Box-Behnken experimental design in the development of pectin-compritol ATO 888 compression coated colon targeted drug delivery of mesalamine

Abstract

A novel oral colon-specific drug delivery system (CDDS) has been developed as one of the site-specific drug delivery systems. This delivery system, by means of combining one or more controlled release mechanisms, hardly releases the drug in the upper part of the gastrointestinal (GI) tract, but rapidly releases drug in the colon following oral administration. The necessity and advantage of CDDS have been recognized and reviewed recently (1-3). Owing to CDDS specifically delivering the drug to the colon, many bene- The aim of this study was to investigate the combined influence of 3 independent variables in the compression coated tablet of mesalamine for ulcerative colitis. A 3--factor, 3-level Box-Behnken design was used to derive a second order polynomial equation and construct contour plots to predict responses. The independent variables selected were: percentage of polymers (pectin and compritol ATO 888) in compression coating (X 1 ), coating mass (X 2 ) and coating force (X 3 ). Fifteen batches were prepared and evaluated for percent of drug released in 5 h (Y 5 ), time required for 50 % mesalamine to dissolve (t 50 ) with rat cecal (RC) content and without rat cecal content (t 50 ), percent of drug released in 24 h in the presence of rat cecal content (Y 24 with RC). Transformed values of independent and dependent variables were subjected to multiple regressions to establish a full-model second-order polynomial equation. F was calculated to confirm the omission of insignificant terms from the full-model equation. The computer optimization process and contour plots predicted the levels of independent variables X 1 , X 2 , and X 3 (0, 0.2 and -0.15, respectively) for colon targeting and total percent of drug released up to 24 h.

Development and characterization of novel hydrogel containing antimicrobial drug for treatment of burns

“…After the 10 th days postoperation, there was complete healing occurred in the A. vera based SSD cubogel with the formation of natural skin, while 70-80% healing occurred in cubogel with SSD and both has faster healing as compared to marketed preparation. [ 42 46 47 48 49 ] In vivo wound, healing study revealed that the cubogel with drug and A. vera shows no scar formation after healing because of antiscaring effect of A. vera and generate normal skin without scaring. [ 50 ] In marketed formulation, the pseudoeschar formed during the healing which hindered the permeation of drug so delay in healing and sometimes leading to infection in the wound.…”

Evolution of the Microstructure of Sustained-release Matrix Tablets during Dissolution and Storage

“…Lipid matrix tablets [8] containing lipid excipients having a melting point higher than 40° and a low polarity are used to sustain drug release [9] . Among such lipids, glyceryl dibehenate (Compritol ® 888 ATO, melting point ranging from 69° to 74° and hydrophilic-lipophilic value of 1) was originally introduced as a lubricant [10] but is now widely used by various techniques to obtain sustained-release tablets: direct compression [11][12][13][14][15][16][17] , wet granulation [18,19] , melt granulation [12][13][14]16,[20][21][22][23] , hot-melt coating [24] , and hot-melt extrusion [25,26] .…”

An Experimental Design Approach for Impurity Profiling of Valacyclovir-Related Products by RP-HPLC

“…Chemically, it is 2-[(2-amino-6-oxo-1,6-dihydro-9 H -purin-9-yl)methoxy]ethyl L-valinate ( Figure 1A ), used for the treatment of herpes simplex and herpes zoster. It is phosphorylated by viral thymidine kinase to acyclovir triphosphate (the active metabolite) which then inhibits herpes viral DNA replication by competitive inhibition of viral DNA polymerase, and by incorporation into and termination of the growing viral DNA chain [ 8 – 11 ].…”

“…Factorial experiments find extensive applications in all research fields which allow the investigation of multiple factors simultaneously and also the examination of one factor at different levels of the other factor or factors. The Box-Behnken experimental design (BBD), developed by Box and Behnken in 1980 is a useful response surface methodology, where the level of one of the factors is fixed at the centre level while combinations of all the levels of the other factors are applied [ 8 – 10 ]. Extensive literature surveys have reported several analytical techniques for the estimation of VCR in both bulk and dosage forms [ 11 – 23 ].…”