• Journal of the Korean Society of Food Science and Nutrition
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• v.28 no.3
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• pp.705-709
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• 1999

To evaluate iron bioavailability in iron fortified milk, in vitro and in vivo method were used. Low molecular weight components(ILC) from milk was isolated and iron was added, then soluble iron from ILC iron complex was determined. Each iron sources and extrinsically labelled with FeCl3 was used for measuring absorption rate of iron from ILC radiolabelled iron complexes as radioiron absorption into the blood one hour after injection into ligated duodenal loops of iron deficient rats. Iron absorption rate was in the order of ferrous lactate(25.56%)$\geq$ferric citrate(24.71%)$\geq$ferrous sulfate(19.67%) when 100ppm iron was used. In separate experiments, iron fortified milks with each iron sources were gavaged into iron deficient rats. When 25ppm iron was added to milk, the order of iron absorption was ferrous sulfate(12.52%)>ferrous lactate(8.07%)>ferric citrate(6.52%) (p<0.05). When 100ppm iron was added to milk, absorption rate was decreased compared to the treatments with added 25ppm of iron. Absorption rate of ferrous sulfate(5.34%) from milk added 100ppm iron was highly lowered, but ferric citrate(6.45%) was not significantly changed. The absorption rate of ferrous lactate(5.82%) was 70% of 25ppm iron added milk.

• Nutrition Research and Practice
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• v.8 no.5
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• pp.550-557
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• 2014

BACKGROUND/OBJECTIVES: Angelica keiskei is a green leafy vegetable rich in plant pigment phytochemicals such as flavonoids and carotenoids. This study examined bioavailability of flavonoids and carotenoids in Angelica keiskei and the alteration of the antioxidant performance in vivo. SUBJECTS AND MATERIALS: Absorption kinetics of phytochemicals in Angelica keiskei were determined in healthy older adults (> 60 y, n = 5) and subjects with metabolic syndrome (n = 5). Subjects consumed 5 g dry Angelica keiskei powder encapsulated in gelatin capsules with a low flavonoid and carotenoid liquid meal. Plasma samples were collected at baseline, 0.5, 1, 2, 3, 4, 5, 6, 7, and 8 h. Samples were analyzed for flavonoids and carotenoids using HPLC systems with electrochemical and UV detection, respectively, and for total antioxidant performance by fluorometry. RESULTS: After ingestion of Angelica keiskei increases in plasma quercetin concentrations were observed at 1-3 and 6-8 hr in the healthy group and at all time points in the metabolic syndrome group compared to baseline (P < 0.05). Plasma lutein concentrations were significantly elevated in both the healthy and metabolic syndrome groups at 8 hr (P < 0.05). Significant increases in total antioxidant performance were also observed in both the healthy and the metabolic syndrome groups compared to baseline (P < 0.05). CONCLUSIONS: Findings of this study clearly demonstrate the bioavailability of phytonutrients of Angelica keiskei and their ability to increase antioxidant status in humans.

• Archives of Pharmacal Research
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• v.26 no.7
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• pp.569-574
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• 2003

Controlled-release amitriptyline pellets (ATP) were formulated and its oral bioavailability was assessed in human volunteers after oral administration under fasting conditions. Core pellets were prepared using a CF granulator by two different methods (powder layering and solvent spraying) and coated with Eudragit RS or RL 100. Physical characteristics and dissolution rates of core pellets and coated pellets were evaluated to optimize the formulation. Powder layering method resulted in a better surface morphology than solvent spraying method. However, physical properties of the products were poorer when prepared by powder layering method with respect to hardness, friability and density. The dissolution profile of amitriptyline coated with Eudragit RS 100 was comparable to that of commercially available amitriptyline enteric-coated pellets ($Saroten^{\circledR}$ retard). After the oral administration of both products at the dose of 50 mg, the mean maximum concentrations ($C_{max}$) were 36.4 and 29.7 ng/mL, and the mean areas under the concentration-time curve ($AUC_{0-96}$) were 1180.2 and 1010.7 ng.h/mL for ATP and Saroten retard, respectively. The time to reach the maximum concentrations ($T_{max}$) was 6 h for both formulations. Statistical evaluation suggested that ATP was bioequivalent to Saroten retard.

