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RISS 인기검색어
- 검색키워드
- 저자 : ( Abid Mehmood Yousaf ) (검색결과 18 건)
- 무료
- 기관 내 무료
- 유료
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Yousaf, Abid Mehmood,Mustapha, Omer,Kim, Dong Wuk,Kim, Dong Shik,Kim, Kyeong Soo,Jin, Sung Giu,Yong, Chul Soon,Youn, Yu Seok,Oh, Yu-Kyoung,Kim, Jong Oh,Choi, Han-Gon Dove Medical Press 2016 INTERNATIONAL JOURNAL OF NANOMEDICINE Vol.11 No.-
<P><B>Purpose</B></P><P>The purpose of the present research was to develop a novel electrosprayed nanospherule providing the most optimized aqueous solubility and oral bioavailability for poorly water-soluble fenofibrate.</P><P><B>Methods</B></P><P>Numerous fenofibrate-loaded electrosprayed nanospherules were prepared with polyvinylpyrrolidone (PVP) and Labrafil<SUP>®</SUP> M 2125 as carriers using the electrospray technique, and the effect of the carriers on drug solubility and solvation was assessed. The solid state characterization of an optimized formulation was conducted by scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopic analyses. Oral bioavailability in rats was also evaluated for the formulation of an optimized nanospherule in comparison with free drug and a conventional fenofibrate-loaded solid dispersion.</P><P><B>Results</B></P><P>All of the electrosprayed nanospherule formulations had remarkably enhanced aqueous solubility and dissolution compared with free drug. Moreover, Labrafil M 2125, a surfactant, had a positive influence on the solubility and dissolution of the drug in the electrosprayed nanospherule. Increases were observed as the PVP/drug ratio increased to 4:1, but higher ratios gave no significant increases. In particular, an electrosprayed nanospherule composed of fenofibrate, PVP, and Labrafil M 2125 at the weight ratio of 1:4:0.5 resulted in a particle size of <200 nm with the drug present in the amorphous state. It demonstrated the highest solubility (32.51±2.41 μg/mL), an excellent dissolution (~85% in 10 minutes), and an oral bioavailability ~2.5-fold better than that of the free drug. It showed similar oral bioavailability compared to the conventional solid dispersion.</P><P><B>Conclusion</B></P><P>Electrosprayed nanospherules, which provide improved solubility and bioavailability, are promising drug delivery tools for oral administration of poorly water-soluble fenofibrate.</P>
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( Abid Mehmood Yousaf ),( Omer Mustapha ),( Dong Wuk Kim ),( Dong Shik Kim ),( Kyeong Soo Kim ),( Sung Giu Jin ),( Chul Soon Yong ),( Yu Seok Youn ),( Yu Kyoung Oh ),( Jong Oh Kim ),( Han Gon Choi ) 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
Purpose: The purpose of the present research was to develop a novel electrosprayed nanospherule providing the most optimized aqueous solubility and oral bioavailability for poorly water-soluble fenofibrate. Methods: Numerous fenofibrate-loaded electrosprayed nanospherules were prepared with polyvinylpyrrolidone (PVP) and Labrafil® M 2125 as carriers using the electrospray technique, and the effect of the carriers on drug solubility and solvation was assessed, The solid state characterization of an optimized formulation was conducted by scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopic analyses. Oral bioavailability in rats was also evaluated for the formulation of an optimized nanospherule in comparison with free drug and a conventional fenofibrate-loaded solid dispersion. Results: All of the electrosprayed nanospherule formulations had remarkably enhanced aqueous solubility and dissolution compared with free drug, Moreover, Labrafil M 2125, a surfactant, had a positive influence on the solubility and dissolution of the drug in the elcctrospraycd nanospherulc. Increases were observed as the PVP/drug ratio increased to 4: I, but higher ratios gave no significant increases. In particular, an electrosprayed nanospherule composed of fenofibrate, PVP, and Labrafil M 2125 at the weight ratio of I :4:0,5 resulted in a particle size of <200 nm with the drug present in the amorphous state, It demonstrated the highest solubility (32,51±2.41μg/ml.), an excellent dissolution (-85% in 10 minutes), and an oral bioavailability -2,5-fold better than that ofthe free drug, It showed similar oral bioavailability compared to the conventional solid dispersion, Conclusion: Electrosprayed nanospherules, which provide improved solubility and bioavailability, are promising drug delivery tools for oral administration of poorly water-soluble fenofibrate.
