Authors :
Abali S. Okorie; Ifeoma C. Ekenna; Ochen Faithfulness
Volume/Issue :
Volume 7 - 2022, Issue 3 - March
Google Scholar :
https://bit.ly/3IIfn9N
Scribd :
https://bit.ly/3IT9u9T
DOI :
https://doi.org/10.5281/zenodo.6406166
Abstract :
The bioavailability of a drug is usually
determined by its aqueous solubility and lipid
permeability. Nevirapine is an antiretroviral drug that
belongs to the BCS II with poor solubility but high
permeability. This study was carried out to improve the
dissolution of nevirapine and also to formulate
extended-release nevirapine tablets. Nevirapine: PEG
4000 were combined in different ratios to produce
physical mixtures and solid dispersions. Micromeritics
studies were carried out on the particles of the solid
dispersions and the physical mixtures. These physical
mixtures and solid dispersions were then compressed
into tablets. Micromeritic studies showed that the
particles had fair to poor flow qualities, particle sizes
were between 0 -20 µm. Organoleptic results showed
round white tablets. The formulated tablets and the
commercial brand passed the hardness test, PM1 and
SD1only failed the friability tests. PM1 and the
commercial brand displayed properties of an
immediate-release tablet with disintegration times
below 15 minutes and all drugs were released before 2
hours. Dissolution efficiency showed that the solid
dispersion tablets with the highest concentration of
polymer had the best DE. Compared with the physical
mixture counterpart, the solid dispersions had a better
dissolution and drug release. The PEG 4000 helped in
extending the release of nevirapine drugs as seen by the
extended-release of the nevirapine: PEG 4000 batches
and the solid dispersion technique improved nevirapine
dissolution.
Keywords :
Nevirapine, dissolution, PEG 4000, solid dispersion, extended-release, physical mixtures, dissolution efficiency, dissolution profiles, polymer.
The bioavailability of a drug is usually
determined by its aqueous solubility and lipid
permeability. Nevirapine is an antiretroviral drug that
belongs to the BCS II with poor solubility but high
permeability. This study was carried out to improve the
dissolution of nevirapine and also to formulate
extended-release nevirapine tablets. Nevirapine: PEG
4000 were combined in different ratios to produce
physical mixtures and solid dispersions. Micromeritics
studies were carried out on the particles of the solid
dispersions and the physical mixtures. These physical
mixtures and solid dispersions were then compressed
into tablets. Micromeritic studies showed that the
particles had fair to poor flow qualities, particle sizes
were between 0 -20 µm. Organoleptic results showed
round white tablets. The formulated tablets and the
commercial brand passed the hardness test, PM1 and
SD1only failed the friability tests. PM1 and the
commercial brand displayed properties of an
immediate-release tablet with disintegration times
below 15 minutes and all drugs were released before 2
hours. Dissolution efficiency showed that the solid
dispersion tablets with the highest concentration of
polymer had the best DE. Compared with the physical
mixture counterpart, the solid dispersions had a better
dissolution and drug release. The PEG 4000 helped in
extending the release of nevirapine drugs as seen by the
extended-release of the nevirapine: PEG 4000 batches
and the solid dispersion technique improved nevirapine
dissolution.
Keywords :
Nevirapine, dissolution, PEG 4000, solid dispersion, extended-release, physical mixtures, dissolution efficiency, dissolution profiles, polymer.
