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Page 18
O c t o b e r 1 9 - 2 0 , 2 0 1 8 | T o k y o , J a p a n
Pharma Congress 2018 & Molecular Medicine 2018
& Psychiatric Disorders 2018
Asian Journal of Biomedical and Pharmaceutical Sciences
|
ISSN: 2249-622X
|
Volume 8
International Conference on
PHARMACEUTICS AND NOVEL DRUG DELIVERY SYSTEMS
19
th
International Conference on
CELLULAR AND MOLECULAR MEDICINE
19
th
Annual Congress on
PSYCHIATRY AND PSYCHIATRIC DISORDERS
&
&
OF EXCELLENCE
IN INTERNATIONAL
MEETINGS
alliedacademies.comYEARS
Eliphaz Mukasa et al., Asian J Biomed Pharmaceut Sci 2018, Volume 8 | DOI: 10.4066/2249-622X-C3-008
FORMULATION OF A NATURAL INTRAORAL
DISPERSIBLE FILM (IDF) FOR INTRAORAL
DELIVERY OF VARIOUS NATURAL DRUGS
USING EDIBLE RICE PAPER FILM AS THE
CARRIER VEHICLE
Eliphaz Mukasa
and
Paul Michael Danckwerts
University of the Witwatersrand, South Africa
Aim & Background:
At present, pharmaceutical researchers are focusing on in-
stantaneous intraoral dispersible technologies as novel drug delivery systems,
because they have outstanding advantages over the traditional oral and parenter-
al routes of drug administration. Some essential natural drugs have low oral bio-
availability due to extensive first pass metabolism and pre-systemic degradation
in the gastrointestinal tract. Currently, a cheap rice paper intraoral dispersible film
(IDF) has been developed
Objectives:
In this study, formulation was optimized using the experimental facto-
rial design. The IDFs were loaded with model, natural, anti-cancer drugs, resvera-
trol and curcumin with low oral bioavailability.
Methods:
They were evaluated for thickness, folding endurance, swelling be-
haviour, among others. These related to their drug release properties. Permeation
was evaluated using the pig mucosal membrane mounted on a Franz diffu sion
cell. Taste testing was done to determine acceptability using a taste panel.
Results & Discussions:
16 formulations showed variations in their profiles. For-
mulation 16 proved optimal. The dissolution rate at steady state concentrations
of resveratrol was 29mg per second and the permeability coefficient was 389 mg/
sec.cm2. Curcumin dissolution rate at steady state concentrations was 0.25mg
per second and the permeability coefficient was 42.71 mg/sec.cm2. Resveratrol
permeability rate was 0.42 mg/sec. and that of curcumin was 0.14 mg/sec. Res-
veratrol flux was 0.21 mg/sec./cm
2
. Curcumin flux was 0.14 mg/sec./cm
2
. Drug
entrapment was 80% for both molecules. The 20 mg of resveratrol and curcumin
dissolved in 47.6 sec. and 71.4 sec. respectively. In this study, after permeation, a
concentration of 6.73mg/ml of resveratrol and 0.061mg/ml of curcumin were de-
tected after two hours of the experiment on administering only 20 mg of each of
the drugs suggesting that curcumin is 100 times less permeable than resveratrol.
The release profile was a burst release. On contrast, curcumin oral dose of 2 g/kg
to rats yielded 1.35±0.23 µg/ml in 0.83 hours and in humans, given the same dose
yielded either undetectable or extremely low (0.006±0.005 µg/ml after one hour
in blood. Two separate mono-glucuronide metabolites yielded a Cmax of ~7.5 µM
following a single 5.0 g oral dosage of Resveratrol.
Conclusion:
The key finding was, ex vivo release profiles of the optimized for-
mulation revealed first order release and later zero order. Therefore, it is evident
Eliphaz Mukasa has worked at Medipharm Industries EA
Ltd., Uganda factory for five years. He is specialized in
cGMP and ORS manufacture. He has studied at Mula-
go Hospital School of Dispensing for a Higher Diploma
in Pharmacy in 1988. He taught at Mulago Paramedical
School for two years. He has attended a clinical instruc-
tor’s course at Mbale Health Manpower Development
Centre in 1999 and worked as an Assistant Drugs Inspec-
tor at Uganda National Drug Authority for seven years. He
has also attended NIPER Chandigarh India for assess-
ment of quality of pharmaceuticals. He did his BPharm in
2012 at Nelson Mandela Metropolitan University, former
University of Port Elizabeth (NMMU) Port Elizabeth South
Africa. He has worked at Johannesburg General Hospital
Charlotte Maxeke for his pharmacist internship in 2013.
Presently he is an M Pharm student at the University
of the Witwatersrand, SA 2013 to 2016. He served as a
Community Service Pharmacist at Nessie Knight Hospi-
tal Sulenkama Qumbu, Eastern Cape, South Africa.
eliphaz.mukasa@yahoo.comBIOGRAPHY
that rice paper IDF could efficiently deliver natural
drugs into the systemic circulation intraorally. How-
ever, further studies need to be performed to prove
increased bioavailability in human subjects