Bosentan
Hydrochloride (BOS) has a large molecular weight, only a little water
solubility, and eleven hydrogen bond acceptors. It has a low bioavailability as
a result. BOS has recently undergone successful development of a new Solid-Self
Emulsifying Drug Delivery System (S-SMEDDS) to increase its oral
bioavailability by enhancing its solubility and permitting high molecular
weight of BOS absorption. Capmul MCM as the oil, Tween 20 as the surfactant,
and Propylene glycol as a co-surfactant were found to be suitable for the
development of Liquid-Self Emulsifying Drug Delivery System based on
solubility, pseudoternary phase diagram, emulsifying efficiency, and
compatibility tests (L-SMEDDS). The formulation of the BOS loaded L-SMEDDS was
created using various oil, surfactant, and co-surfactant concentrations, and it
was then optimised using a variety of evolutionary parameters, including drug
content, robustness to dilution, ultrasonic interferometer, ease of
emulsification, droplet size, and in vitro diffusion studies. By using a spray
drying process, the improved L-SMEDDS were transformed into freely flowing
granules. The characterisation of S-SMEDDS powder revealed no interactions
between the medication and excipients. Variable concentrations of immediately
compressible excipients were used to compress the S-SMEDDS powder. Both the
pre-compression and post-compression parameters used S-SMEDDS formulas. An in
vitro drug release research showed that all S-SMEDDS tablets significantly
enhanced the drug's rate of dissolution when compared to the commercial
formulation. The Cmax and AUC of BOS significantly increased when compared to
the market formulation during in vivo experiments in Sprague-Dowley rats for
the improved formulation (P>0.05). Thus, the current study increased BOS's
oral bioavailability.
Author(s) Details:
Sandeep C. Atram,
Vidyabharati College of Pharmacy, Amravati, Maharashtra-444602,
India.
Vikrant
P. Wankhade,
Vidyabharati
College of Pharmacy, Amravati, Maharashtra-444602, India.
Please see the link here: https://stm.bookpi.org/CAPR-V6/article/view/8089