FORMULATION AND EVALUATION OF ACARBOSE PELLETS BY EXTRUSION SPHERONIZATION TECHNIQUE
Objective: The objective of our work is to formulate and evaluate acarbose pellets for sustain drug delivery. The present study was aimed to develop sustain drug delivery system of acarbose pellets by extrusion spheronization technique using different polymers like Hydroxypropyl methyl cellulose, chitosan, ethylcellulose, microcrystalline cellulose. Pelletization of acarbose was done to achieve sustain drug release profile suitable for oral administration.
Methods: The acarbose pellets were prepared by extrusion spheronization technique. The Fourier transform-infrared spectrum (FT-IR) and Differential scanning calorimetry thermogram of pure drug and drug-polymer blend showed the stable character of acarbose in the pellets. The prepared pellets were evaluated for different quality control parameters like particle size analysis, drug content, and Drug release characteristics.
Results: The results obtained from different quality control parameters are within acceptable range and In vitro dissolution studies indicated that drug release from pellets follows zero-order kinetics with sustain release drug release up to 12 h with the use of ethyl cellulose as a sustain release polymer and mechanism of drug release is non-fickian. The formulated pellets were stable with respect to their physicochemical characters and drug content over a period of 60 d at accelerated stability condition.
Conclusion: From present study, it was concluded that formulation of acarbose pellets by this will be a promising technique for the preparation of pellets to sustain drug release for the treatment of diabetes with better patient compliance.
2. D'Orazio AM, Martorana G, Filippi N. Spiro fused bicyclic derivatives of deoxynojirimycin: synthesis and preliminary biological evaluation. Chem Select 2016;35:2444–7.
3. Canadian Diabetes Association Clinical Practice Guidelines Expert Committee. Canadian Diabetes Association 2008 clinical practice guidelines for the prevention and management of diabetes in Canada. Can J Diabetes 2008;32:1-21.
4. Hillary K, Ronald EA, William HH. Global burden of diabetes prevalence numerical estimates and projections. Diabetic Care 1998;21:141-3.
5. Siddique S, Khanam J, Bigoniya P. Development of sustained release capsules containing ‘‘coated matrix granules of metoprolol tartrate. Pharm Sci Tech 2010;11:1306–14.
6. Nasiri MI. Formulation development and characterization of highly water soluble drug-loaded extended-release pellets prepared by extrusion–spheronization technique. J Coat Tech Res 2019;16:1351–65.
7. Wen C, Lin X, Dong M. An evaluation of 1-deoxynojirimycin oral administration in silkworm through fat body metabolomics based on 1H nuclear magnetic resonance. Bio Med Res Int 2016;45:1–7.
8. Ya'kobovitz MK, Butters TD, Cohen E. Inhibition of ?-glucosidase activity by N deoxynojirimycin analogs in several insect phloem sap feeders. Insect Sci 2016;23:59–67.
9. Segale P, Mannina L, Giovannelli. Formulation and coating of alginate and alginate-hydroxypropylcellulose pellets containing ranolazine. J Pharm Sci 2016;105:3351–8.
10. Jawahar N, Anilbhai HP. Multi-unit particulate system: a novel pellets for oral dosage form. J Pharm Sci Res 2012;4:1915-23.
11. Sibanc R, Kitak T, Govedarica B, Srcic S, Dreu R. Physical properties of pharmaceutical pellets. Chem Eng Sci 2013;86:50–60.
12. Mannina PL, Segale L, Giovannelli. Self-emulsifying excipient platform for improving technological properties of alginate-hydroxypropyl cellulose pellets. Int J Pharm 2016;499:74–80.
13. Barakat NS, Elbagory IM, Almurshedi AS. Controlled release carbamazepine matrix granules and tablets comprising lipophilic and hydrophilic components. J Drug Delivery 2009; 16:57–65.
14. Kiortsis S, Kachrimanis K, Broussali T, Malamataris S. Drug release from tableted wet granulations comprising cellulosic (HPMC or HPC) and hydrophobic component. Eur J Pharm Biopharm 2005;59:73–83.
15. Kuksal A, Tiwary AK, Jain NK, Jain S. Formulation and in vitro, in vivo evaluation of extended-release matrix tablet of zidovudine: influence of the combination of hydrophilic and hydrophobic matrix formers. Pharm Sci Tech 2009;7:1–9.
16. Borgquist P, Zackrisson G, Nilsson B, Axelsson A. Simulation and parametric study of a film-coated controlled-release pharmaceutical. J Controlled Release 2002;80:229–45.
17. Dashevsky A, Kolter K, Bodmeier R. pH-independent release of a basic drug from pellets coated with the extended-release polymer dispersion kollicoat SR 30 D and the enteric polymer dispersion kollicoat MAE 30 DP. Eur J Pharm Biopharm 2004;58:45–9.
18. Narendra C, Srinath M, Babu G. Optimization of bilayer floating tablet containing metoprolol tartrate as a model drug for gastric retention. Pharm Sci Tech 2006;7:23–9.
19. Siddique S, Khanam J, Bigoniya P. Development of sustained release capsules containing coated matrix granules of metoprolol tartrate. Pharm Sci Tech 2010;11:1306–14.
20. Sonawane RO, Patil SD. Fabrication and statistical optimization of starch-?-carrageenan cross-linked hydrogel composite for extended release pellets of zaltoprofen. Int J Bio Macromol 2018;18:5-45.
21. Sonawane RO, Patil SD. Gelatin–?-carrageenan polyelectrolyte complex hydrogel compositions for the design and development of extended-release pellets. Int J Mater Poly Bio 2016;66:812–23.
22. Arora S, Sharma R, Khatkar A, Singh N, Gagoria J. Development characterization and solubility Study of solid dispersion of cefpodoxime proxetil by solvent evaporation method. Int J Chem Tech Res 2010;2:1275-80.
23. Gawale D, Sonawane RO, Pandey VV. Formulation and in vitro characterization of multiple unit sustained release matrix pellets of lornoxicam using natural gums. Ind J Novel Drug Del 2013;5:208-20.
24. Shah HA, Patel RP. Statistical modeling of zaltoprofen loaded biopolymeric nanoparticles: characterization and anti-inflammatory activity of nanoparticles loaded gel. Int J Pharm Invest 2015;5:20-7.
25. Chhipa P, Pethe AM, Upadhyay S, Tekade A. Formulation optimization of sustained-release pellets of itopride hydrochloride using different polymers. J Pharm Res 2009;2: 1404–8.
26. Pahwa R, Chhabra L, Lamba AK, Jindal S, Rathour A. Formulation invitro evaluation of effervescent floating tablets of an antiulcer agent. J Chem Pharm Res 2012;4:1066-73.
27. Khan GM. Controlled release oral dosage forms: some recent advances in matrix type drug delivery systems. J Med Sci 2001;1:350-4.
28. Morkhade DM. Gum copal and gum dammar: novel matrix-forming material for sustained drug delivery. Ind J Pharm Sci 2006;68:53-8.
29. Shiva Kumar HG, Yadav KS, Satish CS. Preparation and evaluation of chitosan–polyacrylic acid hydrogel as stomach specific delivery for amoxicillin and metronidazole. Ind J Pharm Sci 2007;69:91-5.
30. Singh BN. Modified release solid formulations for colonic delivery. Recent Drug Delivery 2007;1:53–63.
This work is licensed under a Creative Commons Attribution 4.0 International License.