• Journal of Veterinary Science
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• v.24 no.1
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• pp.3.1-3.13
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• 2023

Background: Zinc (Zn) is an essential cofactor for physiological homeostasis in the body. Zn oxide (ZnO), an inorganic compound that supplies Zn, exists in various sizes, and its bioavailability may vary depending on the size in vivo. However, comparative studies on the nutritional effects of micro-sized ZnO (M-ZnO) and nano-sized ZnO (N-ZnO) supplementation on Zn deficiency (ZnD) animal models have not been reported. Objectives: This study investigated the nutritional bioavailability of N-ZnO and M-ZnO particles in dietary-induced ZnD mice. Methods: Animals were divided into six experimental groups: normal group, ZnD control group, and four ZnO treatment groups (Nano-Low, Nano-High, Micro-Low, and MicroHigh). After ZnD induction, N-ZnO or M-ZnO was administered orally every day for 4 weeks. Results: ZnD-associated clinical signs almost disappeared 7 days after N-ZnO or M-ZnO administration. Serum Zn concentrations were higher in the Nano-High group than in the ZnD and M-ZnO groups on day 7 of ZnO treatment. In the liver and testis, Nano-Low and Nano-High groups showed significantly higher Zn concentrations than the other groups after 14-day treatment. ZnO supplementation increased Mt-1 mRNA expression in the liver and testis and Mt-2 mRNA expression in the liver. Based on hematoxylin-and-eosin staining results, N-ZnO supplementation alleviated histological damage induced by ZnD in the testis and liver. Conclusions: This study suggested that N-ZnO can be utilized faster than M-ZnO for nutritional restoration at the early stage of ZnD condition and presented Mt-1 as an indicator of Zn status in the serum, liver, and testis.

• Biomolecules & Therapeutics
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• v.25 no.5
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• pp.553-558
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• 2017

Paclitaxel (PTX) is one of the most frequently used anticancer agent for treating refractory ovarian cancer, metastatic breast cancer and non-small cell lung cancer. However, its oral administration is impeded by very low bioavailability (<5%) due to the P-glycopprotein (P-gp) efflux pump effect. This study investigated in vitro and in vivo P-gp inhibitory effects of adamantyl derivatives AC-603 and AC-786 in rats. Two adamantyl derivatives tested in this study increased the cytotoxicity of daunomycin (DNM) in P-gp overexpressed cell line by inhibiting P-gp efflux function. Pharmacokinetics of PTX with orally co-administered P-gp inhibitors were assessed in rats to improve PTX absorption. The pharmacokinetic parameters of PTX were determined in rats after intravenous (2 mg/kg) or oral (25 mg/kg) administration in the presence or absence of verapamil (a positive control), AC-603 or AC-786 (0.5 mg/kg or 5 mg/kg). Compared to control group (PTX alone), experimental groups (PTX with AC-603 or AC-786) significantly increased the area under the plasma concentration-time curve of PTX following oral administration by 1.7-2.2 fold. The volume of distribution and total clearance of PTX were decreased, while other parameters were not significantly changed. In conclusion, co-administration of AC-603 or AC-786 enhanced the relative bioavailability of orally administered PTX as compared to control.

• Journal of Pharmaceutical Investigation
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• v.29 no.2
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• pp.99-103
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• 1999

Self-Emulsifying System(SES), an isotropic mixture of oil and surfactant which forms oil-in-water emulsion, is expected to improve in vitro drug dissolution and enhance in vivo drug absorption. A poorly water soluble drug, ibu-profen(IBP) was incorporated into the SES to improve absorption, and enhance bioavailability of drug. Medium chain triglyceride, glyceryl tricaprylate(GTC) as an oil, and Tween 85 as a surfactant were used to formulate SES. To characterize SESs with various concentrations of Tween 85, the phase separation and solubility of IBP-SEDDS containing IBP as a function of Tween 85 concentration were conducted, and the particle size was measured using photon correlation spectroscopic method. The SES with optimal concentration of Tween 85(35%(w/w)) was selected based on its high drug loading, small particle size and low surfactant concentration. After an oral administration of IBP-SEDDS and IBP suspension in methyl cellulose equivalent to 40.0 mg/kg to rats, the pharmacokinetic parameters were compared. The $C_{max}(163.17\;vs\;88.82\;{\mu}g/ml)$, $AUC(12897.01\;vs\;8751.13\;{\mu}g\;min/ml)$ and Bioavailability(86.44 vs 58.65%) significantly increased but $T_max(10\;vs\;20\;min)$ was significantly advanced. The current SEDDS containing IBP provide an alternative to improve an oral bio-availability of IBP.

