A MUCOADHESIVE GASTRORETENTIVE DOSAGE FORM FOR VALACYCLOVIR
Objective: The objective of the present work was to formulate a gastroretentive dosage form of Valacyclovir, an anti viral drug.
Methods: Valacyclovir gastroretentive mucoadhesive tablets were prepared using polymers such as Carbopol 974P and hydroxy propyl methyl cellulose (HPMC) K4M, in different proportions by wet granulation technique. Compatibility studies were performed by FTIR spectroscopy. The prepared granules were evaluated for bulk density, Carrâ€™s index, Hausnerâ€™s ratio, friability, drug content uniformity, hardness, thickness and post compression parameters.
Results: Results revealed that all the formulated tablets have acceptable physical properties. Based on the in vitro release profile, the formulation B3, containing HPMC (46%), Carbopol (15%) with a drug release of 96.98% was chosen as the optimized batch. The B3 formulation was subjected for zero order and first order kinetics, Higuchi matrix and peppaâ€™s model. It was found to be adherent to the Higuchi model, as the r2 value was higher thereby following Fickian diffusion. Results of in vitro gastric retention time study indicated that the tablet remained adhered to the stomach mucosa and could be seen at the same position after 24h of administration.
Conclusion: The present formulation, i.e. a gastroretentive drug delivery system can be used as an alternative to conventional dosage forms of Valacyclovir with a prospect to increase its residence time in the stomach and decrease its degradation in the intestine thereby increasing its bioavailability.
2. Robinson JR, Vincent HK. Influence of drug properties and routes of drug administration on the design of sustained and controlled release systems. In: Robinson JR, Vincent HL, editors. Controlled drug delivery: Fundamentals and Application. 2nd edition. New York: Marcel Dekker; 2005. p. 4-14.
3. Mathiowitz E, Chickering D, Jacob JS, Santosh C. In: Mathiowitz E. editor. Encyclopedia of Controlled Drug Delivery. New York: John Wiley & sons Inc; 2006. p. 896-11.
4. Nasa P, Mahant S, Sharma D. Floating systems: a novel approach towards gastroretentive drug delivery systems. Int Pharm Sci 2010;2:2-7.
5. Deshpande AA, Shah NH, Rhodes CT, Malick W. Development of a novel controlled-release system for gastric retention. Pharm Res 1997;14(6):815-9.
6. Kawashima Y, Niwa T, Takeuchi H, Hino T, Itoh Y. Hollow microspheres for use as a floating controlled drug delivery system in the stomach. J Pharm Sci 1992;81(2):135-40.
7. Ponchel, Irache. Specific and non-specific bioadhesive particulate systems for oral delivery to the gastrointestinal tract. Adv Drug Delivery Rev 1998;34(2-3):191-219.
8. Hwang SJ, Park H, Park K. Gastric retentive drug-delivery systems. Crit Rev Ther Drug Carrier Syst 1998;15(3):243-84.
9. Khar RK, Ahuja A, Ali J. Mucoadhesive drug delivery. In: NK jain editor. Controlled and novel drug delivery. Delhi: CBS: 2002. p. 353-61.
10. Patil SB, Murthy SR, Mahajan RD, Wagh S. Mucoadhesive polymers. Means of improving drug delivery. Pharm Time 2006;38:25-9.
11. Panchaxari MD, Chirag PP, Rohit S, Anand PG, Vinayak M. J Studies on formulation and evaluation of osmotically controlled drug delivery system of carbamazepine. Int Pharm Sci 2014;6:2239-50.
12. Patel sandipkumar D. Design and evaluation of different gastroretentive drug delivery system of some HMG C0-A reductase inhibitors. Ind J Pharm Sci 2006;68:89-93.
13. Prakash R, Neelima A, Ramesh C. Development of gastroretantive drug delivery system of Cephalexin by using factorial design. ARS Pharm 2009;50:8-24.
14. Ravindra K, Godoi AFL, Bencs L, Van Grieken R. Low-pressure gas chromatography-ion trap mass spectrometry for the fast determination of polycyclic aromatic hydrocarbons in air samples. J Chromatography A 2006;1114(2):278-81.
15. Shinde G, Sudarshini S, Kumarswamy D. Int J Bangale Ganesh. Formulation and evaluation of mucoadhesive tablets of niacin using different bioadhesive polymers. Pharm Bio Sci 2010;2:1-14.
16. Derle D, Joshi O, Ashish P, Patel J, Vaishali P. Effect of tablet excipients on mucoadhesive properties of polyoxyethylene and carbopol 971. Int Pharm Sci 2009;1:198-205.
17. Pradeep B, Nagamadhu M, Bindu Madhavi B, David B, Arjun G, Shekhar K. Formulation and evaluation of valacyclovir hydrochloride microcapsules. Int J Pharm Pharm Sci 2011;3:92-6.
18. Shanmugam M, Jacobs-Gedrim R, Durcan C, Yu B. 2D layered insulator hexagonal boron nitride enabled surface passivation in dye sensitized solar cells. Nanoscale 2013;5(22):11275-82.
19. V S V Kumar R, Hemnath E, Siddhartha T, Rajkumar Y, et al. K, Suresh Venkata Karthik Development and validation of RP-UFLC method for the estimation of terbinafine HCl in pharmaceutical nanoemulsion gel. Int Pharm Sci 2014;6:586-90.
20. Sailaja K, Radhakrishna K, Ganesh GNK, Reddy K S V, et al. Development of osmotically controlled oral drug delivery system for nateglinide an anti-diabetic drug. Int Pharm Sci 2014;6(7):120-5.