QUICK/SLOW BIPHASIC RELEASE OF A POORLY WATER SOLUBLE ANTIDIABETIC DRUG FROM BI-LAYER TABLETS

  • Kaushik Mukherjee Jadavpur University
  • Subrata Chakraborty Dr Meghnad Saha Sarani, Bidhan nagar
  • Biswanath Sa. Jadavpur University

Abstract

Objective: The objective of the present work is to develop a bi-layer tablet consisting of an Immediate Pulse Release [IPR] layer and a sustained release [SR] layer that can produce a distinct biphasic release having two different drug release rates. The IPR layer is intended to release a fraction of the dose rapidly at a faster rate and the SR layer is meant for slow release of the remaining dose at a slower rate for a desired period of time.

Methods: The quantitative determination was carried out by UV spectrophotometer. Solid dispersion was prepared by melt method. IPR layer was prepared by direct compression method, SR layer was prepared by wet granulation method. In-vitro drug release study from tablets was carried out in USP II tablet dissolution rate test apparatus. FTIR, DSC, XRD studies were performed.

Results: 89% of the incorporated drug was released within 30 min in acid solution of pH 1.2 from the IPR tablet prepared with the highest amount of gelucire due to solid state transformation of the drug. The SR layer (SR8) comprising of SAL, CG and CMC produced prolonged drug release (70% in 10 h). The optimized IPR3 layer and SR layers were compressed to form bi-layer tablets from which 23-37% drug was released immediately in 30 min, and the remaining drug was released slowly for 7 to 10 h depending upon the compositions of the tablets.

Conclusion: This study revealed that bi-phasic release of GPZ consisting of an initial quick release and subsequent slow release could be achieved by formulating bi-layer tablets using the existing tablet technology, and such formulation may be able to control hyperglycaemia effectively for a longer period of time


 

Keywords: IPR, SR, Glipizide, Solid Dispersion, Normoglycaemia Bilayer Tablets, Biphasic release