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Yousaf, Abid Mehmood,Kim, Dong Wuk,Oh, Yu-Kyoung,Yong, Chul Soon,Kim, Jong Oh,Choi, Han-Gon Dove Medical Press 2015 INTERNATIONAL JOURNAL OF NANOMEDICINE Vol.10 No.-
<P><B>Background</B></P><P>The intention of this research was to prepare and compare various solubility-enhancing nanoparticulated systems in order to select a nanoparticulated formulation with the most improved oral bioavailability of poorly water-soluble fenofibrate.</P><P><B>Methods</B></P><P>The most appropriate excipients for different nanoparticulated preparations were selected by determining the drug solubility in 1% (w/v) aqueous solutions of each carrier. The polyvinylpyrrolidone (PVP) nanospheres, hydroxypropyl-β-cyclodextrin (HP-β-CD) nanocorpuscles, and gelatin nanocapsules were formulated as fenofibrate/PVP/sodium lauryl sulfate (SLS), fenofibrate/HP-β-CD, and fenofibrate/gelatin at the optimized weight ratios of 2.5:4.5:1, 1:4, and 1:8, respectively. The three solid-state products were achieved using the solvent-evaporation method through the spray-drying technique. The physicochemical characterization of these nanoparticles was accomplished by powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and Fourier-transform infrared spectroscopy. Their physicochemical properties, aqueous solubility, dissolution rate, and pharmacokinetics in rats were investigated in comparison with the drug powder.</P><P><B>Results</B></P><P>Among the tested carriers, PVP, HP-β-CD, gelatin, and SLS showed better solubility and were selected as the most appropriate constituents for various nanoparticulated systems. All of the formulations significantly improved the aqueous solubility, dissolution rate, and oral bioavailability of fenofibrate compared to the drug powder. The drug was present in the amorphous form in HP-β-CD nanocorpuscles; however, in other formulations, it existed in the crystalline state with a reduced intensity. The aqueous solubility and dissolution rates of the nanoparticles (after 30 minutes) were not significantly different from one another. Among the nanoparticulated systems tested in this study, the initial dissolution rates (up to 10 minutes) were higher with the PVP nanospheres and HP-β-CD nanocorpuscles; however, neither of them resulted in the highest oral bioavailability. Irrespective of relatively retarded dissolution rate, gelatin nanocapsules showed the highest apparent aqueous solubility and furnished the most improved oral bioavailability of the drug (~5.5-fold), owing to better wetting and diminution in crystallinity.</P><P><B>Conclusion</B></P><P>Fenofibrate-loaded gelatin nanocapsules prepared using the solvent-evaporation method through the spray-drying technique could be a potential oral pharmaceutical product for administering the poorly water-soluble fenofibrate with an enhanced bioavailability.</P>
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( Abid Mehmood Yousaf ),( Dong Wuk Kim ),( Yu Kyoung Oh ),( Chul Soon Yong ),( Jong Oh Kim ),( Han Gon Choi ) 영남대학교 약품개발연구소 2015 영남대학교 약품개발연구소 연구업적집 Vol.25 No.-
Background: The intention of this research was to prepare and compare various solubility-enhancing nanoparticulated systems in order to select a nanoparticulated formulation with the most improved oral bioavailability of poorly water-soluble fenofibrate. Methods: The most appropriate excipients for different nanoparticulated preparations were selected by determining the drug solubility in 1% (w/v) aqueous solutions of each carrier. The polyvinylpyrrolidone (PVP) nanospheres, hydroxypropyl-β-cyclodextrin (HP-β-CD) nanocorpuscles, and gelatin nanocapsules were formulated as fenofibrate/PVP/sodium lauryl sulfate (SLS), fenofibrate/HP-β-CD, and fenofibrate/gelatin at the optimized weight ratios of 2.5:4.5:1, 1:4, and 1:8, respectively. The three solid-state products were achieved using the solventevaporation method through the spray-drying technique. The physicochemical characterization of these nanoparticles was accomplished by powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and Fourier-transform infrared spectroscopy. Their physicochemical properties, aqueous solubility, dissolution rate, and pharmacokinetics in rats were investigated in comparison with the drug powder. Results: Among the tested carriers, PVP, HP-β-CD, gelatin, and SLS showed better solubility and were selected as the most appropriate constituents for various nanoparticulated systems. All of the formulations significantly improved the aqueous solubility, dissolution rate, and oral bioavailability of fenofibrate compared to the drug powder. The drug was present in the amorphous form in HP-β-CD nanocorpuscles; however, in other formulations, it existed in the crystalline state with a reduced intensity. The aqueous solubility and dissolution rates of the nanoparticles (after 30 minutes) were not significantly different from one another. Among the nanoparticulated systems tested in this study, the initial dissolution rates (up to 10 minutes) were higher with the PVP nanospheres and HP-β-CD nanocorpuscles; however, neither of them resulted in the highest oral bioavailability. Irrespective of relatively retarded dissolution rate, gelatin nanocapsules showed the highest apparent aqueous solubility and furnished the most improved oral bioavailability of the drug (~5.5-fold), owing to better wetting and diminution in crystallinity. Conclusion: Fenofibrate-loaded gelatin nanocapsules prepared using the solvent-evaporation method through the spray-drying technique could be a potential oral pharmaceutical product for administering the poorly water-soluble fenofibrate with an enhanced bioavailability.
