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Formulation and Evaluation of Delayed Release Pantoprazole Tablets


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1 Department of Pharmacy, Shri Jagdish Prasad Jhabarmal Tibrewala University, Vidyanagari, Jhunjhunu, Rajasthan, India
     

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Pantoprazole is a proton pump inhibitor, belongs to group of benzimidazole, used for the treatment of gastric and duodenum ulcers. Pantoprazole undergoes degradation in acid medium of the stomach, can be coated with enteric coating polymer that will safely deliver the drug in the small intestine. In this present study an attempt was made to formulate and evaluate pantoprazole as enteric coated tablet. Delayed release tablets of pantoprazole were prepared by wet granulation method using HPMC, Cassava starch and polyvinyl pyrrolidine as polymer, Avicel PH 102 (MCC) as filler and starch as binder. The prepared tablets were evaluated for hardness, weight variation, friability and drug content uniformity and it was found that the results comply with official standards. The prepared tablets were coated using enteric coating polymer such as cellulose acetate phthalate, Eudragit L100 and Drug coat L100 by dip coating method. The in vitro release was studied using pH 1.2 acidic buffer and pH 6.8 phosphate buffer. The in vitro release study revealed that the prepared tablets were able to sustain release drug in to the intestine. The release kinetics studies showed that the release was first order diffusion controlled and then values obtained from the Korsmeyer-Peppas model showed that the release mechanism was super case-II transport. Stability studies indicated that the developed tablets were stable and retained their pharmaceutical properties at room temperature and 40°C / 75% RH for a period of 1 month. The anti-ulcer activity was evaluated by water immersion stress induced ulcer model. The pantoprazole sodium sesquihydrate coated formulations ECF3 at a dose of 10 mg/kg body weight showed a protection index of 100%.

