Prior to

compression, the prepared granules were evaluated for flow and compression characteristics.

In vitro, newly formulated controlled-release tablets were compared with standard

commercial tablets (Lioresal and baclofen). The excipients used in this study did not alter

physicochemical properties of the drug, as tested by the thermal analysis using differential

scanning calorimetry. The flow and compression characteristics of the prepared granules

significantly improved by virtue of granulation process. Also, the prepared matrix tablets

showed good mechanical properties

Hiroyuki Kojima et al (2008) evaluated the feasibility of using a counter polymer in

polyethylene oxide (PEO)/polyethylene glycol (PEG) polymeric matrices for the extended

release of a large amount of highly water-soluble drug. PEO/PEG matrix tablets (CR-A)

containing four drugs with different water solubilities were prepared to investigate the effect

of drug solubility on the drug-release and diffusion properties of PEO/PEG matrices. Cross-

linked carboxyvinyl polymer (CVP)/PEO/PEG matrix tablets (CR-B) containing a water-

soluble drug, diltiazem hydrochloride (DTZ), were also prepared, and their in vitro

characteristics were compared with those of CR-A. Their in vitro drug release properties were

evaluated using a dissolution test, and the polymeric erosion and drug diffusion properties of

the matrices were also calculated. Drugs with higher solubility in water were released faster

for the CR-A.

Hua-Pinh Uangs et al (1994) evaluated acrylic polymer-wax matrix system for oral

sustained-release tablets of diphenhydramine HCI. A desirable release profile of

diphenhydramine was achieved by incorporating Eudragit L in a carnauba wax matrix. In this

polymer-wax system, carnauba wax maintained the integrity of the matrix, whereas Eudragit

L slowly eroded in the matrix as the drug was released. Thus, the area-to-volume ratio of the

tablet remained constant over the duration of the drug release.

K. Raghuram Reddy et al (2003) developed once-daily sustained-release matrix tablets of

nicorandil. The tablets were prepared by the wet granulation method. Etha-nolic solutions of

ethylcellulose (EC), Eudragit RL-100, Eudragit RS-100, and polyvinylpyrrolidone were used

as granulating agents along with hydrophilic matrix materials like hydroxypropyl

methylcellulose (HPMC), sodium car-boxymethylcellulose, and sodium alginate. Ac-cording



to the theoretical release profile calculation, a once-daily sustained-release formulation should

release 5.92 mg of nicorandil in 1 hour, like conventional tablets, and 3.21 mg per hour up to

24 hours. The results of dissolution studies indicated that formulation F-I (drug-to-HPMC,

1:4; ethanol as granulating agent) could extend the drug release up to 24 hours.

Mine O¨ zyazıcı et al (2006) investigated the swelling and relaxation properties of lipid

matrix on diffusional exponent (n). The second aim was to determine the desired release

profile of metronidazole lipid matrix tablets. They prepared metronidazole lipid matrix

granules using Carnauba wax, Beeswax, Stearic acid, Cutina HR, Precirol_ ATO 5, and

Compritol_ ATO 888 by hot fusion method and pressed the tablets of these granules. Stearic

acid showed the highest and Carnauba wax showed the lowest release rates in all formulations

used. Swelling ratios were calculated after the dissolution of tablets as 9.24%, 6.03%, 1.74%,

and 1.07% for Cutina HR, Beeswax, Precirol_ ATO 5, and Compritol_ ATO 888,

respectively. There was erosion in Stearic acid, but neither erosion nor swelling in Carnauba

wax, was detected.

M.u. Uhumwangho et al (2006) prepared matrix granules of acetaminophen formed by a

melt granulation process whereby the acetaminophen powder was triturated with the melted

wax - goat wax, glyceryl monostearate or carnuba wax. The compressibility of the matrix

granules and their admixture, with diluent granules (lactose, α-cellulose or microcrystalline

cellulose) was investigated. Matrix granules prepared by melt granulation with goat wax or

glyceryl monostearate were too sticky and therefore did not flow at all. They were also poorly

compressible (T values = 0.20MN/m2). By contrast the matrix granules formed with carnuba

wax were free flowing (angle of repose, 18.60). Addition of the diluent further improved

flowability slightly. The matrix granules (without a diluent) were readily compressible (T

value, 1.79MN/m2). Addition of the diluent (80%w/w) reduced T values (MN/m2) slightly to

1.32 (lactose), 1.48 (α-cellulose) and 1.74 (microcrystalline cellulose). Tablets of the matrix

granules only, disintegrated rapidly within 3minutes. 6

Prajapati B.G et al (2010) developed hydrophilic polymer and hydrophobic polymer based

matrix Losartan potassium Extended release tablet which can release the drug up to time of 24

hrs in predetermined rate. Formulation of Losartan potassium matrix tablet was prepared by

the polymer combination in order to get required theoretical release profile. Influence of

hydrophilic and hydrophobic polymer on Losartan potassium was studied. Formulated tablet

were also characterized by physical and chemical parameters. In vitro release profile was

check for 24 hrs to evaluate the SR matrix tablet of Losartan potassium.



Ravouru Nagaraju et al (2009) prepared core-in-cup matrix tablets of Metoprolol succinate

by wet granulation technique. Of all the investigated formulations, the optimized formulation

of MS-09 followed zero-order kinetics of drug release. Trail on MS- 09 was formulated using

7.5% hydrogenated castor-oil (HCO) and 4% of hydroxyl propyl methylcellulose (HPMC

K15M) with an objective to achieve a linear release profile for 24 h. There was no initial burst

release, with 16.17% of drug released during the first hour and release was extended up to 24

hrs. Study of drug release kinetics was performed by application of dissolution data to various

kinetic equations like zero-order; first order, Higuchi and Korsmeyer-Peppa

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