Bioavailabilities of Omeprazole Administered to Rats through Various Routes

Choi, Mi-Sook,Lee, Young-Hee,Shim, Chang-Koo The Pharmaceutical Society of Korea 1995 Archives of Pharmacal Research Vol.18 No.3

Omeprazole, a proton pump inhibitor, was given intravenously (iv), orally (po), intraperitoneally (ip), hepatoportalvenously (pv), and intrarectally (ir) to rats at a dose of 72mg/kg in order to investigate the bioavailability of the drug, The extent of bioavailabilities of omeprazole administered through pv, ip, po, and ir routes were 88.5, 79.4, 40,8, and 38.7%, respectively. Pharmacokinetic analysis in this study and literatures (Regardh et al., 1985 : Watanabe et al., 1994) implied significant dose-dependency in hepatic first-pass metabolism, clearance and distribution, and acidic degradation in gastric fluid. The high bioavailability from the pv administration (88.5%) means that only 11.5% of dose was extracted by the first-pass metabolism through the liver at this dose (72 mg/kg). The low bioavailability from the oral administration (40.8%) in spite of minor hepatic first-pass extraction indicates low transport of the drug from GI lumen to portal vein. From the literature (Pilbrant and Cederberg, 1985), acidic degradation in gastric fluid was considered to be the major cause of the low transport. Thus, enteric coating of oral preparations would enhance the oral bioavailability substantially. The bioavailability of the drug from the rectal route, in which acidic degradation and hepatic first-pass metabolism may not occur, was low (38.7%) but comparable to that from the oral route (40.8 %) indicating poor transport across the rectal membrane. In this case, addition of an appropriate absorption enhancer would improve the bioavailability. Rectal route seems to be an possible alternative to the conventional oral route for omeprazole administration.

Bioavailability of Phosphorus in Two Cultivars of Pea for Broiler Chicks

Woyengo, T.A.,Emiola, I.A.,Kim, I.H.,Nyachoti, C.M. Asian Australasian Association of Animal Productio 2016 Animal Bioscience Vol.29 No.3

The aim was to determine the relative bioavailability of phosphorus (P) in peas for 21-day old broiler chickens using slope-ratio assay. One hundred and sixty eight male Ross 308 broiler chicks were divided into 42 groups 4 balanced for body weight and fed 7 diets in a completely randomized design (6 groups/diet) from day 1 to 21 of age. The diets were a corn-soybean meal basal diet, and the corn-soybean meal basal diet to which monosodium phosphate, brown- or yellow-seeded pea was added at the expense of cornstarch to supply 0.5% or 1% total phosphorus. Monosodium phosphate was included as a reference, and hence the estimated bioavailability of P in pea cultivars was relative to that in the monosodium phosphate. Birds and feed were weighed weekly and on d 21 they were killed to obtain tibia. The brown-seeded pea contained 23.4% crude protein, 0.47% P, whereas the yellow-seeded pea contained 24.3% crude protein and 0.38% P. Increasing dietary P supply improved (p<0.05) chick body weight gain and tibia ash and bone density. The estimated relative bioavailability of p values for brown- and yellow-seeded peas obtained using final body weight, average daily gain, tibia ash, and bone mineral density were 31.5% and 36.2%, 35.6% and 37.3%, 23.0% and 5.60%, and 40.3% and 30.3%, respectively. The estimated relative bioavailability of p values for brown- and yellow-seeded peas did not differ within each of the response criteria measured in this study. In conclusion, the relative bioavailability of P in pea did not differ depending on the cultivar (brown- vs yellow-seed). However, the relative bioavailability of P in pea may vary depending on the response criterion used to measure the bioavailability.

Evaluating the effects of organic matter bioavailability on nanofiltration membrane using real-time monitoring

Park, Sanghun,You, Jeongyeop,Ahn, Yujin,Jung, Woonggyu,Kim, Jihye,Lee, Sungyun,Park, Jongkwan,Cho, Kyung Hwa Elsevier 2018 Journal of membrane science Vol.548 No.-

