Author(s):
Ali Bustani, Yaser Bitar, Wassim Abdelwahed
Email(s):
alibustani07@gmail.com
DOI:
10.52711/0974-360X.2025.00194 
Address:
Ali Bustani1*, Yaser Bitar1, Wassim Abdelwahed2
1Department of Pharmaceutical Chemistry and Quality Control, Faculty of Pharmacy, University of Aleppo, Aleppo, Syria.
2Department of Pharmaceutics, Faculty of Pharmacy, University of Aleppo, Aleppo, Syria.
*Corresponding Author
Published In:
Volume - 18,
Issue - 3,
Year - 2025
ABSTRACT:
Erectile dysfunction (ED) and premature ejaculation (PE) are two common male sexual disorders encountered by clinicians daily. The first-line recommended treatment for ED is the use of phosphodiesterase type 5 (PDE5) inhibitors including Tadalafil (TADA). Dapoxetine (DAPO) has been approved in many countries as an on-demand treatment for PE, but the bitter flavor taste of oral Dapoxetine formulations is a commonly experienced issue. As a result, the taste of Dapoxetine has been effectively masked through encapsulation by Eudragit E100 using a spray-drying method. Production yield and encapsulation efficiency were 77.36%, and 99.03% respectively. The combination of Tadalafil and Dapoxetine are sold in the market as regular tablets. At present, there are no ODTs in the market that contain both Tadalafil and Dapoxetine. This study's goal was to create and describe orally disintegrating tablets (ODTs) that include Tadalafil and Dapoxetine. The ODTs were made through freeze-drying methods and direct compression techniques. Quality controls were conducted. ODTs made using direct compression and freeze-dried methods disintegrated in 62 and 29 sec, respectively. The in vitro dissolution test demonstrated that Tadalafil released from ODTs prepared by freeze-drying occurred more rapidly than from those made by direct compression. Conversely, Dapoxetine released more quickly from ODTs prepared by direct compression compared to those made by freeze-drying. This difference is attributed to the encapsulation of Dapoxetine using Eudragit E100 through spray drying for taste masking. 8.94% of Dapoxetine was released in the phosphate buffer pH 6.8 during the simplified dissolution test from ODTs prepared by freeze-drying in the first three minutes.
Cite this article:
Ali Bustani, Yaser Bitar, Wassim Abdelwahed. Formulation and Evaluation of Orally Disintegrating Tablets of Tadalafil and Dapoxetine HCl prepared by Direct Compression and Freeze-Drying Techniques with Taste Masking of Dapoxetine HCl.. Research Journal of Pharmacy and Technology. 2025;18(3):1336-5. doi: 10.52711/0974-360X.2025.00194
Cite(Electronic):
Ali Bustani, Yaser Bitar, Wassim Abdelwahed. Formulation and Evaluation of Orally Disintegrating Tablets of Tadalafil and Dapoxetine HCl prepared by Direct Compression and Freeze-Drying Techniques with Taste Masking of Dapoxetine HCl.. Research Journal of Pharmacy and Technology. 2025;18(3):1336-5. doi: 10.52711/0974-360X.2025.00194 Available on: https://rjptonline.org/AbstractView.aspx?PID=2025-18-3-55
5. REFERENCES:
1. Hannan PA, Khan JA, Khan A, Safiullah S. Oral dispersible system: A new approach in drug delivery system. Indian J Pharm Sci [Internet]. 2016; 78(1): 2–7. Available from: http://dx.doi.org/10.4103/0250-474x.180244
2. Vishali T, Damodharan N. Orodispersible tablets: A review. Res J Pharm Technol [Internet]. 2020; 13(5): 2522. Available from: http://dx.doi.org/10.5958/0974-360x.2020.00449.7
3. Sunada H, Bi Y. Preparation, evaluation and optimization of rapidly disintegrating tablets. Powder Technol [Internet]. 2002; 122(2–3): 188–98.
