*Corresponding author,
e-mail : i.sopyan@unpad.ac.id (I. Sopyan)
https://doi.org/10.24198/idjp.v2i1.26103
© 2020 Sopyan et al
Vol 2, Issue 1, 2020 (27-33)
http://journal.unpad.ac.id/idjp
A Novel of Floating Tablet Delivery System as A Tool to Enhance Absorbtion of
Drug: A Review
Iyan Sopyan
1,2
, Amelia P. Pertiwi
2
, M. N. Mu’tashim
2
, Kiara P. Dhirgantara
2
, Ega Megawati
2
, Zara
F. Herlian
2
1. Pusat Studi Penghantaran dan Disposisi Obat, Faculty of Pharmacy, Universitas Padjadjaran Jl. Raya
Bandung Sumedang KM 21 Jatinangor, 45363.
2. Undergraduate Program, Faculty of Pharmacy, Universitas Padjadjaran, Jl. Raya Bandung Sumedang
KM 21 Jatinangor, 45363
Received: 5 Feb 2020/Revised: 8 Feb 2020/Accepted: 8 Feb 2020/Published: 12 Feb 2020
ABSTRACT
This assessment of a oating drug for a novel of new drug delivery system (NDDS) is written to elucidate
FDDS based on existing literature. The most recent progresses of FDDS include the formulation and
physiological variables that could aect gastric retention and formulations are discussed in detail.
This review also summarizes method assessments for FDDS pharmaceutical dosage form and its
classication. FDDS. FDDS is made to increase the absorption of the drug that is expected to dissolve
in the stomach so that the drug enters the intestine in a dissolved state and the fraction of the absorbed
drug increases. FDDS approach is the best way to deal with drugs with low solubility in the digestive
tract.
Keywords: Floating Tablet, Evaluation, Gastric Retentive
1. Introduction
Unique of the target drug delivery systems is to
reach a therapeutic concentration of medicine to the
x target and to ensure the optimum drug level. Drugs
that absorbed in the gastrointestinal route easily
will dissolve quickly from the systemic circulation.
If an inadequate drug release prepartion of drug
and the residence time at the upper gastrointestinal
(a prominent place for the absorption of many
drugs) very fast will make bioavailability become
low. Thus, prolonged gastric maintenance is very
important at the control of gastroprotection time
to formulate a system of controlled release in the
stomach for elongated periods of time and could be
estimated (1). The anticipation depend on the state
of the subject and design of formulations itself, the
maintenance activity can last from a several minutes
until hours (usually 12 hours). The scheme of the drug
delivery system is controlled oral (DDS) is usually
referred to to get bioavailability of the drug that is
more probale and repaired (2). The typical drug
has the development of oral drug-delivery systems
that consist of the optimization of dosage form and
GI physiology habits. (3). Floating drug delivery
system (FDDs) is a gastro retentive pharmaceutical
preparation that could delay the gastric residence
time to get adequate bioavailability of a drug (4).
The system is oating in the gastric uid for a low
substance density than the aqueous medium (5).
2. Methods
This review was made by looking at
international journal 2000-2019, the journal taken
was an international journal both indexed and not
indexed scopus, with due regard to important aspects
of the method of making FDDT, characterization
and evaluation.
3. Discussion
3.1 Denition
Floating systems are low-density systems that
have sucient resistance to oat on the stomach and
stay aoat in the gastric without creat an eect on the
gastric emptying rate for long period times. While
the system oats on the gastric contents, the drug
will be released slowly at the desired concentration
of the system. thus, the residue will be cleared from
the stomach. These results will conduct to GRT
I. Sopyan et al / Indo J Pharm 1 (2020) 27-33
28
elevation and be better control of uxes in plasma
drug concentrations. Even so, furthermore to the
content of the stomach minimally required to
enable the achievement of the right of retention of
the principle of buoyancy, oating style minimal
level (F) also required to give a reliable dosage
form oats on the surface of foods (6). It also useful
for proximal gastrointestinal (GI) tracts local drugs,
for example, antibiotics for Helicobacter pylori on
the manage for a peptic ulcer (7), and for drugs that
dicult to dissolve or not stable in intestinal uids
(8).
3.2 Anatomy and physiology the stomach
Topographically, the stomach has ve regions
(Fig. 1): (1) the cardia and gastroesophageal (GE)
junction, (2) the fundus, (3) the antrum, (4), the
corpus and (5) the pylorus (9).
Figure 1. Structure of gastric (9)
In the stomach, part of the proximal made by
fundus. The body acts as a reservoir for undigested
materials and the antrum is the main site for mixing
gestures and acts as a pump for gastric emptying
by propelling actions (10). Gastric emptying occurs
in both the fasting and fed states’ time. During the
fasting state, the inner digestive myoelectric cycle
or migrating myoelectric cycle (MMC) occurs
during 2-3 hours, which is further divided into four
phases (11)
a. Stage 1 (Basic phase)
Last from 30-60 minutes with infrequent
contractions.
b. Stage 2 (Preburst phase)
Last for 20-40 minutes with reccurent action
potential and contractions.
c. Stage 3 (Burst phase)
Last for 10-20 minutes which includes powerful
and regular contractions for quick period.
d. Stage 4
Last for 0-5 minutes and happens between stage
2 and 1 of 2 repeated cycles (Fig.2).
