FORMULATION AND EVALUATION OF SOLID DISPERSION OF TADALAFIL
Tadalafil is used for the treatment of the erectile dysfunction (ED) and pulmonary arterial hypertension. It is having low aqueous solubility thus it shows poor bioavailability of about 28% by after oral administration. To improve its solubility and dissolution profile solid dispersions (SDPs) of Tadalafil was prepared by physical mixing and solvent evaporation method using polyvinyl pyrollidone-K30 (PVP-30) as a hydrophilic polymeric carrier in different proportions with respect to drug (drug to polymer ratio 1:1 to 1:5). Drug and polymer compatibility studies were performed using FTIR study. The best suitable ratio and method was selected on the basis of enhanced aqueous solubility of drugs. Further selected SDPs were evaluated for various parameters like DSC analysis, percentage yield, percent drug content, saturation solubility, percent drug dissolution and stability studies. FTIR study indicated no incompatibility between Tadalafil and PVP-K30. SDPs prepared with drug to polymer ratio 1:3 and solvent evaporation method was found to be best as they shown significant increased (up to 10 fold) in aqueous solubility in comparison with that of others. DSC study also suggested the depression in the crystalline nature of Tadalafil. Selected SDPs exhibited good stability up to 3 months at 25 ± 2°C /60 ± 5% RH. Based on the results it can be concluded that, SDPs shown remarkable increase in the aqueous solubility and dissolution of Tadalafil and it may improve oral bioavailability of drug as compared with plain drug.
2. Mekonnen T. Design and evaluation of fast dissolving buccal films containing Tadalafil. International journal of allied medical sciences and clinical research. 2016; 4(2):155-63.
3. Teofilo V, Bruno S, Paulo C. Solid dispersion as strategy to improve oral bioavailability poor water soluble drugs. Drug discovery today. 2007; 12 (23/24):1068-75.
4. Park K. Dissolution mechanisms of Felodipine solid dispersions. Journal of Controlled Release. 2014; 188:101-103.
5. Shavi GV, Kumar AR, Usha YN, Armugam K, Ranjan O, Ginjupalli K et al. Enhanced dissolution and bioavailability of Gliclazide using solid dispersion techniques. International journal of drug delivery. 2010; 2:49-57.
6. Kumar GA, Choudhary RK, Chaitanya C. Enhancement of solubility and dissolution rate of Irbesartan by solid dispersion technique. Asian Journal of pharmaceutical and clinical research. 2011; 4(2):36-40.
7. Shinkar DM, Dhake AS, Mallikarjuna SC. Development of UV Spectrophotometric method for estimation of Carvedilol in bulk and pharmaceutical formulations. Asian journal of research in chemistry. 2013; 6(10):956-59.
8. Yunoos M, Sankar DG, Kumar BP, Hameed S. UV spectrophotometric method for the estimation of Tadalafil in bulk and tablet dosage form. E-journal of chemistry. 2010; 7(3):833-36.
9. Xu LL, Shi LL, Cao QR, Xu WJ, Cao Y, Zhu XY et al. Formulation and in vitro characterization of novel Sildenafil Citrate- loaded polyvinyl alcohol-polyethylene glycol graft copolymer-based orally dissolving films. International journal of pharmaceutics. 2014; 473:398-406.
10. Dehghan MMJ and Shareef A. Enhancement of dissolution and anti-inflammatory effect of Meloxicam using solid dispersions. International journal of applied pharmaceutics. 2010; 2(1):22-7.
11. Dewan I, Hossain MA, Islam SMA. Formulation and evaluation of solid dispersions of Carvedilol, a poorly water soluble drug by using different polymers. International journal of research in pharmacy and chemistry. 2012; 2(3):585-93.
12. Someshwar K, Rama G, Harikiran L, Krishna K, Srinivas A. Dissolution enhancement of a poorly water soluble drug using water soluble carriers. Journal of advanced pharmaceutical sciences. 2011; 1(1):42-6.
13. Kothawade SN, Kadam NR, Aragade PD, Baheti DG. Formulation and characterization of Telmisatan solid dispersions. International journal of pharmtech research. 2010; 2(1):341-47.
14. Sindhu J, Kishore B, Kaza R, Ranganayakulu D. Design and characterization of fast dissolving films of Telmisartan solid dispersions. International journal of research in pharmaceutical and nano sciences. 2015; 4(3):140-52.
15. Jain AK. Solubilization of Indomethacin using hydrotropes for aqueous injection. European journal of pharmaceutics and biopharmaceutics. 2008; 68:701-14.
16. Kshirsagar SJ, Ubhe A, Malshe J, Sengaokar V. A modified solvent method for preparation of solid dispersions. Iranian journal of pharmaceutical sciences. 2011; 8(1):287-98.
17. Begam M, Datta MV, Gowda DV, Aravindaram AS. Development and characterization of co-ground mixtures and solid dispersions of Aripiprazole with hydrophilic carriers. International journal of pharmacy and pharmaceutical sciences. 2014; 6(2):552-57.
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
The International Journal of Drug Regulatory affairs require a formal written transfer of copyright from the author(s) for each article published. We therefore ask you to complete and return this form, retaining a copy for your records. Your cooperation is essential and appreciated. Any delay will result in a delay in publication.
I/we have read and agree with the terms and conditions stated Page 2 of this agreement and I/we hereby confirm the transfer of all copyrights in and relating to the above-named manuscript, in all forms and media, now or hereafter known, to the International Journal of Drug Regulatory affairs, effective from the date stated below. I/we acknowledge that the IJDRA is relying on this agreement in publishing the above-named manuscript. However, this agreement will be null and void if the manuscript is not published in the IJDRA.
Download link for COPYRIGHT FORM