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References

1. Ying HL, Jia BZ. Modulation of combined-release behaviors from a novel ‘‘tablets-in-capsule” system. J Controlled Release 2004;95:381–9.
2. Lauretta M, Evelyn OM, Maria LT, Ubaldo C. Formulation of biphasic release tablets containing slightly soluble drugs. Eur J Pharm Biopharm 1999;48:37-42.
3. Colombo P, Conte V, Gazzaniga A, Maggi L, Sangalli ME, Peppas NA, et al. Drug release modulation of physical restrictions of matrix swelling. Int J Pharm 1990;31:43-8.
4. Yihong Q, Chidambaramb N, Kolette F. Design and evaluation of layered diffusional matrices for zero-order sustained-release. J Controlled Release 1998;51:123–30.
5. Geeta MP, Madhabhai MP. Compressed matrix dual-component vaginal drug delivery system containing metoclopramide hydrochloride. Acta Pharm 2009;59:273-88.
6. http://www.who.int/diabetes/en. [Last accessed on 10 Jul 2015].
7. Shoback DM, Gardner DG. Greenspan’s basic and clinical endocrinology. New York: Mc Graw Hill Lange; 2011.
8. David M, Nathan N. Long-term complications of diabetes mellitus. N Engl J Med 1993;328:1676-85.
9. Lawrence CP, Brian PF, Parinda HS, Sant PS. Glycemic control and hypoglycemia: is the loser the winner? Diabetes Care 2008;31:2072–6.
10. Songa AS, Meka VS, Nali SR, Sakamuri B, Kolapalli VRM. Design and evaluation of lornoxicam bilayered tablets for biphasic release. Braz J Pharm Sci 2012;48:609-19.
11. Ajit K, Manish B. Development and evaluation of regioselective bilayer floating tablets of Atenolol and Lovastatin for biphasic release profile. Iran J Pharm Res 2009;8:15-25.
12. Ouyang D, Nie S, Li W, Guo H, Liu H, Pan W. In vitro and In vivo evaluation of two extended release preparations of combination metformin and glipizide. Drug Dev Ind Pharm 2005;31:677-85.
13. Suresh B, Chandra ME, Ashok T, Madhusudan RY. Formulation and evaluation of multiple tablets as a biphasic gastroretentive floating drug delivery system for fenoverine. Acta Pharm 2010;60:89–97.
14. Vishnu MP, Bhupendra GP, Harsha VP, karshanbhai MP. Muchoadhesive bilayer tablets of propranolol hydrochloride. AAPS PharmSciTech 2007;8:E1-6.
15. Ganesh R, Falguni M, Jayvadan P. Formulation and evaluation of mucoadhesive glipizide films. Acta Pharm 2011;61:203–16.
16. Rakesh P, Preeti B, Prabodh CS, Vipin K, Harish D. Glipizide: some analytical, clinical and therapeutic vistas. Int J Chem Sci 2010;8:59-80.
17. http://www.gattefosse.com/en/applications/gelucire-4414.html. [Last accessed on 10 Jul 2015].
18. Bhusan BA, Rohit SR, Dhananjay GS, Shitalkumar PS, Dyankumar CD. Physicochemical characterization and enhancement of oral bioavailability of aceclofenac: gelucire 14/44 solid dispersion. Iran J Pharm Sci 2010;6:235-43.
19. Serajuddin ATM. Solid dispersions of poorly water soluble drugs: early promises, subsequent problems, and recent breakthroughs. J Pharm Sci 1999;88:1058-66.
20. Brahmankar DM, Jaiswal SB. Application of pharmacokinetic principles-Biopharmaceutics and Pharmacokinetics. Delhi: Vallabh Prakashan; 1998. p. 311.
21. Agnihotri SA, Aminabhavi TM. Novel interpenetrating network chitosan-poly (ethylene oxide-g-acrylamide) hydrogel microspheres for the controlled release of capecitabine. Int J Pharm 2006;324:103–15.
22. Donbrow M, Samuelov Y. Zero order drug delivery from double layered porous films: release rate profiles from ethylcellulose, hydroxypropylcellulose and polyethylene glycol mixtures. J Pharm Pharmacol 1980;32:463–70.
23. Narashimhan B, Mallapragada SK, Peppas NA. Release kinetics, data interpretation. In: Mathiowitz. ed. Encyclopedia of controlled drug delivery. New York: John Wiley and Sons Inc; 1999.
24. Ritger PL, Peppas NA. A simple euation for description of solute release II. Fickian and anomalous release from swellable devices. J Controlled Release 1987;5:37–42.
25. Sujjareevath J, Munday DL, Cox PJ, Khan KA. Release characteristics of diclofenac sodium from encapsulated natural gum mini-matrix formulation. Int J Pharm 1996;139:53–62.
26. Möckel JE, Lippold BC. Zero-order drug release from hydrocolloid matrices. Pharm Res 1993;10:1066–70.
27. Tejal SJ, Avani AF, Jolly PR, Rajesh PH. Process optimization and characterization of poloxamer solid dispersions of a poorly water-soluble drug. AAPS PharmSciTech 2007;8:E18-24.
28. Liu C, Liu C, Desai KGH. Enhancement of dissolution rate of valdecoxib using solid dispersions with polyethylene glycol 4000. Drug Dev Ind Pharm 2005;31:1-10.
