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Bhandari, Krishna Hari,Newa, Madhuri,Yoon, Sung II,Kim, Jung Sun,Jang, Ki Young,Kim, Jung-Ae,Yoo, Bong Kyo,Woo, Jong Soo,Lee, Jae Hwi,Kim, Dae Duk,Choi, Hang Gon,Yong, Chul Soon Pharmaceutical Society of Japan 2007 BIOLOGICAL & PHARMACEUTICAL BULLETIN Vol.30 No.11
<P>The purpose of this study was to evaluate the physicochemical properties, skin permeation and accumulation profiles of model lipophilic ketorolac fatty ester (esters) prodrugs. Ketorolac linoleate (C18:2), oleate (C18:1) and stearate (C18:0) were evaluated for their solubility, capacity factor, enzymatic hydrolysis, chemical stability, and skin permeation and accumulation profiles using the combination of common permeation enhancing techniques such as the use of supersaturated solution of permeants in the enhancer vehicle, lipophilic receptor solution, enhancer pretreatment of skins, removal of stratum corneum and delipidization of skins <I>etc</I>. Esters were highly lipophilic, chemically stable for the duration of observation, enzymatically unstable in hairless mouse skin/liver homogenates and plasma, and impermeable into the receptor solution. Absence of skin permeation, relative enzymatic stability during permeation and chemical stability of these esters could delineate preliminary possibilities for designing safer topical agents without systemic absorption.</P>
Bhandari, Krishna Hari,Newa, Madhuri,Kim, Jung Ae,Yoo, Bong Kyu,Woo, Jong Soo,Lyoo, Won Seok,Lim, Hyun Tae,Choi, Han Gon,Yong, Chul Soon Pharmaceutical Society of Japan 2007 Biological & pharmaceutical bulletin Vol.30 No.6
<P>Phase solubility behavior of coenzyme Q10 (CoQ10) at 25 °C in various molar solutions of poloxamer 188 (P188) in water was observed and their binary solid dispersions (BSD) at different weight ratios were prepared by a simple, rapid, cost effective, uncomplicated and potentially scalable low temperature melting method. BSDs were characterized by scanning electron microscopy (SEM) and differential scanning calorimetry (DSC), and evaluated for improved solubility at 25 °C and 37 °C and <I>in-vitro</I> release of CoQ10 at 37 °C in distilled water. Solubility of CoQ10 increased with increasing concentrations of P188 in water. Gibbs free energy (Δ<I>G</I>°<SUB>tr</SUB>) values were all negative indicating the spontaneous nature of CoQ10 solubilization and decreased with increasing concentration of P188 demonstrating that the reaction conditions became more favorable as the concentration of P188 increased. DSC and SEM analysis indicated that the homogeneity of dispersion was not at the molecular level. However, BSDs exhibited a remarkably improved aqueous solubility and dissolution of CoQ10.</P>
Evaluation of Skin Permeation and Accumulation Profiles of a Highly Lipophilic Fatty Ester
Bhandari, Krishna Hari,Lee, Dong-Xun,Newa, Madhuri,Yoon, Sung-Il,Kim, Jung-Sun,Kim, Dae-Duk,Kim, Jung-Ae,Yoo, Bong-Kyo,Woo, Jong-Soo,Lyoo, Won-Seok,Lee, Jae-Hwi,Choi, Han-Gon,Yong, Chul-Soon 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.2
The aim was to evaluate the skin permeation and accumulation profiles of a highly lipophilic fatty ester using the combination of various permeation enhancing techniques to study the potential of highly lipophilic fatty esters as local topical agents. Permeation and accumulation profiles of ketorolac stearate (C18:0) were studied using solubility improved formulation, supersaturated solution of permeant in enhancer vehicle, lipophilic receptor solution, enhancer pretreatment, and the removal of stratum corneum and delipidization of skins. Impermeability and minimal skin accumulation of ketorolac stearate could delineate a preliminary possibility for designing safer topical agents without systemic absorption.
Evaluation of Skin Permeation and Accumulation Profiles of a Highly Lipophilic Fatty Ester
Krishna Hari Bhandari,김정선,이동훈,Madhuri Newa,Sung II Yoon,김대덕,김정애,유봉규,우종수,류원석,이재휘,최한곤,용철순 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.2
The aim was to evaluate the skin permeation and accumulation profiles of a highly lipophilic fatty ester using the combination of various permeation enhancing techniques to study the potential of highly lipophilic fatty esters as local topical agents. Permeation and accumulation profiles of ketorolac stearate (C18:0) were studied using solubility improved formulation, supersaturated solution of permeant in enhancer vehicle, lipophilic receptor solution, enhancer pretreatment, and the removal of stratum corneum and delipidization of skins. Impermeability and minimal skin accumulation of ketorolac stearate could delineate a preliminary possibility for designing safer topical agents without systemic absorption.
