Enhanced dissolution of sildenafl dry foam tablets

Attwdee Se Yoon Teerpol Srichn

aDrug and Cosmetic Research and Development Unit,School of Pharmacy,Walailak University,Nakhon Si Thammarat 80161,Thailand

bDepartment of Pharmaceutical Technology,Faculty of Pharmaceutical Sciences,Prince of Songkla University, Songkhla 90112,Thailand

Enhanced dissolution of sildenafl dry foam tablets

Somchai Sawatdeea,*,Apichart Atipairina,Attawadee Sae Yoona, Teerapol Srichanab

aDrug and Cosmetic Research and Development Unit,School of Pharmacy,Walailak University,Nakhon Si Thammarat 80161,Thailand

bDepartment of Pharmaceutical Technology,Faculty of Pharmaceutical Sciences,Prince of Songkla University, Songkhla 90112,Thailand

A R T I C L E I N F O

Article history:

Available online 25 November 2015

Sildenafl citrate

Dry foam tablet

Dissolution

Sildenafl citrate is a highly selective phosphodiesterase-5(PDE-5)inhibitor.It is used for treatment of erectile dysfunction and pulmonary hypertension[1].Sildenafl citrate is categorized in BCS class 2 so it is developed as a citrate salt to increase water solubility(4.1 mg/mL)[2].The conventional product has been developed as a tablet dosage form.It is rapidly absorbed after oral administration,but gives a relatively low oral bioavailability of about 40%and late onset of action[2].Dry foam formulation technology is an alternative approach to overcome such a problem.It is intended to enable a faster and more effcient dissolution by avoiding agglomeration and foating of nonwetted active particles[3].

Sildenafl dry foam was prepared following the method: Sildenafl citrate was suspended in sodium dodecyl sulphate 2%solution.A mixture of maltodextrin and mannitol in a weight ratio of 1:1 was used as diluent by adding to the sildenafl suspension to form a paste and to pass through a nozzle of spray bottle to obtain smooth foam.The homogeneous foam was then dried in a vacuum oven and then passed through a sieve no. 18 to obtain dry foam granules.The granule was characterized by SEM,IR and DSC.The dry foam granules equivalent to sildenafl 100 mg were mixed with croscarmellose sodium,magnesium stearate and lactose to obtain 600 mg and then compressed into tablets.The physical properties and dissolution of tablets were evaluated.The results of SEM,IR and DSC were shown in Fig.1 A,B,C,respectively.Dry foam granules showed that the morphology of granules have many pores and change to amorphous.The physical properties of sildenafl dry foam formulations showed good fow properties(angle of repose<10°),hardness of tablets～5 kg,friability test<1%and disintegration time<5 min.The dissolution behavior was analyzed in 3 media at pH 2.0,4.5 and 6.8.The results showed that sildenafl dry foam tablet had a highest dissolution rate in all media(100%dissolved in 5 min,Fig.1 D).In conclusion,dryfoam tablets released sildenafl to 100%in 5 min faster than conventional sildenafl tablets.

Fig.1–SEM photograph(A),IR spectra(B),DSC thermogram(C)and drug release profles(D)of sildenafl dry foam tablet.

Acknowledgements

The authors would like to acknowledge fnancial support from Walailak University(Grant Number WU57209),Drug and Cosmetic Research and Development Unit and Research and Development Division,School of Pharmacy,Walailak University.

R E F E R E N C E S

[1]Sawatdee S,Hiranphan P,Laphanayos K,et al.Evaluation of sildenafl pressurized metered dose inhalers as a vasodilator in umbilical blood vessels of chicken egg embryos.Eur J Pharm Biopharm 2014;86:90–97.

[2]Jung S,Seo YG,Kim GK,et al.Comparison of the solubility and pharmacokinetics of sildenafl salts.Arch Pharm Res 2011;34:451–454.

[3]Sprunk A,Page S,Kleinebudde P.Infuence of process parameters and equipment on dry foam formulation properties using indomethacin as model drug.Int J Pharm 2013;455:189–196.

*E-mail address:somchai.sa@wu.ac.th,somchai086@hotmail.com.

Peer review under responsibility of Shenyang Pharmaceutical University.

http://dx.doi.org/10.1016/j.ajps.2015.11.042

1818-0876/©2016 Production and hosting by Elsevier B.V.on behalf of Shenyang Pharmaceutical University.This is an open access article under the CC BY-NC-ND license(http://creativecommons.org/licenses/by-nc-nd/4.0/).