<P><B>Abstract</B></P> <P>We studied the influence of bioavailability of organic matter on membrane fouling layer development by comparing the filtration performance of two feed waters (wetland water and graywater). Dissolved organic carbon (DOC) concentration, size exclusion chromatography (SEC), and fluorescence excitation-emission matrix (FEEM) were used to characterize the bioavailability of organic matter in these water samples during the nanofiltration process. The wetland sample contained a high proportion of humic acid- and fulvic acid-like matter with low bioavailability, whereas the graywater sample comprised substantial amounts of aromatic proteins and microbial byproduct-like matter with high bioavailability. In addition, the molecular size distribution revealed that the wetland sample contained a large portion of recalcitrant organic matter, whereas the graywater sample contained easily bioavailable organic matter. After the filtration experiment, the DOC of the wetland sample decreased to 4.8mgC/L, whereas the graywater sample resulted in a lower DOC concentration of 3.4mgC/L. Optical coherence tomography (OCT) illustrated real-time variations in the fouling layer morphology, providing both 2D and 3D images. In addition, confocal laser scanning microscopy (CLSM) quantified the bacterial volume in the fouling layer. The wetland sample yielded a bacterial volume of 11.8µm<SUP>3</SUP>/μm<SUP>2</SUP> from a total fouling volume of 103µm<SUP>3</SUP>/μm<SUP>2</SUP>, whereas the graywater sample yielded a bacterial volume of 53.2µm<SUP>3</SUP>/μm<SUP>2</SUP> from a total fouling layer volume of 134µm<SUP>3</SUP>/μm<SUP>2</SUP>. Fitting of the two-phase Monod model to the fouling layer growth on the membrane resulted in lower-yield coefficients (i.e., the volumes produced per unit amount of substrate, <SUB> Y xs </SUB> ) of 7.46 and 27.95µm<SUP>3</SUP>/μm<SUP>2</SUP> in wetland water and higher-yield coefficients of 13.17 and 47.53µm<SUP>3</SUP>/μm<SUP>2</SUP> in the graywater at first and second phase, respectively. This study addresses the quantitative evaluation of the organic matter bioavailability in terms of membrane fouling using OCT images and a two-phase Monod model.</P> <P><B>Highlights</B></P> <P> <UL> <LI> The difference of bioavailability of DOM influenced the amount of fouling layer growth. </LI> <LI> In situ OCT monitoring provided 2D and 3D morphology of the fouling layer and quantified the volume. </LI> <LI> Two-phase Monod model evaluated the influence of bioavailability of DOM on fouling layer growth. </LI> </UL> </P>

Absorption Study of Genistein Using Solid Lipid Microparticles and Nanoparticles: Control of Oral Bioavailability by Particle Sizes

( Jeong Tae Kim ),( Sonia Barua ),( Hyeongmin Kim ),( Seong-chul Hong ),( Seung-yup Yoo ),( Hyojin Jeon ),( Yeongjin Cho ),( Sangwon Gil ),( Kyungsoo Oh ),( Jaehwi Lee ) 한국응용약물학회 2017 Biomolecules & Therapeutics(구 응용약물학회지) Vol.25 No.4

In this study, the effect of particle size of genistein-loaded solid lipid particulate systems on drug dissolution behavior and oral bioavailability was investigated. Genistein-loaded solid lipid microparticles and nanoparticles were prepared with glyceryl palmitostearate. Except for the particle size, other properties of genistein-loaded solid lipid microparticles and nanoparticles such as particle composition and drug loading efficiency and amount were similarly controlled to mainly evaluate the effect of different particle sizes of the solid lipid particulate systems on drug dissolution behavior and oral bioavailability. The results showed that genistein-loaded solid lipid microparticles and nanoparticles exhibited a considerably increased drug dissolution rate compared to that of genistein bulk powder and suspension. The microparticles gradually released genistein as a function of time while the nanoparticles exhibited a biphasic drug release pattern, showing an initial burst drug release, followed by a sustained release. The oral bioavailability of genistein loaded in solid lipid microparticles and nanoparticles in rats was also significantly enhanced compared to that in bulk powders and the suspension. However, the bioavailability from the microparticles increased more than that from the nanoparticles mainly because the rapid drug dissolution rate and rapid absorption of genistein because of the large surface area of the genistein-solid lipid nanoparticles cleared the drug to a greater extent than the genistein-solid lipid microparticles did. Therefore, the findings of this study suggest that controlling the particle size of solid-lipid particulate systems at a micro-scale would be a promising strategy to increase the oral bioavailability of genistein.

Medicinal Chemistry : Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation

( 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.

Effect of inorganic mesoporous carriers on 1-palmitoyl-2-linoleoyl-3-acetyl-<i>rac</i>-glycerol-loaded solid self-emulsifying drug delivery system: Physicochemical characterization and bioavailability in rats

Kim, Dong Shik,Yang, Eun Su,Yong, Chul Soon,Youn, Yu Seok,Oh, Kyung Taek,Li, Dong Xun,Kim, Jong Oh,Jin, Sung Giu,Choi, Han-Gon Elsevier 2017 Colloids and Surfaces B Vol.160 No.-

