Floating drug mm


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Floating drug mm

  1. 1. Presented by: Maryam albuloshi B.Pharm
  2. 2. CONTENTS Introduction Basic GIT physiology Process of gastric emptying Mechanism of FDDS Approaches for prolonging the gastric residence time Classification IMPORTANCE OF FDDS Factor affecting Floating time Advantage of FDDS Disadvantage of FDDS Evaluation tests Examples Conclusion Reference 1
  3. 3. INTRODUCTION  Floating drug delivery systems is known as hydrodynamically controlled systems.  It is having low bulk density that have sufficiently buoyancy to float over the gastric contents and remain buoyant (floating) in the Gastric juice of stomach without affecting the gastric emptying rate for a prolonged period of time.  This leads to an increased gastric retention time (GRT) and a better control of the fluctuations in plasma drug concentration. 2
  4. 4. BASIC GIT PHYSIOLOGY • Reservoir for ingested material. fundus • Reservoir for ingested material. body •Major site of mixing motion. •Acting as pump to propel gastric contents for gastric emptying.pylorus 3
  5. 5. PROCESS OF GASTRIC EMPTYING Gastric emptying occurs in both fasting and fed states. Fasting state Interdigestive series of electric event take place. It cycles both through stomach and intestine every 2-3 hrs It called as interdigestive myoelectric cycle Its having 4 phases Phase 1 Phase 2 Phase 3 Phase 4 ingestion of a mixed meal fed state (digestive motility pattern) 4
  6. 6. •last from 30-60 minutes with rare contractions. Phase 1-(Basic phase) •last for 20-40 minutes with intermittent action potential and contractions. Phase 2- (Preburst phase) •last for 10-20 minutes which includes intense and regular contractions for short period. Phase 3-(Burst phase) •last for 0-5 minutes and occurs between phase 2 and 1 of 2 consecutive cycles.Phase 4 5
  7. 7. Mechanism of FDDS • FDDS has a bulk density less than gastric fluids and so remain buoyant in the stomach with out affecting the gastric emptying rate for a prolonged period of time. F = F buoyancy - F gravity = (Df - Ds) gv Where, F= total vertical force, Df = fluid density, Ds = object density, v = volume and g = acceleration due to gravity. 7
  9. 9. 9
  10. 10. Floating Drug Delivery System Effervescent System Gas generating system Volatile liquid/ vacuum containing system Non-Effervescent System Single Layer Floating Tablet Bilayer Floating Tablet Alginate Beads Hollow/ floating Microspheres 10
  11. 11. • Prepared from one or more gel forming or highly swellable cellulose type hydrocolloids (e.g. hydroxyl ethyl cellulose, hydroxypropyl methyl cellulose [HPMC] etc ) or polysaccharides, or matrix forming polymers(e.g polyacrylates, and polystyrene) are incorporated in high level (20‐75% w/w) to tablets or capsules. • Gel forming hydrocolloid swells in contact with gastric fluid after oral administration and maintain a relative integrity of shape and bulk density of less than unity within gastric environment. Non effervescent systems 11
  12. 12. Non Effervescent System Single Layer Floating Tablet or hydrodynamically balanced system Bilayer Floating Tablet Alginate Beads Hollow Microspheres/ Microballoons 12
  13. 13. HYDRODYNAMICALLY BALANCED SYSYTEMS: * Prepared by incorporating a high level(20-75%w/w) gel-forming hydrocolloids. E.g.:- Hydoxyethylcellulose, hydroxypropylcellulose, Sod. CMC into the formulation and then compressing these granules into a tablets or capsules * It maintains the bulk density less than 1. * The gelatinous polymer barrier formation results from hydrophilic polymer swelling. 13
  14. 14. Bilayered Floating Tablets These are compressed tablet as containing two layer 1-Immediate release layer 2-Sustained release layer. 14
  15. 15. ALGINATE BEADS - Prepared by dropping sodium alginate solution into aqueous solution of calcium chloride, causing the precipitation of calcium alginate. - Freeze dry in liquid nitrogen at -40oc for 24h. - Beads-spherical and 2.5 mm in diameter. 15
  16. 16. HALLOW MICROSPHERES 1. Hallow microspheres as one of the most promising buoyant systems, as they possess unique advantages of multiple unit systems as well as better floating properties, because of central hallow spaces inside the microsphere. 2. The general techniques involved in their preparation include simple solvent evaporation, and solvent diffusion and evaporation. 16
