Preparation and Optimization of Fast Dissolving HPMC/PVA Blended films of Loperamide Hydrochloride

Abstract

Discovery of new chemical entities is a multifaceted, costly and time consuming process, so recent
trends are shifting towards design and development of innovative drug delivery systems for already
existing drugs. Recently fast dissolving oral films have been introduced in the market that gained the
interest of large number of pharmaceutical companies due to their tremendous advantages such as
easy administration, better patient compliance, rapid drug absorption and rapid onset of action with
instant bioavailability, over other conventional oral dosage forms. Apart from these benefits, fast
dissolving oral films can be used in pediatric, geriatric and bed ridden patients who find difficulty in
swallowing a tablet or capsule. Initially fast dissolving oral films of breath strips, confectionery and
oral care preparations were prepared but now it has become a novel and widely accepted technology
for delivering OTC and prescription medication too.
Fast dissolving films are gaining interest as an alternative to fast dissolving tablets. The films are
designed to dissolve upon contact with a wet surface, such as the tongue, within a few seconds,
meaning the consumer can take the product without need for additional liquid. This convenience
provides both a marketing advantage and increased patient compliance. As the drug is directly
absorbed into systemic circulation, degradation in gastrointestinal tract and first pass effect can be
avoided. The Loperamide hydrochloride mouth dissolving film is prepared by using solvent casting
method. The ingredient used for formulation Loperamide hydrochloride as a Anti-Diarrheal, HPMCE50, HPMC-E15-LV and PVA as film forming polymer, propylene glycol as a plasticizer, Sodium
starch glycolate (2-8%) as super disintegrant, lemon oil (2-5%) as a flavoring agent, citric acid (2-
6%) as a Saliva Stimulating Agent, methylparaben (0.015%) as a preservative.
Film former polymers were selected as independent variables & tensile strength, disintegration time & percentage drug dissolution was selected
as a response variable. The formulations were evaluated based on uniformity of mass, thickness, percent drug content, folding endurance, surface
pH, moisture uptake, percentage swelling, percentage elongation, tensile strength, in vitro disintegration time, in vitro percentage drug
dissolution. The drug Loperamide found to be feasible to develop into Fast mouth dissolving films. The method solvent casting adopted for the
formulation of Loperamide oral films is convenient and economical. The super disintegrants employed in this work found it appreciable. The
drug-excipient compatibility by FT-IR studies revealed no physicochemical interaction. The oral films obtained found clear, enough physical
strength and showed a reasonable degree of disintegration time. The in vitro dissolution studies of all the formulations in contrast to pure drugs
showed a better release profile. From the observations of evaluation results, it was concluded that film formulation F7 containing blend of HPMC
E15 and PVA film formers is found to be the best formulation among the all other formulations.