జర్నల్ ఆఫ్ మాలిక్యులర్ ఫార్మాస్యూటిక్స్ & ఆర్గానిక్ ప్రాసెస్ రీసెర్చ్

నైరూప్య

Formulation, Evaluation and Optimization of Enteric Coated Tablets of Erythromycin Stearate by Multivariate Anova Method

Roychowdhury Santanu*1, Singh Hussandeep , Deora Gaurav and Sharma SanchitaFormulation, Evaluation and Optimization of Enteric Coated Tablets of ErythromycinStearate by Multivariate Anova Method

The present investigation concerns with the
event, optimization and evaluation of an enteric coated
tablets of Erythromycin stearate. Tablets were
prepared by wet granulation method. Enteric coating
of Erythromycin stearate tablets were done using two
hydrophilic polymers like ethyl cellulose and pectin
by multivariate ANOVA method by alternating the
two variables X and Y in rows and columns.
Polyethylene glycol was used as a plasticizer while
isopropanol & water was incorporated as a solvent.
The effects of polymers and isopropanol as a binder
on drug release profile, gastro-resistant properties and
matrix integrity of tablet were investigated.
Developed formulations were evaluated for his or
her physical characteristics, drug content,
disintegration time, friability, hardness, thickness,
swelling index, weight variation, In vitro drug release
profile etc. On the basis of various physical
characteristics parameters, it was found that all the
formulations shows good result. On comparative
kinetic modeling study like (Zero order, First order,
Higuchi model and Korsmeyer-Peppas) it had been
found that each one the formulations follow Higuchi
model and coefficient of correlation (R2 ) values were
nearer to unity. Among those formulations, F4 showed
R2 value of Higuchi model more near as compared to
the opposite formulation.
Oral controlled release drug delivery have recently
been of accelerating interest in pharmaceutical field to
realize improved therapeutic advantages, like simple
dosing administration, patient compliance and
adaptability in formulation.1,2 Drugs with short halflives
and drugs that easilyabsorbed from
gastrointestinal tract (GIT) are eliminated quickly
from the systemic circulation.
For these sorts of drugs the event of oral sustainedcontrolled
release formulations is an effort to release
the drug slowly into the alimentary canal (GIT) and
maintain an efficient drug concentration in the
systemic circulation for a long time.3,2 The basic goal
of any drug delivery systems is to provide a
therapeutic amount of drug to the proper site of body
to achieve therapeutic level promptly and then maintain
the desired drug concentration in systemic circulations.4
The most important objectives of these new drug
delivery systems are: First, it would be single dose,
which releases the active ingredient over an extended
period of your time . Second, it should deliver the active
entity on to the location of action, thus, minimizing or
eliminating side effects. To overcome the limitations of
conventional drug delivery system, enteric coated tablets
have been developed. An enteric coating may be a
barrier that controls the situation of oral medication
within the gastrointestinal system where it's absorbed.
The word “enteric” indicates small intestine; therefore
enteric coatings prevent release of medication before it
reaches the tiny intestine. The enteric coated polymers
remain unionise at low pH, and thus remain insoluble.
But because the pH increases within the GIT, the acidic
functional groups are capable of ionisation, and therefore
the polymer swells or becomes soluble within the
intestinal fluid.
Erythromycin stearate was selected as a model drug
which was obtained from Kwality pharmaceuticals Pvt.
Ltd. as a gift sample. The reagents used were pectin,
ethyl cellulose, lactose, isopropyl alcohol, polyethylene
glycol, magnesium stearate, talcum powder, sodium
hydroxide and potassium dihydrogen orthophosphate.
Tablets were prepared by wet granulation method.
Wet granulation is that the most generally used process
of granulation within the pharmaceutical industry. It
involves addition of a liquid solution (with or without
binder) to powders, to make a wet mass or it forms
granules by adding the powder along side an adhesive,
instead of by compaction. The wet mass is dried then
sized to obtained granules. The liquid added binds the
moist powder particles by a mixture of capillary and
viscous forces within the wet state.7 More permanent
bonds are formed during subsequent drying which leads
to the formation of agglomerates.
Enteric coated tablets of Erythromycin stearate were
prepared using two hydrophilic polymers like ethyl
cellulose and pectin by multivariate ANOVA method by
alternating the two variables X and Y in rows and
columns. Eight formulations were prepared. All those
formulations showed good acceptable
Pharmacotechnical characteristics but F4 showed very excellent result as compared to the opposite
formulations and ready to survive the steadiness
testing. Formulations like F4 showed higher stability
as well as more steady state drug release profile. On
comparative kinetic modeling study (such as Zero
order, Higuchi model, First order and Korsmeyer-
Peppas model) it had been found that each one the
formulations follow Higuchi model and coefficient of
correlation (R2 ) values were near to unity. Among
those formulations, F4 showed R2 value of Higuchi
model more near as compared to the other
formulations. The research entitled and result obtained
reveals that the combine effect of enteric coated agent
in different ratio was suitable for long protection of
active pharmaceutical ingredients, from the acidic
environment of the stomach and to provide a delayedrelease
component for repeat action thus minimizing
the first pass metabolism of drugs.
Keywords: Erythromycin stearate, Ethyl cellulose,
Pectin, Polyethylene glycol, Isopropyl alcohol.