A Comprehensive Review on Gastro Retentive Drug Delivery System
Mansuri
Jahid*, Rehan Deshmukh, Khan Ramiz.V, Sayyed Anas Ali
1.
JIIU’s Ali Allana College of Pharmacy Akkalkuwa, Dist-Nandurbar -425415,
Maharashtra, India
*Correspondence: mansurijahid707@gmail.com; Tel.: (+91 9518983892)
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Article
Information
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Abstract
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Review Article
Received: 23/10/2024
Accepted: 28/10/2024
Published:08/11/2024
Keywords
GRDDS,
Type of GRDDS,
Factors Affecting In GRDDS,
Approaches,
Effervescent System,
Non-Effervescent System,
Polymers,
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The Gastroretentive Drug Delivery System (GRDDS)
is an advanced approach for enhancing the oral delivery of drugs by
prolonging their retention in the stomach. By extending the stomach residence
duration, this approach improves therapeutic efficacy and bioavailability
while addressing issues including site-specific drug absorption and
restricted bioavailability. Dosage forms are kept in the stomach using a
variety of methods, including as floating and non-floating systems, which
maximize retention by taking into account characteristics like density,
shape, and polymer kinds. Additionally, both synthetic and natural polymers
are used in the GRDDS, which affects the therapeutic results and release
patterns. GRDDS has drawbacks, such as issues with formulation and appropriateness
for specific medications, despite its advantages, which include increased
bioavailability and decreased drug waste. These technologies are still being
developed in order to get beyond physiological obstacles and enhance the
results of oral medication delivery.
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INTRODUCTION
The
most popular method of medicine delivery is oral because it is simple to
utilize. Oral medication
absorption usually takes place in the stomach and intestines. The Gastro
Residence Time (GRT) factor contributes to imperfect absorption in the stomach. The medication does
not remain in the stomach due to the existence of gastric emptying time that’s
why it is
necessary to increase GRT. The more time a
medicine spends in the stomach, the more absorption takes place and raising the
drug's bioavailability. Consequently, a drug delivery system such as the
gastroretentive drug delivery system (GRDDS) that can prolong the duration of
interaction with the stomach is required. GRDDS formulations have been the
subject of numerous studies. These have included formulations of nifedipine and
nilotinib to boost bioavailability, antibiotics to boost drug efficacy against
H. pylori treatment, ofloxacin as a delayed release drug delivery system,
increasing the solubility of verapamil medications, furosemide, propranolol,
and other medications.(1) Oral drug delivery systems suffer several challenges, including limited
bioavailability because of the heterogeneity of the gastrointestinal tract,
commensal flora's pH, the dosage form's GI retention duration, surface area,
and enzymatic activity. The gastrointestinal tract (GIT) can present challenges for conventional
drug delivery methods, including low dosage effectiveness, frequent dose
requirements, and partial drug release. Thus, the development of GRDDS may result from the lack of ability
conventional drug delivery methods to keep medications in the stomach. These
systems have a number of advantages, including the capacity to give targeted
medication distribution in the stomach, longer gastric residence time (GRT) of
dose forms in the stomach—up to several hours—and improved drug absorption,
which increases therapeutic efficacy. (2)
The
oral route of drug administration is the most popular and efficient way to
distribute drugs.(3) The oral drug delivery system is the most favored and traditional method
of drug delivery since it is simple to administer, promotes patient compliance,
and offers formulation accessibility. The systemic effects that arise from
medication absorption through the gastrointestinal tract are the target of oral
dose forms. (4) One of the main issues with conventional delivery is that it is not
site-specific. Certain medications can only be absorbed at a particular
locationThey need to be released at an accurate place or in a way that ensures
the maximum quantity of medicine reaches the designated location. (5)
Gastro
retentive drug delivery system refers to the controlled release drug delivery
method that can be kept in the stomach.(6) They may be helpful in maximizing the "absorption window" for
oral controlled drug delivery by continuously delivering the medication before
the window for a longer period of time, assuring maximum bioavailability. Both
in fed and fasting conditions, gastric emptying takes place. Still, there are
differences in the motility patterns between the two states. Orally administered
controlled release dosage forms can be exposed to two difficulties, according
to gastric emptying studies: short stomach residence time and unpredictable gastric
emptying rate. (7)
Physiology of stomach :(8)
The
stomach is divided anatomically into three regions: the body, the antrum
(pylorus), and the fundus. While the antrum is the primary location for mixing
motions and functions as a pump for stomach emptying by thrusting activities,
the proximal portion, composed of the fundus and body, serves as a reservoir
for undigested materials. Both whether a person is fed or fasted, gastric
emptying occurs. An electrical sequence
known as the interdigestive myloelectric cycle, or migrating myoelectric cycle
(MMC), occurs during the fasting state and cycles through the stomach and
intestine every two to three hours.
