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GRDDS

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0% found this document useful (0 votes)
21 views

GRDDS

Uploaded by

sanjotm2
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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GOVERNMENT COLLEGE OF PHARMACY CH.

SAMBHAJINAGAR

GASTRORETENTIVE
DRUG DELIVERY
SYSTEM
GROUP NO – 41 TO 45
NAMES :-
AKANKSHA LAKHE
SUMIT MALODE
SURBHI MALWANKAR
KOMAL MARKAD
SANJOT MHASANE
GASTRORETENTIVE DRUG DELIVERY
SYSTEM
Gastro-Retentive Drug Delivery Systems (GRDDS) are designed to keep a drug in the
stomach for a longer period, improving its absorption and efficacy.
• GRDDS address challenges like poor bioavailability and
incomplete drug release seen with conventional oral
delivery.

• They achieve this by using various techniques like


magnetic fields, swelling polymers, muco-adhesion, and
floating systems.

• GRDDS can be beneficial for drugs that are less soluble


in the stomach's high pH environment or for targeting
specific areas in the upper gastrointestinal tract.
APPROCHES USE IN GRDDS
TYPE
 Floating Dosage Forms: Remains buoyant in the stomach.

 Adhesion to Stomach Wall: Sticks to the stomach lining.

 Swelling of Dosage Form: Expands in the stomach.


.
Floating Drug Delivery Systems (FDDS)
Overview:
Floating drug delivery systems (FDDS) are innovative techniques designed to prolong the gastric
retention time of drugs. These systems float on the gastric contents, providing a prolonged
duration of action, which is advantageous for drugs absorbed mainly in the stomach or upper part
of the small intestine.
Effervescent Systems:

 Gas-Generating Systems:
- Typically contain sodium bicarbonate and citric or tartaric acid.
- React in the stomach's acidic environment to release CO₂ gas, causing the
dosage form to float.
- Commonly used in single-layer or bi-layer tablets

 Volatile Liquid Containing Systems:


- Use volatile liquids like ether or cyclopentane.
- These liquids evaporate at body temperature to generate a floating effect.
 Inflatable Gastrointestinal Delivery Systems:
- Incorporate an inflatable chamber containing liquid or gas.
- Triggered to inflate upon reaching the stomach, ensuring buoyancy.

 Intragastric Osmotically Controlled Drug Delivery Systems:


- Use osmotic pressure to inflate and float in the stomach.
- Allows for controlled drug release through semi-permeable membranes.

Non-Effervescent Systems:
 Colloidal Gel Barrier Systems:
- Utilize polymers such as hydrocolloids that swell in contact with gastric
fluids.
- Form a gel-like barrier that remains buoyant.
 Alginate Beads:
- Created by ion exchange reactions, typically involving sodium alginate.
- Beads form a buoyant gel upon contact with gastric fluids.
 Hollow Microspheres:
- Made from synthetic or natural polymers.
- Contain air or gas to provide buoyancy.
- Offer a high degree of floatation and drug loading capacity.
 Microporous Compartment Systems:
- Incorporate a microporous membrane on the dosage form surface.
- Traps air and prevents water penetration, enabling the form to float.
Bioadhesive or Mucoadhesive or
Gastroadhesive Drug Delivery System
In gastroadhesive drug delivery system, a mucoadhesive polymer is used that adheres to the gastric
mucosal surface and prolong its gastric retention time in the GIT. The property of mucoadhesive polymers to adhere
to the mucus layer makes them very useful excipients in GRRDS. Mucoadhesive polymers can be of natural origin
(e.g., sodium alginate, gelatin, guar gum, etc.) or of semi-synthetic (e.g., HPMC, carbopol, sodium carboxymethyl
cellulose). Mucoadhesive polymers can be cationic, anionic, or neutral.

Adhesion of these polymers to mucus membrane is facilitated by hydration, bonding, or receptor-


mediated adhesion. In hydration-mediated adhesion, hydration of hydrophilic polymer makes it sticky and
mucoadhesive. In bonding-mediated adhesion, a mechanical or chemical bonding is involved. Chemical bonding
involves ionic or covalent bonds or Van der Waal forces between the polymer molecule and the mucus membrane.
Mechanism of Floating Drug Delivery System
Slow release of drug is accompanied with the required rate during the system flow on the
gastric contents. Release of drug is followed by removal of the residual system from the stomach. However,
minimum levels of gastric contents and an appropriate level of floating force (F) are required to achieve
buoyancy retention principle and to keep the dosage form buoyant over meal surface.

The kinetics of floating force can be measured using an apparatus that measures a force
equivalent to F (with respect to time) by keeping the object submerged. If the force (F) is higher on the positive
side, the flow of object is better. By this apparatus, FDDS can be optimised and its drawbacks of unexpected
intragastric buoyancy capability variations, related to stability and durability, can be prevented.

