IN VIVO EVALUATION OF MISOPROSTOL FLOATING MICROSPHERES

Kondi Vanitha, Mohan Varma, Allure Ramesh

Abstract


Prostaglandin  (PG)  has  been  reported  to  be  an  important protective  and  acid  suppressive  factor  in  the  gastric  mucosa.  The objective  of  the  study  was  to  develop  and  evaluate  a  stomach specific  drug  delivery  system  for  controlled  release  of  Misoprostal  a PE analogue for gastric ulcer induced NSAIDs. Floating microspheres were  prepared  by  emulsification-solvent  evaporation  method  using ethyl  cellulose  as  a  polymer,  carbopol  as  mucoadhesive  polymer. Ulcers were induced by the oral administration of absolute ethanol (5 mL/kg)  to  24  h  fasted  Wistar  male  rats  (n=8),  weighing  200  g. Sodium  bicarbonate  solution,  misoprostal  solution  and  drug  loaded microspheres were tested. Formulations were administered orally 1h before the administration of ethanol. Prior to the oral administration, rats  were  anesthetized  with  ethylic  ether.  After  2  h  of  ethanol administration,  animals  were  sacrificed;  the  stomachs  were removed,  opened  along  he  greater  curvature  and  examined  for lesion measurements. Ulcer indexes (UI) were calculated. The in vivo evaluation showed that ulcer  index values were 0.61 ± 0.14 for the sodium  bicarbonate  solution,  0.58  ±0.18  for  the  misoprostal  and 0.11  ±  0.06  for  the  misoprostal-loaded  microspheres.  The  KruskalWallis  test  detected  statistical  differences  (p  =0.002)  between  the ulcer  indexes.  The  multiple  analyses  (Student-Newman-Keuls) showed  that  the  misoprostal  loaded  microspheres  presented  a gastric  ulcer  index  statistically  lower  than  that  of  the  sodium bicarbonate  solution  (p  =  0.001)  and  the  misoprostal  solution  (p  = 0.021).  The  percentages  of  ulceration  inhibition  were  31  and  75% after  the  administration  of  misoprostal  solution  and  microspheres, respectively.  In  conclusion,  the  in  vivo  evaluation  showed  that  the microspheres  presented  ulcer  index  lower  than  the  solutions, showing  that  misoprostal-loaded  microspheres  were  efficient  in protecting the stomach against ulcer formation.

Key words: Misoprostal, microspheres, ulcer index,

 


Full Text:

Untitled

References


Collins, P.W., Pappo, R., and Dajani, E.Z., 1985, Chemistry and synthesis of development of misoprostol. Dig Dis.,30,114-7

Karim. A., 1987, Antiulcer prostaglandin Misoprostol: Single and multiple dose pharmacokinetic profile. Prostaglandins., 33, 40-50

Rajeev Garg and Gupta, G.D., 2010, Gastroretentive Floating Microspheres of Silymarin: Preparation and In Vitro Evaluation, Trop. J. Pharm. Res., 9 , 59-66

Raffin, R.P., Colomé, L.M., Guterres, S.S., Pohlmann, A.R., 2006, Preparation, characterization and in vivo anti-ulcer evaluateon of pantoprazole-loaded microparticles. Eur J. Pharm Biopharm., 63,198 - 204.

Raffin, R.P., Colomé, L.M., Guterres, S.S., Pohlmann, A.R., 2007, Gastro-Resistant Microparticles Containing Sodium Pantoprazole: Stabil-ity Studies and In Vivo Anti-Ulcer Activity. The Open Drug

Delivery J., 1, 28-35

Schoenhard. G., Opperman. J., Kohn, F.E., 1985, Metabolism and pharmacokinetic studies of Misoprostol. Dig Dis Sci.,30,126-18

Tang, O.S., Schweer, H., Seyberth, H.W., Lee SW, and Ho. Pc., 2002a, Pharmacokinetic of different routes of administration of Misoprostol. Human Reprod., 17, 332-6

Watkinson. G., and Akbar, F.A., 1987, Misoprostol in peptic ulcer disease. Prostaglandins., 33, 78-92

Wilson, D.E., Quadros, and.,Rajapaksa .T E., 1986, Effect of Misoprostol on gastric acid and mucus secretion in man. Dig Dis Sci., 31,126-9

Zeman, M.,Fong, S.K., Bentowitz, N.L., Banskter. D., and Darney, D.D., 1997, Absorption kinetics of Misoprostol with oral and vaginal absorption Obstet Gynecol., 90, 88-92




DOI: http://dx.doi.org/10.14499/indonesianjpharm23iss2pp99-103

Refbacks

  • There are currently no refbacks.




Copyright (c) 2017 INDONESIAN JOURNAL OF PHARMACY

Creative Commons License
This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License.

Indonesian J Pharm indexed by:

web
analytics View My Stats