Figure. Anatomical structure2
Risk Factors
In the Delivery of Gastroretentive Medication: (9)
·
Minimal for acid-sensitive drugs. Limited for drugs
that are better absorbed in the lower portion of the digestive system.
·
Concerns with the intended dumping and outcome.
·
A number of variables, such as meal presence, pH,
and stomach motility, influence gastric retention. It is consequently necessary
for the dose form to be able to withstand stomach peristalsis.
·
In vitro and in vivo connections are not good.
·
The cost of phrasing is higher.
·
With toxic, poisonous, or hypersensitivity effects,
withdrawal of the medication can be challenging.
Factors affecting gastric retention time of the dosage form: (8)
1) Density:
The density of the
dosage form should be less than that of the stomach's contents (1.04g/ml).
2) Size:
A dosage form that
is larger than 7.5 mm in diameter stays in the stomach longer than one that is
9.9 mm in diameter.
3) The Shape of the dosage
form:
The tetrahedron
formulation with one or more units remained in the stomach for a longer period
of time when compared to other devices of the same size. Multiple unit
formulations show a more consistent release profile and lack of degradation due
to unit failure when compared to single unit dose forms. They also offer a
higher margin of safety against dosage form failure and coadministration of
units with dissimilar release profiles or containing incompatible chemicals.
Non-floating dose
forms have extremely varying mean stomach residence periods that are largely
depending on their size (larger, medium, or small). Larger dose forms typically
have longer gastric retention times because their size prevents them from
passing through the pyloric antrum and into the intestine as quickly. (1)
4) Fed or unfed
state:
Every one to two
hours, there are intense bursts of motar activity that define the stomach motility during a fast. When the
unit is in the fast state, the stomach is cleared of undigested material, which
causes the MMC to be delayed and the GRT to be prolonged. In other words, the
unit's GRT might be relatively short if the formulation and MMC times are the
same.
5) Nature of meal:
When the stomach
is fed indigestible polymers or fatty acids, the motility pattern of the
stomach changes to a fed state, which prolongs the release of medication and
slows down gastric emptying.
6) Caloric content:
GRT can be increased
by 4-10 with a meal that is high
in protein and fat.
7) Frequency
of feed:
The GRT can increase
by more than 400 minutes when numerous meals are supplied as opposed to a
single meal because of the low frequency of MMC.
8) Gender:
Males have a mean
ambulatory GRT of 3.4 hours, which is smaller than that of females of the same
age and race (4.6 hours), regardless of height, weight, or body surface. In
general, this indicates that women empty their stomachs more slowly than men
do.
9) Age:
GRTs are notably
longer in those over 70 years old.
10) Concomitant
drug administration:
GRT can be
extended by opiates such as codeine and anticholinergic medications such as
atropine and propetheline.
Advantages Of GRDDS :(10,8)
·
Its improves bioavailability.
·
It can reduces drug waste.
·
Enhances the solubility of medications that are
less soluble in the high pH environment of the small intestine.
·
It also enhanced therapeutic effectiveness
·
It can be
used to overcome the difficult of the gastric retention time (GRT) as well as the gastric emptying time (GET).
·
Medication dose forms that are gastroretentive
reduce the variation in drug effects and concentrations.
·
Drug efficiency can be increased by using
gastroretentive drug delivery, which can reduce the body's counteractivity.
·
It
enhances the pharmacological effects and improves the chemical outcomes.
Disadvantages Of GRDDS :(11,8)
·
Unsuitable for drugs those are unstable
inacidic environment.
·
Unsuitable for drugs with limited acid solubility. E.g. Phenytoin.
·
Medication that, when released slowly, irritates
the stomach or creates sores.
·
Drugs
that absorb equally well through
GIT.
·
Floating drug delivery systems
require high fluid level in stomach to float and work
effectively.
·
GRDDS is fed into the system
after the meal as time of stay in stomach
depends on digestive state.
·
The patient must be positioned upright for the
medication to stay in the stomach.
·
The
Hydrogel based swelling system
takes longer time to swell
after administration.
·
Upon
multiple administrations, size increasing drug delivery systems pose the
threat to life owing to possible
hazard of permanent retention in stomach.
