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( Prabagar Balakrishnan ),( Chung Kil Song ),( Hyun Ji Cho ),( Su Geun Yang ),( Dae Duk Kim ),( Chul Soon Yong ),( Han Gon Choi ) 영남대학교 약품개발연구소 2012 영남대학교 약품개발연구소 연구업적집 Vol.22 No.0
To study the effect of β-cyclodextrin (βCD) inclusion complex on the bioavailability of clotrimazole frompoloxamer-based suppository, formulations composed of P 188, propylene glycol and different molar ratio of clotrimazole-βCD inclusion complex were prepared. Clotrimazole (1%) has been formulated in a suppository using the thermo sensitive polymer P188 (70%) together with propylene glycol (30%). To increase its aqueous solubility, clotrimazole was incorporated as its inclusion complex at various molar ratios with βCD (1:0.25, 1:0.5, 1:1, and 1:2). The inclusion complex was characterized by differential scanning calorimetry (DSC), XRD and phase solubility studies. It was observed that the complexation with βCD, particularly at high molar ratio (F3 (1:1) and F4 (1:2)) decreased the release profile of clotrimazole considerably. However, suppositories containing inclusion complex at low molar ratio (F1 (1:0.25) and F2 (1:0.5)) showed excellent release profile compared to control formulation. In vivo study in rats at 15 mg/Kg dose showed that the F1 and F2 (82.39 ± 15.40 and 67.05 ± 8.79, respectively) significantly increased the AUC compared to that of F3 (41.48 ± 11.51), F4 (23.34 ± 8.37) and control (46.7 ± 7.87) suppositories. Thus, the suppositories containing inclusion complexes prepared at low drug to βCD molar ratio (F1) could be a potential suppository formulation to increase the bioavailability of hydrophobic drugs such as clotrimazole.
Prabagar Balakrishnan,최한곤,송충길,Hyun-Jong Cho,양수근,Dae Duk Kim,용철순 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.7
To study the effect of β-cyclodextrin (βCD) inclusion complex on the bioavailability of clotrimazole from poloxamer-based suppository, formulations composed of P 188, propylene glycol and different molar ratio of clotrimazole-βCD inclusion complex were prepared. Clotrimazole (1%) has been formulated in a suppository using the thermo sensitive polymer P188 (70%)together with propylene glycol (30%). To increase its aqueous solubility, clotrimazole was incorporated as its inclusion complex at various molar ratios with βCD (1:0.25, 1:0.5, 1:1, and 1:2). The inclusion complex was characterized by differential scanning calorimetry (DSC), XRD and phase solubility studies. It was observed that the complexation with βCD, particularly at high molar ratio (F3 (1:1) and F4 (1:2)) decreased the release profile of clotrimazole considerably. However, suppositories containing inclusion complex at low molar ratio (F1 (1:0.25) and F2 (1:0.5)) showed excellent release profile compared to control formulation. In vivo study in rats at 15 mg/Kg dose showed that the F1 and F2 (82.39 ± 15.40 and 67.05 ±8.79, respectively) significantly increased the AUC compared to that of F3 (41.48 ± 11.51), F4 (23.34 ± 8.37) and control (46.7 ± 7.87) suppositories. Thus, the suppositories containing inclusion complexes prepared at low drug to βCD molar ratio (F1) could be a potential suppository formulation to increase the bioavailability of hydrophobic drugs such as clotrimazole.
Enhanced Bioavailability of Poorly Water-Soluble Clotrimazole by Inclusion with β-Cyclodextrin
Balakrishnan Prabagar,Bong-Kyu Yoo,우종수,Jung-Ae Kim,이종달,Ming Guan Piao,최한곤,용철순 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.2
Clotrimazole, a poorly water-soluble antimycotic agent, is a promising agent for various diseases including cancer and sickle cell anemia. To improve the oral bioavailability of clotrimazole, the inclusion compound of clotrimazole with β-cyclodextrin was prepared by spray-drying method and characterized by phase solubility, differential scanning calorimetry and dissolution. Furthermore, the pharmacokinetics after oral administration in rats was then performed compared with clotrimazole powder. The solubility of clotrimazole increased linearly as a function of β-cyclodextrin concentration, resulting in AL type phase solubility diagram which revealed a formation of inclusion compound in a molar ratio of 1:2, with the apparent association constant of 230.2 M-1. The dissolution rate of clotrimazole in the inclusion compound increased greatly compared to clotrimazole powder in pH 7.4 phosphate buffer solution. The inclusion compound gave significantly higher initial plasma concentrations, Cmax and AUC of clotrimazole than did clotrimazole powder when they were administered as suspension form, indicating that the drug from inclusion compound could be more orally absorbed in rats. Thus, the oral bioavailability of clotrimazole could be improved markedly by inclusion complexation, possibly due to an increased dissolution rate.
