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Please cite this article in press as S. Jyothi Sri et al., Formulation and In-Vitro Evaluation of Benazepril Mouth
Dissolving Films, Indo Am. J. P. Sci, 2018; 05(01).
INTRODUCTION:
Oral route is most preferred route by medical it rapidly disintegrates and dissolves to release the
practitioners and manufacturer due to highest medication for or mucosal and intra gastric
acceptability of patients. But oral drug delivery absorption, without chewing and intake of water.
systems still need some advancement to be made These films have a potential to deliver the drug
because of their some drawbacks related to particular systemically through intra gastric, sublingual or
class of patients which includes geriatric, pediatric buccal route of administration and has been used for
and dysphasic patients associated with many medical local action. It gives rapid absorption and instant
conditions as they have difficulty in swallowing or bioavailability of drugs due to high blood flow. As
chewing solid dosage forms. Many pediatric and the fast-dissolving film is taken through the
geriatric patients are unwilling to take solid sublingual route, rapid absorption of drug is possible,
preparations due to fear of choking. Fast dissolving which finally leads to quick onset of drug action and
drug-delivery systems were first developed in the late prevent the first pass-metabolism of the drug [3].
1970s as an alternative to conventional dosage forms
for pediatric and geriatric patients who experience MATERIALS AND METHODS:
difficulties in swallowing traditional solid-dosage Materials:
forms. These systems consist of the solid dosage Benazepril purchased from Dr. Reddy’s Lab’s,
forms that disintegrate and dissolve quickly in the Hyderabad, HPMC E5, HPME E3LV, HPME 5 CPS
oral cavity without the administration of water. Maltodextrin, Polyethylene glycol, Aspartame,
Research and development in the oral drug delivery Mannitol, Citric acid were purchased from S.D. Fine
segment has led to transition of dosage forms from chemicals, Mumbai .Amaranth purchased from
simple conventional tablets or capsules to modified oxford laboratory, Mumbai.
release tablets or capsules to oral disintegrating tablet
(ODT) to wafer to the recent development of oral fast Methods
dissolving films (OFDFs). Amongst the plethora of Preformulation Studies:
avenues explored for the rapid drug releasing It is defined as the determination of physical,
products, oral strip technology is gaining much chemical and mechanical properties of a new drug
attention [1, 2]. The aim of this is to highlight the substance alone and when combined with excipients
potential role of fast dissolving drug delivery in [4]. The overall objective of preformulation studies is
achieving effective drug delivery of antihypertensive to generate information useful in developing stable,
drug. Furthermore, the concept of a fast dissolving safe and effective dosage form.
drug delivery is reviewed and discussed
Solubility:
The work is aimed to develop and optimize fast The maximum equilibrium amount of solute that can
dissolving oral films of Benazepril to ensure dissolve per amount of solvent is the solubility of that
satisfactory drug release with the help of polymers solute in that solvent under the specified conditions.
and thereby avoid first pass metabolism, enhance Solubility is one of the characteristic properties of a
bioavailability and rapid onset of action .There has substance and is used to describe the substance, to
been increased demand for the novel dosage form to indicate a substance's polarity and to help to
gain more patient compliance. Fast dissolving films distinguish it from other substances.
recently have acquired great importance in the
pharmaceutical industry due to their unique Melting Point:
properties and specific advantages like no need of The melting point of a substance is the temperature at
water for disintegration, accurate dosing, and rapid which the material changes from a solid to a liquid
onset of action, ease of transportability, ease of state. Pure crystalline substances have a clear, sharply
handling, pleasant taste and improved patient defined melting point.The melting point was
compliance. Fast dissolving film is a type of drug determined by using Capillary tube method.
delivery system, which when placed in the oral cavity
Evaluation of films:
Table 4: Evaluation Parameters of films F1-F9
CODE Thickness Weight Folding Surface Content In vitro
(µm) variation Endurance pH uniformity/ Disintegrati
(mg) (Count) Assay (%) on
Time (sec)
F1 74±2 57.14±0.6 58±2 6.55±0.03 98.8±0.2 25±2
F2 75±1 52.22±0.1 54±2 6.74±0.01 92.44±0.46 24±2
F3 80±3 58.4±0.1 62±1 6.54±0.011 89.65±0.14 30±2
F4 82±2 60.2±0.1 64±4 6.6±0.02 95.5±0.21 22±2
F5 80±1 71.5±0.5 86±3 6.89±0.010 97.32±0.3 20±2
F6 88±1 62.55±0.1 70±1 6.88±0.01 98.7±0.8 18±2
F7 86±2 70.5±0.3 95±4 6.93±0.02 86.7±2.2 14±2
F8 83±6 66.65±0.3 106±4 6.93±0.11 99.7±0.5 10±3
F9 87±1 71.3±0.1 96±1 6.94±0.01 98.6±0.45 14±2
Fig. 3: Zero order kinetic plot, first order kinetic plot of optimized formulation (F8)
Fig. 4: Higuchi kinetic plot, Korsmeyer–Peppas kinetic plot of optimized formulation (F8)
FT-IR Studies:
FTIR studies were carried out on drug and drug-excipient samples. In FTIR spectra of the pure drug the observed
peaks at 2989.97 cm-1 due to C-H stretching, 1590.50 cm-1 due to C=C aromatic stretching, 3195.78 cm-1 due to N-H
stretching, 1377.73 cm-1 due to C-O stretching were in the range of reference peaks. It ensures its purity.
Fig. 6: FT-IR Spectra of Benazepril with maltodextrin (1:1), FT-IR Spectra of optimized formulation