Title: Formulation of Floating Tablets of Candesartan Cilexetil with Increased Bioavailibility and Controlled Release Property
Abstract: AIM AND OBJECTIVES: Almost all drugs have side effects, this is due to toxic nature of the drug entity. Further
due to the travelling or mailing of drug to one place to another place in body may produce side
effects in different organs unnecessarily. So it is necessary to achieve the drug to specific
targeted site. Lot of approaches is available. But most of the approaches are having practical
difficulties. One of the good and significant approaches is to deliver the drug as floating tablets,
which is termed as floating drug delivery systems.
The present research focused on the delivery of candesartan cilexetil via floating drug
delivery system. This remains in the site of application i.e. in GIT. By this the degradation of
drug is minimized. Further it may produce good therapeutic concentration in the system.
Floating drug delivery systems can remain in the gastric region for several hours and
hence significantly prolong the gastric residence time of drugs. Prolonged gastric retention
improves bioavailability, reduces drug waste, and improves solubility for drugs that are less
soluble in a high pH environment.
Hypertension is a chronic disease condition in which the systemic arterial blood
pressure is elevated. Anti-hypertensive drugs are used in the treatment of several cardiovascular
disorders, particularly angina pectoris, supraventricular tachycardia and hypertension.
Candesartan Cilexetil, an antihypertensive drug competes with angiotensin II for
binding at the AT1 receptor subtype. As angiotensin II is a vasoconstrictor which also
stimulates the synthesis and release of aldosterone, blockage of its effects results in a decrease
in systemic vascular resistance.
The present work was aimed to prepare floating tablets of Candesartan Cilexetil with
increased bioavailability and controlled release property. SUMMARY: Oral delivery of drugs is one of the most preferable routes of delivery due to the ease of
administration, patient compliance and flexibility in formulation etc.
Floating systems significantly extend the period of time, over which drug may
be released and prolongs dosing intervals and increase patient compliance. These
systems retain in stomach and improve the absorption window and thus enhance the
bioavailability.
Floating dosage forms are oral dosage forms of tablets, capsules, or micro beads
and contain hydrocolloids that allow floating by swelling thereby prolong the residence
time of dosage form within G.I tract.
Floating drug delivery or gastroretentive systems gastric emptying is an
extremely variable process and ability to prolong and control the emptying time is a
valuable asset for dosage forms, which reside in the stomach for a longer period of time
than conventional dosage forms.
Floating drug delivery system (FDDS) could prolong GRT to obtain sufficient
drug bioavailability . The system basically floats in the gastric fluid because of its
lower density compared to that of the aqueous medium. FDDS is desirable for drugs
with an absorption window in the stomach or in the upper small intestine.
Certain factors like density, size, shape, fast or fed conditions, nature of meal,
age, posture, other drugs, biological factors may affect the gastric retention.
Candesartan cilexetil is a drug used in the treatment of hypertension. In the
present project floating tablets were designed and executed.
Floating tablets of candesartan cilexetil were developed to prolong gastric
residence time and to increase its bioavailability.Six formulations (CF1 to CF6) of floating tablets of candesartan cilexetil were
prepared by using individual and combination of polymers. HPMC, carbopol 934 and
xanthum gum were used as polymer to retard the release of the drug in controlled
manner.
Flow properties of the prepared granules for CF1 – CF6 were determined and it
was found that the results were within the standard limits and specifications.
The floating tablets were prepared by direct compression method. Direct
compression method is a suitable method for drugs which are sensitive to heat and
moisture. Probably it saves the time also. In the present project the formulations were
easily and quickly prepared because of the employment of direct compression.
The compressed tablets (CF1 – CF6) were evaluated for various tests quality
control tests weight variation, content uniformity, friability, hardness, floating time,
floating lag time and in vitro release studies.
The hardness and friability of the tablets (CF1 – CF6) were within the limits.
The weight variations of the tablets (CF1 – CF6) were found to be within the
limits.
The content uniformity of the prepared tablets (CF1 – CF6) were within the
limits.
The floating time and floating lag time for the prepared formulations (CF1 –
CF6) was good.
From the in vitro release studies the trials CF1, CF2, CF3, CF4, CF5 and CF6
percent release at the end of the 24th hour was found to be 69.22±0.36, 66.33±0.12,
89.63±0.41, 92.33±0.21, 99.12±0.43, and 93.19±0.55 respectively. From the in vitro
release results it was found that the trial CF5 was best amongst the trials. The formulation (CF5) with hydroxypropylmethyl cellulose and xanthum gum
was found to be best formulation with floating time of 8 hrs and in vitro drug release
of about 99.12±0.43% at the end of 24th hour.CONCLUSION: The present work was based on the floating drug delivery of candesartan cilexetil.
Floating tablets of candesartan cilexetil were formulated and evaluated. Based on the in
vitro evaluation studies, optimized trial was found to be CF5 with good in vitro
properties.
Hence it is ideal to formulate floating tablets for candesartan cilexetil.
However in future it is needed to carryout in vivo studies to implement candesartan
cilexetil as commercial product.
Publication Year: 2015
Publication Date: 2015-04-01
Language: en
Type: dissertation
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