Different Gastroretentive approaches :
Different approaches have
been pursued to increase the retention of oral dosage forms in the stomach.
Some are formulated as a single component whereas others are formulated as a
multi-component dosage forms. GRDDS can be broadly categorized into floating
and non-floating system.(12)
(I)
FLOATING drug delivery
SYSTEM :
In contrast to the high-density drug delivery
system, Floating systems stay in the stomach for extended periods of time
without influencing the gastric contents because their density is lower than
that of the stomach's contents. Floating drug delivery systems are also known as low density system. (12)
Classification of floating drug delivery system:
(4)
(A) Effervescent
system:
1. Gas generating system
2. Inflatable
liquid-containing system
(B)
Non- effervescent system:
1. Colloidal gel barrier
systems
2. Microporous
Compartment System
3. Alginate beads
4. Raft forming systems
A. Effervescent system:
These
are matrix-type systems made using effervescent substances like sodium bicarbonate, tartaric acid and swellable polymers like methylcellulose. The matrices are fabricated so that upon coming in the stomach, CO2 is released by the acidic nature of the gastric contents and is entrapped in the jellified hydrocolloid. This keeps the dose form buoyant and causes it to move upward. The dose
form floats on the chyme due to a decrease in specific gravity.
1.
Gas generating system:
The primary mechanism in this system is the reaction between sodium
bicarbonate, citric acid, and tartaric acid, which produces CO2 gas. The
system's density is lowered by the gas generated, enabling it to float on
stomach contents. CO2
is produced by salts and
citric/tartaric acid, which is trapped in the system's jellified hydrocolloid
layer, which lowers its specific gravity and causes it to float over the chime.
Essentially, this method uses a multi-layered continuous release tablet
as its seed. Tartaric acid and sodium bicarbonate are present in the
effervescent inner layer. The outermost layer consists of a swellable membrane
layer composed of PVA shellac and other components.(13)
Fig. Effervescent drug delivery system2
2.
Inflatable liquid-containing system:
These
feature an inflatable chamber that fills with a liquid (cyclopentane or ether)
that gasifies at body temperature and causes the chamber to expand in the
stomach. These are buoyant structures using a hollow deformable element that is
regulated by osmoticism. The medication is kept in the first chamber of the
system, while the volatile system is kept in the second. medication delivery by
floating that isn't effervescent.(13)
A. Non-effervescent system:
The
mechanism underlying the non-effervescent FDDS is polymer swelling or
bioadhesion to the GI tract mucosal layer. The medication expands after being
swallowed and imbibition of gastric juice prevents it from leaving the stomach.
The medicine is mostly combined with gel, which causes it to retain its shape
and swell when it comes into touch with stomach fluid. These systems are
sometimes called "plug-type systems" because of their propensity to
become lodged in the vicinity of the pyloric sphincter. The most widely
utilized excipients in non-effervescent floating drug delivery systems include
matrix-forming polymers like polyacrylate, polymethacrylate, and polycarbonate,
gel-forming or highly swellable cellulose type hydrocolloids, and
polysaccharides. (14)
MECHANISM OF FLOATING SYSTEM
: (14)
FDDS has a bulk density less
than gastric fluids so that they remain buoyant in the stomach without
affecting the gastric emptying rate for a prolonged period of time.
F=F buoyancy-F gravity
= (Df-Ds) gv Where,
F=total vertical
force, Df=fluid density, Ds=object density, V=volume,
g=acceleration due to
gravity.
