title: A drug release study from hydroxypropylmethylcellulose (HPMC) matrices using QSPR modeling.
abstract: This investigation is aimed at characterization of the mode of release from two different substitution types of HPMC and the effect of chemical structure of drugs using the QSPR (Quantitative - Structure-Property Relationship) technique. To this end, release profiles of HPMC matrices of several drugs containing the same formulation and compressed at a constant pressure were studied. QSPR method was used to establish statistically significant relationships between release parameters and the structural descriptors. Structural descriptors consisted of molecular mechanical, quantum mechanical and graph-theoretical parameters, as well as the partition coefficient and the aqueous solubility of the drugs. The results showed that the most important factors determining the release profile from both HPMC K4M and HPMC E4M matrices were the aqueous solubility of drugs (which could be substituted efficiently by dipole moment) and the size of the drug molecules. Comparison of drug release from matrices prepared using the two grades of HPMC showed very distinct differences for some drugs, as evaluated by the similarity factor. The results indicated that the source of the difference could be sought in the drug properties (as exemplified by the aqueous solubility and surface area) as well as the rate of erosion (that depends mainly on the polymer type).
authors.affiliation: Drug Applied Research Center and School of Pharmacy, Tabriz University of Medical Sciences, Daneshgah Street, Tabriz, Iran. t.ghafourian@kent.ac.uk
authors.forename: Taravat
authors.initials: T
authors.lastname: Ghafourian
authors.forename: Taravat
authors.initials: T
authors.lastname: Gafourian
authors.forename: Arezoo
authors.initials: A
authors.lastname: Safari
authors.forename: Khosro
authors.initials: K
authors.lastname: Adibkia
authors.forename: Fatemeh
authors.initials: F
authors.lastname: Parviz
authors.forename: Ali
authors.initials: A
authors.lastname: Nokhodchi
mesh_terms: D002626:Chemistry, Pharmaceutical; D004058:Diffusion; D004337:Drug Carriers; D004339:Drug Compounding; D065347:Hypromellose Derivatives; D007700:Kinetics; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D008956:Models, Chemical; D015233:Models, Statistical; D015394:Molecular Structure; D008970:Molecular Weight; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D011312:Pressure; D021281:Quantitative Structure-Activity Relationship; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods*
chemical_list: D004337:Drug Carriers; D004364:Pharmaceutical Preparations; D065347:Hypromellose Derivatives; D008747:Methylcellulose