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June 24, 2016
Published
June 1, 2016
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Abstract
ABSTRACT
Diltiazem hydrochloride (diltiazem HCl), a calcium channel blocker is widely used in the
management of angina pectoris and hypertension. Because of its short biological half-life (3.5 h)
and low oral bioavailability (40%) due to extensive hepatic metabolism leading to high frequency
drug dosing. Therefore, diltiazem HCl is a suitable drug for transdermal formulation to improve
bioavailability of the drug, patient’s convenience and compliance due to less frequent
administration. The objective was to characterized the physicochemical properties and permeation
of matrix film transdermal diltiazem HCl that prepared with polymers (PVA & EC) and PEG 400
as penetration enhancer.
In this study, six formulation were prepared in different ratio of film forming polymers (5:5
& 7:3), and 15%, 20%, 25% of PEG 400. Developed transdermal film were characterized for Â
weight uniformity, thickness, folding endurance, moisture uptake, drug content and in vitro
permeation study using commercial semi permeable membrane. The crystall of drug excipient
interaction were evaluated using X-ray diffraction technique.
All the formulations were found to be suitable for formulating in terms of physicochemical
characteristics and there was no significant differences. The in vitro skin permeation profiles
showed increased flux values with increase of PEG 400 as penetration enhancer. The X-ray
diffraction studies revealed that the crystallinity of the drug decreased as the proporsion of PVA in
the film increased. Â
Keywords : diltiazem HCl, PEG 400, PVA, patch transdermal, permeation
Diltiazem hydrochloride (diltiazem HCl), a calcium channel blocker is widely used in the
management of angina pectoris and hypertension. Because of its short biological half-life (3.5 h)
and low oral bioavailability (40%) due to extensive hepatic metabolism leading to high frequency
drug dosing. Therefore, diltiazem HCl is a suitable drug for transdermal formulation to improve
bioavailability of the drug, patient’s convenience and compliance due to less frequent
administration. The objective was to characterized the physicochemical properties and permeation
of matrix film transdermal diltiazem HCl that prepared with polymers (PVA & EC) and PEG 400
as penetration enhancer.
In this study, six formulation were prepared in different ratio of film forming polymers (5:5
& 7:3), and 15%, 20%, 25% of PEG 400. Developed transdermal film were characterized for Â
weight uniformity, thickness, folding endurance, moisture uptake, drug content and in vitro
permeation study using commercial semi permeable membrane. The crystall of drug excipient
interaction were evaluated using X-ray diffraction technique.
All the formulations were found to be suitable for formulating in terms of physicochemical
characteristics and there was no significant differences. The in vitro skin permeation profiles
showed increased flux values with increase of PEG 400 as penetration enhancer. The X-ray
diffraction studies revealed that the crystallinity of the drug decreased as the proporsion of PVA in
the film increased. Â
Keywords : diltiazem HCl, PEG 400, PVA, patch transdermal, permeation