29-08-2014, 02:29 PM
Formulation and Characterization of Fast Dissolving Buccal Films A Review Project Report
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ABSTRACT
There is always increasing demand for patient convenience and compliance related research and
a novel method is the development of fast dissolving buccal films, which dissolve or disintegrate
instantly on the patient buccal mucosa. This fast dissolving drug delivery system (FDDS) is
suited for the drugs which undergo high first pass metabolism and is used for improving
bioavailability with reducing dosing frequency to mouth plasma peak levels, which in turn
minimize adverse/side effects and also make it cost effective. In the present review, recent
advancements and literature regarding fast dissolving buccal films is compiled and it suggests
that this delivery system can be adopted by various pharmaceutical companies in the future at
the large scale
INTRODUCTION
Fast-dissolving buccal film drug delivery systems have rapidly gained acceptance as an
important new way of administering drugs. They are usually used for pharmaceutical and
nutraceutical products. It is the newest frontier in drug delivery technology that provides a very
convenient means of taking medications and supplements. There are multiple fast-dissolving
over the counter and prescribed products on the market worldwide, most of which have been
launched recently. There have also been significant increases in the number of new chemical
entities under development using a fast-dissolving drug delivery technology.
Now the main question arises that what are fast dissolving buccal films. A fast-dissolving buccal
film drug delivery system, in most cases, is a film containing active ingredient that dissolves disintegrates in the saliva remarkably fast, within a few seconds without the need for water or
chewing. Some drugs are absorbed well from the mouth, pharynx and esophagus as the saliva
passes down into the stomach. In such cases, bioavailability of drug is significantly greater than
those observed from conventional tablet dosage form. Most fast-dissolving delivery system films
must include substances to mask the taste of the active ingredient. This masked active ingredient
is then swallowed by the patient's saliva along with the soluble and insoluble excipients
Salient Features of Fast Dissolving films
Fast dissolving buccal films provide ease of administration for patients who are mentally ill,
disabled and uncooperative; requires no water; have quick disintegration and dissolution of the
dosage form. They can be unobstructive and can be designed to leave minimal or no residue in
the mouth after administration and also provides a pleasant mouth feel. This delivery system has
no risk of chocking. It allows high drug loading and has the ability to provide advantages of
liquid medication in the form of solid preparation. Fast dissolving films are adaptable and
ameanable to existing processing and packaging machinery, cost effective and have excellent
mucoadhesion. Fast dissolving films can be formulated in various shapes and sizes [7-11].
Advantages of fast dissolving buccal films
Fast dissolving films are easy to administer and handle, hence leads to better patient compliance.
Fast dissolving buccal film is a drug delivery film that is placed on a mucosal or in oral cavity.
They provide suitability for a wide variety of drugs. It has improved bio-availability for certain
therapeutic ingredients. It has small size for improved patient compliance. As most of the drugs
are unpalatable, fast dissolving buccal films usually contain a medicament in taste masked form.
Films has ability to dissolve rapidly without the need for water provides an alternative to patients
with swallowing disorders as a result of extremities and dysphasia, and to patients suffering from
nausea, such as those patients receiving chemotherapy. The large surface area available in the
strip dosage form allows rapid wetting in the moist buccal environment. It is also used for local
and systemic delivery. Because of availability of larger surface area it leads to rapid
disintegration and dissolution in the oral cavity. The sublingual and buccal delivery of a drug via
thin film has the potential to improve the onset of action, lower the dosing, and enhance the
efficacy and safety profile of the medicament. Film is more advantageous as it is stable, durable
and quicker dissolving than other conventional dosage forms. As compared to drops or syrup
formulations, precision in the administered dose is ensured from each of the strips. Films also
enable improved dosing accuracy
Formulation considerations
Formulation involves the intricate application of aesthetic and performance characteristics such
as taste masking, fast dissolving, physical appearance, mouth feel etc. Fast dissolving film is a
thin film with an area of 5-20 cm2
containing an active ingredient. The immediate dissolution, in
water or saliva respectively, is reached through a special matrix from water-soluble polymers.
Drugs can be incorporated up to single dose of 15 mg [4]. Formulation considerations have been
reported as important factors affecting mechanical properties of the films, such as shifting the
glass transition temperature to lower temperature. The excipients used in formulation of fast
dissolving buccal films are also discussed in detail. From the regulatory perspectives, all
excipients used in the formulation should be generally regarded as safe (i.e. GRAS-listed) and
should be approved for use in oral pharmaceutical dosage forms.
Active pharmaceutical agents
The active substance is may be from any class of pharmaceutically active substances that can be
administered orally or through the buccal mucosa respectively. According to literature, API can
be added from 5%-25% w/w of total weight of polymer. For the effective formulation, dose of
drug should be in mgs (less than 20 mg/day). The drugs which are potent, show high first pass
metabolism and patient non- compliant are best candidates for fast dissolving buccal films.
Researchers have shown interest in development of fast dissolving films for drugs like:
Pediatrics (antitussive, expectorants, antiasthamatics), Geriatrics (antiepileptic, expectorants),
Gastrointestinal diseases, Nausea (e.g. due to cytostatic therapy), Pain (e.g. migraine), CNS (e.g.
antiparkinsonism therapy).
Among which preferred active agents include chlorpheniramine maleate, brompheniramine
maleate, dexchloropheniramine, triprolidine hydrochloride, acrivastine, azatadine maleate,
loratidine, phenylephrine hydrochloride, dextromethorphan hydrochloride, ketoprofen,
sumatriptan succinate, zolmitriptan, loperamide, famotidine, nicotine, caffeine, diphenhydramine
hydrochloride, and pseudophedrine hydrochloride, and their amounts per strip can be well known
in the art.
Flavoring agents
Flavoring agents can be selected from the synthetic flavor oils, oleo resins, extract derived from
various parts of the plants like leaves, fruits and flowers. Flavors can be used alone or in the
combination. Any flavor can be added such as essential oils or water soluble extracts of menthol,
intense mints such as peppermint, sweetmint, spearmint, wintergreen, cinnamon, clove, sour fruit
flavor such as lemon , orange or sweet confectionary flavors [19] such as vanillin, chocolate ,or
fruit essence like apple , raspberry, cherry, pineapple. The amount of flavor needed to mask the
taste depends on the flavor type and its strength.
Permeation studies
Permeation studies are carried using the modified Franz diffusion cell by using porcine buccal
mucosa. The mucosa is mounted between the donor and receptor compartment of Franz diffusion
cell. The receptor compartment is filled with buffer and maintained at 37 °C ± 0.2 °C and the
hydrodynamics were maintained by stirring with a magnetic bead at 50 rpm. One previously
weighed film is placed in intimate contact with the mucosal surface of the membrane that should
be previously moistened with a few drops of simulated saliva. The donor compartment is filled
with 1 ml of simulated saliva of pH 6.8. Samples are withdrawn at suitable interval, replacing the
same amount with the fresh medium. The percentage of drug permeated is determined by
measuring the absorbance by selected analytical method.
CONCLUSION
Fast dissolving buccal films have gained popularity because of better patient compliance, rapid
drug delivery system, drug is directly absorbed into systemic circulation, first pass metabolism
and degradation in gastrointestinal tract can be avoided. Fast dissolving buccal films can be a
better option to optimize therapeutic efficacy of various active pharmaceutical ingredients in the
future.