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Suharto Chakma,Prakash Khadka,조강희,김형민,노지은,박경희,Sandeep Karki,Sonia Barua,이재휘 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.5
Celecoxib is a non-steroidal, anti-inflammatory drug used in the treatment of pain and inflammation associated with rheumatoid arthritis, and several other inflammatory disorders. It is a class II compound according to the Biopharmaceutics Classification System owing to its low water solubility and high membrane permeability. The objective of this study was to improve the solubility and dissolution rate of celecoxib using solid surfactant technology that might be useful in developing solid dosage forms. Solid surfactant was developed by mixing and grinding together a liquid surfactant (Tween 80) with various inorganic carriers like FujicalinⓇ (Dibasic Calcium Phosphate Anhydrous), PineflowⓇ (Porous-structured Maltodextrin), NeusilinⓇ (Magnesium Alumino metasilicate) and AerosilⓇ (Colloidal Silicon dioxide) in a mortar and pestle in different ratios of liquid surfactant and the carrier to obtain solid surfactants. The celecoxib tablets prepared with solid surfactants were then evaluated for their solubility and dissolution properties. Among the fillers used, Fujicalin showed the highest solubilization capacity for celecoxib. The dissolution behaviors of various tablets prepared with solidified surfactants were compared to those of conventional celecoxib tablets in a simulated gastric fluid. Celecoxib tablets prepared using solidified surfactants showed improved dissolution behaviors when compared to the conventional counterparts. Fujicalin solidified Tween 80 was further analyzed by powder X-ray diffraction analysis, differential scanning calorimetry thermographs and reverse phase high performance liquid chromatography.
박석용,최성업,이경혜,양종범,조승완,노지은,김형민,Prakash Khadka,이재휘,조정원 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.8
This study aimed at the evaluation of plasma level profiles of choline produced after the oral administration of choline alphoscerate (CA). For this purpose, a high-performance liquid chromatography/tandem mass spectrometry (HPLC/MS/MS) analytical method was developed and validated. Baseline correction technique was employed to monitor the CA-related choline in plasma by subtracting background levels of choline from total choline levels measured after the drug administration. Choline was well separated in the plasma matrix under the analytical conditions employed for HPLC/MS/MS and the analytical method developed for the monitoring of choline in plasma was well validated. The endogenous choline levels in plasma under fasting condition were measured to be 7.78 ± 1.74 µmol/L for test period 1 and 7.88 ± 1.78 µmol/L for test period 2, respectively, and were considerably increased after consumption of meals. The corrected choline levels in plasma produced only by the oral administration of CA could be evaluated by subtracting the background levels of choline monitored before the drug was administered. The pharmacokinetic parameters estimated for test and control formulations were quite similar based on the comparison of Cmax, AUC12h , and T max, indicating that these are biologically equivalent dosage forms. The results of our study consequently suggest that the baseline correction method in evaluating plasma concentration profiles of endogenous substances is useful.
노지은,김영석,김형민,박경희,이권은,Prakash Khadka,윤지애,박주현,장숙태,이종휘,정지훈,이재휘 대한약리학회 2015 The Korean Journal of Physiology & Pharmacology Vol.19 No.1
Retinyl palmitate (RP)-loaded pectinate micro- and nano-particles (PMP and PNP) were designedfor stabilization of RP that is widely used as an anti-wrinkle agent in anti-aging cosmeceuticals. PMP/PNP were prepared with an ionotropic gelation method, and anti-oxidative activity of the particleswas measured with a DPPH assay. The stability of RP in the particles along with pectin gel andethanolic solution was then evaluated. In vitro release and skin permeation studies were performedusing Franz diffusion cells. Distribution of RP in each skin tissue (stratum corneum, epidermis, anddermis) was also determined. PMP and PNP could be prepared with mean particle size diameters of593∼843 μm (PMP) and 530 nm (i.e., 0.53 μm, PNP). Anti-oxidative activity of PNP was greaterthan PMP due largely to larger surface area available for PNP. The stability of RP in PMP and PNPwas similar but much greater than RP in pectin bulk gels and ethanolic solution. PMP and PNP showedthe abilities to constantly release RP and it could be permeated across the model artificial membraneand rat whole skin. RP was serially deposited throughout the skin layers. This study implies RP loadedPMP and PNP are expected to be advantageous for improved anti-wrinkle effects.