  17. 17. • These are matrix type of systems with the help of swellable polymers such as methycellulose and chitosan and various effervescent eg, sodium bicarbonate, tartaric acid and citric acid. • They are formulated in such a way that when in contact with the acidic gas content ,CO2 is liberated and gets entrapped in swollen hydrocolloids, which provides buoyancy to the dosage form. Effervescent system 17
  18. 18. 1. Gas Generating System Intra gastric single layer floating tablet Intra gastric bilayer floating tablet Multiple unit floating pills 18 2. Volatile liquid /vacuum containing System Intra gastric floating GIDDS Inflatable GIDDS Intra gastric osmotically CDDS
  19. 19. Factor affecting Floating time 1 • Effect of Dosage Form Size& Shape 2 • Gender, Posture & Age 3 • Effect of Food & Specific Gravity 4 • Type of Formulation 5 • Nature of Meal & Frequency of Food 19
  20. 20. IMPORTANCE OF FDDS Suitable dosage forms for the drugs those are primarily absorbed in the stomach. Beneficial in the treatment of gastric diseases. Lower dosing and less side effects The gastric emptying time in humans which normally averages 2-3 hours through the major absorption zone (stomach and upper part of intestine) can result in incomplete drug release from the drug delivery system leading to reduced efficacy of administered dose. 20
  21. 21. Advantages of FDDS Enhanced bioavailability Sustained drug delivery/reduced frequency of dosing Targeted therapy for local ailments in the upper GIT Reduced fluctuations of drug concentration Improved selectivity in receptor activation Reduced counter-activity of the body Extended effective concentration. Minimized adverse activity at the colon 21
  22. 22. Disadvantage of FDDS The drug substances that are unstable in the acidic environment of the stomach are not suitable candidates to be incorporated in the systems. These systems require a high level of fluid in the stomach for drug delivery to float and work efficiently. Not suitable for drugs that have solubility or stability problem in GIT. 22
  23. 23. EVALUATION TESTS IN-VITRO TEST IN-VIVO TEST • Floating lag time • Floating time • Dissolution study • Resultant weight test • X ray method • Gamma-scintigraphy • Gastroscopy • Ultra sonography 23
  24. 24. Marketed Products of GRDDS Brand name Delivery system Drug (dose) Company name Valrelease® Floating capsule Diazepam (15mg) Hoffmann-LaRoche, USA Madopar® HBS (Prolopa® HBS) Floating, CR capsule Benserazide (25mg) and L- dopa (100mg) Roche Products, USA Liquid Gaviscon® Effervescent Floating liquid alginate preparations Al hydroxide (95 mg), Mg Carbonate (358 mg) GlaxoSmithkline, India Topalkan® Floating liquid alginate Preparation Al – Mg antacid Pierre Fabre Drug, France Conviron® Colloidal gel forming FDDS Ferrous sulphate Ranbaxy, India Cytotech® Bilayer floating capsule Misoprostol (100μg/200μg) Pharmacia, USA Cifran OD® Gas-generating floating form Ciprofloxacin (1gm) Ranbaxy, India 24
  25. 25. Widely used drug and dosage forms S .No Dosage Form Drugs 1. MICROSPHERE Aspirin, Griseofulvin, p-nitroglycerine, ibuprofen, Terfinadine, Tranilast. 2. GRANULES Diclofenac sodium, Indomethacin, Prednisolone 3. FILMS Cinnarizine 4. CAPSULE Chlrdiazepoxide, Diazepam, Furosemide, L-Dopa, Benserazide, Misoprostol, Propanolol 5. TABLET/ PILLS Acetaminophen, ASA, Amoxicilin Trihydrate,Ampicilin, Atenolol, Chlorphenarimine,Cinnazirine, Diltiazem,Flourouracil, Isosorbide Mononitrate & dinitrate, p-aminobenzoic acid, Prednisolone, Quinidine Gluconate,Ribiflavin 5-p, Sotalol,Theophylline, Verapamil 25
  26. 26. CONCLUSION: floating drug delivery systems have an efficient means of enhancing the bioavailability and controlled delivery of many drugs. Dosage forms with a prolonged GRT will bring about new and important therapeutic options The currently available polymer-mediated Non effervescent and effervescent FDDS, designed on the basis of delayed gastric emptying and buoyancy principles, appear to be a very much effective approach to the modulation of controlled oral drug delivery. 26
  27. 27. REFERENCE • Controlled drug delivery system concept and advance ,by S.R.VYAS,196-215 • International Journal of Pharmaceutical Research & Allied Sciences, Volume 1, issue 4 (2012),20-28 • Journal of Current Pharmaceutical Research 2011 ;7 (1): 6-20 • Pharmacophore International Research Journal 2013, Vol. 4 (1), 26-38
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