4. Bafail RSM. Disintegration testing for orally disintegrating tablets (ODTs): An overview. Trop J Pharm Res [Internet]. 2024; 22(11): 2399–406. Available from: http://dx.doi.org/10.4314/tjpr.v22i11.21
5. Stange U, Führling C, Gieseler H. Freeze drying of orally disintegrating tablets containing taste masked naproxen sodium granules in blisters. Pharm Dev Technol [Internet]. 2015; 20(8): 1018–24. Available from: http://dx.doi.org/10.3109/10837450.2014.959179
6. Ölmez S, Sevtap I. Advantages and quality control of orally disintegrating tablets. Fabad J Pharm Sci. 2009; 34: 167–72.
7. Swamivelmanickam M, Venkatesan P, Sangeetha G. Preparation and evaluation of mouth dissolving tablets of loratadine by direct compression method. Res J Pharm Technol [Internet]. 2020; 13(6): 2629. Available from: http://dx.doi.org/10.5958/0974-360x.2020.00467.9
8. Anjan K, Mahapatra RP, Swain B, Revathi N, Nirisha PN. Orodispersible Tablets: A review on Formulation Development Technologies and Strategies. Research J Pharm and Tech. 2013; 6(9): 941–53.
9. Goel H, Rai P, Rana V, Tiwary AK. Orally disintegrating systems: innovations in formulation and technology. Recent Pat Drug Deliv Formul [Internet]. 2008; 2(3): 258–74. Available from: http://dx.doi.org/10.2174/187221108786241660
10. Ma D, Wang A, Wang H, Yang J, Luo D, Zhao Z, et al. A review of studies on the treatment of premature ejaculation with traditional Chinese medicine. Integr Med Nephrol Androl [Internet]. 2024; 11(3). Available from: http://dx.doi.org/10.1097/imna-d-24-00008
11. Sadishkumar S, Kumar S, Mohith SN, Prathiba R, Abilash S, Mahesh AR. In Silico Investigation of Chemical Components of Fragaria ananassa Species as Aphrodisiac Agents for Erectile Dysfunction. Research Journal of Pharmacy and Technology [Internet]. 2024; 17(7): 3315–9. Available from: http://dx.doi.org/10.52711/0974-360X.2024.00518
12. Shah M, Patel D. Development and characterization of tadalafil solid dispersion using skimmed milk for improved the solubility and dissolution release profile. Res J Pharm Technol [Internet]. 2020; 13(12): 6212–7. Available from: http://dx.doi.org/10.5958/0974-360x.2020.01083.5
13. Dorsey P, Keel C, Klavens M, Hellstrom WJG. Phosphodiesterase type 5 (PDE5) inhibitors for the treatment of erectile dysfunction. Expert Opin Pharmacother [Internet]. 2010; 11(7): 1109–22. Available from: http://dx.doi.org/10.1517/14656561003698131
14. Shin YE, Rojanasarot S, Hincapie AL, Guo JJ. Safety profile and signal detection of phosphodiesterase type 5 inhibitors for erectile dysfunction: a Food and Drug Administration Adverse Event Reporting System analysis. Sex Med [Internet]. 2023; 11(5): qfad059. Available from: http://dx.doi.org/10.1093/sexmed/qfad059
15. McMahon CG, McMahon CN, Leow LJ. New agents in the treatment of premature ejaculation. Neuropsychiatr Dis Treat [Internet]. 2006; 2(4): 489–503. Available from: http://dx.doi.org/10.2147/nedt.2006.2.4.489
16. Gao J, Peng D, Zhang X, Hao Z, Zhou J, Fan S, et al. Prevalence and associated factors of premature ejaculation in the Anhui male population in China: Evidence-based unified definition of lifelong and acquired premature ejaculation. Sex Med [Internet]. 2017; 5(1): e37–43. Available from: http://dx.doi.org/10.1016/j.esxm.2016.11.002
17. Krishnakumar P, Sundarrajan T, Kathiravan MK, Manikandan K. Spectroscopic estimation of dapoxetine HCl using multivariate analysis. Res J Pharm Technol [Internet]. 2020; 13(6): 2715. Available from: http://dx.doi.org/10.5958/0974-360x.2020.00483.7
