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전명관,Kamal Hossain,Seung-Hyuk Choi,Sang-Jun Ban,Hwansig Moon,최후균 한국약제학회 2012 Journal of Pharmaceutical Investigation Vol.42 No.3
A novel transdermal drug delivery system with the eutectic mixture of lidocaine and prilocaine was developed. The permeation of lidocaine and prilocaine proportionally increased as the weight ratio of poly(vinyl alcohol) to poly(acrylic acid) changed from 1:1 to 7:1. However, the adhesive property of the matrix significantly degraded over the ratio of 5:1. The incorporation of humectants in the matrix had a noticeable effect on the permeation of lidocaine and prilocaine. The flux of lidocaine increased as the ratio of lidocaine in the eutectic mixture increased. The permeation rate decreased significantly from the cataplasm containing 3.5:1 and 4:1 ratio of lidocaine to prilocaine due to recrystallization. When total drug concentration of the cataplasm with the ratio of 3:1increased from 1.33 to 4 % against adhesive gel weight, the permeation of both lidocaine and prilocaine increased. However, crystallization was observed beyond 2.66 % w/w of combined drug load. Enhancers were not effective in the present study as most of the enhancer showed very low or no enhancement effect. No significant changes in the appearance and the drug content in the cataplasm were observed for 3 months.
Application of Carbopol/PVP interpolymer complex to prepare mucoadhesive floating granule
전명관,Prabhat Bhusal,최후균 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.6
Novel mucoadhesive floating granule was preparedusing Carbopol/PVP interpolymer complex to deliverhydrophilic drugs in a controlled manner. Acetaminophenwas used as a model drug. Maximum floatability of thegranules was obtained at the ratio of 1/1, where 95 % of thegranules floated for 12 h. As the concentration of sodiumbicarbonate increased, both the floating duration and therelease rate of the drug increased. The granules withoutsodium bicarbonate floated only for 2 h and floating onsettime was 15 min. The release rate of drug graduallyincreased as the drug content in the granule increased. Asthe drug content in the granules increased, duration ofadhesion decreased. However, the decrease in adhesionduration was minimal up to 40 % of drug content. Therelease rate from the granules prepared by dry granulationmethod was faster than that by wet granulation. Thegranules prepared by dry granulation method led to formationof highly porous structure; whereas, that by wetgranulation method showed non-porous structure. Theoptimum size of the granules to retard the release of themodel drug was within the range of 3–4 mm. Based onboth mucoadhesive and buoyant properties, the floatinggranules are expected to reside in the upper part of thestomach for sufficient period of time and release the drug ina sustained manner.
이명학,전명관,최후균 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.7
Chitosan/Carbopol®971NF (poly acrylic acid) interpolymer complexes were prepared in pH 3.0, 4.0, and 5.0 medium to control the ratio of chitosan and Carbopol®971NF in the interpolymer complex. FT-IR analysis confirmed that the mechanism of complexation involved an electrostatic interaction between the NH3 + of chitosan and COO− of Carbopol®971NF. An increase in the pH of the preparation medium was accompanied by an increase in the ratio of chitosan in the chitosan/Carbopol®971NF complex. The maximum yield of interpolymer complexes prepared at pH 3, 4, and 5 (IPC3, IPC4, IPC 5) were obtained at ratios of 1/10, 1/5, and 1/4 (chitosan/Carbopol®971NF), respectively. At pH 1.2, the overall drug release from IPC tablets did not show significant differences. However, at pH 6.8, the rate of drug release from the IPC5 tablet was higher than that from the IPC4 tablet. The release rate from the IPC3 tablet was observed to increase with time. The release mechanism was increasingly dominated by the relaxational contribution in the order of IPC3, IPC5, and IPC4 at pH 6.8. The diffusional contribution was dominated only in the early stage of drug release and the relaxational contribution gradually increased with time.
Solid Dispersion as a Strategy to Improve Drug Bioavailability
박준형,전명관,조훈,최후균,Park, Jun-Hyung,Chun, Myung-Kwan,Cho, Hoon,Choi, Hoo-Kyun The Korean Society for Biotechnology and Bioengine 2011 KSBB Journal Vol.15 No.6
Solid dispersion is one of well-established pharmaceutical techniques to improve the dissolution and consequent bioavailability of poorly water soluble drugs. It is defined as a dispersion of drug in an inert carrier matrix. Solid dispersions can be classified into three generations according to the carrier used in the system. First and second generations consist of crystalline and amorphous substances, respectively. Third generation carriers are surfactant, mixture of polymer and surfactants, and mixture of polymers. Solid dispersions can be generallyprepared by melting method and solvent method. While melting method requires high temperature to melt carrier and dissolve drug, solvent method utilizes solvent to dissolve the components. The improvement in dissolution through solid dispersions is attributed to reduction in drug particle size, improvement in wettability, and/or formation of amorphous state. The primary characteristics of solid dispersions, the presenceof drug in amorphous state, could be determined by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and fourier-transformed infrared spectroscopy (FTIR). In spite of the significant improvement in dissolution by solid dispersion technique, some drawbacks have limited the commercial application of solid dispersions. Thus, further studies should be conducted in a direction to improve the congeniality to commercialization.
Development of matrix based transdermal delivery system for ketotifen
이은영,최후균,전명관,장재상 한국약제학회 2014 Journal of Pharmaceutical Investigation Vol.44 No.4
The purpose of this study was to investigate thefeasibility of developing transdermal drug delivery systemfor ketotifen used for asthma, allergic conjunctivitis, andrhinitis. The permeation of ketotifen in silicone, polyisobutylene,styrene–butadiene–styrene and acrylic-rubberhybrid and acrylic pressure sensitive adhesive matrix wasevaluated. Due to good adhesion force and high permeability,acrylic-rubber hybrid adhesive was chosen. Permeationrate was found to increase linearly as the drugconcentration in acrylic-rubber hybrid adhesive increased. However, when the drug concentration was 5 % or more inthe matrix, recrystallization of ketotifen was observed. Therecrystallization process was not inhibited by crystallizationinhibitors tested. Significant increase in flux wasobtained using Brij 30, Crovol A40, Span 80 andLauroglycol FCC as permeation enhancers.
Development of transdermal drug delivery system of selegiline
이은영,최승혁,전명관,최후균 한국약제학회 2016 Journal of Pharmaceutical Investigation Vol.46 No.2
Selegiline transdermal drug delivery system (TDDS) of drug-in-adhesive matrix type was developed using acrylic-rubber hybrid pressure sensitive adhesive (PSA). The permeation rate of selegiline was the highest from silicone, followed by acrylic-rubber hybrid, acrylics. Although the permeation rate of silicone PSA was higher than that of acrylic-rubber hybrid PSA, the cold flow of silicone PSA was unacceptable. When the drug concentration was increased from 3.5 to 8 % w/w of polymer weight, the drug permeation rate also increased proportionally. The correlation coefficient (R2) between selegiline content in the TDDS and the average cumulative amount permeated was 0.999. When the stability study of the TDDS was carried out at the accelerated condition of 40 C/75 % relative humidity for 12 weeks, no significant changes in both the physical appearance and the drug content were observed. The drug permeation rate from the TDDS was much higher than that from Emsam. The average cumulative flux of selegiline from the TDDS was 2 times higher than that from Emsam.