• Journal of Pharmaceutical Investigation
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• v.24 no.4
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• pp.265-271
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• 1994

Cefazolin ethoxycarbonylethyl ester (CFZ-ET) was synthesized to improve oral absorption and bioavailability of the parent drug by esterification of sodium cefazolin (CFZ-Na). The successful synthesis of CFZ-ET was identified with analysis of UV spectra, FT-lR spectra and NMR spectra. Partition coefficient studies showed that CFZ-ET was more lipophilic than CFZ-Na and the ester was hydrolyzed into the parent drug in vivo. Although CFZ-ET did not have antimicrobial activity in vitro, the plasma taken after the oral administration of CFZ-ET had antimicrobial activity. Based on above observations, CFZ-ET might be rapidly hydrolyzed to CFZ in the body. Therefore, it may be concluded that CFZ-ET could be a novel prodrug of CFZ which can improve the bioavailability of CFZ-Na.

• Archives of Pharmacal Research
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• v.26 no.10
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• pp.778-784
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• 2003

N'-(1-alkyl-2,3-dihydro-2-oxo-1H-3-indolyliden)-4-pyridinecarboxylic acid hydrazide derivatives, 3(a-g), were synthesized in a trial to overcome the resistance developed with the therapeutic uses of isoniazid (INH). The lipophilicity of the synthesized derivatives supersedes that of the INH as expressed by Clog p values. The synthesized compounds and INH were tested against bovin, human sensitive and human resist strains of Mycobacterium tuberculosis. Compounds 3a, 3d, 3f and 3g with 1-unsubstituted, 1-propyl, 1-propynyl and 1-benzyl groups respectively exhibited equipotent growth inhibitory activity (MIC 10 $\mu$mol) against the tested strains as compared with INH however the later has no activity against human resist strain. Pharmacokinetic study revealed that the rate and extent of absorption of the tested derivatives (3d and 3f) significantly higher than that of INH (p＜0.05). The relative bioavailabilities ($F_R%$) were 183.15 and 443.25 for 3f and 3d respectively as compared to INH. These results preliminary indicate the possible use of the prepared derivatives for treatment of tuberculosis infections in order to overcome the resistance developed with INH.

• Journal of Pharmaceutical Investigation
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• v.37 no.6
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• pp.349-354
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• 2007

For decades, the various virtues of ${\alpha}-lipoic$ acid (ALA), a natural material synthesized in most cells, have been intensively studied and proved. Recently it was reported that ALA caused significant bodyweight reduction via appetite suppression. Unfortunately, the efficacy requires an administration over 50 mg/kg. The low bioavailability and the short plasma half life of ALA lead us to explore novel pharmaceutical dosage forms using nanoparticles. In this study, the effect of polymeric stabilizers on the bioavailability improvement of ALA nanoparticles was investigated. The reduction of particle size via nano-comminution technology was successful resulting in volume average particle sizes of 320 - 340 nm. The in vitro release rate of ALA did not reflect the decrease of particle size, possibly because of the self polymerization of ALA during nano-comminution. The type of polymeric stabilizers could not affect the release rate either. However, the in vivo food intake results of ALA showed that nano-suspensions were more effective than microparticles or a salt form. The nano-suspension containing polyvinyl pyrrolidone as the primary stabilizer and polyacrylic acid as the secondary stabilizer showed more improved efficacy for 2 hours.

• Toxicological Research
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• v.35 no.4
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• pp.403-410
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• 2019

Curcumin, a hydrophobic polyphenol isolated from the Curcuma longa L. plant, has many pharmacological properties, including antioxidant, anti-inflammatory, and chemo-preventive activities. Curcumin has been shown to have potential in preventing nonalcoholic fatty liver disease (NAFLD). However, the low bioavailability of curcumin has proven to be a major limiting factor in its clinical adoption. Theracurmin, a highly bioavailable curcumin that utilizes micronized technology showed improved biological absorbability in vivo. The aim of this study was to investigate the role of theracurmin in modulating hepatic lipid metabolism in vivo. A fatty liver mouse model was produced by feeding mice a high fat diet (HFD; 60% fat) for 12 weeks. We found that treatment for 12 weeks with theracurmin significantly lowered plasma triacylglycerol (TG) levels and reduced HFD-induced liver fat accumulation. Theracurmin treatment lowered hepatic TG and total cholesterol (T-CHO) levels in HFD-fed mice compared to controls. In addition, theracurmin administration significantly reduced lipid peroxidation and cellular damage caused by reactive oxygen species in HFD-fed mice. Overall, these results suggest that theracurmin has the ability to control lipid metabolism and can potentially serve as an effective therapeutic remedy for the prevention of fatty liver.