FORMULATION DEVELOPMENT AND CHARACTERIZATION OF GASTRORETENTIVE DRUG DELIVERY SYSTEMS OF LORATADINE
DOI:
https://doi.org/10.22159/ijap.2019v11i6.35194Keywords:
Buoyant, Non-effervescent, Low-density lipids, Direct compressionAbstract
Objective: The main objective of the research work is to develop a single unit non-effervescent drug delivery system of Loratadine (LTD) by direct compression process to prolong the gastric residence time (GRT).
Methods: LTD non-effervescent tablets were prepared with different polymers like hydroxypropyl methylcellulose (HPMC) K15M, HPMC K100M (i.e.: 1:1, 1:2, 1:3) as release retardants. Glyceryl behenate (Compritol 888 ATO) and Glyceryl palmitostearate (Precirol ATO 5) were used (1:1, 1:2, 1:3) as low-density lipids to impart buoyancy for longer period.
Results: The drug (LTD) and excipient (i.e. HPMC, low-density lipid aids, etc.,) interaction studies were carried out by Fourier Transform Infrared Spectroscopy (FTIR) and there was no likely interaction involving them. The developed LTD floating matrix tablets were characterized by pre and post-compression parameters and all results were, found within the pharmacopoeial limits. The cumulative percentage of drug release ranges from 56.87±0.25 % (F12) to 99.87±0.09 % (F2). The drug release profiles of the all formulations (F1 to F12) were subjected to various pharmacokinetic parameters and the optimized formulation (F3) followed the Korsmeyer Peppas (R2=0.996) model with non-Fickian diffusion (n>0.5). The obtained data by radiographic images of F3 formulation showed the GRT is 6±0.5 h (n=3).
Conclusion: Hence, from all evaluation studies, it was evident that F3 formulation was optimized (99.82±1.63 % drug release in 12 h).
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References
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35. Dudhipala N, Narala A, Janga KY, Bomma R. Amoxycillin trihydrate floating-bioadhesive drug delivery system for eradication of helicobacter pylori: preparation, in vitro and ex vivo evaluation. J Bioequivalence Bioavailability 2016;8:118-24.
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37. Pandala S, Bakshi V, Jadi RK. Formulation development and in vitro characterization of zolmitriptan controlled release drug delivery systems. INNOSC Theranostics Pharmacol Sci 2019;2:6-11.
38. Reddy RA, Ramesh B, Kishan V. Drug excipient interaction during formulation development, in vitro and in vivo evaluation of gastroretentive drug delivery system for nizatidine. Int J Pharm Sci Nanotech 2013;6:2281-93.
39. Bomma R, Veerabrahma K. Statistical optimization of floating-bioadhesive drug delivery system for risedronate sodium: in vitro, ex vivo and in vivo evaluation. Int J Drug Delivery 2014;6:36-49.
40. Parmar K, Patel J, Sheth N. Self nano-emulsifying drug delivery system for embelin: design, characterization and in vitro studies. Asian J Pharma Sci 2015;10:396-404.
41. Bera H, Boddupalli S, Nandikonda S, Kumar S, Nayak AK. Alginate gel-coated oil-entrapped alginate-tamarind gum-magnesium stearate buoyant beads of risperidone. Int J Biol Macromol 2015;78:102-11.
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43. Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm 2010;67:217-3.
44. Singhvi G, Singh M. In vitro drug release characterization models. Int J Pharm Stud Res 2011;2:77-84.
45. Costa P, Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharma Sci 2001;13:123-33.
46. Lopes CM, Bettencourt C, Rossi A, Buttini F, Barata P. Overview on gastroretentive drug delivery systems for improving drug bioavailability. Int J Pharm 2016;510:144-58.
47. Bera H, Boddupalli S, Nandikonda S, Kumar S, Nayak AK. Alginate gel-coated oil-entrapped alginate-tamarind gum-magnesium stearate buoyant beads of risperidone. Int J Biol Macromol 2015;78:102-11.
48. Satishbabu BK, Sandeep VR, Ravi RB, Shrutinag R. Formulation and evaluation of floating drug delivery system of famotidine. Ind J Pharm Sci 2010;72:738–44.
49. Adel S, ElKasabgy NA. Design of innovated lipid-based floating beads loaded with an antispasmodic drug: in vitro and in vivo evaluation. J Liposome Res 2014;24:136-49.
50. Jadi RK, Bomma R, Sellappan V. Development of a new single unit dosage form of propranolol HCl extended-release non-effervescent floating matrix tablets: in vitro and in vivo evaluation. J Appl Pharm Sci 2016;6:112-8.
