Gastroretentive Drug Delivery System Intro, Needs, Merits, Demerits, Approaches, Factors Affecting, Conclusion

1. Dr. Babasaheb Ambedkar Technological University,
Lonere.
डॉ. बाबासाहेब आंबेडकर तंत्रशास्त्र विद्यापीठ
Lonere - 402103 Tal - Mangaon, Dist – Raigad (M.S.) India
Shree Mahavir Education Society’s
Mahavir Institute Of Pharmacy, Nashik

2. Course structure and contents for
PRACTICE SCHOOL (BP706PS)
B. Pharm Final Year (SEM VII)
DOMAIN – 5
FORMULATION
DEVELOPMENT
A Review On Gastro
Retentive Drug Delivery
System

3. A Review Article By:
KATURE KAMLESH N.
Final Year B. Pharmacy
(1952811823047)
Guided by:
Prof. Mohini Shinde

4. Conclusion
References
INDEX
Abstract
Needs for GRDDS
Merits
Demerits
Approaches of gastric retention
Factors affecting on GRDDS
Marketed products of GRDDS

5. • A Controlled release dosage forms have been extensively used to
improve therapy with several important drugs. However, the
development processes are faced with several physiological difficulties
such as the inability to restrain and localize the system within the
desired region of the gastrointestinal tract and the highly variable
nature of the gastric emptying process. This variability may lead to
unpredictable bioavailability and times to achieve peak plasma levels.
Abstract

6. • Are locally active in the stomach. E.g. Antacids, Misoprostol
• Have an absorption window in stomach or in the upper small
intestine E.g. L-dopa, PABA
• Are unstable the intestine or colonic environment E.g. Captopril
• Exhibit low solubility at high pH values E.g. Diazepam, Verapamil
• Alter normal flora of the colon E.g. Antibiotics
• Absorbed by transporter mechanism E.g. Paclitaxel
Needs for GRDDS

7. Merits
• Enhanced bioavailability
• Improved selectivity in receptor activation
• Reduced counter-activity of the body
• Reduced fluctuations of drug concentration
• Extended effective concentration.
• Minimized adverse activity at the colon.

8. Demerits
• Requires high level of fluid in the stomach for drug delivery.
• Not suitable for drug that have solubility problem in GIT.
• Drugs which are irritant to gastric mucosa are also not suitable.
• Drugs that have very limited acid solubility not used.

9. Approaches of GRDDS
GRDDS APPORACHES
HIGH DENSITY
SYSTEM
FLOATING
SYSTEM
MUCOADHESIVE
SYSTEM
SWELLABLE
SYSTEM

11. Floating system
• One of the most essential techniques to achieving stomach
retention and appropriate drug bioavailability.
• Dosage form should have less bulk density than that of the
gastric fluids (1.004–1.001 gm/cm3),
• so that it can float on gastric fluid for entire duration of therapy,
and the medicine is released slowly with a controlled rate.

12. • Gastric contents have a density close to water.
• A density close to 2.5g/cm³ is necessary for
significant prolongation of gastric residence time.
• The commonly used excipients in high density system
includes barium sulphate, zinc oxide, iron powder, and
titanium dioxide
• The major drawback with such systems is that it is
technically difficult to manufacture them with a large
amount of drug (>50%) and to achieve the required density.
High-density system

13. Swellable system
• In swellable system, the dosage form is designed in such a
way that its size is small enough to administer through oral
route but once it reaches the stomach,
• It goes in gastric fluid and swells; thus its size is expanded
and will be difficult to move on through the pyloric
sphincter.
• This improves the residence time of formulation in stomach.

14. Mucoadhesive system
• MDDSs are non-floating systems formulated to achieve gastric
retention of drugs, these are prepared with various mucoadhesive
polymers to get attach inside the lumen of the stomach wall and
survive the gastrointestinal motility for a longer period, these are
also beneficial as site specific drug absorption in infected area.
• Eg of some mucoadhesive excipients are polycarbophil, lectins,
carbopol, chitosan, carboxymethylcellulose (CMC), pectin etc.

15. Factors Affecting GRDDS
• Density
• Size and Shape of the dosage form
• Single or Multi unit formulation
• Age
• Gender
• Body posture
• Frequency of intake
• Diseased state of an individual

16. BRAND NAME ACTIVE INGREDIENTS
Cifran OD® Ciprofloxacin
Madopar® L-Dopa and Benserazide
Valrelease® Diazepam
Topalkan® Aluminium-magnesium antacid
Almagate FlatCoat® Aluminium-magnesium antacid
Liquid Gavision® Aluminium hydroxide
Conviron® Ferrous sulfate
Cytotec® Misoprostal
Marketed Products of GRDDS

17. • But no single GRDDS all required features so a
combination one or more floating & non-floating system
along with suitable excipients were selected to formulate
such a dosage form that yields maximum therapeutic
efficacy of drugs
Conclusion
• It has been observed that for oral drug delivery gdds has emerged
as a boon for controlled delivery of drugs that exhibit absorption
window along with there enhanced bioavailability. As it known that
to obtain maximum therapeutic benefit from certain drug, it is
essential to delay their gastric residence time , various technical
approaches had been formulated to achieve it.

18. Reference
• Article of Amit Kumar Nayak, Gastroretentive drug delivery
systems: a review, Asian Journal of Pharmaceutical and Clinical
Research,
March 2010, Page No. : 8.
• Article Of Shivram Shinde, Imran Tadwee And Sadhana Shahi,
Gastroretentive drug delivery systems: a review, International
Journal of Pharmaceutical Research & Allied Sciences,
January 2011, Page No. : 10.
• Article of Meenakshi Jassal, Ujjwal Nautiyal, Jyotsana Kundlas,
A review : Gastroretentive drug delivery systems,
Indian Journal of Pharmaceutical and Biological Research (IJPBR),
March 2015, Page No. : 1.