Figure 2. Gastrointestinal motility model (11)
The stomach has three layers of muscular: an
inside circular layer, a mid longitudinal layer, and
an outside but incomplete oblique layer. Motor
functions in the stomach are separated by region.
The fundus relaxes as uids and solids enter
the esophagus, a response known as accesible
relaxation, and further as food enters the funds,
a process is known as adaptive relaxation (12).
This response permits the liquid to pool in the
fundus bag while the solid components of the meal
remain in the mainstream of ow to the pylorus.
After the ingestion of a mixed meal, the pattern of
contractions variation from fast to that of the fed
state which is also termed as digestive motility
pattern.
3.3 Advantages of oating drug delivery systems
1. Tablets or capsules in the oating tablet forms
will remain in the liquid for a prolonged time
even at the high pH of the intestine region.
2. In the stomach, Floating Drug Systems are
advantageous for local action, ex: Antacids
3. Floating drugs delivery systems dosage forms
are advantageous in the case essential of
intestinal movement and in diarrhea to keep
the drug in the oating state in the stomach to
obtain a relatively better response.
4. Acidic stus like aspirin cause annoyance on
the stomach barrier when coming in contact
I. Sopyan et al / Indo J Pharm 1 (2020) 27-33
29
with it hence; HBS/FDDS formulations may be
valuable for the administration of aspirin and
other similar drugs.
5. The Floating Drug Delivery Systems are
advantageous for drugs absorbed by the
stomach ex: Antacids and Ferrous salts (13).
3.4 Disadvantages of Floating Drug Delivery
Systems
1. Floating systems are not viable for those drugs
that have solubility or stability problems in
gastric uids.
2. Nifedipine, which is well absorbed along the
entire GI tract and which undertake signicant
rst-pass metabolism, may not be appropriate
candidates for Floating Drug Delivery Systems
since the slow gastric clearing may cause
reduced systemic bioavailability (BA). Also,
there are limitations to the applicability of
FDDS for drugs that are irritant to the gastric
mucosa.
3. Floating Drug Delivery Systems need a
suciently high level of uids in the stomach
so that the drug dosages form oat within and
work eciently.
4. These systems also involve the presence of
food to delay their gastric emptying. (14).
3.5 Clasication of oating mechanism
Floating drug delivery systems (NDDS) are
characterized based on two varieties of preparation
variables: eervescent and Non-eervescent
system (15,16) such as Fig. 3.
Non-eervescent System
The non-eervescent FDDS primarily based on
the system of swelling of polymer or the adhesion to
the mucosal layer in the gastrointestinal tract. Two
of the most common excipient for non-eervescent
FDDS are gel-forming or highly swellable cellulose
type of hydrocolloid, polysaccharides and also
matrix-forming material such as polycarbonate,
polyacrylate, polystyrene, polymethacrylate as
well as a bio-adhesive polymer such as chitosan
and Carbopol (17).
Colloidal gel barrier system
Sheth and Tossounian rst design the
Hydrodynamically Balanced System (HBS) that
contains drugs with gel-forming hydrocolloid,
back in 1975. The system corporate a high level of
gel-forming around 20-75% w/w, highly swellable,
cellulose type hydrocolloids, polysaccharides and
also matrix-forming polymers. When coming in
contact with gastric uid, these hydrocolloids in
the system will hydrate and forming a colloidal gel
barrier around the surface, these gel barriers control
the rate of penetration of the uid to the device and
the release of the drug (18).
Bilayer oating tablet
Bilayer oating tablet contain of two-layer of
immediate-release tablet that release the rst dose
of the system while the sustained release layer
absorb the gastric uid and form a colloidal gel
barrier on the supercial, it preserves the bulk
density to less than one and will remain oating in
the stomach (18).
Figure 3. Classication of oating system (15)
I. Sopyan et al / Indo J Pharm 1 (2020) 27-33
30
Micro-porous compartment system
A Microporous section has pores placed on the
top and bottom of the wall containing a packed
medicine reservoir. The peripheral wall drug
reservoir is completely sealed to seal the insoluble
drug with the stomach surface. The entrapped in the
room will be used to oat the system on the stomach
contents and into the uid hole that will dissolve
the drug to be absorbed in the intestine (20).
Alginate beads
Multi-unit oating dosage forms are made from
freeze-dried calcium alginate. Round beads with
2.5 mm diameter can be equipped with dripping
sodium alginate soluble to a calcium chloride
solution, this process will result in precipitation of
calcium alginate which can form a porous system
that can reinforce the capacity to oat for more than
12 hours and have some more time long (21).
Hollow microspheres
Hollow microspheres are micro balloons
occupied with medication in the outer shell of
the polymer and used by the emulsion solvent
diusion method. Ethanol solution: aqueous
dichloromethane and enteric solution of a PVA of a
turn temperature of 400
o
C. The resulting gas phase
is spread into polymer droplets by vaporization
of dichloromethane forming an internal holow in
a polymeric microsphere with the drug formed an
internal cavity in the microsphere of polymer with
the drug. The micro-balloons will oat constantly
over the surface of acidic dissolution media that
hold a surfactant for more than 12 hours (in vitro)
(22).
