Objective:
The low bioavailability and narrow absorption window of Loratadine (LD), stable in acidic pH following
oral administration favors development of a gastro retentive formulation.
Methods:
Gastro retentive floating tablets of LD were prepared by using direct compression method with
hydrophilic polymers like HPMC K100M, CARBOPAL 940 and standard excipients like micro
crystalline cellulose (MCC), sodium bicarbonate, magnesium stearate and talc. These polymers and
excipients were utilized to make 14 formulations (F1-F14), the physical characteristics of tablets were
evaluated, including hardness, friability, floating time, thickness, weight variation, in-vitro buyoncy
studies, in -vitro dissolution studies, in –vivo xray studies.
Results:
The drug- polymer compatibility studies indicated that there was no compatibility problems with the
polymers used in the study, the effect of polymer concentration on buoyancy and drug release was studied. the optimized formulation (F7) sustained the drug release in 12 hours than the marketed product,
maintained total floating time of 12 hours with floating lag time of 30 seconds, Carbopal 940 had shown a
more sustained release profile because it remains un ionized in acidic dissolution media, showed a non
fickian diffusion and followed the zero order, higuchi model, After three months of storage at 450C with
75 % RH, it showed no significant changes in physical appearance, dug content, floatability. In-vivo x-ray
studies were conducted to note the gastric residence time of floating tablets, time was found to be 4 hours.
Conclusion:
The floating principle improved gastro retention time, which was considered to be favorable for
expanding the absorption window of drugs.
Key words: Floating tablets, Gastric residence time, Gastro retentive drug delivery system,
Loratadine, In-vitro buoyancy.
Publication date: 01/01/2022
https://ijbpas.com/pdf/2022/January/MS_IJBPAS_2022_6410.pdf
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https://doi.org/10.31032/IJBPAS/2022/11.1.6410
