• Journal of the Korean Society of Food Science and Nutrition
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• v.42 no.4
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• pp.497-504
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• 2013

This study examined the characteristics of ionized calcium and in vitro calcium bioavailability rate of calcium from four natural sources: shellfish shell, oyster shell, starfish, egg shell. The levels of dissolved calcium and calcium ions increased at different concentrations of natural calcium (up to 8.0% (w/v)). However, there were insignificant differences in the levels of dissolved calcium and calcium ions between samples at calcium concentrations above 8.0% (w/v). In addition, no significant differences were observed (depending on the calcium source and concentration) with an ionization yield of about 90%. The temperature of the solutions also had little influence on the ionization of calcium. The highest calcium ion content was observed when solutions were left to dissolve calcium for 18 hours. The highest in vitro calcium bioavailability rate achieved among the different calcium solutions was BS (67.3%), with overall bioavailability rates about two times higher than the rates observed in commercially sold calcium supplements and natural calcium. In addition, the in vitro calcium bioavailability rate for ionized calcium in market milk, soy milk, and orange juice was more than twice as high as calcium carbonate. Overall, we expect a high and diverse bioavailability of ionized calcium from natural resources.

• Journal of Pharmaceutical Investigation
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• v.37 no.6
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• pp.339-347
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• 2007

SMEDDS is mixture of oils, surfactants, and cosurfactants, which are emulsified in aqueous media under conditions of gentle agitation and digestive motility that would be encountered in the gastro-intestinal(GI) tract. The main purpose of this work is to prepare self-microemulsifying drug delivery system(SMEDDS) for oral bioavailability enhancement of a poorly water soluble drug, atorvastatin calcium. Solubility of atorvastatin calcium was determined in various vehicles. Pseudo-ternary phase diagrams were constructed to identity the efficient self-emulsification region and particle size distributions of the resultant micro emulsions were determined using a laser diffraction sizer. Optimized formulations for in vitro dissolution and bioavailability assessment were $Capryol^{(R)}$ 90(50%), Tetraglycol(16%), and $Cremophor^{(R)}$ EL(32%). The release rate of atorvastatin from SMEDDS was significantly higher than the conventional tablet ($Lipitor^{(R)}$), 2-fold. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin calcium by the oral route.

• Journal of Pharmaceutical Investigation
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• v.27 no.4
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• pp.295-301
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• 1997

Nitrendipine, a slightly soluble calcium channel blocking agent forms a solid dispersion system with $hydroxypropyl-{\beta}-cyclodextrin$, which exhibits better dissolution characteristics than the uncomplexed drug. The dissolution rate of nitrendipine was markedly increased in solid dispersion system in pharmacopeial disintegration media at pH 1.2 and pH 6.8. Four different dosage forms of nitrendipine were administered to rats: (a) nitrendipine in the solution of PEG 400; (b) nitrendipine solid dispersion system with $hydroxypropyl-{\beta}-cyclodextrin$ in a molar ratio of 1:2 by solvent evaporation method and administered in capsule form; (c) physical mixture of nitrendipine with $hydroxypropyl-{\beta}-cyclodextrin$ in a molar ratio of 1:2 and administered in capsule form; (d) nitrendipine alone administered in capsule form. Relative bioavailability after the oral administration of various dosage forms to rats with a dose of 10 mg/kg equivalent to nitrendipine was compared with that of nitrendipine in the solution of PEG 400. The AUC of solid dispersion was significantly bigger than that of nitrendipine powder. $T_{max}$ of solid dispersion was significantly shorter and $C_{max}$ was higher than that of nitrendipine powder. These results indicate that the bioavailability of nitrendipine could be improved markedly by inclusion complexation. An interesting correlation also appears to exist between the in vitro dissolution data and the area under the plasma concentration-time curves.

