Objective: Paracetamol is a common antipyretic and analgesic medicine used in childhood illness by parents and physicians worldwide. Paracetamol has a bitter taste that is considered as a significant barrier for drug administration. This study aimed to develop an oral dosage form that is palatable and easy to swallow by pediatric patients as well as to overcome the shortcomings of liquid formulations. Methods: The paracetamol was encapsulated in beads, which were prepared mainly from alginate and chitosan through electrospray technique. The paracetamol beads were sprinkled on the instant jelly prepared from glycine, ι-carrageenan and calcium lactate gluconate. The paracetamol instant jelly characteristics, in terms of physical appearance, texture, rheology, in vitro drug release and palatability were assessed on a human volunteer. Results: The paracetamol instant jelly was easily reconstituted in 20 mL of water within 2 min to form jelly with acceptable consistency and texture. The jelly must be ingested within 30 min after reconstitution to avoid the bitter taste. The palatability assessment carried out on 12 human subjects established the similar palatability and texture of the paracetamol instant jelly dosage comparable to the commercial paracetamol suspension and was found to be even better in overcoming the aftertaste of paracetamol. Conclusion: Such findings indicate that paracetamol instant jelly will compensate for the use of sweetening and flavoring agents as well as develop pediatric dosage forms with limited undesired excipients.
Telmisartan suffers from low oral bioavailability
due to its poor water solubility. The research work presents a formulation
of solid dispersed (SD) telmisartan formulation as a ternary mixture
of a drug, a polymeric carrier (poly(vinylpyrrolidone) (PVP) K30),
and an alkalizer (Na
2
CO
3
). The preparation method,
which was lyophilization of an aqueous solution containing the ingredients,
was free from any organic solvent. The developed SD formulations resulted
in a significant improvement in
in vitro
dissolution
(>90% drug dissolution in 15 min) compared to pure telmisartan.
Solid-state characterization by scanning electron microscopy (SEM),
differential scanning calorimetry (DSC), and X-ray diffraction (XRD)
studies indicated the conversion of crystalline telmisartan into an
amorphous form. Fourier transform infrared (FTIR) spectroscopy revealed
the drug–polymer interaction that was responsible for reducing
the chances of recrystallization. A short-term stability study showed
that selected SD formulations were stable in terms of
in vitro
dissolution and retained their amorphous structure in ambient and
accelerated conditions over 2 months. Selected formulations (drug/PVP
K30/Na
2
CO
3
as 1:1:2 or 1:2:2 weight ratio) resulted
in >2.48 times relative oral bioavailability compared to marketed
formulations. It was considered that the incorporation of an alkalizer
and a hydrophilic polymer, and amorphization of telmisartan by lyophilization,
could enhance
in vitro
dissolution and improve oral
bioavailability.
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