Colloidal gel barrier
systems :
The first hydrodynamically balanced system (HBS) was invented by Sheth
and Tossounian in 1975. In order to keep the
medication buoyant in the stomach contents, this treatment uses a
pharmaceutical that contains gel-forming hydrocolloids. This system is made up
of tablets or capsules that have a high concentration of one or more
matrix-forming polymers such polycarbophil, polyacrylates, and polystyrene, and
gel-forming, highly swellable cellulose hydrocolloids like HEC, HPMC, NaCMC,
and Polysacchacarides. When the system's hydrocolloid comes into contact with
gastric fluid, it hydrates and forms a colloidal gel barrier that surrounds the
gel surface. The air retained by the expanded polymer has a density less than
unity, which makes this dosage form buoyant. (13)
Microporous Compartment System:
The
principle behind this approach is to enclose a drug reservoir within a
microporous chamber with apertures positioned on both the upper and lower
surfaces. To ensure that no undissolved medication comes into contact with the
gastric mucosal surface, the drug reservoir compartment's peripheral walls are
sealed completely. The delivery system floats above the contents of the stomach
because trapped air is present in the flotation chamber. The medication is
dissolved by gastric fluid that enters through the apertures and constantly
transports the dissolved drug into the intestine for absorption.(13)
Alginate beads:
Calcium alginate that has
been freeze-dried has been utilized to make floating dosage forms containing
numerous units. Calcium alginate precipitates when a sodium alginate solution
is dropped into an aqueous solution of calcium chloride, resulting in spherical
beads with a diameter of roughly 2.5 mm. The beads are then snapped apart and
frozen in liquid nitrogen before being freeze dried at -40° for 24 hours,
resulting in a porous structure with up to 12 hours of floating force .(13)
Raft forming systems:
The
creation of a viscous cohesive gel in contact with stomach contents is the main
mechanism underlying the production of rafts, where each segment of liquid
expands to form a continuous layer known as a raft. Gelation begins with the formation of double helical
junction zones, which are followed by the aggregation of double helical
segments, which are then cationcomplexed and hydrogen bonded to form
three-dimensional networks. The raft floats and
functions as a barrier to stop stomach contents like HCl and enzymes from
refluxing into the oesophagus due to the buoyancy brought on by CO2 generation.(13)
Non-Floating Drug Delivery Systems
:
Mucoadhesive
or Bioadhesive Systems:(15)
The mucoadhesive system was first introduced
by Park and Robinson. This system is intricate
and has multiple working systems. Mucoadhesive systems have the ability to
adhere to the gastric mucous membrane, hence extending the GRT. Bioadhesive
polymers are used in this technique. These polymers have the ability to stick to
the stomach's epithelial surface. By improving the affinity and length of
contact between the gastroretentive drug delivery mechanism, gastric retention
is prolonged. The negatively charged mucosal surface and positively charged
polymer may interact to facilitate the bioadhesive process. Among the
excipients that have been employed are gliadin, polycarbophil, lectins,
chitosan, and carbopol. Owing to the creation of disulphide bonds both within
and across chains, these conjugates can significantly improve cohesive
characteristics, leading to an almost zero order release of the model drug.(2) Utilized polymers in the formulation can adhere to the mucosal membrane
through receptor-mediated, bonding, or hydration mechanisms.
·
Hydration Mediated Adhesion: Hydrophilic polymers
become clingy and mucoadhesive
upon hydration.
·
Bonding Mediated Adhesion: May involve mechanical or chemical bonding.
·
Receptor Mediated Adhesion: Takes place between
certain polymers and specific
receptors that are defined on gastric cells.
Oral dosage forms attach themselves to the mucin or gastric epithelial
cell surface, which improves the closeness and duration of the drug's contact
with the biological membrane. As a result, the period of gastric residency will
increase. Developing floating systems combined with mucoadhesion properties is
one method to get over some of the system's obstacles. This will enhance the
dose form's adhesion to the stomach wall's mucous lining. Studies find this
system appealing because of its effective responses achieved by formulations.
It is among the methods that FDDS is focusing on the most.
Figeur. GRDDS based on (a) expandable systems and (b)
superporous hydrogel systems(2)
High Density System:
High-density
systems are made to sink to the bottom of the stomach because their density is
higher than that of gastric fluids. Usually made of heavier materials or denser
polymers, these systems,Prolonged interaction between the drug delivery system
and the gastrointestinal mucosa is made possible by the high-density
characteristic (16).When the pellets' density is at least 1.5 g/ml, they have a
longer stomach residence duration when fed state and fasted state.(15)
Figure.
GRDDS based on (a) low-density systems and (b) high-density systems.(2)
Swelling system:
Swelling systems
are made to absorb stomach fluid and swell to a large size. They are sometimes
referred to as superporous hydrogels or swelling prevents the system. The
system is unable to cross the pyloric sphincter and enter the small intestine
as a result of this enlargement. The drug is released as the
system swells and gradually erodes.(16)
Figure. (a)Exapandable system and (b) superporous hydrogel systems(2)
Exapandable system :
Expandable
drug delivery systems are made to increase in volume or form in order to have a
longer GRT. It was originally used for veterinary purposes, but later on, human
applications were added. Three general design considerations must be made for
the system to work properly: reduced in size to facilitate evacuation after
full medication release, inflated in the stomach to obstruct passage through
the pyloric sphincter, and small for simple oral consumption. Because this
device can block the pyloric sphincter, it is often referred to as a "plug
type system." Similar to swelling systems, expandable systems enlarge when
in contact with stomach contents. The medication can be supplied gradually over
time thanks to expandable systems, which are specifically designed to expand in
a controlled manner. These systems could be made up of a variety of hydrated
polymer-based materials.(16)
The various expandable and superporous system
in GRDDS generally , consists of
drug and swellable polymer and high swellable polymer respectively. (16)
Polymers used in gastric
retention systems:(17)
Mainly two types of polymers
are used in formulation, it may be naturally occurring or may be synthetic or
may be semisynthetic. A natural polymers has a some advantages such as :
Natural polymers:
Advantages of natural polymers
:
·
It can be low cost.
