Improved Rapid Action of Dapoxetine Hydrochloride & L-arginine Solid Dispersion Using Film Formulation

Gi Won Lee; Hun Hwi Cho; Sung Hyun Jeon; Min Joung Choi; David Kim; Han Sol Kim; Jeong Eun Song; Gilson Khang

Macromolecular Research, Vol.27, No.4, 354-359, April, 2019

DOI10.1007/s13233-019-7047-y Export Citation

Improved Rapid Action of Dapoxetine Hydrochloride & L-arginine Solid Dispersion Using Film Formulation

Gi Won Lee, Hun Hwi Cho, Sung Hyun Jeon, Min Joung Choi, David Kim, Han Sol Kim, Jeong Eun Song , and Gilson Khang^†

Department of BIN Convergence Technology, Department of PolymerNano Science &Technology and Polymer Materials Fusion Research Center, Chonbuk National University, 567 Baekje-daero, Deokjin, Jeonju 54896, Korea

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Dapoxetine Hydrochloride (DH) have been developed for the treatment of premature ejaculation for men. DH promotes the ejaculatory delay as the selective serotonin inhibitor. However, it is necessary to delay time about 1?3 hours to absorb drug after oral administration. Therefore, rapid action is needed to reduce DH’s delay time. In this study, after making the Solid Dispersion (SD) with L-arginine (L-A) using rotary evaporation, we made Oral Thin Film (OTF) formulation for the immediately SD’s release. Characterizations of the samples were performed to analyze the morphology, crystallinity, the moecular structure by Scanning Electron Microscopy (SEM), Fourier Transform Infrared Spectroscopy (FTIR) and Powder X-Ray Diffractometer (PXRD). And, thermal porperty was also measured by Differential Scanning Calorimeter (DSC). Then, the dissolution test was used to analyze dissolution rate of the immediately released formulation via Batch (BAT). In this results, OTF is good formulation against the others and the BAT 3 is more dissoluble than other BATs. So, it is useful to cure the premature ejaculation.

Keywords:dapoxetine hydrochloride;l-arginine;rapid action;film formulation

[References]

Hatzimouratidis K, Amar E, Eardley I, Giuliano F, Hatzichristou D, Montorsi F, Vardi Y, Wespes E, Eur. Urol., 57, 804 (2010)
Patrick DL, Althof SE, Pryor JL, Rosen R, Rowland DL, Ho KF, McNulty P, Rothman M, Jamieson C, J. Sex. Med., 2, 358 (2005)
Akhvlediani N, Matyukhov I, Urologiia, 5, 106 (2017)
Butcher MJ, Serefoglu EC, EMJ Urol., 5, 106 (2017)
Smith-Harrison L, Starke NR, Smith RP, Kovac JR, Expert Opin. Investig. Drugs, 26, 669 (2017)
Nagaoka S, Asagoshi M, Kato K, Takata Y, Insect Biochem. Mol. Biol., 84, 40 (2017)
Shimoda H, Taniguchi K, Nishimura M, Matsuura K, Tsukioka T, Yamashita H, Inagaki N, Hirano K, Yamamoto M, Kinosada Y, Eur. J. Pharm. Biopharm., 73, 361 (2009)
Jug M, Hafner A, Lovric J, Kregar ML, Pepic I, Vanic Z, Cetina-Cizmek B, Filipovic-Grcic J, J. Pharm. Biomed. Anal., 147, 350 (2018)
Chamsai B, Limmatvapirat S, Sungthongjeen S, Sriamornsak P, Drug Dev. Ind. Pharm., 43, 2064 (2017)
Jahan K, Sultana Z, Karim S, Ali MH, Uddin J, WJSE, 2, 103 (2017)
Tian M, Wang YN, Wang R, Fane AG, Desalination, 401, 142 (2017)
Cocci A, Capece M, Cito G, Russo GI, Falcone M, Timpano M, Rizzo M, Camera PAD, Morselli S, Campi R, J. Sex. Med., 14, 1606 (2017)
Patil PS, Patil S, Tadavi SA, Gujarati N, Pawar SP, World J. Pharm. Pharm. Sci., 6, 657 (2017)
Liu C, Chang D, Zhang X, Sui H, Kong Y, Zhu R, Wang W, AAPS PharmSciTech, 18, 2957 (2017)
Alayoubi A, Haynes L, Patil H, Daihom B, Helms R, Almoazen H, Pharm. Dev. Technol., 22, 1012 (2017)
Kadam VS, Bharkad VB, Shete GA, Jameel A, Shendarker GR, Jadhav SV, World J. Pharm. Pharm. Sci., 6, 2052 (2017)
Abdlekawy KS, Donia AM, Elbarbry F, Eur. J. Drug Metabol. Pharmacokinet., 42, 397 (2017)
Attia AK, Saad AS, Alaraki MS, Elzanfaly ES, Adv. Pharm. Bull., 7, 329 (2017)
Doherty J, Cinque G, Gardner P, Appl. Spectrosc. Rev., 52, 560 (2017)
El-Refai K, Teaima MH, El-Nabarawi MA, Drug Dev. Ind. Pharm., 44, 988 (2018)

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[2] Patrick DL, Althof SE, Pryor JL, Rosen R, Rowland DL, Ho KF, McNulty P, Rothman M, Jamieson C, J. Sex. Med., 2, 358 (2005)

[3] Akhvlediani N, Matyukhov I, Urologiia, 5, 106 (2017)

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[6] Nagaoka S, Asagoshi M, Kato K, Takata Y, Insect Biochem. Mol. Biol., 84, 40 (2017)

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[9] Chamsai B, Limmatvapirat S, Sungthongjeen S, Sriamornsak P, Drug Dev. Ind. Pharm., 43, 2064 (2017)

[10] Jahan K, Sultana Z, Karim S, Ali MH, Uddin J, WJSE, 2, 103 (2017)

[11] Tian M, Wang YN, Wang R, Fane AG, Desalination, 401, 142 (2017)

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[13] Patil PS, Patil S, Tadavi SA, Gujarati N, Pawar SP, World J. Pharm. Pharm. Sci., 6, 657 (2017)

[14] Liu C, Chang D, Zhang X, Sui H, Kong Y, Zhu R, Wang W, AAPS PharmSciTech, 18, 2957 (2017)

[15] Alayoubi A, Haynes L, Patil H, Daihom B, Helms R, Almoazen H, Pharm. Dev. Technol., 22, 1012 (2017)

[16] Kadam VS, Bharkad VB, Shete GA, Jameel A, Shendarker GR, Jadhav SV, World J. Pharm. Pharm. Sci., 6, 2052 (2017)

[17] Abdlekawy KS, Donia AM, Elbarbry F, Eur. J. Drug Metabol. Pharmacokinet., 42, 397 (2017)

[18] Attia AK, Saad AS, Alaraki MS, Elzanfaly ES, Adv. Pharm. Bull., 7, 329 (2017)

[19] Doherty J, Cinque G, Gardner P, Appl. Spectrosc. Rev., 52, 560 (2017)

[20] El-Refai K, Teaima MH, El-Nabarawi MA, Drug Dev. Ind. Pharm., 44, 988 (2018)