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김동욱,김영훈,Abid Mehmood Yousaf,김동식,권택관,박정희,김영일,박재현,진성규,김경수,조관형,Dongxun Li,김종오,용철순,우종수,최한곤 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.4
To develop a montelukast sodium–loadedstable oral suspension bioequivalent to the commercialgranules in rats, several montelukast sodium-loaded suspensionswere prepared with a suspending agent, stabilizersand anti-aggregation agents, and their stabilities wereinvestigated by visually observing the sedimentation phenomenonand determining the concentration of the degradationproduct. Moreover, dissolution and pharmacokineticstudies of the optimized formulation were examined in ratscompared to commercial montelukast sodium-loadedgranules. Avicel RC-591 (Avicel), a suspending agent,prevented the sedimentation of these suspensions at[2.496(w/v) per cent composition. Amongst the stabilizers tested,fumaric acid provided the lowest concentration of montelukastsulphoxide (a degradation product) in these suspensionsat 40 C, demonstrating its excellent stabilizingactivity. Furthermore, as an anti-aggregation agent, glyceringave lower amounts of degradation product than thosewith poloxamer 407 and Tween 80. In particular, montelukast-loaded oral suspension, an aqueous suspensioncontaining montelukast sodium/Avicel/fumaric acid/glycerinat a concentration of 312/2496/15.6/62.4 (mg/100 ml),and the commercial granules exhibited similar dissolutionprofiles in 0.5 % (w/v) aqueous solution of sodium laurylsulphate. Moreover, the pharmacokinetics in rats providedby this suspension was comparable to that of the commercialgranules, suggesting that they were bioequivalent. In addition, it was physically and chemically stable at40 C for at least 6 months. Thus, this montelukastsodium-loaded oral suspension, with bioequivalence to thecommercial granules and excellent stability, could be aprospective dosage form for the treatment of asthma.
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진성규,김정훈,Abid Mehmood Yousaf,손미윤,장선우,김동욱,김종오,용철순,최한곤 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.2
The aim of this research was to evaluate the gelproperties, skin permeation and in vivo drug efficacy of anovel dexibuprofen-loaded emulsion gel for topical delivery. In this study, the dexibuprofen-loaded emulsion geland ibuprofen-loaded emulsion gel were prepared withisopropanol, Tween 80, propylene glycol, isopropyl myristateand carbopol. Their mechanical properties such ashardness and adhesiveness were assessed. Moreover, theirskin permeation, anti-inflammatory and anti-nociceptiveefficacy were evaluated using Franz diffusion cell with thehairless mouse skin, the carrageenan-induced paw oedematest and paw pressure test in rat’s hind paws compared withthe commercial hydrogel, respectively. The dexibuprofenemulsion gel and ibuprofen emulsion gel provided significantlyhigher hardness and adhesiveness than the commercialhydrogel. The dexibuprofen emulsion gel enhancedskin permeability by about twofold and 3.5-fold withoutlag time compared to the ibuprofen emulsion gel and thecommercial hydrogel, respectively, suggesting its fasterskin permeation. Moreover, the anti-inflammatory efficacyand alleviation in carrageenan-induced inflammation wasin the order of dexibuprofen emulsion gel[commercialhydrogel[ibuprofen emulsion gel. The dexibuprofenemulsion gel furnished significantly higher nociceptivethresholds than the ibuprofen emulsion gel and the commercialhydrogel, leading to the most improved anti-nociceptiveefficacy. Thus, this dexibuprofen-loaded emulsiongel with good mechanical property, rapid skin permeationand excellent anti-inflammatory and anti-nociceptive efficacywould be a strong candidate for the topical delivery ofanti-inflammatory dexibuprofen.