<P><B>Abstract</B></P> <P>The purpose of this study was to assess the impact of inorganic mesoporous carriers on the physicochemical properties and oral bioavailability of 1-palmitoyl-2-linoleoyl-3-acetyl-<I>rac</I>-glycerol (PLAG)-loaded solid self-emulsifying drug delivery system (solid SEDDS). Numerous PLAG-loaded solid SEDDS formulations were prepared by spray drying technique with sodium laurylsulfate (SLS), butylated hydroxyanisole (BHA) and inorganic mesoporous materials as a surfactant, antioxidant and solid carrier, respectively. The mesoporous materials, such as calcium silicate, silicon dioxide and magnesium aluminosilicate were used as the solid carriers. Their physicochemical properties, solubility, dissolution and pharmacokinetic studies in rats were performed compared with drug alone. Three solid SEDDSs composed of PLAG/BHA/SLS/mesopous carrier at the weight ratio of 1:0.0002:0.25:0.5 resulted in a small emulsion droplet and excellent drug loading efficiency. The solid SEDDS formulations prepared with calcium silicate and silicon dioxide showed a rough-surfaced irregular shape and rough-surfaced spheres, respectively. Magnesium aluminosilicate generated a sticky powder, due to its relatively low specific surface area, resulting in insufficient adsorption of PLAG. These solid SEDDSs improved the solubility, dissolution and oral bioavailability of PLAG. Ultimately, the solid SEDDS prepared with silicon dioxide resulted in the best drug loading efficiency, shape, solubility, dissolution and oral bioavailability due to its great specific surface area. Therefore, mesoporous carriers with different specific surface areas markedly influenced the physicochemical properties, solubility, dissolution and oral bioavailability of PLAG-loaded solid SEDDS.</P> <P><B>Highlights</B></P> <P> <UL> <LI> The effect of mesoporous carriers on PLGA-loaded solid SEDDS were assessed. </LI> <LI> Numerous PLGA-loaded solid SNEDDS were prepared using spray drying technique. </LI> <LI> Calcium silicate, silicon dioxide and magnesium aluminosilicate were used as the mesoporous carriers. </LI> <LI> The solid SEDDS prepared with silicon dioxide gave most excellent loading efficiency and bioavailability. </LI> <LI> Mesoporous carriers markedly influenced the physicochemical properties and bioavailability of solid SEDDS. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

Cadmium solubility and bioavailability in soils amended with acidic and neutral biochar

Qi, Fangjie,Lamb, Dane,Naidu, Ravi,Bolan, Nanthi S.,Yan, Yubo,Ok, Yong Sik,Rahman, Mohammad Mahmudur,Choppala, Girish Elsevier 2018 Science of the Total Environment Vol.610 No.-

<P><B>Abstract</B></P> <P>This study was designed to investigate the effects of acidic and neutral biochars on solubility and bioavailability of cadmium (Cd) in soils with contrasting properties. Four Cd contaminated (50mg/kg) soils (EN: Entisol, AL: Andisol, VE: Vertisol, IN: Inceptisol) were amended with 5% acidic wood shaving biochar (WS, pH=3.25) and neutral chicken litter biochar (CL, pH=7.00). Following a 140-day incubation, the solubility and bioavailability/bioaccessibility of cadmium (Cd) were assessed. Results showed that both biochars had no effect on reducing soluble (pore water) and bioavailable (CaCl<SUB>2</SUB> extractable) Cd for higher sorption capacity soils (AL, IN) while CL biochar reduced those in lower sorption capacity soils (EN, VE) by around 50%. Bioaccessibility of Cd to the human gastric phase (physiologically based extraction test (PBET) extractable) was not altered by the acidic WS biochar but reduced by neutral CL biochar by 18.8%, 29.7%, 18.0% and 8.82% for soil AL, EN, IN and VE, respectively. Both biochars reduced soluble Cd under acidic conditions (toxicity characteristic leaching procedure (TCLP) extractable) significantly in all soils. Pore water pH was the governing factor of Cd solubility among soils. The reduction of Cd solubility and bioavailability/bioaccessibility by CL biochar may be due to surface complexation while the reduced mobility of Cd under acidic conditions (TCLP) by both biochars may result from the redistribution of Cd to less bioavailable soil solid fractions. Hence, if only leaching mitigation of Cd under acidic conditions is required, application of low pH biochars (e.g., WS biochar) may be valuable.</P> <P><B>Highlights</B></P> <P> <UL> <LI> The acidic biochar did not reduce soil soluble/bioavailable/bioaccessible Cd. </LI> <LI> The neutral biochar reduced soluble/bioavailable Cd of low sorption capacity soils. </LI> <LI> The neutral biochar reduced bioaccessible Cd of the four studied soils. </LI> <LI> Both acidic and neutral biochars reduced Cd mobility under acidic conditions. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

