• Title/Summary/Keyword: Bioavailability

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Importance of micronutrients in bone health of monogastric animals and techniques to improve the bioavailability of micronutrient supplements - A review

  • Upadhaya, Santi Devi;Kim, In Ho
    • Asian-Australasian Journal of Animal Sciences
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    • v.33 no.12
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    • pp.1885-1895
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    • 2020
  • Vitamins and minerals categorized as micronutrients are the essential components of animal feed for maintaining health and improving immunity. Micronutrients are important bioactive molecules and cofactors of enzymes as well. Besides being cofactors for enzymes, some vitamins such as the fat-soluble vitamins, vitamin A and D have been shown to exhibit hormone-like functions. Although they are required in small amount, they play an influential role in the proper functioning of a number of enzymes which are involved in many metabolic, biochemical and physiological processes that contribute to growth, production and health. Micronutrients can potentially have a positive impact on bone health, preventing bone loss and fractures, decreasing bone resorption and increasing bone formation. Thus, micronutrients must be provided to livestock in optimal concentrations and according to requirements that change during the rapid growth and development of the animal and the production cycle. The supply of nutrients to the animal body not only depends on the amount of the nutrient in a food, but also on its bioavailability. The bioavailability of these micronutrients is affected by several factors. Therefore, several technologies such as nanoparticle, encapsulation, and chelation have been developed to improve the bioavailability of micronutrients associated with bone health. The intention of this review is to provide an updated overview of the importance of micronutrients on bone health and methods applied to improve their bioavailability.

Bioavailability of Lycopene from Tomato Products

  • Shi, John;Naughton, Laura-Mac;Kakuda, Yukio;Bettger, William;Yeung, David;Jiang, Yueming
    • Preventive Nutrition and Food Science
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    • v.9 no.1
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    • pp.98-106
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    • 2004
  • 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.

Effects of Morin on the Bioavailability of Doxorubicin for Oral Delivery in Rats

  • Son, Hong-Mook;Choi, Jun-Shik
    • Journal of Pharmaceutical Investigation
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    • v.39 no.4
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    • pp.243-248
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    • 2009
  • The purpose of this study was to investigate the effects of morin, an antioxidant, on the bioavailability of doxorubicin (DOX) in rats. Thus, DOX was administered intravenously (10 mg/kg) or orally (50 mg/kg) with or without oral morin (0.5, 3 and 10 mg/kg). In the presence of morin, the total area under the plasma concentration-time curve (AUC) of DOX was significantly greater than that of the control. In the presence of 3 and 10 mg/kg of morin, the peak concentration $C_{MAX}$) was significantly higher than that of the control. Consequently, the absolute bioavailability (AB) of DOX in the presence of morin was 3.7-8.3%, which was significantly enhanced compared with those of the control group (2.7%). The relative bioavailability (RB) of DOX was 1.36 to 3.02 times higher than those of the control group. Compared to the intravenous control, the presence of morin increased the AUC of DOX, but was not significantly affected. The enhanced bioavailability of oral DOX by oral morin may be due to the inhibition of both P-glycoprotein (P-gp) and cytochrome P450 (CYP) 3A in the intestine and/or liver by morin. This result may suggest that the development of oral DOX combination with morin is feasible, which is more convenient than the i.v. dosage forms. The present study raised the awareness about the potential drug interactions by concomitant use of DOX with morin.

The Study on the Bioavailability of the Phenytoin Products (페니토인 제제의 생체이용률에 관한 연구)

  • 박경호;김낙두;이민화
    • YAKHAK HOEJI
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    • v.30 no.1
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    • pp.14-23
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    • 1986
  • This study was conducted to investigate the correlation between the dissolution rates and the bioavailabilities of commercial phenytoin products, and also the correlation between their biovailabilities in rabbits and those in humans. Dissolution test was conducted in pH 9. 0 alkaline borate buffer (0.2M) using basket method with seven phenytoin products commercially available. According to the dissolution rate, the phenytoin products were divided into three groups, such as rapid, intermediate and slow group. Three phenytoin products from each group were selected for the bioavailability test in rabbits and humans. The bioavailability test was carried out in rabbits and normal volunteers using cross over design. Single doses of 20mg/kg and 300mg/man were orally administered to rabbits and normal volunteers respectively. Average $C_{max}$, $t_{max}$ and AUC of three phenytoin products were determined from the serum concentration-time curve in rabbit and human experiments. The relative bioavailability evaluation was conducted using AUC of three phenytoin products. The correlations between the dissolution rate constants and bioavailabilities (AUC) of three phenytoin products in rabbits as well as those in humans were not found. Whereas, there was significant correlation between average AUC of three phenytoin products in humans and those in rabbits (r=0.993, p<0.1). From the results of this experiment, it can be concluded that the bioavailability of phenytoin products in humans may be predicted from the results of the rabbit experiment. Also it is assumed that the prediction of the bioavailability of phenytoin products in humans may be difficult from the only results of in vitro dissolution test.