18. Martin-Tuite P, Shindel AW. Management options for Premature Ejaculation and Delayed Ejaculation in men. Sex Med Rev [Internet]. 2020; 8(3): 473–85. Available from: http://dx.doi.org/10.1016/j.sxmr.2019.09.002
19. El-Said IA, Aboelwafa AA, ElGazayerly ON. Optimization of taste-masked dapoxetine oral thin films using factorial design: in vitro and in vivo evaluation. Pharm Dev Technol [Internet]. 2021; 26(5): 522–38. Available from: http://dx.doi.org/10.1080/10837450.2021.1894445
20. Corona G, Rastrelli G, Limoncin E, Sforza A, Jannini EA, Maggi M. Interplay between premature ejaculation and erectile dysfunction: A systematic review and meta-analysis. J Sex Med [Internet]. 2015; 12(12): 2291–300. Available from: http://dx.doi.org/10.1111/jsm.13041
21. Mohseni Rad H, Zahirian Moghadam T, Hosseinkhani A, Nima Soluki N, Amani F. Comparison of Dapoxetine /Tadalafil and Paroxetine/Tadalafil combination therapies for the treatment of the premature ejaculation: A randomized clinical trial. Urol J [Internet]. 2021; 19(2): 138–43. Available from: http://dx.doi.org/10.22037/uj.v18i.6644
22. Seftel AD. Re: Efficacy and safety of dapoxetine in men with premature ejaculation and concomitant erectile dysfunction treated with a phosphodiesterase type 5 inhibitor: randomized, placebo-controlled, phase III study. J Urol [Internet]. 2014; 191(4): 1077–8. Available from: http://dx.doi.org/10.1016/j.juro.2014.01.070
23. Development and Optimization of Liquisolid Tablets Containing Tadalafil and dapoxetine as a Combined Therapy for Male Sexual Dysfunction.
24. Pahwa R, Gupta N. Superdisintegrants in the development of orally disintegrating tablets: a review. International journal of pharmaceutical sciences and research. 2011; 2(11).
25. Gittings S, Turnbull N, Roberts CJ, Gershkovich P. Dissolution methodology for taste masked oral dosage forms. J Control Release [Internet]. 2014; 173: 32–42. Available from: http://dx.doi.org/10.1016/j.jconrel.2013.10.030
26. Andayani R, Hasbi H, Febriyenti F. Analysis of chlorpheniramine maleate in microcapsules formulation with eudragit E PO polymer using spray drying method. Res J Pharm Technol [Internet]. 2023; 5279–84. Available from: http://dx.doi.org/10.52711/0974-360x.2023.00855
27. Pagar HB, Shinde UP, Agrawal YS, Barhate SD, Luhade TS, Sonawane RO. Taste Masking: A Review. Research J Pharm and Tech. 2012; 5(2): 152–7.
28. Ghanchi SD, Dhawale SC. Taste Masking Technologies of Pharmaceuticals. Research J Pharm and Tech. 2011; 4(10): 1513–8.
29. Council of Europe. European Pharmacopoeia. 8th ed. Strasbourg: Council of Europe; 2014.
30. Affas S, Sakur AA. Spectrophotometric Method for Simultaneous Estimation of Dapoxetine and some Phosphodiesterase-5 inhibitors in new combinations. Res J Pharm Technol. [Internet]. 2019; 12(11): 5193. Available from: http://dx.doi.org/10.5958/0974-360x.2019.00899.0
31. Al-khattawi A, Mohammed AR. Compressed orally disintegrating tablets: excipients evolution and formulation strategies. Expert Opin Drug Deliv [Internet]. 2013; 10(5): 651–63. Available from: http://dx.doi.org/10.1517/17425247.2013.769955
32. United States Pharmacopeial Convention. United States pharmacopeia 30. Rockville, MD; 1991.
33. Siewert M, Dressman J, Brown CK, Shah VP, FIP, AAPS. FIP/AAPS guidelines to dissolution/in vitro release testing of novel/special dosage forms. AAPS PharmSciTech [Internet]. 2003; 4(1): E7. Available from: http://dx.doi.org/10.1208/pt040107