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  1. Theoretically-derived molecular descriptors important in human intestinal absorption
    Agatonovic-Kustrin S, Beresford R, Yusof AP
    J Pharm Biomed Anal, 2001 May;25(2):227-37.
    PMID: 11275432
    A quantitative structure-human intestinal absorption relationship was developed using artificial neural network (ANN) modeling. A set of 86 drug compounds and their experimentally-derived intestinal absorption values used in this study was gathered from the literature and a total of 57 global molecular descriptors, including constitutional, topological, chemical, geometrical and quantum chemical descriptors, calculated for each compound. A supervised network with radial basis transfer function was used to correlate calculated molecular descriptors with experimentally-derived measures of human intestinal absorption. A genetic algorithm was then used to select important molecular descriptors. Intestinal absorption values (IA%) were used as the ANN's output and calculated molecular descriptors as the inputs. The best genetic neural network (GNN) model with 15 input descriptors was chosen, and the significance of the selected descriptors for intestinal absorption examined. Results obtained with the model that was developed indicate that lipophilicity, conformational stability and inter-molecular interactions (polarity, and hydrogen bonding) have the largest impact on intestinal absorption.
    Matched MeSH terms: Intestinal Absorption/physiology*
  2. Absorption, distribution and elimination behaviours of cadmium treated by in vitro DIN from WLP residue using SAAM II modeling
    Yasmin Mohd Idris Perama, Nur Shahidah Abdul Rashid, Syazwani Mohd Fadzil, Khoo Kok Siong
    Sains Malaysiana, 2018;47:611-618.
    Mathematically, the human alimentary tract organs were simplified in the model structure as separate compartments with
    pathways of transfer that are kinetically homogenous and equally distributed. The development of gastro-compartment
    model follows the first order kinetics of differential equations to describe cadmium absorption, distribution and elimination
    in the human digestive system. With the aid of in vitro DIN assay, an artificial gastric and gastrointestinal fluid were
    prepared using water leach purification (WLP) residue as a sample that contained toxic metals cadmium. The Simulation,
    Analysis and Modelling II (SAAM II) V2.1 software is employed to design models easily, simulate experiments quickly and
    analyze data accurately. Based on the experimental inputs and fractional transfer rates parameter incorporated to the
    gastro-compartment model, the concentration of cadmium against time profile curves were plotted as the model output.
    The curve presented concentration of cadmium in both gastric and gastrointestinal fluid where initially absorption phase
    (first hour) occurred followed by the distribution phase (second to third hours) and elimination process (third to fifth
    hours). The concentration of cadmium obtained from the simulated model structures was in good agreement with the
    fitted model predicted measurements as statistical t-test conducted showed the values were not significantly different.
    Therefore, modeling approach with SAAM II software gave realistic and better estimation of cadmium dissolution into
    the human gastrointestinal tract.
    Matched MeSH terms: Intestinal Absorption; Gastrointestinal Absorption
  3. Intestinal permeability studies of sulpiride incorporated into self-microemulsifying drug delivery system (SMEDDS)
    Chitneni M, Peh KK, Darwis D, Abdulkarim M, Abdullah GZ, Qureshi MJ
    Pak J Pharm Sci, 2011 Apr;24(2):113-21.
    PMID: 21454158
    The objective of the present study was to determine the intestinal absorption of sulpiride incorporated into SMEDDS by means of single-pass intestinal perfusion method (SPIP) in rat and to compare the effective permeability coefficient obtained with that of drug solution and micellar solution. The prepared SMEDDS and micelles formulations were investigated for droplets size. SPIP experiment was performed using the three formulations in three of the secluded regions of the small intestine (duodenum, jejunum, and ileum). The amount of the drug in the samples was estimated by HPLC and the effective permeability coefficients in rats were calculated. The human intestinal permeability was predicted based on rat effective permeability coefficient value. The dilution stability of the formulations was also determined. The average droplet size of SMEDDS and micelles was 9.27 nm and 7.20 nm respectively. The effective permeability coefficient of sulpiride was appreciably lower in the ileum weighed against jejunum and duodenum when administered as a solution (P<0.05). The estimated human absorption of sulpiride for the SMEDDS dilutions was superior to that from solution (P<0.05) and similar to micellar solution. The micellar dilutions were unstable whereas the SMEDDS dilutions were stable. Based on the above results, SMEDDS can be a potential candidate for improving the peroral absorption of the sulpiride.
    Matched MeSH terms: Intestinal Absorption*
  4. Oral epigallocatechin gallate reduces intestinal nadolol absorption via modulation of Oatp1a5 and Oct1 transcriptional levels in spontaneously hypertensive rats
    Tan HJ, Ling WC, Chua AL, Lee SK
    Phytomedicine, 2021 Sep;90:153623.
    PMID: 34303263 DOI: 10.1016/j.phymed.2021.153623
    BACKGROUND: Concurrent use of epigallocatechin-3-gallate (EGCG) and medication may lead to botanical-drug interactions, subsequently therapeutic failure or drug toxicity. It has been reported that EGCG reduces plasma nadolol bioavailability in normotensive models. Nevertheless, evidence on the effects of EGCG on hypertensive model, and the possible underlying mechanism have not been elucidated.

    OBJECTIVES: This study aims (i) to investigate the effects of EGCG on nadolol pharmacokinetics (maximum plasma concentration, time to achieve maximum concentration, area under the time-plasma concentration curve, plasma half-life and total clearance) and subsequently its impact on blood pressure control; and (ii) to identify transcriptional regulatory roles of EGCG on the nadolol intestinal and hepatic drug-transporters in SHR.