Medicinal Chemistry : Preparation and Characterization of Fenofibrate-Loaded Nanostructured Lipid Carriers for Oral Bioavailability Enhancement

( Tuan Hiep Tran ),( Thiruganesh Ramasamy ),( Duy Hieu Truong ),( Han Gon Choi ),( Chul Soon Yong ),( Jong Oh Kim ) 영남대학교 약품개발연구소 2015 영남대학교 약품개발연구소 연구업적집 Vol.25 No.-

The aim of this study is to investigate the potential of nanostructured lipid carriers (NLCs) in improving the oral bioavailability of a lipid lowering agent, fenofibrate (FEN). FEN-loaded NLCs (FENNLCs) were prepared by hot homogenization followed by an ultrasonication method using Compritol 888 ATO as a solid lipid, Labrafil M 1944CS as a liquid lipid, and soya lecithin and Tween 80 as emulsifiers. NLCs were characterized in terms of particle size and zeta pote\ntial, surface morphology, encapsulation efficiency, and physical state properties. Bioavailability studies were carried out in rats by oral administration of FEN-NLC. NLCs exhibited a spherical shape with a small particle size (84.9±4.9 nm). The drug entrapment efficiency was 99% with a loading capacity of 9.93±0.01% (w/w). Biphasic drug release manner with a burst release initially, followed by prolonged release was depicted for in vitro drug release studies. After oral administration of the FEN-NLC, drug concentration in plasma and AUCt-∞ was fourfold higher, respectively, compared to the free FEN suspension. According to these results, FENNLC could be a potential delivery system for improvement of loading capacity and control of drug release, thus prolonging drug action time in the body and enhancing the bioavailability.

Enhanced phosphorus bioavailability and heavy metal removal from sewage sludge ash through thermochemical treatment with chlorine donors

Jeon, Seulki,Kim, Dong-Jin THE KOREAN SOCIETY OF INDUSTRIAL AND ENGINEERING 2018 JOURNAL OF INDUSTRIAL AND ENGINEERING CHEMISTRY -S Vol.58 No.-

<P><B>Abstract</B></P> <P>Direct application of sewage sludge ash (SSA) to agriculture is mostly prohibited due to its heavy metals and limited bioavailability. Thermochemical treatment of SSA with Cl-donors were carried out to remove heavy metals and enhance P bioavailability. MgCl<SUB>2</SUB> and CaCl<SUB>2</SUB> removed more heavy metal than other Cl-donors. Pb was completely removed followed by Cd, Zn, Cu. They also increased P bioavailability by the conversion of Al–P to Ca/Mg–P which was confirmed by chemical fractionation. XRD confirmed the conversion of AlPO<SUB>4</SUB> to Ca<SUB>5</SUB>(PO<SUB>4</SUB>)<SUB>3</SUB>Cl, Ca<SUB>3</SUB>(PO<SUB>4</SUB>)<SUB>2</SUB>, and Mg<SUB>3</SUB>(PO<SUB>4</SUB>)<SUB>2</SUB> by the thermochemical treatment.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Thermochemical treatment of SSA was performed to remove heavy metals and enhance P bioavailability. </LI> <LI> CaCl<SUB>2</SUB> and MgCl<SUB>2</SUB> were effective Cl-donors for heavy metal removal. </LI> <LI> MgCl<SUB>2</SUB> increased P bioavailability of SSA by 53%. </LI> <LI> Thermochemical conversion of Al–P to Ca/Mg–P was confirmed by XRD and chemical fractionation. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

Bioavailability of Lycopene from Tomato Products

Shi, John,Naughton, Laura-Mac,Kakuda, Yukio,Bettger, William,Yeung, David,Jiang, Yueming The Korean Society of Food Science and Nutrition 2004 Preventive Nutrition and Food Science Vol.9 No.1

Tomatoes and tomato products are the major source of lycopene in the diet. The bioavailability of lycopene is different in raw tomatoes compared to processed tomato products. This is due to the chemical and physical properties of the different lycopene isomers. All-trans-lycopene is found in raw tomatoes and is a poor bioavailable source, whereas, processed tomato products are more bioavailable because they contain more cis-isomers. Heat and mechanical processing of tomatoes induces rupture of the cell walls, thereby releasing lycopene from its food matrix. Heat processing also induces cis-trans isomerization and disrupts protein-carotenoid complexes. Many dietary components also impact lycopene bioavailability, like the amount and type of fat present with the intake and processing of tomato products, the amount and type of fiber present, and the interaction between carotenoids. Fundamentally, anything that enhances formation and incorporation of lycopene in bile acid micelles increases bioavailability, and the opposite is true in that anything that interferes with micelle formation decreases bioavailability.