title: Novel coprocessed excipients composed of lactose, HPMC, and PVPP for tableting and its application.
abstract: New coprocessed excipients composed of α-lactose monohydrate (a filler), HPMC E3 (a binder), and PVPP (a superdisintegrant) were developed by spray drying in this study to improve the tableting properties of lactose. Factors affecting the properties of the coprocessed excipients were investigated by a 3 × 3 × 2 factorial design. These factors include lactose grade (90 M, 200 M, and 450 M), percentage of HPMC (3.5%, 7.0%, and 10.5%), and percentage of PVPP (0% and 3.5%). The results show that the compactability of the excipients could be significantly improved by increasing either the percentage of HPMC or the primary particle size of lactose. The addition of 3.5% PVPP had little effect on the compactability, but significantly improved the disintegration ability. The developed coprocessed excipients have much lower yield pressures and much higher working efficiency during tableting compared to the main raw material (α-lactose monohydrate). These improvements are mainly attributed to the addition of HPMC and the proximately 30% amorphous lactose formed during process. Both HPMC and amorphous lactose were homogeneously distributed on the surface of the secondary particles, maximizing their effect. Furthermore, the low hygroscopicity and high glass transition temperature of HPMC led to a high yield. The drug loading capacity of the newly coprocessed excipients is also excellent. In summary, the tri-component coprocessed excipients investigated are promising and worthy of further development.
authors.affiliation: College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China; Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China.
authors.forename: SongTao
authors.initials: S
authors.lastname: Wang
authors.affiliation: College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China.
authors.forename: JinZhi
authors.initials: J
authors.lastname: Li
authors.affiliation: College of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China; Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China. Electronic address: duotang@163.com.
authors.forename: Xiao
authors.initials: X
authors.lastname: Lin
authors.affiliation: Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, PR China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Feng
authors.affiliation: Novartis Pharmaceuticals (China), Building 8, Halei Road 898, Shanghai 201203, PR China. Electronic address: xiang.kou@novartis.com.
authors.forename: Xiang
authors.initials: X
authors.lastname: Kou
authors.affiliation: Novartis Pharmaceuticals (China), Building 8, Halei Road 898, Shanghai 201203, PR China.
authors.forename: Sreehari
authors.initials: S
authors.lastname: Babu
authors.affiliation: Novartis institutes for biomedical research, Inc. 500 technology square, Cambridge, MA 02139, USA.
authors.forename: Riccardo
authors.initials: R
authors.lastname: Panicucci
mesh_terms: D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D065347:Hypromellose Derivatives / Q000737:chemistry*; D007785:Lactose / Q000737:chemistry*; D011205:Povidone / Q000031:analogs & derivatives* / Q000737:chemistry; D013607:Tablets
chemical_list: D005079:Excipients; D013607:Tablets; C077842:polyvinylpolypyrrolidone; D065347:Hypromellose Derivatives; D011205:Povidone; D007785:Lactose
keywords: Compactability; Coprocessed excipients; HPMC; Lactose; Spray drying