·
Have a biocompatible .
·
Its easily
available the means its locally availability.
·
Alos its biodegradable.
·
It can be non- toxic.
·
These polymers
are environment friendly.
·
Increased viscosity due to rapid swelling.
·
Also its non-irritating.
Natural Polymers
have some disadvantages like:
·
Extraction process
very complicated and high cost
·
High degree
of variability
·
Uncontrolled rate of hydration
·
Microbial contamination
·
Reduced viscosity
on storage.
There are so many type of
natural polymers such as :
1)
Chitosan:
Chitosan is a
naturally occurring swellable polymer that is an N-deacetylate derivative of
chitin.Chitosan is a biocompatible, non-toxic polymer that degrades naturally.
It can be applied in two ways to oral extended release tablets: directly
compressing the material or granulating it. It has no smell, is soluble in
water but partially insoluble in 95% ethanol, and has creamy or white flakes or
powder. It functions as a disintegrant, coating agent, mucoadhesive, tablet
binder, and viscosity enhancer.Chitosan has a significant impact on the
transport of drugs to the stomach, intestines, and colon. A prolonged release
behavior is achieved by chitosan at a concentration equal to 50% of the tablet
weight.
2)
Guar gum:
Cymopsis
tetragonolobus seeds are the natural source of guar gum, a naturally occurring
non-ionic polysaccharide that is a member of the Leguminosae family. In solid
dosage forms, it serves as a disintegrant, binder, and polymer.It dissolves in
water but not in inorganic solvents. It is an odorless, pale yellow powder with
no taste. It is primarily made up of high molecular weight polysaccharides
(50000–8000000) that are mannose and galactomannans. The presence of particles,
PH, and temperature all affect gum's viscosity.
3)
Xanthan gum:
It is a well-known
edible gum made of glucose, mannose, and glucuronic acid that is a natural
biopolymer. It can be employed as an emulsifying, suspending, thickening,
stabilizing, gelling, and raising viscosity agent. Zero order drug release
kinetics are a benefit of Xanthan gum over HPMC drug release, which has been
demonstrated to occur more quickly at greater electrolyte concentrations
(potassium or sodium chloride). When included in tablets, xanthan gum makes an
excellent choice for a controlled release formulation. Its natural origin,
biocompatibility, safety, and affordability make it a valuable ingredient in
pharmaceutical products.
4)
Sodium alginate:
Soil bacteria and
brown seaweeds synthesize alginate, a polysaccharide. It is non-immunogenic, PH
sensitive, biocompatible, and bioadhesive. Many biological activities of sodium
alginate include immunological modulatory, anti-tumor, anti-coagulant, and
vascular endothelial growth factor activities.
5)
Carrageenan:
It is frequently
employed as a thickening and bulking agent. These polysaccharides, which form
gels, are taken from species of red sea weeds like Euchema and Chondrus
crispus. Its toughness and viscoelastic nature made it suitable for use as an
excipient ingredient in tablets during granulation and compression.
6)
Pectin:
Pectin is
essentially a D-galacturonic acid polymer containing (1-4) links. Pectin is a
cheap, non-toxic polysaccharide that is taken out of apple pits or citrus peel.
It can also be used as a gelling and thickening agent. When making beads,
calcium pectinate is often utilized at a concentration of 1–5%. It is utilized
as a carrier material for various controlled release systems and remains stable
in low pH solutions. Cross-linked gel beads can be made buoyant by a variety of
techniques, some of which include freeze-drying, using volatile or fixed oils,
gas-forming chemicals, and more.
7)
Gum karaya:
Gum Karaya
dissolves very little in water, very little in 0.1 NHCL, and very little in 95%
ethanol. Alkali solutions with PH values above 6.5 and additional similar
organic solvents. Gum karaya swells in water and is utilized as a release rate
regulating polymer. Zero order medication release and matrix degradation are
seen when using this gum.
