Formulation and In vitro Evaluation of Floating Microspheres of Misoprostol

DOI:

https://doi.org/10.37285/ijpsn.2017.10.1.6

Authors

  • K Vanitha
  • M. Mohan Varma
  • Ramesh Alluri

Abstract

Misoprostol is a synthetic prostaglandin PGE1 analogue, which has proved to be an effective anti-secretory agent for oral use. The major indications of Misoprostol are in the prevention and treatment of NSAID-induced gastric and duodenal ulcers. Its half-life is 20-40 minutes. More than one third of patients with ulcers are resistant to H2 antagonists. So, these patients can be healed on Misoprostol. The objective of the present study was to formulate gastroretentive floating drug delivery system of an antiulcer drug Misoprostol. Floating microspheres of Misoprostol were prepared by an emulsification solvent evaporation technique using hydroxy propyl methyl-cellulose (HPMC K 100M) and ethyl cellulose. The percentage yield and drug entrapment efficiencies of these floating microspheres were within the range between: 70 ± 2.8 to 98 ± 2.9 % and 39.27 to 82.39 %, respectively. The determined mean particle size for all the microspheres were 250 ± 7.28 to 400 ± 2.32 µm. The flowability of these microspheres was found good. A high performance liquid chromatography (HPLC) method with ultra-violet (UV) detection was selected for the method of analysis.  The drug release was found to delay for 12 hours with the increasing drug to polymer ratio. The drug release kinetics followed Korsemeyer-Peppas and Higuchi model with anomalous (non-Fickian) diffusion mechanism for the drug release. The FTIR and DSC studies showed that there was an absence of chemical interaction between the drug and the excipients. The in vitro drug release from Misoprostol floating microspheres showed the drug release was dependent on the drug to polymer ratio. The drug release was found delayed with the increasing drug to polymer ratio.

 

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Keywords:

Floating microspheres, emulsion solvent evaporation method, Misoprostol

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Published

2017-01-31

How to Cite

1.
Vanitha K, Varma MM, Alluri R. Formulation and In vitro Evaluation of Floating Microspheres of Misoprostol. Scopus Indexed [Internet]. 2017 Jan. 31 [cited 2024 May 18];10(1):3608-15. Available from: https://www.ijpsnonline.com/index.php/ijpsn/article/view/828

Issue

Vol. 10 No. 1 (2017): January-February 2017

Section

Research Articles
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Scopus
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Europe PMC

