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정용진,서권일,이기동,윤광섭,강미정,김광수 동아시아식생활학회 1998 동아시아식생활학회지 Vol.8 No.1
To utilize deteriorated sweet persimmon effectively, response surface methodology(RSM) was used to determine the optimal vinegar fermentation conditions and monitored by a divided two stage fermentation. The optimum conditions for maximum alcohol content were obtained when the first stage (alcohol fermentation) was carried out with an initial sugar concentration of 18.5°Brix, agitation rate of 140.8 rpm, fermentation time of 127.6 hr. When sugar concentration was 14°Brix, maximum alcohol content(7.1%) was predicted at fermentation conditions of 160 rpm in agitation rate, 140 hr in fermentation time. The optimum conditions for maximum acidity were obtained when second stage(vinegar fermentation) was carried out 249.5 rpm in agitation rate, 148.8 hr in fermentation time. Predicted values at the optimum conditions were similar to experimental values.
( Youn Gee Seo ),( Dae Hwan Kim ),( Thiruganesh Ramasamy ),( Jeong Hwan Kim ),( Nirmal Marasini ),( Yu Kyoung Oh ),( Dong Wuk Kim ),( Jin Ki Kim ),( Chul Soon Yong ),( Jong Oh Kim ),( Han Gon Choi ) 영남대학교 약품개발연구소 2013 영남대학교 약품개발연구소 연구업적집 Vol.23 No.0
The main purpose of this study was to investigate the potential of self-nano-emulsifying drug delivery system (SNEDDS) in improving the bioavailability of docetaxel (DCT) and its chemotherapeutic effect. The DCT-loaded SNEDDS was prepared by employing rational blends of capryol 90, labrasol, and transcutol HP using ternary phase diagram. The liquid nano-emulsion was spray-dried into solid SNEDDS (D-SNEDDS) using an inert porous carrier, colloidal silica. The optimized formulation was characterized in terms of physico-chemical and pharmacokinetic parameters. Furthermore, anti-tumor efficacy of D-SNEDDS was compared with commercial marketed product, Taxotere(®). The various compositions of SNEDDS were screened and found optimal at a volume ratio of 10/75/15 for capryol 90, labrasol, and transcutol HP, respectively. We observed a high oral bioavailability of 17% DCT for D-SNEDDS than compared to only 2.6% for pure DCT solution. Notably, D-SNEDDS exhibited an augmented anti-tumor efficacy with a reduced toxicity profile when compared with intravenously administered Taxotere(®), the commercialized formulation of DCT. Taken together, D-SNEDDS could be a potential candidate for an oral dosage form of DCT with enhanced antitumor activity and reduced toxicity. ⓒ2013 ELsevier B. B. All rights reserved.
( Youn Gee Seo ),( Dong Wuk Kim ),( Woo Hyun Yeo ),( Thiruganesh Ramasamy ),( Yu Kyoung Oh ),( Young Joon Park ),( Jung Ae Kim ),( Dong Hoon Oh ),( Sae Kwang Ku ),( Jin Ki Kim ),( Chul Soon Yong ),( J 영남대학교 약품개발연구소 2013 영남대학교 약품개발연구소 연구업적집 Vol.23 No.0
PURPOSE: To investigate the potential of thermosensitive and biadhesive nanomicelles in improving the bioavailability of docetaxel (DCT) and its chemotherapeutic effect. METHOD: DCT-loaded nanomicelles were prepared by emulsufication and characterized in terms of physico-chemical and visco-elastic parameters. The optimzed formulation was evaluated for in vivo localization, pharmacokinetic and anti-tumor efficacy. RESULTS: The hydrodynamic size of DCT-loaded nanomicelles was approximately 13 nm and thenanomicelles exhibited a sufficient gelation strength (9250 mPa·s) and bioadhesive force (2100 dyn/cm²) to be retained in the upper part of rectum. We observed a high rectal bioavailability of 29% DCT compared to that following oral administration in rats, as it successfully evaded the multidrug efflux transporters and hepatic first-pass metabolism. Plasma concentration around ∼50 ng/mL was maintained throughout the study period (12 h) while Taxotere® attained subtherapeutic range within 4 h of drug administration. Results also revealed that the rectally administered DCT-loaded nanomicellesexhibited a significant anti-tumor effect (200 mm³) with a reduced toxicity profile when compared to orally administered DCT (950 mm³). Furthermore, histological study showed that the rectal mucosa was completely intact with no signs of irritation upon treatment with DCT-loaded nanomicelles. CONCLUSIONS: Taken together, our novel thermosensitive and biadhesive nanomicellesdemonstrated the ability to improve the bioavailability and chemotherapeutic potential of DCT in vivo. To the best of our knowledge, this is the first report describing the rectal delivery of DCT-loaded nanomicelles.
