title: Orodispersible films and tablets with prednisolone microparticles.
abstract: Orodispersible tablets (ODTs) and orodispersible films (ODFs) are solid oral dosage forms disintegrating or dissolving rapidly when placed in the mouth. One of the main issues related to their preparation is an efficient taste masking of a bitter drug substance. Therefore, the aim of this study was to prepare and evaluate the microparticles intended to mask a bitter taste of the prednisolone and use them in further preparation of two orodispersible dosage forms. Microparticles based on the Eudragit E PO or E 100 as a taste-masking agent were prepared with spray-drying technique. Tablets containing microparticles, co-processed ODT excipient Pharmaburst, and lubricant were directly compressed with single-punch tablet press. Orodispersible films were prepared by casting polymeric solutions of hydroxypropyl methylcellulose containing uniformly dispersed microparticles. Physicochemical properties of microparticles were evaluated, as well as mechanical properties analysis, disintegration time measurements and dissolution tests were performed for prepared dosage forms. Both formulations showed good mechanical resistance while maintaining excellent disintegration properties. The dissolution studies showed good masking properties of microparticles with Eudragit E 100. The amount of prednisolone released during the first minute in phosphate buffer 6.8 was around 0.1%. After incorporation into the orodispersible forms, the amount of released prednisolone increased significantly. It was probably the effect of faster microparticles wetting in orodispersible forms and their partial destruction by compression force during tableting process.
authors.affiliation: Department of Pharmaceutical Technology and Biopharmaceutics, Jagiellonian University Medical College, ul. Medyczna 9, 30-688 Krakow, Poland.
authors.forename: Witold
authors.initials: W
authors.lastname: Brniak
authors.affiliation: Department of Pharmaceutical Technology and Biopharmaceutics, Jagiellonian University Medical College, ul. Medyczna 9, 30-688 Krakow, Poland.
authors.forename: Ewelina
authors.initials: E
authors.lastname: Maślak
authors.affiliation: Department of Pharmaceutical Technology and Biopharmaceutics, Jagiellonian University Medical College, ul. Medyczna 9, 30-688 Krakow, Poland.
authors.forename: Renata
authors.initials: R
authors.lastname: Jachowicz
mesh_terms: D000179:Acrylates / Q000737:chemistry; D000284:Administration, Oral; D004304:Dosage Forms; D004339:Drug Compounding; D065347:Hypromellose Derivatives / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D011109:Polymethacrylic Acids / Q000737:chemistry; D011239:Prednisolone / Q000737:chemistry*; D012995:Solubility; D013649:Taste
chemical_list: D000179:Acrylates; D004304:Dosage Forms; C477020:Eudragit E100; D011108:Polymers; D011109:Polymethacrylic Acids; D065347:Hypromellose Derivatives; C518398:Eudragit E PO; D011239:Prednisolone
keywords: Microparticles; Oral thin film; Orally disintegrating tablet; Orodispersible film; Orodispersible tablet; Taste-masking