Prabagar, Balakrishnan,Yoo, Bong-Kyu,Woo, Jong-Soo,Kim, Jung-Ae,Rhee, Jong-Dal,Piao, Ming Guan,Choi, Han-Gon,Yong, Chul-Soon 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.2
Clotrimazole, a poorly water-soluble antimycotic agent, is a promising agent for various diseases including cancer and sickle cell anemia. To improve the oral bioavailability of clotrimazole, the inclusion compound of clotrimazole with ${\beta}$-cyclodextrin was prepared by spray-drying method and characterized by phase solubility, differential scanning calorimetry and dissolution. Furthermore, the pharmacokinetics after oral administration in rats was then performed compared with clotrimazole powder. The solubility of clotrimazole increased linearly as a function of ${\beta}$-cyclodextrin concentration, resulting in A$_L$ type Phase solubility diagram Which revealed a formation of inclusion compound in a molar ratio of 1:2, with the apparent association constant of 230.2 M$^{-1}$. The dissolution rate of clotrimazole in the inclusion compound increased greatly compared to clotrimazole powder in pH 7.4 phosphate buffer solution. The inclusion compound gave significantly higher initial plasma concentrations, Cmax and AUC of clotrimazole than did clotrimazole powder when they were administered as suspension form, indicating that the drug from inclusion compound could be more orally absorbed in rats. Thus, the oral bioavailability of clotrimazole could be improved markedly by inclusion complexation, possibly due to an increased dissolution rate.
조현종,Prabagar Balakrishnan,Hongxia Lin,Min-Koo Choi,김대덕 한국약제학회 2012 Journal of Pharmaceutical Investigation Vol.42 No.3
Transport studies of model drugs were conducted across the human nasal epithelial (HNE) and normal human bronchial epithelial (NHBE) cell monolayers cultured by air–liquid interface method. Physicochemical properties (e.g., molecular weight, calculated partition coefficient, dose number) of model drugs were quoted from literatures and apparent permeability coefficients (Papp)across the HNE and NHBE cell monolayers were directly measured. A linear relationship was observed between the Papp values of model drugs in the HNE and NHBE cell monolayers. As the molecular weight of model drugs increased, the Papp showed a decreasing pattern while the increase of partition coefficients resulted in the increment of Papp. These results indicated that the transport of model drugs across both cell monolayers followed mainly the passive diffusion mechanism, although substrates mediated by drug transporters showed a deviating pattern. It was also interesting to note that almost all model drugs could be grouped into the same biopharmaceutics classification system as that classified by the human intestinal permeability when the Papp was plotted as a function of dose number (D0) of each drug.
Microemulsion-based Hydrogel Formulation of Itraconazole for Topical Delivery
( Eun A Lee ),( Prabagar Balakrishnan ),( Chung Kil Song ),( Joon Ho Choi ),( Ga Ya Noh ),( Chun Geon Park ),( Ae Jin Choi ),( Suk Jae Chung ),( Chang Koo Shim ),( Dae Duk Kim ) 한국약제학회 2010 Journal of Pharmaceutical Investigation Vol.40 No.5
Microemulsion-based Hydrogel Formulation of Itraconazole for Topical Delivery
Lee, Eun-A,Balakrishnan, Prabagar,Song, Chung-Kil,Choi, Joon-Ho,Noh, Ga-Ya,Park, Chun-Geon,Choi, Ae-Jin,Chung, Suk-Jae,Shim, Chang-Koo,Kim, Dae-Duk The Korean Society of Pharmaceutical Sciences and 2010 Journal of Pharmaceutical Investigation Vol.40 No.5
The present study was aimed at preparing microemulsion-based hydrogel (MBH) for the skin delivery of itraconazole. Microemulsion prepared with Transcutol as a surfactant, benzyl alcohol as an oil and the mixture of ethanol and phasphatidyl choline (3:2) as a cosurfactant were characterized by solubility, phase diagram, particle size. MBHs were prepared using 0.7 % of xanthan gum (F1-1) or carbopol 940 (F1-2) as gelling agents and characterized by viscosity studies. The in vitro permeation data obtained by using the Franz diffusion cells and hairless mouse skin showed that the optimized microemulsion (F1) consisting of itraconazole (1% w/w), benzyl alcohol (10% w/w), Transcutol (10% w/w) and the mixture of ethanol and phospahtidylcholine (3:2) (10% w/w) and water (49% w/w) showed significant difference in the flux (${\sim}1{\mu}g/cm^2/h$) with their corresponding MBHs (0.25-0.64 ${\mu}g/cm^2/h$). However, the in vitro skin drug content showed no significant difference between F1 and F1-1, while F1-2 showed significantly low skin drug content. The effect of the amount of drug loading (0.02, 1 and 1.5% w/w) on the optimized MBH (F1-2) showed that the permeation and skin drug content increased with higher drug loading (1.5%). The in vivo study of the optimized MBH (F1-2 with1.5% w/w drug loading) showed that this formulation could be used as a potential topical formulation for itraconazole.