( Youn Gee Seo ),( Dong Wuk Kim ),( Abid Mehmood Yousaf ),( Jong Hyuck Park ),( Pahn Shick Chang ),( Hyung Hee Baek ),( Soo Jeong Lim ),( Jong Oh Kim ),( Chul Soon Yong ),( Han Gon Choi ) 영남대학교 약품개발연구소 2015 영남대학교 약품개발연구소 연구업적집 Vol.25 No.-
To develop a novel self-nanoemulsifying drug delivery system (solid SNEDDS) with better oral bioavailability of tacrolimus, the solid SNEDDS was obtained by spray-drying the solutions containing the liquid SNEDDS and colloidal silica. Its reconstitution properties were determined and correlated to solid state characterisation of the powder. Moreover, the dissolution and pharmacokinetics in rats was done in comparison to the commercial product. Among the liquid SNEDDS formulations tested, the liquid SNEDDS comprised of Capryol PGMC, Transcutol HP and Labrasol (10:15:75, v/v/v) presented the highest dissolution rate. In the solid SNEDDS, this liquid SNEDDS was absorbed in the pores and attached onto the surface of the colloidal silica. Drug was present in the amorphous state in it. The solid SNEDDS with 5% w/v tacrolimus produced the nanoemulsions and improved the oral bioavailability of tacrolimus in rats. Therefore, this solid SNEDDS would be a potential candidate for enhancing the oral bioavailability of tacrolimus.
아지도싸이미딘의 지속성방출형담체로서의 소수성시클로덱스트린유도체
박기배,이광표,서보연 한국약제학회 1996 Journal of Pharmaceutical Investigation Vol.26 No.2
This study has been undertaken to evaluate hydrophobic cyclodextrin(CD) derivatives as a sustained release carrier of azidothymidine(AZT). AZT. which has potent activity against AIDS and AIDS-related complex as thymidine analogue, has been reported that it has significant toxicity and short half life. Therefore, it is necessary to design sustained release oral dosage form to avoid undesirable side effects attributable to an excessive plasma concentration and to reduce the frequency of administration of AZT. Inclusion complexes of AZT with acetyl-β-cyclodextrin (ACβCD) and triacetyl-β-cyclodextrin(TAβCD) were prepared by solvent evaporation methcd. Interactions of AZT with CD were investigated by Differential Scanning Calorimetry(DSC) and Infrared Spectrophotometry(IR). The decreasing order of water solubilities of AZT and AZT-CD inclusion complexes were as follows: AZT (27.873±0.015,㎎/㎖)) AZT-ACβCD (3.377±0.03) > AZT-TAβCD (2.528±0.001). Partition coefficients of AZT-ACβCD and AZT-TAβCD inclusion complexes were increased by 1.27-fold. 1.54-fold in pH 1.2 and 1.32-fold. 1.47-fold in pH 6.8 in comparison with that of AZT. The mean dissolution time (MDT, min) which represents the rapidity of dissolution rate of AZT, AZT-ACβCD. AZT-TAβCD were 5.12. 14.02 and 19.38 min in PH 1.2 and 2.52, 15.19 and 18.19 min in pH 6.8. AZT was very rapidly and completely dissolved in pH 1.2 and pH 6.8 within 5 minutes. But AZT-CD inclusion complexes showed the sustained release pattern in comparison with AZT alone. The simultaneous in situ nasal and jejunal recirculation study to compare the intrinsic absorptivity and the property of absorption sites revealed that the absorption of AZT-TAβCD (N:35.35±1.08% J:27.47±1.18% was more than that of AZT (N: 16.89±2.25%. J:15.86±2.33%. The above results suggest that TAβCD which is a hydrophobic cyclodextrin may serve as sustained release carrier with absorption enhancing effect.
시클로덱스트린과의 포접에 의한 케토고나졸의 비점막 흡수증가
박기배,이광표,노현구,안홍직,서보연,온윤성 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.2
Inclusion complexes of ketoconazole(KT) with α^-, β^- cyclodextrin(CD) and dimethyl-β-cyclodextrin (CD) and dimethyl-β-cyclodextrin(DMβCD) as nasal absorption enhancer were prepared in 1:2 molar ratios by freeze-drying and solvent evaporation methods. In order to compare with the intrinsic absorptivity of KT in the jejunum(J) and the nasal cavity(N), the in situ simultaneous perfusion method was employed. The in situ recirculation study revealed that KT-CD inclusion complexes with the greater stability constant and the faster dissolution rate proportionally increased the absorption of KT in the J and N of rats. The rank order of apparent KT permeability(P_(app) : ㎝/sec × 10^(-5)±S.E.), corrected by surface area of absorption, was 5.10±0.3(N, KT-DMβCD) >4.13±0.4(N, KT-β-CD) >3.52±0.2(N, KT-α-CD) >2.76±0.3(J, KT-DMβCD) >2.61±0.5(J, KT-β-CD) >2.42±0.4(J, KT-α-CD) at pH 4.0. The in crease in permeability of KT-DMβCD inclusion complex was 2.6 folds in the J and 4.5 folds in the N when the perfusing solution was changed from the buffer(pH 4.0) to saline. The absorption rate of KT-DMβCD inclusion complex after nasal administration was more rapid than those of ketoconazole alone and KT-DMβCD inclusion complex after oral administration to rats. In comparision with an oral administration of ketoconazole suspension in corn oil, the relative bioavailability was calculated 137.3% for the oral and 195.0% for nasal KT-DMβCD inclusion complex in rats. The present results suggest that KT-DMβCD inclusion complex may serve as a potential nasal absorption enhancer for the nasal delivery of ketoconazole.