DESIGN, DEVELOPMENT AND IN VITRO EVALUATION OF COMBINED FLOATING-BIOADHESIVE DRUG DELIVERY SYSTEMS OF ATENOLOL
Objective: A combination of the Floating-Bioadhesive system will overcome the drawbacks of floating & bioadhesive systems if used alone and will have a significant effect on improving the therapeutic effect of the drug involved. The present study involves the formulation and in vitro evaluation of atenolol floating-Bioadhesive tablet for prolonged residence in the stomach for the treatment of hypertension.
Methods: The tablets were prepared by direct compression method using directly compressible polymers such as, Hydroxy Propyl Methyl Cellulose (HPMC) K15M, Guar gum, Carbopol, and sodium alginate. The tablets were evaluated for buoyancy test, mucoadhesion force, swelling study, drug content, ex-vivo mucoadhesion strength and in-vitro release profile. Sodium bicarbonate was used for producing the effervescent base for the buoyancy of tablets.
Results: Formulation F9 contains polymer sodium alginate which has shown highest percentage cumulative drug release up to 99.12%. No significant change was observed in physical appearance, drug content, float ability or in vitro dissolution pattern after storage at 45 Â°C/75% RH for three months.
Conclusion: In this present research work it was concluded that the cumulative drug release increased when the viscosity and concentration of the polymer was increased. The swelling properties were increased with increasing polymer concentration and contributed to the drug release from the tablet matrix.
2. Melander A, Stenberg P, Liedholm H, Schersten B, Wahlin-Boll E. Food induced reduction in bioavailability of atenolol. Eur J Clin Pharmacol 1979;16:327â€“30.
3. Amidon GL, Lennernas H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutical drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995;12:413â€“20.
4. Ingani HM, Timmermans J, Moes AJ. Conception and in vivo investigation of peroral sustained release floating dosage forms with enhanced gastrointestinal transit. Int J Pharm 1987;35:157-64.
5. Deshpande, NH Shah, CT Rhodes. Development of a novel controlled release system for gastric retention. J Pharm Res 1997;14:815-9.
6. Remington. 19th Edn. The science and practice of pharmacy; 1995. p. 1669-70.
7. Abubakr ON, Jun SZ. In vitro evaluation of the release of albuterol sulfate from polymer gels: effect of fatty acids on drug transport across biological membranes. Drug Dev Ind Pharm 2002;6:965â€“9.
8. Rahman Z, Khar RK. Design and evaluation of bilayer floating tablets of captopril. Acta Pharma 2006;56:49â€57.
9. Senapati MK, Srinatha A, Pandit JK. In vitro release characteristics of matrix tablets: study of karaya gum and guar gum as release modulators. Int J Pharm Sci 2006;68:824-6
10. Government of India ministry of health and family welfare. The Pharmacopoeia of India. Controller of publication; 1996.
11. Seham SAE, Nahed DM, Gehanne ASA. Development of in situ gelling and mucoadesive mebeverine hydrochloride solution for rectal administration. Saudi Pharm J 2003:11:159-77.
12. Gupta A, Garg S, Khar RK. Measurement of bioadhesive strength of muco-adhesive buccal tablets: design of an in-vitro assembly. Indian Drugs 1992;30:152-5.
13. Jain SK, Awasthi AM, Jain NK. Calcium silicate based microspheres of rapiglinide for gastro retentive floating drug delivery: preparation and in vitro characterization. J Controlled Release 2005;107:300-9.
14. K Viveksarathi, K Kannan, S Selvamuthu Kumar, R Manavalan. Formulation development and in-vitro evaluation of gastro retentive floating tablets of atenolol. J Pharm Sci Res 2011;3:1632-6.
15. Sunil Kumar, M Das, KS Gupta, R Kumar, A Chongdar, LK Ghosh. Design, development, optimization and evaluation of gastro-retentive floating tablets of atenolol, scholars research library. Der Pharm Lett 2013;5:436-56.