F = F buoyancy − F gravity
= (Df − Ds) g.v
Where, F = Total vertical force.
Df = Fluid density.
Ds = Object density.
v = Volume.
g = Acceleration due to gravity.
Factors Affecting Gastric Retention Time of
the Dosage Form
1) Density: Dosage form should have a less density than that of the gastric contents (1.004gm/ml).
2) Size: Dosage form with a diameter of more than 7.5mm show more gastric residence time as compared to
the dosage form having 9.9mm diameter.
3) Shape of the Dosage Form: The tetrahedron-shaped dosage form remains for a longer period in the
stomach than other devices of similar size. More predictable release profile is observed for single or multiple
unit formulation, along with insignificantly impaired performance due to failure of the units.
As compared to single unit dosage form, multiple unit formulations allow co-administration of units with
different release profile or showing incompatibility with gastric substances and have a large safety margin
against dosage form failure.
4) Fed or Unfed State: During fasting the gastrointestinal motility shows periods of strong motor activity at
intervals of 1.5-2 hours. The Migrating Motor Complex (MMC) allows passing of undigested food material
from the stomach; and if the timing of the formulation coincides with that of MMC, the GRT of the unit can be
very short; but, MMC is delayed and GRT is longer during fasting.
5) Nature of Meal: The motility pattern of the stomach changes to a fed state due to intake of indigestible
polymers or fatty acids. This reduces the gastric emptying rate and prolongs the drug release.
Advantages
1) It increases the bioavailability and curative efficiency of drugs.
2) It increases the economic usage of dosage.
3) It reduces the risk of antibiotic resistance by stabilising therapeutic levels over prolonged periods by
removing fluctuations.
4) It increases the efficiency of drug release in case of short half-life drugs.
5) It causes flip-flop of pharmacokinetics.
6) It ensures patient compliance with reduced dosage frequency.
7) It removes the drawbacks of Gastric Retention Time (GRT) and Gastric Emptying Time (GET) as the
system remains buoyant on gastric fluid due to its lower bulk density than gastric fluids.
8) It is used to treat problems related to stomach and small intestine as the system sustains the drug release,
thus increases the gastric residence time and provides local therapy on these organs.
9) It provides a narrow curative index.
10) It reduces any fluctuations in drug concentration and their effects.
11) It is a highly efficient system due to reduced counter activity by the body.
Disadvantages
1) It increases the level of fluids required in the stomach.
2) It is not suitable for drugs having low solubility in gastric fluid, causing gastrointestinal irritation,
ineffective in acidic environment, and meant for selective release in the colon.
3) In such a system, adherence of drugs with the mucus cannot be predicted due to the continuous renewal of
mucus wall of stomach.
4) GRDDS is fed into the system after the meal; the drug’s residence time in stomach depends on digestive
state of the subject.
5) The drug’s residence time in stomach depends on the subject being positioned upright.
6) Drugs which are formulated as hydrogel-based swelling system takes longer time to swell.
7) In case of multiple administrations, concentration of drug increases in the body, and this may be life-
threatening due to the possible hazard of permanent retention in stomach.
8) Super-porous systems have a drawback of problematical storage of hydrolysable and biodegradable
polymers.
Applications
1) Enhanced Bioavailability: Riboflavin Gastroretentive Dosage From (GRDF) shows enhanced bioavailability as
compared to the non-GRDF polymeric formulations. Many other processes, related to drug absorption and transit in
the GIT, act concurrently to influence the drug absorption rate.
2) Sustained Drug Delivery/Reduced Frequency of Dosing: Drugs having short biological half-life, and sustained
and slow input from GRDF enhance the pharmacokinetic factors and decrease the dosing frequency. This property
increases patient compliance, and thus improves therapy.
3) Targeted Therapy for Local Ailments in the Upper GIT: Local therapy can be exerted on stomach and small
intestine with prolonged and sustained administration of the drug from GRDF to the stomach. Such targeted therapy
helps to achieve the therapeutic drug concentrations locally; while, minimal systemic concentrations are achieved
after drug absorption and distribution.
4) Reduced Fluctuations of Drug Concentration: By continuous intake of the drug following GRDF
administration, blood-drug concentrations can be maintained within a narrower range as compared to the immediate
release dosage forms. This minimises the fluctuations in drug effects and prevents the adverse effects caused due to
higher concentration.
5) Site Specific Drug Delivery: Drugs having limited absorption sites in upper small intestine can be formulated as
a floating dosage form. Controlled and slow delivery of drug to the stomach provides local therapeutic levels and
also limits the systemic exposure to the drug. This approach also decreases side effects caused by the drug in blood
circulation. Along with this, dosing frequency is also reduced by the prolonged gastric availability from a site
directed delivery system.
THANK YOU

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