8)
Psyllium husks:
Psyllium
originates from Plantagoovata seed and husk. Psyllium belongs to the class of
mucilaginous fibers because of its potent water-forming gelling property. This
husk is affordable, readily available, inert, swellable, biocompatible, and
environmentally benign. Because of its release-delaying qualities, this husk is
a dependable method of delivering medications to the gastrointestinal tract.
9)
Tamarind gum:
The seeds of the
Tamarindus Indica tamarind tree are used to make tamarind gum. This gum is a
polysaccharide made up of 1:2:3 galactosyl, xylosyl, and glutathione.
Xyloglucan, a key structural polysaccharide found in plant main cell walls, is
employed in the pharmaceutical industry as a thickening, stabilizing, gelling,
and binding agent. Drug release can be studied and a matrix tablet made with
tamarind gum is created utilizing the wet granulation technique. Tablet
preparation can be done with varying polymer concentrations. An increase in
polymer content is associated with a decrease in medication release.
(II)synthetic
polymers:
Advantages of synthetic polymers
:
·
This type of
polymers are inert
·
Also it has a high solubility
·
Mainly it is used in the sustained release
preparations
·
Also the synthetic polymers
are easily dissolved in water.
Disadvantages of Synthetic Polymer:
·
Toxic
·
Synthetic process is very complicated and high cost
·
Poor biocompatible
·
Acute and chronic adverse
effect
There are so many type of Synthetic
polymers such as :
1) HPMC:
HPMC is a
semisynthetic polymer that is white to slightly off-white in color, odorless,
and tasteless. grainy or fibrous, fluid powder. This is employed in the
manufacturing of microspheres and floating tablets. HPMC is a member of the
hydrophilic polymer family, which expands when exposed to fluids and forms a
gel layer around the polymer matrix's dry core.HPMC are commonly used in oral,
ophthalmic, nasal, and topical formulations as binder, emulsifying agent, and
thickening agent. They are also utilized as coating solutions for longer
release and as tablet binder. There are several molecular weights of HPMC, such
as 10,000, 20,000, and 30,000 Dalton.
2) Ethyl cellulose:
It has a melting
point of between 2400 and 25500C, is white in color, and has no flavor or
smell. It comes in grades such as K, N, and T type and is not biodegradable in
nature. It is also non-toxic and non-irritating. Moreover, it is a long-chain
polymer made up of acetal links connecting b-anhydro glucose units. Ethyl
cellulose, which is the ethyl ether of cellulose, is used as a coating, filler,
and tablet binder as well as an agent to increase viscosity.
3) Acrylic acid derivatives:
It is derived from
the acids methacrylic and acrylic. It is available in many grades, such as
Eudragit RL, E, and RS, and is mostly utilized for the manufacturing of
floating microspheres. Both RL100 and RS 100 are commonly used granular forms
with swelling polymer that is both PH independent and mucoadhesive. Its nature
is non-toxic, non-absorbent, and non-biodegradable. Quaternary amino groups are
present in grades RS and RL, which are utilized in formulations for prolonged
release.
EVALUATION PARAMETERS OF GRDDS: (18)
1. Drug-excipient interaction :
FTIR and HPLC are
used in the process. The drug-excipient interaction is indicated by the
emergence of a new peak and/or the loss of the original drug or excipient
peaks.
2. Floating lag time :
It measures how long it takes
for a tablet to come out of the dissolving media and onto the surface. It is
expressed in either seconds or minutes.
3. In vitro drug release and duration of
floating:
It is ascertained by churning
a simulated gastric fluid with a pH of 1.2 at 37±2oC at a speed of 50 or 100
rpm using a USP II equipment (paddle). Samples in aliquots are gathered, and
their drug content is examined. The amount of time that the drug floats on the
medium's surface is known as the floating time.
4. In vivo evaluation of gastric retention:
Analysis of the position of the dosage form in the
GIT involves an imaging technique such as
γ-scintigraphy and X-ray.
CONCLUSION
Retention
technologies have been thoroughly investigated in recent years for the delivery
of medications to the gastrointestinal tract. When taking medications orally, a
gastro-retentive strategy can help reduce the frequency of doses and is
definitely advantageous for medications in the stomach or upper intestine. To
fully utilize the technology, a few obstacles must be removed. The human
gastrointestinal tract is unpredictable, which is why many scientists are still
figuring out how to exploit it most effectively. The physiological event in the
GIT must be taken into account while choosing the right medications and
excipient combinations and creating formulation strategies.
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