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pharmacokinetic parameters were quite different for conventional formulation and NLCs.
Bosentan NLCs absorb through the lymphatic system containing Peyer’s patches.
For the preparation of Microemulsion Capmul MCM C8 was selected as oil, Polysorbate
20 (Tween 20) as a surfactant and Transcutol HP as a co-surfactant. From
Pseudoternary phase diagram ratio of Smix (surfactant: co-surfactant) (1:1) selected.
From the Microemulsion area of ternary diagram different batches were prepared, but the
drug was precipitate from the formulation which can be avoid by adding precipitate
inhibitor. Pluronic F 127 was utilized as precipitate inhibitor in the concentration of 1.5%.
The optimized formulation ME 8 contain oil (30 %V/V), Smix (60 %V/V) and water (10
%V/V). The prepared Microemulsion evaluated for globule size 96.71±0.11 nm, %
transmittance 99.45±0.54 % and >99 % drug content. Transmission electron microscopy
confirm the spherical shape of globule. The physicochemical parameter of ME 8 was
performed and to enhance the stability of Microemulsion and for oral administration
liquid ME converted in to solid ME by using adsorbent. Aeroperl 300 was selected as an
adsorbent in the drug to adsorbent ratio (1:0.5 %W/W) based on physicochemical
properties. From the in-vitro drug release investigation, observed that after 7 hours
cumulative % drug release (CDR) of ME 8 was found to be 78.87±0.17% and solid
Microemulsion (SME 3) shows 76.83±0.29% CDR. The pure drug shows only 27.63±0.23%
CDR in 7 hours, which indicate that ME revealed better drug release than pure drug. There
was a 2.8 fold increases in solubility compare to pure drug. From the In-vivo data
compared to convention formulation, there was significant change in pharmacokinetics
data observed. Stability study for 60 days was carried out. Microemulsion also shows a
satisfactory result in every segment including drug entrapment and solubility
enhancement. But in case of cost effectiveness and drug content point of view
Microemulsion was a best formulation among all the three products.
Key words: Direct compression method; Factorial design; Haemolytic study; hot
homogenization technique, Pseudo ternary phase diagram; Precipitate inhibitors; In-vivo
study
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