Bi layer tablet


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Bi layer tablet

  1. 1. 1
  2. 2. INTRODUCTION Bilayer tablets can be a Bilayer primary option to avoid tableting chemical incompatibilities between API by physical separation, and to enable the+ development of different drug release profiles (immediate release with extended release)1. 2
  3. 3. ADVANTAGES Release of both drugs starts immediately Combination of incompatible drugs2Physical/chemical incompatibility can be prevented by physical separation of two drugs. Combination of different release profilesImmediate release and sustained release profile can be achieved in single tablet by forming IR layer and SR layer. Reduced Pill BurdenBy reducing individual dose of two drug due to their additive effect .Example: Salbutamol + Theophylline 3
  4. 4. Reduce the side effects Reduced by using one drug of thecombination for this purpose2.Amiloride may prevent hypokalemia caused byhydrochlorthiazide19, 20Elegance to the product 4
  5. 5. Co-morbid Co-morbid Conditions meansConditions 2 pertaining to a disease or other pathological process that occurs simultaneously with another18. Hypertension Heart Disease Treat different ailments in the same patient (co-morbidity), at the same time Obesity and with one pill Diabetes Example: Combination of β- blocker and ACE Hyperlipidemia inhibitor or Diuretics is beneficial to treat Hypertention and Heart failure. Only Allows for synergistic combination 5
  6. 6.  Drug produces additive/synergistic effectAnti- asthmatic: Salbutamol + Theophylline Drugs having opposite side effects, may reduce the side effectOmeprazole + NSAIDSHydroclorothiazide + Amiloride Incompatible drugs Low biological half life (ideal for modified release bilayer) Unstable at intenstinal pH ( ideal for bilayer floating) High first pass metabolism with low biological half life (ideal for buccoadhesive bilayer) 6
  7. 7. DIFFERENT TYPES Bilayer modified release tabletExample:Aceclofenac9 : NSAIDS, COX-2 inhibitor; t/2 = 3-4 hrsMetoclopramide HCL + Ibuprofen13, 14:Metoclopramide HCL is anti emetic; Given as immediate release dose and Ibuprofen is NSAID; given as SR dose, due to its low t/2 (2 hrs).This is widely used combination in treatment of migraine. It improve the absorbance of Ibuprofen, whose absorption is less due to gastric stasis10 especially in migraine. 7
  8. 8.  Bilayer floating tabletExample:Rosiglitazone maleate6,7,8Oral anti-diabetic; t/2 = 3-4 hrs; its solubility is decreased by increasing pH.Metoprolol Tartrate3,4,5Β1-selective adrenergic blocker; t/2 = 3-4 hrs; it degraded in colonCaptopril11,12ACE inhibitor; 37.5 – 75 mg dose is required in three times; most stable at 1.2 pH. 8
  9. 9.  Bilayer bucoadhesive tabletExample:Propranolol HCLNon-selective β-adrenergic blocker; t/2 = 3-5 hrs; high first pass metabolism.Drug in buccoadhesive layer, Backing layer is consist of Ethyl Cellulose. 9
  10. 10. PRACTICAL PROBLEMS IN DEVELOPING BILAYER TABLETSWhat are Fixed Dose Combinations???15, 16, 17 15, 16, 17Maintenance Dose (A) =(KE × Minimum EffectiveConcentration ×Vd)/1000 (mg/hr)Where, KE = elimination rate constant Vd = volume of distributionA = 0.693 × b ×h / t ½Where, b = Immediate release dose h = time for release t ½ = biological half life 10
  11. 11.  Layer-separation Order of layer sequence Layer weight ratio Elastic mismatch of the adjacent Layers Cross contamination between layers. 11
  12. 12. 1. Patel Mehul, et al; Challenges in the formulation of bilayered tablets: a review. IJPRD; Vol. 2; 2010, 30-42.2. Pharmaceutical Development with Focus on Paediatric formulations. WHO/FIP TRAINING WORKSHOP;28 April 2008 – 2 May 2008.3. Hoffman BB. Catecholamines, sympathomimetics drugs, and adrenergic receptor antagonists. In: Hardman JG, Limbird LE, eds. Goodman and Gilman’s The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill; 2001:255Y256.4. Kendall MJ, Maxwell SR, Sandberg A, Westergren G. Controlled release metoprolol. Clinical pharmacokinetic and therapeutic implications. Clin Pharmacokinet. 1991;21:319Y330.5. Hwang SJ, Park H, Park K. Gastric retentive drug-delivery systems. Crit Rev Ther Drug Carrier Syst. 1998;15:243Y284. 12
  13. 13. 6. J. E. F. Reynolds. Martindale-the extra Pharmacopoeia. Director of the Council of Royal Pharmaceutical Society of Great Britain, 2005, 34: 345.7. G. K. McEvoy. AHFS Drug Information. Authority of the board of the American Society of the Health-System Pharmacists, 2004, 3055-3058.8. M. C. Chapel Sky, K. Thompson-culkin, A. K. Miller, et al. Pharmacokinetics of rosiglitazone in patients with varying degrees of renal insuffi ciency. J. Clin. Pharmacol., 2003, 43: 252-259.9. British Pharmacopoeia 2005 v1983ol-1. P.No:40 & http/www .medindia .net/doctors/drug-information/aceclofenac htm.10. 13
  14. 14. 11. C. Dollery, Therapeutics Drugs, Churchill Livingstone, New York 1999, pp. c38–c43.12. N. H. Anaizi and C. Swenson, Instability of captopril solution, Am. J. Hosp. Pharm. 50 (1993) 486–488.13. B. G. Wells, J. T. DiPiro, T. L. Schwinghammer, and C. W. Hamilton. Pharmacotherapy Handbook, McGraw-Hill, New York, 2006, pp. 535–547.14. Bhavesh Shiyani, Surendra Gattani and Sanjay Surana. Formulation and Evaluation of Bi-layer Tablet of Metoclopramide Hydrochloride and Ibuprofen, AAPS PharmSciTech, Vol. 9, No. 3, September 2008, 818-827.15. Deelip Derle, Omkar Joshi, Ashish Pawar, Jatin Patel, Amol Jagadale; formulation and evaluation of buccoadhesive bi-layer tablet of propranolol hydrochloride. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 1, Issue 1, July- Sep. 2009; 206-212. 14
  15. 15. 16. Gosh R., Modern concept in pharmacology and therapeutics, 24 th edition, Hilton and Co., p 761.17. Chong H. Choe, Selim S. Bouhaouala, Itzhak Brook, Thomas B. Elliott, Gregory B. Knudson. In Vitro development of resistance to Ofloxacin and doxycycline in Bacillus anthracis sterne, Antimicrobial agents and chemotherapy. June 2000; 44(6): 1766.18. Cedillo-Ramírez E, Villafuerte-Robles L, Hernandez-leon A Effect of added Pharmatose DCL11 on the sustained-release of metronidazole from Methocel K4M and Carbopol 971P NF floating matrices, Dev Ind Pharm 2001; 31(4): 200-208.19. effects-of-amiloride.html21. effects-of-hydrochlorothiazide.html 15
  16. 16. THANK YOU 16