A Theoretical-Empirical Analysis on the Initial Dissolution Rate of Drugs from Polydispersed Particles
スポンサーリンク
概要
- 論文の詳細を見る
The purpose of this work is to clarify the relationship of mean particle size to the dissolution rate of polydispersed particles for Biopharmaceutical Classification System (BCS) Class II drugs. An equation for the initial dissolution rate of polydispersed particles relative to mean particle diameter was theoretically derived from the Noyes–Whitney equation assuming spherical particles and sink conditions. To verify the relationship of dissolution to the mean particle diameters, the dissolution rates of 6 types of hypothetically-generated log-normal polydispersed particles and 3 different sized particles of aprepitant, a designated BCS class II drug, were compared with known mean diameters calculated according to surface area-weighted mean diameter (D3,2, commonly referred to as the Sauter mean diameter), length-weighted mean diameter (D3,1) and number-weighted mean diameter (D3,0). The results confirmed that the initial dissolution rates of polydispersed particles reflect the mean diameter and correlated best with the reciprocal of D3,2 at the start of dissolution, in accord with our theoretical conclusions. The particle size required for sufficient dissolution of aprepitant was also investigated by examining the relationship between D3,2 and oral absorption predicted using a physiological-based model.
- 公益社団法人 日本薬学会の論文
著者
-
HIGO Shoichi
Discovery Platform Technology Department, Chugai Pharmaceutical Co., Ltd.
-
Higo Shoichi
Discovery Platform Technology Department Chugai Pharmaceutical Co. Ltd.
-
Yamashita Shinji
Faculty Of Pharmaceutical Sciences Setsunan University
-
Takano Ryusuke
Discovery Platform Technology Department, Chugai Pharmaceutical Co., Ltd.
-
Takata Noriyuki
Discovery Platform Technology Department, Chugai Pharmaceutical Co., Ltd.
-
Shiraki Koji
Discovery Platform Technology Department, Chugai Pharmaceutical Co., Ltd.
-
Hayashi Yoshiki
Pre-clinical Research Department, Chugai Pharmaceutical Co., Ltd.
関連論文
- Investigation of the Intestinal Permeability and First-Pass Metabolism of Drugs in Cynomolgus Monkeys Using Single-Pass Intestinal Perfusion
- Slow Release of Tetracycline from a Mucoadhesive Complex with Sucralfate for Eradication of Helicobacter pylori
- P-gp誘導 Caco-2 細胞 : P-gp高感度 Assay System の構築
- ELECTROPHYSIOLOGICAL INVERSTIGATIONS ON THE DRUG PERMEATION ACROSS STRATUM CORNEUM (I)
- Effects of Sodium or Glucose Exclusion from the Incubation Medium on Drug Transfer across Rat Jejunal Membrane in Vitro : An Electrophysiological Study(Pharmaceutical)
- EFFECTS OF ABSORPTION PROMOTERS ON THE SELECTIVE PERMEABILITY OF RAT INTESTINAL MEMBRANE TO IONS : ANALYSIS OF PERMEABILITY ENHANCING MECHANISMS BY USING DIFFUSION POTENTIALS
- INVESTIGATIONS OF INFLUX AND ACCUMULATION PROCESSES OF β-LACTAM ANTIBIOTICS AND THEIR ROLE IN THE TRANSMURAL TRANSFER ACROSS RAT JEJUNUM
- FURTHER INVESTIGATIONS ON THE TRANSPORT MECHANISM OF CEPHALEXIN AND AMPICILLIN ACROSS RAT JEJUNUM
- EFFECT OF PHARMACEUTICAL ADJUVANTS ON THE RECTAL PERMEABILITY OF DRUGS
- ELECTROPHYSIOLOGICAL APPROACH TO THE ACTION OF TAURINE ON RAT GASTRIC MUCOSA
- New Methods to Evaluate Intestinal Drug Absorption Mediated by Oligopeptide Transporter from In vitro Study using Caco-2 Cells
- Quantitative Evaluation of the Gastrointestinal Absorption of Protein into the Blood and Lymph Circulation
- Effect of Experimental Acute Renal and Hepatic Failure on Absorption of Tacrolimus in Rat Small Intestine
- 消化管の efflux 機構は,"Phase ゼロ"の elimination!?
- Evaluation of Human P-Glycoprotein (MDR1/ABCB1) ATPase Activity Assay Method by Comparing with in Vitro Transport Measurements : Michaelis-Menten Kinetic Analysis to Estimate the Affinity of P-Glycoprotein to Drugs(Biopharmacy)
- Application of Dissolution-Permeation/PAMPA System for Prediction of Oral Drug Absorption of Nanoparticle
- In Vitro Dissolution/Permeation System to Predict the Oral Absorption of Poorly Water-Soluble Drugs: Effect of Food and Dose Strength on It
- A Theoretical-Empirical Analysis on the Initial Dissolution Rate of Drugs from Polydispersed Particles
- DEGRADATION AND PERMEATION OF PEPTIDE DRUGS IN RAT SMALL INTESTINE AND CACO-2 CELL SYSTEMS
- Effect of Experimental Acute Renal and Hepatic Failure on Absorption of Tacrolimus in Rat Small Intestine
- Preparation of spray-dried microparticles using Gelucire 44/14 and porous calcium silicate or spherical microcrystalline cellulose to enhance transport of water-insoluble pranlukast hemihydrate across Caco-2 monolayers