Correlation between in vitro and in vivo erosion behaviour of erodible tablets using gamma scintigraphy

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 77; no. 1; pp. 148 - 157
• Main Authors: Ghimire, Manish, Hodges, Lee Ann, Band, Janet, Lindsay, Blythe, O’Mahony, Bridget, McInnes, Fiona J., Mullen, Alexander B., Stevens, Howard N.E.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 2011; Elsevier
• Subjects: Adult; Biological and medical sciences; Cellulose - analogs & derivatives; Cellulose - chemistry; Cross-Over Studies; Delayed-Action Preparations - chemistry; Drug Compounding - methods; Drug Delivery Systems; Erosion; Excipients - chemistry; Fatty Acids - chemistry; Gamma scintigraphy; Gastrointestinal Transit; General pharmacology; Glyceryl behenate; Granulation method; Humans; In vitro/ in vivo correlation (IVIVC); Kinetics; Low-substituted hydroxypropylcellulose; Male; Medical sciences; Middle Aged; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Radionuclide Imaging; Solubility; Tablets; Technetium Tc 99m Pentetate - pharmacokinetics; Young Adult; Low-substituted hydroxypropylcellulose; Gamma scintigraphy; In vitro/ in vivo correlation (IVIVC); Granulation method; Glyceryl behenate; Erosion; Pharmaceutical technology; Granulation; In vitro/in vivo correlation (IVIVC); Scintigraphy; In vitro; In vivo; Cellulose derivatives; Dosage form; Cellulose(hydroxypropyl); Tablet; Cellulose ether; In vitro in vivo correlation
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2010.10.005

Effect of manufacturing methods on in vitro and in vivo erosion profiles of wax-disintegrant based matrix tablets using gamma scintigraphy. In vitro and in vivo erosion behaviour of erodible tablets consisting of glyceryl behenate and low-substituted hydroxypropylcellulose manufactured using three different methods: direct compression (DC), melt granulation (MG) and direct solidification (DS) was investigated. In vitro erosion behaviour was studied using gravimetric and scintigraphic methods. For scintigraphic investigations, the radiolabel was adsorbed onto activated charcoal and incorporated into tablets at a concentration that did not affect the erosion profile. A clinical study was carried out in six healthy volunteers using gamma scintigraphy. Tablet erosion was affected by the preparation method and was found to decrease in the order of preparation method, DC > MG > DS tablets. The mean in vivo onset time for all tablets (DC: 6.7 ± 3.8 min, MG: 18.3 ± 8.1 min, DS: 67 ± 18.9 min) did not differ significantly from in vitro onset time (DC: 5.3 ± 1 min, MG: 16.8 ± 3.9 min, DS: 61.8 ± 4.7 min). The mean in vivo completion times were found to be 36.6 ± 9.7 (DC tablets), 70 ± 18.3 min (MG tablets) and 192.5 ± 39.9 min (DS tablets). Among the three different erodible tablets, MG tablets showed the highest correlation between in vitro and in vivo mean erosion profile and suggested a potential platform to deliver controlled release of water-insoluble compounds.