Ratnaparkhi et al Journal of Drug Delivery & Therapeutics; 2013, 3(4), 229-236 229
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RESEARCH ARTICLE
FORMULATION AND EVALUATION OF CHRONOTHERAPEUTIC DRUG DELIVERY
SYSTEM OF MELOXICAM
*
Ratnaparkhi Mukesh P., Khade Ravindra B., Chaudhari Shilpa P.
Marathawada Mitra Mandals College of Pharmacy, University of Pune, Pune, India- 411 033
*
Corresponding Author’s Tel +919960865355, E mail ID: mukeshparkhi@yahoo.co.in
INTRODUCTION
Oral controlled release drug delivery systems offer a
number of advantages over the conventional immediate
release delivery preparations. These systems are designed
to deliver the drugs at a controlled and predetermined rate
thus maintaining their therapeutically effective
concentration in systemic circulation for prolonged period.
On the other hand, for certain therapies a pulsatile drug
release pattern, where the drug is released after well-
defined lag time, exhibits significant advantages. It is well
documented that most of the body functions display
circadian rhythms, e.g. heart rate, stroke volume, blood
pressure, blood flow, body temperature, gastric-pH.
1
Moreover, in a number of organs their functions vary with
the time of the day. It is increasingly recognized that there
are rhythmic and temporal patterns in the manifestation of
many disease states. The symptoms for a number of
diseases, such as bronchial asthma, myocardial infarction,
angina pectoris, hypertension, rheumatic diseases etc.
follow a circadian rhythm.
2
Circadian rhythms are self-sustaining, endogenous
oscillations that occur with a periodicity of about 24
Hours.
3
Interestingly, the term circadian is derived from
the Latin circa which means “about” and dies which can be
defined as “a day”. Normally, circadian rhythms are
synchronized according to internal biologic clocks related
to the sleep-wake cycle. Our circadian rhythm is based on
sleep-activity cycle and is influenced by our genetic
makeup and thereby affects our body’s function
throughout day and night (24-hour period). Circadian
rhythm regulates many body functions in humans like
metabolism, physiology, behaviour, sleep pattern, hormone
production
4
as many conditions show circadian pattern,
advantage could be taken by timing and adjusting the
administration of drugs according to the circadian rhythm
of the disease.
Oral pulsatile administration could be useful for the
treatment of certain diseases, such as asthma, gastric ulcer,
hypertension, ischemic heart disease, arthritis, etc., which
exhibit circadian rhythms. A pulsatile release profile is
characterized by a lag time followed by rapid and complete
drug release. Most pulsatile systems are reservoir systems
and usually covered with a barrier. This barrier can be
dissolved, eroded or removed at a predetermined period of
time after which the drug is dissolved and rapidly released.
Meloxicam is an nonsteroidal anti-inflammatory drug
(NSAID) with analgesic and antipyretic properties.
Prostaglandins are substances that contribute to
inflammation of joints. Meloxicam inhibits prostaglandin
synthetase (cylooxygenase 1 and 2) and leads to a decrease
of the synthesis of prostaglandins, therefore, inflammation
is reduced.
5
Pulsatile drug delivery system is a controlled
drug delivery system where drug is released after a pre-
programmed lag time. Various approaches have been used
to design a pulsatile release formulation, erodible devices
provided with hydrophilic polymer coating are widely used
and such a system when exposed to dissolution medium
undergo swelling, dissolution and/or erosion. Lag time in
such a system can be controlled by using various
hydrophilic polymers such as HPMC, polyethylene oxide,
sodium alginate, sodium CMC. The concentration and
viscosity of these polymers play a significant role in
controlling the lag time and release pattern.
6
A Capsular system in which the body part coated with
impermeable polymer and hydrophilic matrix plug sealing
the drug formulation is used to prepare pulsatile drug
delivery system. Upon contact with aqueous fluids a rapid
dissolution would occur and plug undergoes a gradual
swelling and finally expluded from the body thus allowing
the drug to release. The lag time in such formulation
controlled by the time needed for the plug removal and its
duration depends on the physical, chemical nature, size
and position of the plug.
7
ABSTRACT
The objective of this work is to formulate a pulsatile drug delivery system using Meloxicam drug. The drug delivery system
was designed to deliver the drug in such a way that it could be most useful to the patient of rheumatoid arthritis. A core in cup
(three component tablet) is prepared where in core tablet, an impermeable material surrounding the tablet except the top and
soluble hydrophilic polymer layer at the top is designed. The core tablet contains Meloxicam, ethyl cellulose is used as
impermeable membrane and polyethylene oxide used as soluble hydrophilic polymer layer. The release profile of press coated
tablet exhibited a lag time followed by burst release, in which outer shell ruptured into two halves. The effect of the core, the
polymer characteristics and quantity at the top cover layer, on the lag time and drug release was investigated. The prepared
tablets were evaluated for uniformity of weight, hardness, friability, wetting time, in-vitro disintegration time, stability study
and drug release study. Fourier transform infrared spectroscopy study showed compatibility between Meloxicam and coating
material.
Keywords: Pulsatile Release Tablet, Press-coated tablet, Rheumatoid arthritis.