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Iron Nutriture and Related Dietary Factors in Apparently Healthy Young Korean Women(2) : Analysis of Iron in Major Food Items and Assessment of Intake and Availability of Dietary Iron (우리나라 젊은 성인 여성의 철분영양상태와 이에 영향을 미치는 식이요인 분석 (2) : 주요 식품의 철분 분석과 철분 섭취량 및 이용율 평가)

  • 계승희
    • Journal of Nutrition and Health
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    • v.26 no.6
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    • pp.703-714
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    • 1993
  • The iron content of 178 food items were analyzed by ICP to provide database to calculate dietary intake of iron in Korea. The analysis data showed significant deviations of iron contents in some food items compared with Food Composition Table of KRNI which is most widely used at present. Three day dietary intake records were collected from 96 female college students to estimate mean daily iron intake and bioavailability of dietary iron. Mean daily intake of total iron in the study subjects was 13.2mg and heme iron intake was 0.94mg, 6.7% of total iron intake. BGioavailability of dietary iron was calculated by two methods. Total absorbable iron was calculated by the method of Monsen, body iron storage of the subjects being estimated with serum ferritin concentrations, was 1.21mg and bioavailability of dietary iron was thus 9.3%. Bioavailability calculated with the method by Hallberg was 11.22%. Two values of dietary iron bioavailability of the present study are lower than the reported values in adult women consuming typical western diets but within the range estimated for vegetarians. Considering high prevalence of iron deficiency based on serum ferritin concentrations and low bioavailability of diet in young adult Korean women, more efforts should be made to increase the content and bioavailability of iron in diet of Korea adult women.

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Effect of Solubilizing and Microemulsifying Excipients in Polyethylene Glycol 6000 Solid Dispersion on Enhanced Dissolution and Bioavailability of Ketoconazole

  • Heo, Min-Young;Piao, Zong-Zhu;Kim, Tae-Wan;Cao, Qing-Ri;Kim, Ae-Ra;Lee, Beom-Jin
    • Archives of Pharmacal Research
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    • v.28 no.5
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    • pp.604-611
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    • 2005
  • Polyethylene glycol (PEG) 6000-based solid dispersions (SDs), by incorporating various pharmaceutical excipients or microemulsion systems, were prepared using a fusion method, t o compare the dissolution rates and bioavailabilities in rats. The amorphous structure of the drug in SDs was also characterized by powder X-ray diffractometry (XRD) and differential scanning calorimetry (DSC). The ketoconazole (KT), as an antifungal agent, was selected as a model drug. The dissolution rate of KT increased when solubilizing excipients were incorporated into the PEG-based SDs. When hydrophilic and lipophilic excipients were combined and incorporated into PEG-based SDs, a remarkable enhancement of the dissolution rate was observed. The PEG-based SDs, incorporating a self microemulsifying drug delivery system (SMEDDS) or microemulsion (ME), were also useful at improving the dissolution rate by forming a microemulsion or dispersible particles within the aqueous medium. However, due to the limited solubilization capacity, these PEG-based SDs showed dissolution rates, below 50% in this study, under sink conditions. The PEG-based SD, with no pharmaceutical excipients incorporated, increased the maximum plasma concentration (C$_{max}$) and area under the plasma concentration curve (AUC$_{0-6h}$) two-fold compared to the drug only. The bioavailability was more pronounced in the cases of solubilizing and microemulsifying PEG-based SDs. The thermograms of the PEG-based SDs showed the characteristic peak of the carrier matrix around 60$^{\circ}C$, without a drug peak, indicating that the drug had changed into an amorphous structure. The diffraction pattern of the pure drug showed the drug to be highly crystalline in nature, as indicated by numerous distinctive peaks. The lack of the numerous distinctive peaks of the drug in the PEG-based SDs demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix of the amorphous structure. The utilization of oils, fatty acid and surfactant, or their mixtures, in PEG-based SD could be a useful tool to enhance the dissolution and bioavailability of poorly water-soluble drugs by forming solubilizing and microemulsifying systems when exposed to gastrointestinal fluid.

Effects of Baicalein on the Bioavailability of Nicardipine in Rats

  • Son, Hong-Mook;Choi, Jun-Shik
    • Journal of Pharmaceutical Investigation
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    • v.40 no.5
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    • pp.291-296
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    • 2010
  • This study was to investigate the effect of baicalein, an antioxidant, on the bioavailability of nicardipine after orally or intravenously administered nicardipine in rats. Nicardipine was administered orally (12 mg/kg) or intravenously (4 mg/kg) with or without orally administered baicalein (0.4, 2 or 10 mg/kg) to rats. In the inhibitory effect of baicalein on CYP3A4 activity, baicalein inhibited CYP3A4 activity with $IC_{50}$ values of 9.2 ${\mu}M$. The cell-based P-gp activity test using rhodamine-123 also showed that baicalein (30-10 ${\mu}M$, p<0.01) significantly inhibited P-gp activity. Compared with the control group (given nicardipine alone), the area under the plasma concentration-time curve (AUC) was significantly (2 mg/kg, P<0.05; 10 mg/kg, P<0.01) increased by 25.9-60.0%, and the peak concentration ($C_{max}$) was significantly (10 mg/kg, P<0.01) increased by 40.0% in the presence of baicalein after orally administration of nicardipine. Consequently, the relative bioavailability (R.B.) of nicardipine was increased by 1.26- to 1.60-fold and the absolute bioavailability (A.B.) was significantly (2 mg/kg, P<0.05; 10 mg/kg, P<0.01) increased by 26.0-59.9%. Compared to the i.v. control, baicalein did not significantly change pharmacokinetic parameters of nicardipine in i.v. administration. Accordingly, the enhanced oral bioavailability of nicardipine might be mainly due to increased intestinal absorption caused by P-gp inhibition rather than to reduced elimination of nicardipine by baicalein. The increase in the oral bioavailability might be mainly attributed to enhanced absorption in the small intestine via the inhibition of P-gp and reduced first-pass metabolism of nicardipine via the inhibition of the CYP3A subfamily in the small intestine and/or in the liver by baicalein. Based on these results, nicardipine dosage should be adjusted when given concomitantly with baicalein.