Newa, Madhuri,Bhandari, Krishna Hari,Li, Dong Xun,Kim, Jong Oh,Yoo, Dong Sung,Kim, Jung-Ae,Yoo, Bong-Kyu,Woo, Jong-Soo,Choi, Han-Gon,Yong, Chul-Soon Pharmaceutical Society of Japan 2008 Biological & pharmaceutical bulletin Vol.31 No.5
<P>To improve its dissolution, ibuprofen solid dispersions (SDs) were prepared in a relatively easy and simple manner, characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR), and evaluated for solubility, <I>in-vitro</I> drug release and oral bioavailability of ibuprofen in rats. Loss of individual surface properties during melting and resolidification as revealed by SEM micrographs indicated the formation of effective SDs. Absence or shifting towards the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of drug–polymer interactions. FT-IR spectra showed the presence of drug crystalline in SDs. Quicker release of ibuprofen from SDs in rat intestine resulted in a significant increase in <I>AUC</I> and <I>C</I><SUB>max</SUB>, and a significant decrease in <I>T</I><SUB>max</SUB> over pure ibuprofen. Preliminary results from this study suggested that the preparation of fast dissolving ibuprofen SDs by low temperature melting method using polyethylene glycol 4000 (PEG 4000) as a meltable hydrophilic polymer carrier could be a promising approach to improve solubility, dissolution and absorption rate of ibuprofen.</P>
Life Science : Enhanced Dissolution of Ibuprofen Using Solid Dispersion with Poloxamer 407
( Madhuri Newa ),( Krishna Hari Bhandari ),( Dong Hoon Oh ),( Young Ran Kim ),( Joon Ho Sung ),( Jong Oh Kim ),( Jong Soo Woo ),( Hang Gon Choi ),( Chul Soon Yong ) 영남대학교 약품개발연구소 2009 영남대학교 약품개발연구소 연구업적집 Vol.19 No.-
Enhanced Dissolution of Ibuprofen Using Solid Dispersion with Poloxamer 407
Newa, Madhuri,Bhandari, Krishna Hari,Oh, Dong-Hoon,Kim, Young-Ran,Sung, Joon-Ho,Kim, Jong-Oh,Woo, Jong-Soo,Choi, Han-Gon,Yong, Chul-Soon 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.11
To improve its dissolution, ibuprofen solid dispersions (SDs) were prepared, characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR), and evaluated for solubility, and in-vitro ibuprofen release. Loss of individual surface properties during melting and re-solidification as revealed by SEM micrographs indicated the formation of effective SDs. Absence or shifting towards the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of drug-polymer interactions. FTIR spectra showed the presence of drug crystalline in SDs. The effect of improved dissolution on the oral absorption of ibuprofen in rats was also studied. Quicker release of ibuprofen from SDs in rat intestine resulted in a significant increase in AUC and $C_{max}$, and a significant decrease in $T_{max}$ over pure ibuprofen. Comparison of the enhanced solubility, dissolution, AUC, and $C_{max}$ of ibuprofen from different poloxamers suggested that the preparation of ibuprofen SDs using P 407 as a meltable hydrophilic polymer carrier could be a promising approach to improve its solubility, dissolution and absorption rate.
Enhanced Dissolution of Ibuprofen Using Solid Dispersion with Poloxamer 407
Madhuri Newa,Krishna Hari Bhandari,오동훈,김영란,성준호,김종호,우종수,최한곤,용철순 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.11
To improve its dissolution, ibuprofen solid dispersions (SDs) were prepared, characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR), and evaluated for solubility, and in-vitro ibuprofen release. Loss of individual surface properties during melting and re-solidification as revealed by SEM micrographs indicated the formation of effective SDs. Absence or shifting towards the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of drug-polymer interactions. FTIR spectra showed the presence of drug crystalline in SDs. The effect of improved dissolution on the oral absorption of ibuprofen in rats was also studied. Quicker release of ibuprofen from SDs in rat intestine resulted in a significant increase in AUC and Cmax, and a significant decrease in Tmax over pure ibuprofen. Comparison of the enhanced solubility, dissolution, AUC, and Cmax of ibuprofen from different poloxamers suggested that the preparation of ibuprofen SDs using P 407 as a meltable hydrophilic polymer carrier could be a promising approach to improve its solubility, dissolution and absorption rate.