Ro, Jieun,Kim, Yeongseok,Kim, Hyeongmin,Park, Kyunghee,Lee, Kwon-Eun,Khadka, Prakash,Yun, Gyiae,Park, Juhyun,Chang, Suk Tai,Lee, Jonghwi,Jeong, Ji Hoon,Lee, Jaehwi The Korean Society of Pharmacology 2015 The Korean Journal of Physiology & Pharmacology Vol.19 No.1
Retinyl palmitate (RP)-loaded pectinate micro- and nano-particles (PMP and PNP) were designed for stabilization of RP that is widely used as an anti-wrinkle agent in anti-aging cosmeceuticals. PMP/PNP were prepared with an ionotropic gelation method, and anti-oxidative activity of the particles was measured with a DPPH assay. The stability of RP in the particles along with pectin gel and ethanolic solution was then evaluated. In vitro release and skin permeation studies were performed using Franz diffusion cells. Distribution of RP in each skin tissue (stratum corneum, epidermis, and dermis) was also determined. PMP and PNP could be prepared with mean particle size diameters of $593{\sim}843{\mu}m$ (PMP) and 530 nm (i.e., $0.53{\mu}m$, PNP). Anti-oxidative activity of PNP was greater than PMP due largely to larger surface area available for PNP. The stability of RP in PMP and PNP was similar but much greater than RP in pectin bulk gels and ethanolic solution. PMP and PNP showed the abilities to constantly release RP and it could be permeated across the model artificial membrane and rat whole skin. RP was serially deposited throughout the skin layers. This study implies RP loaded PMP and PNP are expected to be advantageous for improved anti-wrinkle effects.
In vitro Metabolic Modulation of Aryl Sulfotransferases by Pharmaceutical Excipients
Ro, Jieun,Kim, Hyeongmin,Shim, Byung Ho,Kim, Iksoo,Kim, Jeong Tae,Kim, Hyunil,Cho, Jae Min,Khadka, Prakash,Yun, Gyiae,Park, Kyunghee,Park, Young Joo,Lee, Kwon-Eun,Han, Jeongoh,Lee, Jaehwi Korean Chemical Society 2014 Bulletin of the Korean Chemical Society Vol.35 No.8
( Ik Soo Kim ),( Hyeong Min Kim ),( Jie Un Ro ),( Kang Hee Jo ),( San Deep Karki ),( Prakash Khadka ),( Gyi Ae Yun ),( Jae Hwi Lee ) 한국응용약물학회 2015 Biomolecules & Therapeutics(구 응용약물학회지) Vol.23 No.3
β-Lapachone has drawn increasing attention as an anti-inflammatory and anti-cancer drug. However, its oral bioavailability has not been yet assessed, which might be useful to develop efficient dosage forms possibly required for non-clinical and clinical studies and future market. The aim of the present study was thus to investigate pharmacokinetic properties of β-lapachone as well as its first-pass metabolism in the liver, and small and large intestines after oral administration to measure the absolute bioavailability in rats. A sensitive HPLC method was developed to evaluate levels of β-lapachone in plasma and organ homogenates. The drug degradation profiles were examined in plasma to assess the stability of the drug and in liver and intestinal homogenates to evaluate first-pass metabolism. Pharmacokinetic profiles were obtained after oral and intravenous administration of β-lapachone at doses of 40 mg/kg and 1.5 mg/kg, respectively. The measured oral bioavailability of β-lapachone was 15.5%. The considerable degradation of β-lapachone was seen in the organ homogenates but the drug was quite stable in plasma. In conclusion, we suggest that the fairly low oral bioavailability of β-lapachone may be resulted from the first-pass metabolic degradation of β-lapachone in the liver, small and large intestinal tracts and its low aqueous solubility.