• The Korean Journal of Physiology and Pharmacology
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• v.22 no.1
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• pp.35-42
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• 2018

Ascorbic acid is one of the most well-known nutritional supplement and antioxidant found in fruits and vegetables. Calcium ascorbate has been developed to mitigate the gastric irritation caused by the acidity of ascorbic acid. The aim of this study was to compare calcium ascorbate and ascorbic acid, focusing on their antioxidant activity and effects on gastric juice pH, total acid output, and pepsin secretion in an in vivo rat model, as well as pharmacokinetic parameters. Calcium ascorbate and ascorbic acid had similar antioxidant activity. However, the gastric fluid pH was increased by calcium ascorbate, whereas total acid output was increased by ascorbic acid. In the rat pylorus ligation-induced ulcer model, calcium ascorbate increased the gastric fluid pH without changing the total acid output. Administration of calcium ascorbate to rats given a single oral dose of 100 mg/kg as ascorbic acid resulted in higher plasma concentrations than that from ascorbic acid alone. The area under the curve (AUC) values of calcium ascorbate were 1.5-fold higher than those of ascorbic acid, and the $C_{max}$ value of calcium ascorbate (91.0 ng/ml) was higher than that of ascorbic acid (74.8 ng/ml). However, their $T_{max}$ values were similar. Thus, although calcium ascorbate showed equivalent antioxidant activity to ascorbic acid, it could attenuate the gastric high acidity caused by ascorbic acid, making it suitable for consideration of use to improve the side effects of ascorbic acid. Furthermore, calcium ascorbate could be an appropriate antioxidant substrate, with increased oral bioavailability, for patients with gastrointestinal disorders.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.31 no.2
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• pp.149-159
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• 1998

To utilize the oyster shell containing a lot of calcium, we investigated the bioavailability of calcium compounds from oyster shell. First, calcium oxide was prepared by burning of oyster shell at $1200^{\circ}C$. Its purity was approximately $98.5\%$. Calcium compounds, $CaCl_2$, and $CaHPO_4$, from the calcium oxide were prepared by chemical reaction. Effect on calcium absorption by the calcium compounds from oyster shell was improved using fish skin gelatin peptides.(FSGP), which was prepared by enzymatic hydrolysis of fish skin gelatin for 4hr with tuna pyloric caeca crude enzyme (TPCCE). in vitro experiment, calcium absorption by addition of FSGP in a mixture solution of calcium and phosphate was higher approximately $70\%$ than that by control. in vivo using calcium deficient rats, a group taken the diets with $3\%$ FSGP and $CaHPO_4$ was significantly improved amount of calcium and ash in femur and strength of femur. These results suggest that calcium compounds from oyster shell and FSGP could be used as an effective dietary calcium source.

• Korean Journal of Food Science and Technology
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• v.54 no.4
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• pp.422-430
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• 2022

The effects of phytase and cellulase treatment on the bioavailability of iron, calcium, and zinc in whole wheat flour and their food applications were evaluated in this study. Whole wheat flour was treated with phytase and cellulase either individually or in combination and incubated at 50℃ for 2 h; the concentrations used for the individual enzymes were 2%, 10%, and 20%. The concentration of the combination enzyme was 20% with a mixing ratio of 5:5. Total dietary fiber and phytate contents were reduced as the concentrations of phytase and cellulase increased. The bioavailability of iron, calcium, and zinc was notably improved after in vitro digestion in 20% cellulase, combination enzyme, and 20% phytase, respectively. Muffins made with cellulase- and phytase-treated whole wheat flour showed improved quality and bioavailability of minerals. Phytase- and cellulase-treated whole wheat flour may be useful for development of functional food products with improved bioavailability of minerals.

• Journal of Nutrition and Health
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• v.30 no.1
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• pp.40-47
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• 1997