Keywords

Pantoprazole, Delayed Release, HPMC, PVP, Cassava Starch.
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  • Health encyclopedia diseases and conditions. http://www.healthscout.com. (Accessed on 14/11/2009)
  • American academy of family physicians. http://familydoctor. org/online/famdocon/home/common/digestive/disorders/186.html
  • http://www.emedmag.com/html/pre/gic/consults/071503.asp. (Accessed on 01/12/2009)
  • http://en.wikipedia.org/wiki/Peptic_ulcer. (Accessed on 14/11/2009)
  • Snowden FM. Emerging and reemerging diseases: a historical perspective. Immunol October 2008; 225: 9-26.
  • http://www.experiencefestival.com/a/Peptic_ulcer_ Pathophysiology. (Accessed on 14/11/2009)
  • Rowley FA. The Air war in the compressing room, part 1, tablets & capsules magazine. 2005.
  • Gennaro AR. Remington: The science and Practice of Pharmacy. (NY): Lippincott Williams and Wilkins 1990; 2: 1660-62.
  • Chein YW. Novel drug delivery systems. (NY): Marcel Dekker, INC; 2nd ed. New York: 1992; 140.
  • Swarbick J, Boylan JC. Encyclopedia of pharmaceutical technology. (NYand Basel): Marcel Dekker, ING; 1990; (3).
  • Hoffman A. Pharmacodynamics aspects of sustained release preparations. Advance Drug Deliv Rev 1998; 33: 185-99.
  • Ehrlich P. Immunology and cancer research. In collected papers of Paul Ehrlich, London: Pergamon Press; 1902; 442.
  • Lipowski. Australian Patent 109. 1938; 438.
  • Banker GS, Rhodes CT. Modern pharmaceutics. (NY and BASEL): Marcel Deckker, Inc; 3rd ed. 2005; 501-09.
  • http://en.wikipedia.org/wiki/Enteric_coating. (Accessed on 12/11/2009)
  • http://www.peakatp.com/pdf/peak_delivery.pdf. (Accessed on 12/11/2009)
  • Laine L, Peterson WL. Bleeding peptic ulcer. N Eng J Med 1994; 331: 717- 27.
  • Gibinski K. Step by step towards the natural history of peptic ulcer disease. J Clin Gastroenterology 1983; 5: 299-302.
  • Lai KC, Lam SK, Hui WM. Lansoprazole reduces ulcer relapse after eradication of Helicobacter pylori in NSAIDs users. Gastroenterology 2000; 118: 251.
  • Duvnjak M, Supanc V, Troskot B, Kovacevic I, Antic Z, Hrabar D, et al. Comparison of intravenous pantoprazole with intravenous ranitidine in prevention of re-bleeding from gastroduodenal ulcers. Gut 2001; 49(3): 2379.
  • Raffin RP, Colome LM, Schapoval EES, Pohlmann AR, Guterres SS. Increasing sodium pantoprazole photostability by microencapsulation: Effect of the polymer and the preparation technique. Eur J Pharm Biopharm 2008; 3:1014-18.
  • Oliveira HP, Albuquerque JJF, Nogueiras C, Rieumont J. Physical chemistry behavior of enteric polymer in drug release systems. Int J Pharm 2009; 45: 432-39.
  • Harris MS, Javeria T, Hamid AM. Evaluation of drug release kinetics from Ibuprofen matrix tablets using HPMC. Pak J Pharma Sci. 2006; 19(2): 19-24.
  • Cronlein J, Fegely K, Young C. Characterization of Delayed Release Lansoprazole Multiparticulates: Impact of Biorelevant Dissolution Media.5th world meeting on pharmaceutics 2006.
  • Basak SC, Kumar PS, Manavalan R, Narendranath, KA. Preparation and evaluation of enteric coated pancreatin tablets. Ind J Pharm Sci 2002; 64: 260- 64.
  • Turkoglu M, Varol H, Celikok M. Tableting and stability evaluation of enteric coated omeprazole pellets. Eur J Pharm and Biopharm 2004; 57: 279- 86.
  • Pandey VP, Phanindrudu A, Manavalan R, Livingston J. In vitro study on capsule formulations of omeprazole containing enteric coated granules. Boll Chim Farm 2002; 141: 419-22.
  • Raffin RP, Pohlmann AR, Guterres SS. Preparation, characterization, and in vivo anti-ulcer evaluation of pantoprazole-loaded microparticles. Eur J Pharm and Biopharm 2006; 63: 198-204.
  • Brunner G, Harke U. Long-term therapy with pantoprazole in patients with peptic ulceration resistant to extended high-dose ranitidine treatment. Aliment Pharmacol Ther 1994; 8(1): 59-64.
  • Comoglu T, Gonul N, Dogan A, Basci N. Development and In vitro evaluation of pantoprazole-loaded microspheres. Drug delivery 2008; 15: 295-302.
  • Colome LM, Haas SE, Jornada DS. Development of HPMC and Eudragit S100 blended microparticles containing sodium pantoprazole. Pharmazie 2007; 62: 361-64.
  • Matsuo M, Arimori K, Nakamura C. Delayed release tablets using hydroxyl ethyl cellulose as a gel forming matrix. Int J Pharm 1996; 138: 225-33.
  • Hua D, George R, Scott V, Ali R. In-vitro dissolution testing of delayed release multi-particulate systems. Controlled release society annual meeting July 2008.
  • Fan LF, Du Q, Xiang B, Li CL, Bai M, Chang YZ, Cao DY. Design and in vitro/in vivo evaluation of multi-layer film coated pellets for omeprazole. Int J Pharm 1996; 18: 25-33.
  • Ravi KP, Prakash B, Murali KM, Santha YM, Asha DC. Simultaneous Estimation of domperidone and pantoprazole in solid dosage form by UV spectrophotometry, July 2006; 3(12): 142-145.
  • Saini V. Antiulcer activity of pantoprazole from multiple-unit tablet dosage form. Int J PharmTech Res Oct-Dec 2009; 1(4): 1092-1093.
  • Mahesh DC, Paras J, Sachin C, Rajesh S, Pradeep RV. Novel sustained release, swellable and bioadhesive gastroretentive drug delivery system for ofloxacin. Int J Pharma January 2006; 316: 86-92.
  • Reddy KR, Mutalik S, Reddy S. Once-daily sustained release matrix tablets of nicorandil Formulation and in vitro evaluation. AAPS Pharmsci Tech 2003; 4: E61.
  • Pantoprazole sodium sesquihydrate available at: http:// www Rx list.com. (Accessed on 24/11/2009)
  • Indian Pharmacopoeia. Delhi: The controller of publications. 1996; (1).
  • British Pharmacopoeia. London: The stationary office. 2003; (1).
  • Wade A, Weller P. Handbook of pharmaceutical excipients. London: Pharmaceutical press 1994; 4: 151-52.
  • Cooper J, Gunn C. Powder flow and compaction. IN: Carter SJ, eds. Tutorial pharmacy, New Delhi: CBS publishers and distributors; 1986; 211-33.
  • Lachman L, Liberman HA, Nicholas Gl. Sustained release dosage forms, in; 2nd ed, Varghese publishing house, Mumbai, 1987; 439-40.
  • Levin M. Changing Tabletting Machines in Scale-Up and Production: Ramifications for SUPAC Background Notes for FDA CDER DPQR Seminar April 3, 2000.
  • Vueba ML, Carvalho LB, Veiga F, Sousa JJ, Pina ME. Influence of cellulose ether polymers on ketoprofen release from hydrophilic matrix tablets. Eur J Pharm and Biopharm 2004; 58: 51-59.
  • Bonin EA, Campos AC, Coelho JC, Matias JE, Malafaia O, Jonasson TH. Effect of Pantoprazole Administered Subcutaneously on the Healing of Sutured Gastric Incisions in Rats. Eur Surg Res 2005; 37: 250-256.
  • Malairajan P, Gopalkrishnan G, Narasimhan S, Jessi KV. Evaluation of anti ulcer activity of polyalthia longifolia (sonn.) thwaites in experimental animals. Ind J Pharmacol 2008; 40(3):125-128.
  • Alderman DA. A review of cellulose ethers in hydrophillic matrices for the oral controlled release dosage froms. Tech Prod Mfr 1984; 5: 1-9.
  • Carstensen JT. Pharmaceutics of solids and solid dosage forms. New York: John Wiley and Sons; 1977; 100.
  • Mockel JE, Lippold BC. Zero-order drug release from hydrocolloid matrices. Pharm Res 1993; 10: 1066-70.
  • Swarbrick J. Advances in controlled drug delivery. STP Pharma 1996; 6: 53-56.

