ORAL BIOAVAILABITY IMPROVEMENT OF FAMOTIDINE BASED ON SOLID LIPID NANOPARTICLE TESTED TO MALE WISTAR RAT
Famotidine is an active compound which as an agent of histamine antagonist receptor (H2). Famotidine has low bioavailability and only 40-45% absorbed by human body. The low bioavailability of famotidine potentially decreases the activity as agent histamine antagonist receptor for severe pathologi...
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| Format: | Theses |
| Language: | Indonesia |
| Online Access: | https://digilib.itb.ac.id/gdl/view/45314 |
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| Institution: | Institut Teknologi Bandung |
| Language: | Indonesia |
| Summary: | Famotidine is an active compound which as an agent of histamine antagonist
receptor (H2). Famotidine has low bioavailability and only 40-45% absorbed by
human body. The low bioavailability of famotidine potentially decreases the
activity as agent histamine antagonist receptor for severe pathological conditions.
Based on these conditions, an alternative method namely solid lipid nanoparticle
(SLN) was prepared to overcome the problem and bioavailability study was
conducted on male Wistar rats. SLN famotidine was prepared using high speed
homogenization and followed by ultra-sonication in two formula (SLN 1&2).
Characterization of SLN was accomplished on entrapment efficiency (EE),
particle size analysis and zeta potential, morphology, melting point, and physical
stability. Famotidine’s bioavailability with doses of 40 mg/kg BW was evaluated
to male Wistar rat per orally. The particle size of the generated nanoparticles was
in the range of 100-200 nm. EE of famotidine in SLN 1&2 were 82.3 ± 4.39 %
and 81.12 ± 3.79 % . Zeta potential value of SLN 1&2 and suspension were -1.06
mV, -2.89 mV, and 0.09 mV respectively. The melting point of SLN 1&2 were
62,1
0
C and 58,82
0
C, that not much different to the melting point of glyceryl
monostearate (55,50C). The morphology of the nanoparticles was spheric. The
particle size of the SLN 1&2 were relative stable in the nanometer range in period
of one week (SLN 1) and two weeks (SLN 2). Relative bioavailability (AUC0-?)
of the SLN 1&2 increased about 4.28 and 4.66 times higher than the suspension.
The parameters t1/2el, tmax, and t1/2ab were analyzed using ANOVA test and the
result were not significant difference (p<0.05). Solid lipid nanoparticles (SLN)
can be used as alternative method to increase the bioavailability of famotidine.
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