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Pendahuluan
Helicobacter pylori (H. pylori) infect more than half of the
world population, making it one of the most prevalent infections.
H. pylori is now accepted as the most common cause of
histologicgastritis and is responsible for the majority of cases of
pepticulcer disease and gastric cancer. Approximately 1 in 6
(17%)persons with H. pylori infection will develop peptic ulcer
disease,and each year 1% to 2% of these will experience a major or
life-threatening complication.
Therefore, some researchers had prepared and reported
newamoxicillin trihydrate formulations, such as float
tablet,mucoadhesive tablet and pH-sensitive excipient
compositionmucoadhesive microspheres etc., which were able to
reside inthe gastrointestinal tract for an extended period of time
for amore effective H. pylori eradication
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Material Amoxicillin trihydrate (powder) and Eudragit
RS100 was obtained as gift sample from RanbaxyPvt. Ltd
Gurgaon
Hydroxypropylmethyl cellulose (K4M) wasobtained as gift sample
from Orchid Lab, Chennai
Span 80 was purchased from Loba Chemicals. Pvt.Ltd. Mumbai
Light Liquid Paraffin, Acetone AR, ConcentratedHCl LR, Potassium
dihydrogen phosphate AR,Sodium hydroxide LR were purchased from
NiceChemicals Pvt. Ltd. Cochin
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Preparation of MucoadhesiveMicrospheres
Amoxicillin trihydrate microspheres were formulated usingsolvent
evaporation technique, Using Eudragit RS100 asmatrix polymer.
Eudragit was dissolved in required quantity ofacetone, the HPMC K4M
and drug was dispersed with thepolymer solution. The dispersed
content was placed drop
wise in light liquid paraffin containing span80 maintained
at40oC while stirring at 75050 rpm. The solvent, acetone wasthen
removed by continuous stirring at room temperature forthree hours
to produce spherical microspheres. Themicrosphere were than
separated from liquid paraffin byfiltration through whatmann filter
paper, the microsphereswere collected and washed three times with
n-hexane anddried using vacuum filtration. The product was then
air-driedto obtain microspheres
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Evaluasi
Physico-chemical and Morphologicalcharacterization of
microspheres
Swelling studies In vitro wash-off test Determination of drug
content Encapsulation efficiency In vitro dissolution studies
Kinetics of drug release
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Morphological characterization ofmicrospheres
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Swelling studiesSwelling Ratio (SR) = (We-W0)/W0
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In vitro wash-off test
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Drug release
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Drug release behavior
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Kesimpulan
Amoxicillin trihydrate mucoadhesive microspheres wereprepared
successfully by using the solvent evaporationmethod
From the study, it was concluded that the amoxicillintrihydrate
mucoadhesive microsphere prepared with HPMCK4 and Eudragit RS100
shows delayed release rate of drugas the concentration of both the
polymer weresimultaneously increased.
The formulation F7 (Amoxicillin trihydrate 250mgequivalent to
235 mg of Amoxicillin, HPMC K4M 480mg,Eudragit RS100 1000mg) was
selected as optimizedformulation for further factorial design; with
96.15% ofdrug release at 12th hour. The prepared microspheresproved
to be good candidate for site-specific drug release
