title: Effect of different excipients on the physical characteristics of granules and tablets with carbamazepine prepared with polyethylene glycol 6000 by fluidized hot-melt granulation (FHMG).
abstract: The objective of this study was to investigate the properties of granules and tablets with carbamazepine which were prepared employing a fluidized hot-melt granulation (FHMG) technique. The FHMG process was carried out at 65°C. Macrogol 6000 (PEG 6000) was used as a binder at the content 10% (w/w) of the granulated mass. Granules containing up to 70% (w/w) of the drug and 20-90% (w/w) of a filler (lactose, mannitol, calcium hydrogen phosphate (Di-Cafos), pregelatinized starch, and microcrystalline cellulose (MCC)) were produced. When the drug content was 30% (w/w), the yield of the process was satisfying (>95%) and flowability of the granules was better than placebo granules or drug-loaded granules prepared by wet granulation. Type of a filler had strong impact on physical properties of granules, and size distribution of the particles was the most homogenous when lactose or Di-Cafos were used. The FHMG technique enabled preparation of granules with better compressability compared with the wet-granulated product or with non-granulated powders. Tablets with shorter disintegration time than 10 min were obtained with 2.0% crospovidone added as a disintegrant. In comparison to tablets prepared from the wet-granulated mass, employment of the FHMG method resulted in tablets with faster dissolution of carbamazepine (more than 80% of the drug released within 15 min). This was achieved with mannitol or lactose/MCC, as fillers.
authors.affiliation: Pharmaceutical Works Polpharma SA, Starogard Gdański, Poland. radoslaw.kraciuk@polpharma.com
authors.forename: Radosław
authors.initials: R
authors.lastname: Kraciuk
authors.forename: Malgorzata
authors.initials: M
authors.lastname: Sznitowska
mesh_terms: D000927:Anticonvulsants / Q000737:chemistry*; D002130:Calcium Phosphates / Q000737:chemistry; D002220:Carbamazepine / Q000737:chemistry*; D002482:Cellulose / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D006358:Hot Temperature; D007700:Kinetics; D007785:Lactose / Q000737:chemistry; D008353:Mannitol / Q000737:chemistry; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D011208:Powders; D012995:Solubility; D013213:Starch / Q000737:chemistry; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods
chemical_list: D000927:Anticonvulsants; D002130:Calcium Phosphates; D004337:Drug Carriers; D005079:Excipients; D011208:Powders; D013607:Tablets; D002220:Carbamazepine; D008353:Mannitol; D011092:Polyethylene Glycols; D002482:Cellulose; D013213:Starch; D007785:Lactose; C485829:calcium phosphate, dibasic, anhydrous; C109691:microcrystalline cellulose