2. Shah R, Patel S, Patel H, Pandey S, Shah S, Shah D. Formulation development of carvedilol compression coated tablet. Int J Pharm Pharma Sci 2013;18:906-15.
3. Nachaegari SK, Bansal AK. Co-processed excipients for solid dosage forms. Pharm Technol 2004;28:52-65.
4. York P. Solid-state properties of powders in the formulation and processing of solid dosage forms. Int J Pharma 1983;14:1-28.
5. Badawy SI, Hussain MA. Microenvironmental pH modulation in solid dosage forms. J Pharm Sci 2007;96:948-59.
6. Davies P. Oral solid dosage forms. Mark G. editor. In: Pharmaceutical pre-formulation and formulation, 2nd ed. New York; CRC Press; 2015. p. 367-430.
7. Jadi RK, Chinnala KM. A comprehensive review on gastroretentive drug delivery systems. Ind Am J Pharm Sci 2016;3:115-28.
8. Dixit N, Maurya SD, Sagar BP. Sustained release drug delivery system. Ind J Res Pharm Biotech 2013;1:305-10.
9. Prinderre P, Sauzet C, Fuxen C. Advances in gastro retentive drug-delivery systems. Expert Opin Drug Delivery 2011;8:1189-203.
10. Mandal UK, Chatterjee B, Senjoti FG. Gastro retentive drug delivery systems and their in vivo success: a recent update. Asian J Pharma Sci 2016;11:575-84.
11. Nokhodchi A, Raja S, Patel P, Asare Addo K. The role of oral controlled release matrix tablets in drug delivery systems. Bio-Impacts 2012;2:175-87.
12. Dhiman S, Singh TG, Rehni AK, Sood S, Arora S. Gastroretentive: a controlled release drug delivery system. Asian J Pharm Clin Res 2011;4 Suppl 1:5-13.
13. Harshad P, Omkar L. Formulation and evaluation of bilayer tablet containing diclofenac sodium as a sustained release and aloe vera gel powder as immediate release. Int J Curr Pharm Res 2019;11:70-8.
14. Shivshankar RM. Advances of hydrazone linkers in polymeric drug delivery. J Crit Rev 2019;6:1-4.
15. Tanner T, Marks R. Delivering drugs by the transdermal route: review and comment. Skin Res Technol 2008;14:249-60.
16. Willingham E, Agras K, Vilela M, Baskin LS. Loratadine exerts estrogen-like effects and disrupts penile development in the mouse. J Urol 2006;175:723-6.
17. Simons FE. Advances in H1-antihistamines. New Eng J Med 2004;351:2203-17.
18. Baena Cagnani CE. Safety and tolerability of treatments for allergic rhinitis in children. Drug Safety 2004;27:883-98.
19. Kumria R, Nair AB, Al-Dhubiab BE. Loratidine buccal films for allergic rhinitis: development and evaluation. Drug Dev Ind Pharm 2014;40:625-31.
20. Bernstein IL, Bernstein DI. The efficacy and safety of loratadine in the management of chronic idiopathic urticaria. J Allergy Clin Imm 1988;81:211.
21. Kirshner JJ, Heckler CE, Tiffany S, Reichel C, McAuliffe C, Morrow GR. A phase II study of loratidine (L) to prevent pegfilgrastim-induced pain (PIP). J Clin Oncol 2011;29 Suppl 15:e19704.
22. Siraj S, Khurshid M, Nazim S. Various perspectives of gastroretentive drug delivery system: a review. Am J Adv Drug Delivery 2013;1:443-51.
23. Mishra S, Pathak K. Formulation and evaluation of oil entrapped gastroretentive floating gel beads of loratadine. Act Pharma 2008;58:187-97.
24. Sharma AR, Khan A. Gastroretentive drug delivery system: an approach to enhance gastric retention for prolonged drug release. Int J Pharma Sci Res 2014;5:1095-106.
25. Radhakrishnan P, Singh SK, Verma PR. Pharmaceutical formulations to increase gastric residence time: concepts and strategies. Drug Delivery Lett 2017;7:190-200.
26. Jadi RK, Tatikonda A, Reedy PR, Venisetty RK. Design and characterization of pregabalin swellable core osmotic pumps. Int J Pharm Res Allied Sci 2016;5:8-15.
27. Togaru V, Venisetty RK, Bakshi V, Jadi RK. Formulation development and in vitro evaluation of propranolol hydrochloride extended-release matrix tablets. Emergent Life Sci Res 2017;3:38-47.
28. Roy H, Parida KR, Nandi S, Panda SK, Mohapatra DK. Design of fast dissolving amlodipine besylate tablet formulations. Asian J Pharm 2014;6:51-9.
