title: Preparation of sildenafil citrate microcapsules and in vitro/in vivo evaluation of taste masking efficiency.
abstract: The aim of the present study was to prepare the particulate taste-masking system to mask the bitter taste of sildenafil citrate (SC), a well-known phosphodiesterase-5 inhibitor used for erectile dysfunction (ED) and pulmonary artery hypertension (PAH). It was evaluated for the taste masking efficiency by the in vitro measurement using electronic tongue (e-tongue) system and the in vivo human panel sensory test. Microcapsules were prepared by microencapsulation with a gastro-soluble polymer, Eudragit(®) E100 (E100), using a spray drying technique at four different weight ratios (2:1, 1:1, 1:2, and 1:3). Characters of prepared microcapsules and the effect of polymer ratio on the taste masking were investigated. The particle morphology and the distribution of SC in microcapsules were observed by SEM-EDS and physical properties were evaluated by PXRD, Raman spectroscopy, and DSC. By drug dissolution studies at pH 1.2 buffer and DW, it was found that E100 was not able to alter the drug release in stomach. As the result of taste evaluation studies, there were a good correlation (R(2)=0.9867) between the weight ratio of polymer and the taste masking efficiency expressed in the distances on the PCA map of the e-tongue data, and a relevance of the e-tongue measurement with the result of sensory test.
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon, Gyeonggi-do 440-746, Republic of Korea.
authors.forename: Eun-Jin
authors.initials: EJ
authors.lastname: Yi
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon, Gyeonggi-do 440-746, Republic of Korea; College of Pharmacy, Woosuk University, Wanju-gun, Jeonbuk 565-701, Republic of Korea.
authors.forename: Ju-Young
authors.initials: JY
authors.lastname: Kim
authors.affiliation: College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju, Gyeongnam 660-751, Republic of Korea.
authors.forename: Yun-Seok
authors.initials: YS
authors.lastname: Rhee
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon, Gyeonggi-do 440-746, Republic of Korea.
authors.forename: Su-Hyeon
authors.initials: SH
authors.lastname: Kim
authors.affiliation: College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 361-763, Republic of Korea.
authors.forename: Hyo-Joong
authors.initials: HJ
authors.lastname: Lee
authors.affiliation: College of Pharmacy, Chungbuk National University, Cheongju, Chungbuk 361-763, Republic of Korea. Electronic address: kaize17@naver.com.
authors.forename: Chun-Woong
authors.initials: CW
authors.lastname: Park
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon, Gyeonggi-do 440-746, Republic of Korea. Electronic address: espark@skku.edu.
authors.forename: Eun-Seok
authors.initials: ES
authors.lastname: Park
mesh_terms: D000179:Acrylates / Q000737:chemistry*; D000328:Adult; D002214:Capsules; D004339:Drug Compounding; D055615:Electrical Equipment and Supplies; D005260:Female; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008297:Male; D058986:Phosphodiesterase 5 Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D010879:Piperazines / Q000737:chemistry* / Q000494:pharmacology*; D011108:Polymers / Q000737:chemistry*; D011687:Purines / Q000737:chemistry / Q000494:pharmacology; D000068677:Sildenafil Citrate; D016037:Single-Blind Method; D012995:Solubility; D013450:Sulfones / Q000737:chemistry* / Q000494:pharmacology*; D013649:Taste / Q000187:drug effects*; D055815:Young Adult
chemical_list: D000179:Acrylates; D002214:Capsules; C477020:Eudragit E100; D058986:Phosphodiesterase 5 Inhibitors; D010879:Piperazines; D011108:Polymers; D011687:Purines; D013450:Sulfones; D000068677:Sildenafil Citrate