DEVELOPMENT AND EVALUATION OF FAST DISSOLVING TABLETS OF FOSINOPRIL BY SUBLIMATION METHOD
Abstract
Fosinopril is an antihypertensive, angiotensin converting enzyme inhibitor. This is used in the treatment of various cardiovascular disorders such as heart failure, to reduce proteinuria and renal disease in patients with nephropathies, and to prevent stroke, myocardial infarction, and cardiac death in high-risk patients and hypertension. In present research work an attempt has been made to prepare fast dissolving tablets of Fosinopril with increased rate of dissolution may leads to increase bioavailability. The fast dissolving tablets of Fosinopril were prepared by using sublimation method. Croscarmellose sodium is used as a superdisintegrant. Camphor, Urea and Menthol are used as a sublimating agent. The prepared tablets were evaluated for various parameters like weight variation, hardness, friability, disintegration time, drug content, water absorption ratio, wetting time, in-vitro drug release, FTIR, DSC studies and short term stability studies. IR spectral analysis and DSC study showed that there was no drug interaction with formulation additives of the tablet. The blend was examined for the pre-compressional parameters. The prepared tablets formulations were evaluated for post-compressional parameters. The values of pre-compression parameters evaluated were within prescribed limits and indicated good free flowing property. All the post-compressional parameter are evaluated were prescribed limits and results were within IP acceptable limits. The disintegration time of 17 to 52 sec, water absorption ratio of 50.75 to 84.41%, wetting time of 23.41 to 36.61sec. In-vitro dissolution studies on the promising formulations SF3, SF6 and SF9 formulations were carried out in 6.8 phosphate buffer solution. This data reveals that overall, the formulation SF3, SF6 and SF9 shows nearly faster drug release. The formulations SF3, SF6 and SF9 50 % of drug released in 0.67 min, 0.73min, and 0.69 min, respectively, and 90 % of drug released in 2.93 min, 4.88 min, and 3.83 min, respectively when compared to other tablet formulation. Among all the formulation SF3 were found to be promising and showed a disintegration time of 17 sec, 50 % of drug released in 0.67 min, and 90 % of drug released in 2.93 min. The stability study conducted as per the ICH guidelines and the formulations were found to be stable. The results concluded that fast dissolving tablets Fosinopril showing enhanced dissolution, will lead to improved bioavailability, improved effectiveness and hence better patient compliance.
Keywords:
Fast dissolving tablet, Fosinopril, Croscarmellose sodium, Camphor, Menthol, Disintegration timeDOI
https://doi.org/10.25004/IJPSDR.2012.040402References
2. http://www.rxlist.com/cgi/generic/fosinopril.html
3. http://en.wikipedia.org/wiki/fosinopril
4. www.cims.com
5. Agarwal V, Bhavesh H, Kothari, Derek V. Moe R K. Khankari. Drug Delivery: Fast-Dissolve Systems. In: James swarbrick. Encyclopedia of pharmaceutical technology, 3rded.USA: Informa healthcare 2007:1104-5.
6. Nangude TD, Chatap .VK, Bhise KS, Sharma D.K. Mouth dissolving tablets: Geriatrics and pediatrics friendly drug delivery system. Indian Drugs 2007; 44(6): 471-3.
7. Indurwade NH, Rajyaguru TH, Nakhat PD. Novel approach- Fast dissolving tablets. Indian Drugs 2002; 39(8): 405-8.
8. Lachman L, Libermann HA, Kanig JL. The theory and practice of industrial pharmacy. Varghese Publishing House, 3rd edition; 1991; 297-301.
9. Vijaya KS, Mishra DN. Rapidly disintegrating oral tablets of meloxicam. Indian Drugs 2006; 43(2): 117-21.
10. Raju SA, Rampure MV, Shrisand SB, Swamy PV, Nagendra DK, Baswaraj B, Raghunandan D. Formulation and evaluation of orodispersible tablets of alfuzosin. Int. J Pharm. Tech. Res. 2010; 2 (1): 84-88.
11. Stephen BR, Rajveer CH, Sudarshini SA, Kishore Reddy. Preparation and evaluation of mucoadhesive microcapsules of nimodipine. Int. J Res. Pharm. Sci. 2010; 1(2): 219-224.
12. Desai SA, Kharade SV, Petkar KC and Kuchekar BS. Orodissolving tablets of promethazine hydrochloride. Ind J Pharm Edu Res. 2006; 40(3): 172-4.
13. Stephen BR, Rajveer CH, Prashant KC, Ganesh SB, Gajanan VS. Studies of dissolution behavior of sustained release solid dispersions of nimodipine. Int. J Pharm. Review and Res. 2010; 3(1): 77-82.
Published