29. El Ragehy NA, Badawey AM, Khateeb SE. Stability indicating methods for the determination of loratadine in the presence of its degradation product. J Pharm Biomed Anal 2002;28:1041-53.
30. Hilbert J, Radwanski E, Weglein R, Luc V, Perentesis G, Symchowicz S, et al. Pharmacokinetics and dose proportionality of loratadine. J Clin Pharm 1987;27:694-8.
31. Yeleken G, Kot?owska H, Sznitowska M, Golenia E, Ustenova G. Development of direct compressed loratadine minitablets. J Pharma Sci Res 2017;9:401-6.
32. Kumar AD, Rani JM, Sudhakarbabu AM, Rao VP. Formulation optimization and evaluation of loratadine gastroretentive tablets. Int J Bio Pharma Res 2013;4:1190-5.
33. Bomma R, Naidu RS, Yamsani M, Veerabrahma K. Development and evaluation of gastroretentive norfloxacin floating tablets. Acta Pharm 2009;59:211-21.
34. Guguloth M, Bomma R, Veerabrahma K. Development of sustained-release floating drug delivery. J Pharm Sci Technol 2011;65:198-206.
35. Dudhipala N, Narala A, Janga KY, Bomma R. Amoxycillin trihydrate floating-bioadhesive drug delivery system for eradication of helicobacter pylori: preparation, in vitro and ex vivo evaluation. J Bioequivalence Bioavailability 2016;8:118-24.
36. Prasad RR, Kumar JR, Vasudha BA, Chettupalli AK. Formulation development and evaluation of allopurinol solid dispersions by solvent evaporation technique. Int J Appl Pharm 2018;10:168-71.
37. Pandala S, Bakshi V, Jadi RK. Formulation development and in vitro characterization of zolmitriptan controlled release drug delivery systems. INNOSC Theranostics Pharmacol Sci 2019;2:6-11.
38. Reddy RA, Ramesh B, Kishan V. Drug excipient interaction during formulation development, in vitro and in vivo evaluation of gastroretentive drug delivery system for nizatidine. Int J Pharm Sci Nanotech 2013;6:2281-93.
39. Bomma R, Veerabrahma K. Statistical optimization of floating-bioadhesive drug delivery system for risedronate sodium: in vitro, ex vivo and in vivo evaluation. Int J Drug Delivery 2014;6:36-49.
40. Parmar K, Patel J, Sheth N. Self nano-emulsifying drug delivery system for embelin: design, characterization and in vitro studies. Asian J Pharma Sci 2015;10:396-404.
41. Bera H, Boddupalli S, Nandikonda S, Kumar S, Nayak AK. Alginate gel-coated oil-entrapped alginate-tamarind gum-magnesium stearate buoyant beads of risperidone. Int J Biol Macromol 2015;78:102-11.
42. Van Lenthe E, Ehlers A, Baerends EJ. Geometry optimizations in the zero-order regular approximation for relativistic effects. J Chem Phys 1999;110:8943-53.
43. Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm 2010;67:217-3.
44. Singhvi G, Singh M. In vitro drug release characterization models. Int J Pharm Stud Res 2011;2:77-84.
45. Costa P, Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharma Sci 2001;13:123-33.
46. Lopes CM, Bettencourt C, Rossi A, Buttini F, Barata P. Overview on gastroretentive drug delivery systems for improving drug bioavailability. Int J Pharm 2016;510:144-58.
47. Bera H, Boddupalli S, Nandikonda S, Kumar S, Nayak AK. Alginate gel-coated oil-entrapped alginate-tamarind gum-magnesium stearate buoyant beads of risperidone. Int J Biol Macromol 2015;78:102-11.
48. Satishbabu BK, Sandeep VR, Ravi RB, Shrutinag R. Formulation and evaluation of floating drug delivery system of famotidine. Ind J Pharm Sci 2010;72:738–44.
49. Adel S, ElKasabgy NA. Design of innovated lipid-based floating beads loaded with an antispasmodic drug: in vitro and in vivo evaluation. J Liposome Res 2014;24:136-49.
50. Jadi RK, Bomma R, Sellappan V. Development of a new single unit dosage form of propranolol HCl extended-release non-effervescent floating matrix tablets: in vitro and in vivo evaluation. J Appl Pharm Sci 2016;6:112-8.
Published
07-11-2019
How to Cite
SAPAVATU, S. N., & JADI, R. K. (2019). FORMULATION DEVELOPMENT AND CHARACTERIZATION OF GASTRORETENTIVE DRUG DELIVERY SYSTEMS OF LORATADINE. International Journal of Applied Pharmaceutics, 11(6), 91–99. https://doi.org/10.22159/ijap.2019v11i6.35194
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