formulation approaches for gastro retentive drug delivery
TRANSCRIPT
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FORMULATION APPROACHES FOR GASTRORETENTIVE DRUG DELIVERY SYSTEM
SARDAR BHAGWAN SINGH P.G. INSTITUTE OF BIO MEDICAL SCIENCES AND RESEARCH, BALAWALA, DEHRADUN, UTTARAKHAND
PRESENTED BY- GUIDED BY- NAMAN PANT Mrs. GAURI KUKRETIM.Pharm. (Pharmaceutics) Assistant professor
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ORGANIGATION-• Introduction
• Anatomy of stomach
• Factors affecting gastric retention
• Formulation Approaches
•Advantages and disadvantages
•Evaluation of gastro retentive drug delivery system
•Marketed formulations
•Conclusion
•References
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INTRODUCTION-
DEFINITION-o These are the drug delivery systems which posses
the ability of retaining the drug in the GIT particularly in the stomach for prolonged period of time.
o After the drug release for required time period the dosage form should get degraded without causing any gastric disturbance.
(1) Rohilla Ankur et al, International research journal of pharmacy,2(5),2011,Pp72-78
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Anatomy of stomach-
Article in expert opinion on drug delivery, Research gate,DOI:10.1517/17425.247.2011
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Factors affecting gastric retention-Size and shape of dosage form
Density
Patient age, body weight, and body
postureDisease state
Fasting and fed condition of
patient
(1) Vyas SP, Khar RK, Controlled drug delivery, Vallabh prakashan, ed(2),2012, Pp199-201(2) Research gate, article in expert openion on drug delivery, DOI:10.1517/174.25247.2011
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Formulation approaches-
Floating system
Swelling
Expending
Modified shape systems
Tetrahedron
Round shaped device
Bioadhesive system
High densit
y system
(1)Makwan A, Sameja K, Journal of drug delivery and therapeutics,2012,2(3),P.p12-21(2) Garg R, Gupta GR, Tropical journal of pharmaceutical research,september2008,7(3),P.p1055-
1066(3) Mohamad HG,FurquanNK, International journal of health research, march2009,2(1),P.p33-54
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Floating systems-The system which have bulk density lower then the gastric
content is called Floating drug delivery system.They have the potential for continuous release of drug and
remain buoyant in the stomach for a prolonged period of time.
Types
Hydrodynamically balanced system
Gas generating system
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Expendable systems-
It is small enough to swallowed. After coming into contact with the gastric fluids, they get expended to a larger size so that gastric retention is achieved.
(1) Research gate, article in expert openion on drug delivery, DOI:10.1517/174.25247.2011
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Gas generating systems-
These formulation contain carbonates or bicarbonates which generates CO2 due to their reaction with gastric acid.
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Floating microspheres-Solvent evaporation methodSolvent diffusion method
Yeoce PG, Shagufta K, Patel AF, Indian journal of pharmaceutical science, 2005, 67(3), P.p 265-272
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RAFT forming system-Systems consists of some gel forming agents. Eg- Sodium
alginate solution containing carbonate or bicarbonate.These systems produce a layer on the top of the gastric
fluids.
(1) Vyas SP, Khar RK, Controlled drug delivery, Vallabh prakashan, ed(2),2012, Pp199-215
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Super porous hydrogels-Pore size between 10nm-10µm.They swell to larger size and can withstand pressure with
gastric contraction and due to this larger size their passage through pyloric sphincter is prevented.
1)Makwan A, Sameja K, Journal of drug delivery and therapeutics,2012,2(3),P.p12-21
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Bioadhesives-In these systems the dosage form will stick to the mucosal
surface in the gastrointestinal tract as a result of which prolonged gastric retention can be achieved.
Vyas SP, Khar RK, Controlled drug delivery, Vallabh prakashan, ed(2),2012, Pp211-215
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Advantages-Improved drug absorption, because of increased gastro retention time of
drug.
Delivery of drug for local action in the stomach.
Reduce cost of drug and better patient compliance.
Reduction of over dose and minimize side effects
1)Makwan A, Sameja K, Journal of drug delivery and therapeutics,2012,2(3),P.p12-21(2)Garg R, Gupta GR, Tropical journal of pharmaceutical research,september2008,7(3), P.p
1055-1066
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Disadvantages-
Dose dumping
Poor In Vitro – In Vivo correlation
Patient variation
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Limitations-They require a sufficient level of fluids in the stomach for buoyancy
Not feasible for those drugs that have solubility and stability problems in GI fluid.
Drugs that are irritant to gastric mucosa are not suitable for GRDDS.
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Evaluation of gastroretentive drug delivery system-
General tests
• Hardness• Friability• Weight variation• Content uniformity• Dissolution• Drug release
Buoyancy time • Buoyancy lag time• Buoyancy duration
Swelling studies
• %Swelling index= Wo-(Wi+Wo)͟͟/Wi×100
• Where, Wo= wt. of swollen tablet with OHP sheet
• Wi= Wt. of initail tablet• Wb= Wt. of OHP paper
Chaturvadi K, Umadevi S, Vaghani S, Scientica pharmaceutica,Scipharma2010,78:927-939
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Marketed formulations-Microspheres
• Griseofulvin
• Ibuprofen
• Tranilast
Capsules
• Diazepam
• Furosemide
• Misoprostol
• Propranolol
Tablets
• Atenolol
• Ampicillin
• Fluorouracil
• Prednisolone
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Some commercial Gastroretentive Drugs-Company Product Drug
Ranbaxy Cifran OD Ciprofloxacin
GSK Gaviscon liquid Antacid
Cipla Ciplox OD Ciprofloxacin
Sanofi Xatral OD Alfuzosin
Fabre Topalkoun Antacid
Baya Cipro XR Ciprofloxacin
Bristol Myers Squibb Kombiglyze XR Matformin
(1) Research gate, article in expert openion on drug delivery, DOI:10.1517/174.25247.2011
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Conclusion-Gastroretentive drug delivery systems are the most
preferable systems in order to deliver the drugs which have a narrow absorption window near the gastric region. Now a days a number of drug delivery devices are being developed which aim at releasing the drug at gastric region. Even though these drug delivery systems have several advantages they also have disadvantages like their invitro-invivo correlation is very less.
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