29. Hirasawa N, Ishise S, Miyata H. An attempt to stabilize nivaldipine solid dispersion by the use of ternary systems. Drug Dev Ind Pharm 2003;29:997-1004.
30. Zheng Y, Haworth IS, Zuo Z, Chow MS, Chow AH. Physicochemical and structural characterization of Quercetin-β-Cyclodextrin complexes. J Pharm Sci 2005;94:1079-89.
31. Verheyen S, Blaton N, Kinget R, Van den Mooter G. Mechanism of increased dissolution of diazepam and temazepam from polyethylene glycol 6000 solid dispersions. Int J Pharm 2002;249:45-58.
32. Appa RB, Shivalingam MR, Kishore Reddy YV, Somesekhara R, Rajesh K, Sunitha N. Formulation and evaluation of aceclofenac solid dispersions for dissolution rate enhancement. Int J Pharm Sci Drug Res 2010;2:146-50.
33. Hülsmann S, Backensfeld T, Keitel S, Bodmeier R. Melt extrusion-an alternative method for enhancing the dissolution rate of 17-estradiol hemihydrates. Eur J Pharm Biopharm 2000;49:237-42.
34. Gilbert SB, Niel RA. Tablets. In: Leon L, Herbert AL, Joseph LK. ed. The theory and practice of industrial pharmacy. Bombay: Verghese Publishing House; 1991.
35. Deepti DH, Madan AK. Solid dispersion adsorbates for enhancement of dissolution rates of drugs. PDA J Pharm Sci Technol 2007;61:97–101.
36. Gupta MK, Goldman D, Bogner RH, Tseng Y. Enhanced drug dissolution and bulk properties of solid dispersions granulated with a surface adsorbent. Pharm Dev Technol 2001;6:563–72.
37. Tapan KG, Biswanath Sa. Statistical evaluation and influence of polymers concentration on disintegration time and diazepam release from quick disintegrating rapid release tablet. Yakugaku Zasshi 2009;129:1069-75.
38. Gaurav T, Ruchi T, Brijendra S, Awani KR. Development and optimization of multi-unit solid dispersion systems of poorly water soluble drug. Res J Pharm Tech 2008;1:1444-9.
39. Jinu I, Santanu K, Swastika G, Animesh G. Microwave-induced solid dispersion technology to improve bioavailability of glipizide. J Pharm Pharmacol 2012;65:219-29.
40. Karataş A, Yüksel N, Baykara T. Improved solubility and dissolution rate of piroxicam using gelucire 44/14 and labrasol. II Farmaco 2005;60:777–82.
41. Aslani P, Kennedy RA. Studies on diffusion in alginate gels, I. Effects of cross-linking with calcium or zinc ions on diffusion of acetaminophen. J Controlled Release 1996;42:75–82.
42. Polk A, Amsden B, Yao KD, Peng T, Goosen MFA. Controlled release of albumin from chitosan-alginate microcapsules. J Pharm Sci 1994;83:178–85.
43. Kikuchi A, Kawabuchi M, Sugihara M, Sakurai Y, Okano T. Controlled release of macromolecular dextran from calciumalginate gel beads. Proc Int Symp Controlled Release Bioact Mater 1996;23:737–8.
44. Bowersock TL, Hogenesch H, Suckow M, Guimond P, Martin S, Borie D. Oral vaccination of animals with antigens encapsulated in alginate microspheres. Vaccine 1999;17:1804–11.
45. Collett J, Moreton C. Modified-release peroral dosage forms. In: Aulton ME, ed. Pharmaceutics: the science of dosage form design. London: Churchill Livingstone; 2002.
46. Maestrelli F, Cirri M, Corti G, Mennini N, Mura P. Development of enteric coated calcium pectinate microspheres intended for colonic delivery. Eur J Pharm Biopharm 2008;69:508–18.
47. Kim CJ, Lee PI. Composite poly (vinyl alcohol) beads for controlled drug delivery. Pharm Res 1992;9:10–6.
48. Rakesh S, Siddhartha M, Biswanath S. Effect of ionic crosslink on the release of metronidazole from partially carboxymethylated guar gum tablet. Carbohydr Polym 2014;106:414–21.
49. Giunchedi P, Gavini E, Moretti MD, Pirisino G. Evaluation of alginate compressed matrixes as prolonged drug delivery systems. AAPS PharmSciTech 2000;1:131–6.
50. Nilufer Y, Arzu E, Kanık TB. Comparison of in vitro dissolution profiles by ANOVA-based, model-dependent and-independent methods. Int J Pharm 2000;209:57–67.
51. Shah VP, Tsong Y, Sathe P, Liu J P. In vitro dissolution profile comparison–statistics and analysis of the similarity factor, f2. Pharm Res 1998;15:889-96.
52. Anne R, Suyadevara V, Nayakanti D, Uttlapalli TN, Pavuluri LK. Formulation and evaluation of irbesartan fast dissolving tablets. Asian J Pharm 2013;2:61-7.
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How to Cite
Mukherjee, K., S. Chakraborty, and B. Sa. “QUICK/SLOW BIPHASIC RELEASE OF A POORLY WATER SOLUBLE ANTIDIABETIC DRUG FROM BI-LAYER TABLETS”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 7, no. 11, Oct. 2015, pp. 250-8, https://innovareacademics.in/journals/index.php/ijpps/article/view/8461.
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