*Corresponding author,

e-mail : i.sopyan@unpad.ac.id (I. Sopyan)

https://doi.org/10.24198/idjp.v2i1.26103

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

, M. N. Mu’tashim

, Kiara P. Dhirgantara

, Ega Megawati

, Zara

F. Herlian

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

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

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

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

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

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

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

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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