References

Al-Suwayeh SA, El-Shaboury MH, Al-Baraki SM, Elgorashy AS, Taha EI (2009). In vitro and in vivo evaluation of sustained release Hydralazine hydrochloride tablets prepared by thermal granulation technique. Australian J Basic ApplSci 3: 2866-2875.
Amrutkar PP, Chaudhari PD and Patil SB (2012). Design and in vitro evaluation of multiparticulate floating drug delivery system of zolpidem tartarate. Colloids Surf B: Biointerf 89: 182-187.
Aulton ME (2002). Pharmaceutics, the Science of Dosage Form Design, 2nd ed., Churchill Livingstone, New York, 289-305
Carr R (1965). Evaluating flow properties of solids. ChemEng 18: 163-168.
Chen J, Blevins WE, Park H, Park K (2000). Gastric retention properties of superporous hydrogel composites. J Control Release 65: 73-82
Clas SD, Dalton CR, Hancock BC (1999).Differential scanning calorimetry: applications in drug development. Pharm Sci Tech Today 2: 311-320.
Collins PW, Rappo R, Dajani EZ (1985). Chemistry and synthetic development of Misoprostol. Dig Dis Sic 30: 114-117.
Dinarvand R, Mirfattahi S, Attyabi F (2002). Preparation, characterization and in vitro evaluation of isosorbiddinitrate microspheres. J Microencapsule 19: 73-81
Durgacharan A. Bhagwat,Mangesh A Bhutkar, Sachin S. Todkar, Shrinivas K. Mohite, Yogesh S. Gattani (2009). Formulation and evaluation of Controlled Release Microspheres of Isosorbidedinitrate. International Journal of PharmTech Research. 1: 125-128
Garg R, Gupta GD (2008). Progress in controlled gastroretentive delivery systems. Trop. J. Pharm. Res 7(3): 1055-1066.
Garg S, Sharma S (2003). Gastroretentive drug delivery systems. Business Briefing: Pharmatech 2: 160-166.
Gladziwa U and Klotz U (1994). Pharmacokinetic optimization of the treatment of peptic ulcer in patients with renal failure. Clin. Pharmacokinet 27: 393-408.
Hwang SJ, Park H and Park K (1998). Gastric Retentive Drug-Delivery Systems. Crit Rev Ther Drug Carrier System 15(3): 243-284.
ICH Guidelines, Stability testing of new drug substances and products, Q1A (R2) Step 4 version, dated 6 February 2003.
Ishak RAH, Awad GAS, Mortada ND, Nour SAK (2007). Preparation, in vitro and in vivoevaluation of stomach specific Metronidazole-loaded alginate beads as local anti-Helicobacter pylori therapy. J Control Release 119: 207-214.
Jhansipriya marabathuni V, Deveswaran R, Bharath S, BasavarajBV (2012). Designand optimization of multi-particulate gastroretentive delivery system of ranitidine hydrochloride, Int J Pharm PharmSci 4: 597-603
Malakar J, Nayak AK, Pal D (2012). Development of cloxacillin loaded multiple-unit alginate-based floating system by emulsion-gelation method. Int J BiolMacromol 50: 138-147.
Marianne Oth, Michel Franz, Jacques Timmermans and Andres Moes (1992). The Bilayer Floating Capsule: A Stomach directed drug delivery system for Misoprostol. Pharmaceutical Research 9: 298-302
Mehta J, Patidar K, Patel V, Kshatri N, Vyas N (2010). Development & validation of an in vitro dissolution with HPLC analysis for Misoprostol in formulated dosage form. Anal Methods 2: 72-75.
Mishra J, Kumar DA (2013). Recent advances in gastro retentive drug delivery system: A review. Mintage journal of Pharmaceutical & Medical sciences 2: 25-27.
MurtazaG, Ahamad M, Khan SA, Hussain I (2012). Evaluation of cefixime-loadedchitosan microspheres: Analysis of dissolution data using DDSolver. Disso Technol 2: 13-19.
Nayak AK and Malakar J (2010). Formulation and in vitro evaluation of gastroretentivehydrodynamically balanced system for ciprofloxacin HCl. J Pharmacy Educ Res 1: 65-68
Nayak AK, Malakar J (2011). Formulation and in vitro evaluation of hydrodynamically balanced system for Theophylline delivery. J Basic Clin Pharm 2(3): 133-137
Nayak AK, Pal D (2011). Development of pH–sensitive tamarind seed polysaccharide-alginate composite beads for controlled diclofenac sodium delivery using response surface methodology. Int J BiolMacromol. 49: 784-793.
Nellore RV, Rekhia GS, Hussain AS, TillmandLG and Augsburger LL (1998). Development of metoprolol tartrate extended-release matrix tablet formulations for regulatory policy consideration. J Control Rel 50: 247-256.
Pal D, Nayak AK (2011). Development, optimization, and anti-diabetic activity of gliclazide-loaded alginate-methyl cellulose mucoadhesive microcapsules. AAPS Pharm Sci Tech 12: 1431-1441.
Peppas NA (1985). Analysis of Fickian and non Fickian drug releasefrom polymers. Pharm. Acta Health. 60: 110-111.
Rajeev Garg and Gupta GD (2010). Gastroretentive floating microspheres of silymarin: Preparation and in vitro evaluation. Tropical J Pharm Res 9: 59-66.
Rao KR, Senapati P, Das MK (2005). Formulation and in vitro evaluation of ethylcellulose microspheres containing zidovudine. J. Microencapsul 22: 863-876
Shargel L and Andrew YU (1999). Applied biopharmaceutical and Pharmacokinetics. 4th Edition, Prentice- Hall International pp-169-175.
Someshwar K, Chithaluru K, Ramarao T, Kumar KK (2011). Formulation and evaluation of effervescent floating tablets of Tizanidine hydrochloride. Acta Pharm 61: 217-226
Tripathi GK, Singh S, Nath G (2011). Evaluation of pH trigger oil entrapped buoyant beads of acetohexamic acid for eradication of Helicobecter pylori. Int J PharmTech Res 3: 1359-1368.
Vidhyaa Kumari , Vignesh Muruganandham (2012). Formulation, Development & Characterization of Ofloxacin Microspheres. Indo Global Journal of Pharmaceutical Sciences 2(2): 130-141.
YangQ, Owusu-A and babioG (2000). Biodegradable progesterone microspheredelivery systems for osteoporosis therapy. Drug Dev Ind Pharm 26: 61-70.