Dietary peptides have recently received attention regarding their beneficial effects on nutrient metabolism since the caseinphosphoptides obtained from casein hydrolysate are generally believed to enhance the intestinal absorption of Ca. The two experiments were conducted to investigate the effects of various hydrolyzed fractions of gluten on Ca bioavailability. The gluten hydrolysate of dietary components was produced by enzymatic hydrolysis of gluten whereas gluten hydrolysate supernationt and its precipiate resulted from centrifugation. In experiment I, the rats were for 4 weeks fed the 4 kinds of diets containing same amount of nitrogen and calories and diffeing only in the forms of nitrogen sources. The diets were gluten (G), gluten hydrolysat(GH), gluten hydrolysate supernatant(GHS) and gluten hydrolysate precipitatie(GHP). Determination was made for the body weight gain, serum Ca concentration, Ca solubility in small intestinal contents, bone weight, length and stength, bone ash and Ca content, and Ca balance, respectively. No significant difference was noticed as regards growth, serum Ca, and bone dimension and Ca content among rat groups. More significant increase was observed with regard to Ca absorption and intestinal solubility in the rats receiving the GH or GHS diet which containe crude gluten peptides, than in those subjected to G or GHP diet. In experiment II, in vitro determination for Ca solubility was made to ascertain the mechanism responsible for the effects of gluten peptides on Ca absorption. The 10mM Ca in potassium phosphate buffer solution(pH 7.0) incubated for 3 hours at 37$^{\circ}C$ by the GHS fraction, was observed to be capable of increasing the Ca solubility at 5-25mg/ml concentration of gluten peptides. These observations suggest that the gluten peptides from gluten hydrolysate may enhance the Ca absorption efficiency by increasing the solubility of Ca in small intestine.

• Journal of Pharmaceutical Investigation
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• v.27 no.1
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• pp.57-64
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• 1997

$Amino-{\beta}-lactam$ antibiotics are absorbed by the dipeptide transporter in the small intestine. These uptakes are coupled to a proton influx. The inward proton gradient is partly induced by the $Na^+/H^+$ exchanger and calcium ion is involved in control of this antiport. Interaction between ampicillin which is one of the $Amino-{\beta}-lactam$ antibiotics and nifedipine which is one of calcium channel blocking agents was studied in rats in vivo and with rabbit jejunum mounted on the Sweetana/Grass diffusion cells in vitro. Bioavailability of ampicillin was increased significantly when nifedipine was co-administered orally in rats. There were no differences in the distribution phase and the elimination phase when ampicillin was given either alone or with nifedipine intravenously. Conditions for in vitro experiments were determined. The lift rate of $O_2/CO_2$ gas was controlled to 3 bubbles/sec and ampicillin was stable in the Kreb's buffer at pH 6.0. Absorption of ampicillin was the greatest when the completely-stripped serosal membrane was used. Transport of ampicillin from mucosal to serosal side in the rabbit jejunum was enhanced by 32% in the presence of nifedipine (p=0.059). Above results suggest that nifedipine might increase the plasma level of ampicillin via the improved absorption in the intestine rather than the reduction in the elimination or/and alteration in the distribution.

• Journal of Pharmaceutical Investigation
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• v.36 no.4
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• pp.271-276
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• 2006

Felodipine, a calcium-antagonist of dihydropyridine type, is a poorly water soluble drug and has very low bioavailability. As preceding studies, use of solid dispersion systems and surfactants(solubilizers) has been suggested to increase dissolution and to improve bioavailability of felodipine. But in case of solid dispersion systems, large amount of toxic organic solvents should be used and manufacturing process time become longer than conventional process. In case of using surfactants, as time elapsed, decreasing of dissolution rate of felodipine due to crystallization has been reported. In this study, Copovidon as a hydrophilic polymer and $Transcutol^{\circledR}$ as a surfactant were combined to formulations if order to increase dissolution of felodipine and conventional wet granulation process were applied to manufacturing of formulations. The effect of Copovidon and $Transcutol^{\circledR}$ on the dissolution oi felodipine was investigated in-vitro. When Copovidon and $Transcutol^{\circledR}$ used simultaneously, the dissolution rate of felodipine was prominently increased compared with when used separately and the maximum increase in the dissolution of felodipine was 5.8 fold compared to control. This is most probably due to synergy effect by combination of Copovidon and $Transcutol^{\circledR}$. Felodipine sustained release tablets were successfully formulated using several grades of HPMC as a release retarding agent. The stability of felodipine sustained release tablet was evaluated after storage at accelerated condition($40^{\circ}C/75%\;RH$) for 6months in HDPE(High density polyethylene) bottle. Neither significant degradation nor change of dissolution rate for felodipine was observed after 6months. In conclusion, felodipine sustained release tablet was successfully formulated and dissolution of felodipine, poorly water soluble drug, was prominently increased and also stability was guaranteed by using combination system of hydrophilic polymer and surfactant.