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  • Formulation and Evaluation of Delayed Release Pantoprazole Tablets

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Authors

Viral Patel
Department of Pharmacy, Shri Jagdish Prasad Jhabarmal Tibrewala University, Vidyanagari, Jhunjhunu, Rajasthan, India

Abstract


Pantoprazole is a proton pump inhibitor, belongs to group of benzimidazole, used for the treatment of gastric and duodenum ulcers. Pantoprazole undergoes degradation in acid medium of the stomach, can be coated with enteric coating polymer that will safely deliver the drug in the small intestine. In this present study an attempt was made to formulate and evaluate pantoprazole as enteric coated tablet. Delayed release tablets of pantoprazole were prepared by wet granulation method using HPMC, Cassava starch and polyvinyl pyrrolidine as polymer, Avicel PH 102 (MCC) as filler and starch as binder. The prepared tablets were evaluated for hardness, weight variation, friability and drug content uniformity and it was found that the results comply with official standards. The prepared tablets were coated using enteric coating polymer such as cellulose acetate phthalate, Eudragit L100 and Drug coat L100 by dip coating method. The in vitro release was studied using pH 1.2 acidic buffer and pH 6.8 phosphate buffer. The in vitro release study revealed that the prepared tablets were able to sustain release drug in to the intestine. The release kinetics studies showed that the release was first order diffusion controlled and then values obtained from the Korsmeyer-Peppas model showed that the release mechanism was super case-II transport. Stability studies indicated that the developed tablets were stable and retained their pharmaceutical properties at room temperature and 40°C / 75% RH for a period of 1 month. The anti-ulcer activity was evaluated by water immersion stress induced ulcer model. The pantoprazole sodium sesquihydrate coated formulations ECF3 at a dose of 10 mg/kg body weight showed a protection index of 100%.

Keywords


Pantoprazole, Delayed Release, HPMC, PVP, Cassava Starch.

References