Eervescent system
In an eervescent system, preparation are
designed to produce carbon dioxide gas. Among
them are carbonates, generating gases, and other
organic acids. The design of the formulation aims
to decrease the density system that can be oating
in the gastric uid (23). The free CO
2
gas can mix
rapidly in the tablet matrix in the case of single-
layered tablets (24). The other way is trough
combining a matrix that contains a part of liquid,
where later from the fusion will produce gas that
will evaporate at body temperature (25). This
eervescent system can be categorized into two
groups, gas producing system and volatile liquid
containing the system.
Volatile liquid
The volatile liquid containing systems Inatable
chamber with a liquid can be incorporated which
provides sustained gastric retention of the drug
delivery system (26). Liquids in this system
include cyclopentane, either that gasies at body
temperature which can lead to inammation of the
chamber in the stomach. They contain a hollow
deformable unit which is osmotically controlled
oating systems. The system is diered into two
compartments the rst section contains a drug and
there is volatile liquid in the second compartment
(27). Gas generating systems, It contains polymers
that gasify at body temperatures eervescent
compounds such as swellable polymers like
methodical and polysaccharides tartaric acid,
sodium bicarbonate, and citric acid. Resin
beads loaded with bicarbonate and coated with
ethylcellulose is the most common approach for
the preparation of these systems. The ethylcellulose
coating is permeable to water which releases CO
2
due to which it oats (28).
Raft forming systems
Raft forming systems consume a foundamental
mechanism by forming a thick interconected gel in
contact with gastric uid, in which apiece part of
the portion of the liquid forms a continuous layer
called a raft. The formation of carbon dioxide gas
can make this raft aoat. Also, carbon dioxide
can prevent the discharge of gastric uid into the
esophagus (29). This system usually contains a
gelling agent, a carbonate or a bicarbonate base to
make a less dense system and can make it oat in
the gastric solution (30).
3.6 Factors aecting gastric retention time of the
preparation
1. Density-should be lower than that of the gastric
contents (1.004 g/ml)
2. Size- the diameter of more than 7.5 mm (31).
3. Incidence of feeding- GRT can rise by more
than 400 min when consecutive foods are
I. Sopyan et al / Indo J Pharm 1 (2020) 27-33
31
dispense compared to a single meal due to low-
frequency MMC.
4. Caloric content- can be increased by 4-10 with
foods high in protein and fat.
5. Gender- average outpatient GRT in men (3.4 h)
less than age and race matching with women
(4.6 hours) regardless of height, body weight
and surface (32).
3.7 Evaluation of oating tablet
Hardness
Tablets are sited between two anvils of hardness
tester and the force (kg) is gradually increased to
get a proper reading. Readings on a noticeable scale
are recorded for the pressure, which is required to
break the tablet (33).
Drug content
Five tablets for each group were taken and
ground. The powder equal to 100 mg of the drug
was weighed and moved to a beaker glass and
then 0.01 N HCl was added and then shaken for
5 minutes and added 0.01 N HCl to make up to
100 ml and the solution was then produced for 15
min and ltered through the lter paper Whatman.
Finally, a solution was diluted appropriately and
then measured spectrophotometrically at 203
nanometers using UV-Visible spectrophotometer
(Jasco V530 with 0.01N HCl blank). (34).
Determination of the drug content uniformity
The portion of drug content provides how much
volume of drug is in the formulation. It should not
exceed the limits obtained by standard monographs.
The drug content is determined using HPLC, NIRS,
HPTLC, Microtitrimetric method, and ICPAES
(35).
Swelling index
The swelling behavior of the measuring unit is
determined by the weight assignment. The tablet
swelling index corresponds to the tablet site in
the dissolution tool basket (type 1) using a pH 6.8
buer dissolution medium at 37 ± 0.5ºC. The trials
were conducted in triplicate for each time point, the
swelling index was calculated using the following
formula (36).
........................Eq. 1
Disintegration test
The time of tablet disintegration was carried
out by using a therminate tablet disintegration test
device (37).
Floating properties
The eect of formulation variables on the
oating properties of gastric drug delivery systems
is determined by using a continuous oating
monitoring system and statistical trial design (38).
In-vitro dissolution studies
The rate of release of Ondansetron Hydrochloride
from oating tablets is determined using the USP
Dissolution Testing Apparatus 2 (paddle method).
The dissolution test was done using 900 ml 0.1
N HCl for 12 hours. The sample (5 ml) of the
solution was quite from the dissolution apparatus
every hour and the sample were changed with a
new dissolution medium. The sample was ltered
through a 0.45μm membrane lter and diluted to
a concentration corresponding to 0.1 N HCl for 12
hours. The transmitan or absorbance of this solution
was quantied at 310 nm (37).
4. Conclusion
Drugs that are removed quickly from the blood
stream can be surmounted by Floating drug delivery
system (FDDs) that can delay gastric retention of
the dosage form and the enhance of drug absorption.
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