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Kim, Dong Wuk,Yousaf, Abid Mehmood,Li, Dong Xun,Kim, Jong Oh,Yong, Chul Soon,Cho, Kwan Hyung,Choi, Han-Gon Elsevier 2017 Asian journal of pharmaceutical sciences Vol.12 No.1
<P>The purpose of the present research was to develop a suitable, simple, precise, accurate, robust, and reproducible RP-HPLC method for a reliable simultaneous quantification of docetaxel (DTX) and curcumin (CCM) in rat plasma samples using paclitaxel (PTX) as an internal standard. The samples were assayed by the Agilent 1260 Infinity HPLC instrument using a Capcell Pak C-8 column (4.6mmx 150 mm, 5 mu m) under isocratic conditions. The mobile phase consisted of acetonitrile and triple distilled water (40/60, v/v) with a flow rate of 1.0 ml/min. The eluent was monitored at 230 nm for simultaneous measurement of curcumin and docetaxel. The method was validated by determining system suitability, selectivity, sensitivity, linearity, inter-day and intra-day precision, accuracy, robustness, and stability in accordance with the guidelines of the United States Food and Drug Administration (FDA). The developed chromatographic method proved to be simple, precise, accurate, robust and reproducible. Moreover, the samples showed stability at room temperature over a period of 48 h. Thus, this method would be employed for routine simultaneous quantification of docetaxel and curcumin in rat plasma samples. (C) 2017 Shenyang Pharmaceutical University. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).</P>
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( Sung Giu Jin ),( Abid Mehmood Yousaf ),( Kyeong Soo Kim ),( Dong Wuk Kim ),( Dong Shik Kim ),( Jin Ki Kim ),( Chul Soon Yong ),( Yu Seok Youn ),( Jong Oh Kim ),( Han Gon Choi ) 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
The purpose of this study was to investigate the influence of different hydrophilic polymers on the swelling, bioadhesion and mechanical strength of hydrocolloid wound dressings (HCDs) in order to provide an appropriate composition for a hydrocolloid wound dressing system. In this study, the HCDs were prepared with styrene-isoprene-styrene copolymer (SIS) and polyisobutylene (PIB) as the base using a hot melting method. Additionally, numerous SISIPIB-based HCDs were prepared with six hydrophilic polymers, and their wound dressing properties were assessed. Finally, the wound healing efficacy of the selected formulations was compared to a commercial wound dressing. The swelling ratio, bioadhesive force and mechanical strengths of HCDs were increased in the order of sodium alginate> sodium CMC = poloxamer = HPMC > PYA = PVP, sodium alginate> sodium CMC = poloxamer > PYA> HPMC = PVP and sodium alginate > PYA >PVP = HPMC = sodium CMC> poloxarmer, respectively. Among the hydrophilic polymers tested, sodium alginate most enhanced the swelling capacity, bioadhesive force and mechanical strengths. Thus, the hydrophilic polymers played great role in the swelling, bioadhesion and mechanical strength of SISIPIB-based HCDs. The HCD formulation composed of PIB, SIS, liquid paraffin and sodium alginate at the weight ratio of 20/25/12/43 gave better wound dressing properties and more excellent wound healing efficacy than the commercial wound dressing. Therefore, the novel HCD formulation could be a promising hydrocolloid system for wound dressings.
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( Hyeon Woo Moon ),( Abid Mehmood Yousaf ),( Kwan Hyung Cho ),( Chul Soon Yong ),( Jong Oh Kim ),( Han Gon Choi ) 영남대학교 약품개발연구소 2014 영남대학교 약품개발연구소 연구업적집 Vol.24 No.0
A simple, rapid, accurate, precise and robust HPLC method was developed for the simul-taneous determination of fimasartan and amlodipine in tablet dosage form. Furthermore, stability of active ingredients was evaluated under normal and stress conditions. The isocratic elution was accomplished by Nlucleosil C18 column (250 mm × 4.6 mm, 5 ㎛)at 40 ℃. The mobile phase consisted of acetonitrile and 0.02 M monopotassium phosphate buffer (pH 2.2) in the ratio of 50=50 (v/v) was eluted at 1.0 ml/min. The eluent was moni-tored by the UV detector for fimasartan and amlodipine at 237 nm for 8 min, detection .time. The validation of HPLC method was carried out in accordance with the ICH guidelines.
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