floating tablets enalapril maleate


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floating tablets enalapril maleate

  2. 2. OBJECTIVE The aim of the present study was to develop a gastro retentive drug delivery system containing Enalapril maleate. The preparation of floating matrix tablets of Enalapril maleate by incorporating low density polymer Hydroxy propyl methyl cellulose K15 and K50.The tablets were prepared by wet granulation method of Enalapril maleate, polymers, and other excipients are mixed and then compressed on a punching machine..The floating matrix tablets were evaluated for uniformity weight, hardness, friability, drug content, and dissolution studies , analytical studies.
  3. 3. INTRODUCTION Floating drug delivery system is also called the hydro dynamically balanced system (HBS). Floating drug delivery systems (FDDS) have a bulk density less than gastric fluids and so remain buoyant in the stomach without affecting gastric emptying rate for a prolonged period of time. While the system is floating on the gastric contents, the drug is released slowly at the desired rate from the system. After release of drug, the residual system is emptied from the stomach. This results in an increased GRT and a better control of the fluctuations in plasma drug concentration. Floating drug delivery system divided into: 1. Non-effervescent systems a. Colloidal gel barrier systems b. Bi-layer floating tablets c. Micro porous compartment systems
  4. 4. d. e. 2. a. b. Multi particulate system Micro balloons / Hollow Microspheres Effervescent systems Volatile liquid containing systems Gas generating systems APPLICATION OF FLOATING DRUG SYSTEM: 1. Enhanced Bioavailability 2. Sustained drug delivery 3. Site specific drug delivery systems 4. Absorption enhancement 5. Minimized adverse activity at the colon 6. Reduced fluctuations of drug concentration DELIEVERY
  5. 5. ADVANTAGES OF FLOATING DRUG DELIVERY SYSTEMS: 1. Remains in the solution for prolonged time even at the alkaline pH of the intestine. 2. Advantageous for drugs meant for local action in the stomach e.g.: Antacids 3. Useful for the administration of aspirin and other similar drugs. 4. Minimizing the mucosal irritation due to drugs, by drug releasing slowly at controlled rate. 5. Ease of administration and better patient compliance. DISADVANTAGES OF FLOATING DRUG DELIVERY SYSTEMS: 1. Not feasible for those drugs that have solubility or stability problems in gastric fluids. 2. The presence of food to delay their gastric emptying. 3. Drugs that cause irritation and lesion to gastric mucosa are not suitable to be formulated as floating drug delivery systems.
  6. 6. PAST WORK ON IMMEDIATE RELEASE TABLETS Drug technique conclusion reference Ketoprofen emulsion solvent diffusion technique drug retained in the micro particles decreased with increase in ERL content Karnel et al (2001) Ranitidine hydrochloride Direct compression addition of citric acid causes an enhancement in drug release Dave et al (2004) Clarithromycin wet granulation tablet composition and mechanical strength on the floating properties and drug release were improved Patel et al (2006) famotidine effervescent technique effervescent-based floating drug delivery was a promising approach to achieve in vitro buoyancy Jaimini et al (2007) Captopril wet granulation technique Incorporation of hydrophobic polymer EC in granulation fluid showed good drug release pattern. Patel et al (2008) Atorvastatin calcium melt granulation technique. it released the drug in a controlled manner Kumar et al (2008) trinetazidine dihydrochloride dry coating technique dry coated floating duration with extended release of drug over a prolonged period of time. Abdelbary et al (2010)
  7. 7. WET GRANULATION Material issuance & receiving Compression Weighing Lubrication & mixing Sieving Dry screening Dry mixing Drying Preparation of granulating fluid Screening of damp mass Granulation
  8. 8. PHYSICO-CHEMICAL CHARACTERIZATION METHODS PREFORMULATION STUDIES COMPATIBILITY STUDIES WITH EXCIPEINTS POSTFORMULATION STUDIES Organoleptic properties Bulk density Shape of Tablets Melting Point Determination Tapped density Tablet Dimensions HPLC Solubility test Angle of Repose Hardness Dissolution test Carr’s Index Hausner ratio Friability test FTIR Tablet Density DSC Buoyancy / Floating Test Weight Variation Test U.V Spectrophotom etric Studies
  9. 9. COMPOSITION OF ENALAPRIL MALEATE FLOATING TABLETS Ingredient F1(mg) F2(mg) F3(mg) F4(mg) 5 5 5 5 HPMC 15 100 80 - - HPMC 50 - - 100 80 Guar gum 50 50 50 50 Sodium bicarbonate 20 40 20 40 Citric acid 10 10 10 10 PVP 5 5 5 5 Magnesium stearate 5 5 5 5 Talc 5 5 5 5 Total 200 200 200 200 Enalapril maleate
  10. 10. RESULT ANALYSIS 1. Organoleptic properties: PROPERTY OBSERVATION Colour White off-white yellowish crystalline powder Odour Odourless Taste Characteristic 2. Melting Point Determination: 143-144.5 ºc 3. Solubility : Sparingly soluble in water; freely soluble in methanol; practically insoluble in methylene chloride. It dissolves in dilute solutions of alkali hydroxides. 4. Calibration curve: R2 value 0.9994 5. Preformulation studies: a. Bulk density: 0.64167 gm/ml b. Tapped density: 0.72-0.79 gm/ml c. Carr’s index: 9-22. d. Angle of repose: 22-30 e. Hausner ratio: 1.16-1.17
  11. 11. 6. a. b. c. d. e. Postformulation studies: Hardness: 2.0-4.0 (kg/cm²) Thickness test: 5.1-5.6 mm Friability test: below 1.0% Weight variation: 10.5-11.7% Buoyancy / Floating Test: Lag time were calculated less than 1 min and floating time maximum 10 hours. 7. Compatibility studies: a. Fourier Transform Infra-Red Spectroscopy (FTIR): indicating the absence of any chemical interaction between Enalapril maleate and Polymers. b. Differential Scanning Calorimetry (DSC): The DSC analysis of pure ENM showed a sharp endothermic peak at 152.55 C.
  12. 12. CONCLUSION From the results and inference we can certainly say that floating type gastro retentive drug delivery system holds a lot of potential for drug having limited oral bioavailability due to having a narrow absorption window in the upper part of small intestine. Enalapril maleate is very sensitive drug and having stability problems. We can certainly explore this drug delivery which may lead to improved bioavailability and ensured therapy with many existing drugs. It is the responsibility of future scientists working in this area to effectively use the potential of this drug delivery system for the benefit of mankind.