    METHODS: Male SHR were pre-treated with a daily dose of EGCG (10 mg/kg body weight, i.g.) for 13 days. On day-14, a single dose of nadolol (10 mg/kg body weight) was given to the rats 30 min after the last dose of EGCG administration. Systolic blood pressure (SBP) was measured at 6-h and 22-h post-nadolol administration. Plasma and urinary nadolol concentrations were quantified using high-performance liquid chromatography, and pharmacokinetic parameters were analyzed by using non-compartmental analysis. Hepatic and ileal Oatp1a5, P-gp, and Oct1 mRNA expressions were determined by real-time PCR.

    RESULTS: SBP of SHR pre-treated with EGCG and received nadolol was significantly higher than those which were not pre-treated with EGCG but received nadolol. Pre-treatment of EGCG resulted in a marked reduction of plasma nadolol maximum concentration (Cmax) and area under the time-plasma concentration curve (AUC) by 53% and 51% compared to its control. The 14-day treatment with oral EGCG led to a significant downregulation of mRNA levels of ileal Oatp1a5, P-gp, and Oct1 genes by 4.03-, 8.01- and 4.03-fold; and hepatic P-gp, and Oct1 genes by 2.61- and 2.66-fold.

    CONCLUSION: These data concluded that exposure to EGCG could lead to reduced nadolol bioavailability and therefore, uncontrolled raised blood pressure and higher risks of cardiovascular events. Our data suggest that the reduced nadolol bioavailability is associated with the downregulation of ileal Oatp1a5 and Oct1 mRNA levels that subsequently lead to poor absorption of nadolol to the systemic circulation.

    Matched MeSH terms: Intestinal Absorption*
  5. Intestinal permeability of mitragynine in rats using in situ absorption model
    Jagabalan JDY, Murugaiyah V, Zainal H, Mansor SM, Ramanathan S
    J Asian Nat Prod Res, 2019 Apr;21(4):351-363.
    PMID: 29667422 DOI: 10.1080/10286020.2018.1461088
    The intestinal permeability of mitragynine was investigated in situ using a single pass intestinal perfusion (SPIP) absorption model, in small intestine of rat using mitragynine in the absence/presence of the permeability markers, P-gp and/or CYP3A4 inhibitors. Mitragynine demonstrated high intestinal permeability (Peff of 1.11 × 10-4 cm/s) that is in the range of highly permeable drugs such as propranolol (Peff of 1.27 × 10-4 cm/s) indicating that it readily crosses the intestine. The addition of azithromycin (P-glycoprotein inhibitor) and ciprofloxacin (CYP3A4 inhibitor) or combination of both has no effect on intestinal permeability of mitragynine across the rat small intestine.
    Matched MeSH terms: Intestinal Absorption*
  6. Fulltext Small intestinal absorption studies and biopsy findings in Asians, in Singapore
    Jayaratnam FJ, Tan KK, Jacob E, Seah CS, Kho KM
    Singapore Med J, 1970 Dec;11(4):275-82.
    PMID: 5511860
    Investigations in 30 healthy control subjects of Indian, Chinese and Malay ethnic origin, revealed that all the Chinese and about two thirds of the Indians and Malays had a normal capacity to absorb D—xylose, Vitamin A, Co58 labelled Vitamin B12 and dietary fat. About a third of the Indians and Malays were unable to absorb one or two of the four test substances used in the absorption studies. Jejunal biopsies did not differ in the 3 ethnic groups and were normal or mildly abnormal. 27 patients presenting with anorexia, a sore tongue and pallor were also investigated. Indians formed the majority of the patients. Diarrhoea occurred in only 51 % of the patients. All had a megaloblastic anaemia. Absorption studies revealed malabsorption of xylose, Vitamin A and Vitamin B12 in the majority but steatorrhoea occurred in only 26% of the patients. Jejunal biopsies were mildly abnormal in 8% and moderately or severely abnormal in 92 % of the patients. All responded to folic acid or Vitamin B12 therapy. 16 patients were restudied after 5 to 24 months therapy and the majority were found to have improved. Results of investigations and response to therapy indicate that these patients were suffering from tropical sprue. These studies indicate that tropical sprue in Singapore affects Indians mainly and can often present without diarrhoea and steatorrhoea.
    Matched MeSH terms: Intestinal Absorption*
  7. Fulltext Isolated Hypophosphataemia Mimicking Cerebrovascular Accident
    Hanizah Ngadiron, Razrim Rahim, Firdaus Hayati, Nornazirah Azizan, Affirul Chairil Ariffin
    Borneo Journal of Medical Sciences, 2019;13(1):29-32.
    MyJurnal
    Hypophosphataemia occurs in an abnormally low serum phosphate level. Three main mechanisms are postulated: decreased intestinal absorption, increased renal excretion, and extracellular shifts to intracellular compartments. It is potentially a fatal disease if not intervene. The management is merely treating the underlying disorder, giving phosphate supplement and requiring close biochemical monitoring. The incidence of symptomatic isolated hypophosphataemia is extremely rare. In this case report, a 33-year-old man presented with three days history of dysphagia, inability to complete sentences and generalized muscle weakness. He developed blurred vision especially upon exposure to bright light. He had a history of single parathyroidectomy for parathyroid adenoma 2 years ago. Physical examinations were unremarkable. Laboratory investigations were normal except for phosphate level of 0.30 mmol/L. Intravenous KH2PO4 with a dosage of 10 mmol was administered in slow bolus in 3 hours. His symptoms resolved slowly after correction. Although isolated hypophosphataemia is rare but need to recognize the symptoms and signs of hypophosphataemia and treat accordingly.
    Matched MeSH terms: Intestinal Absorption
  8. Absorption of calcium from milk and tempeh consumed by postmenopausal Malay women using the dual stable isotope technique
    Haron H, Shahar S, O'Brien KO, Ismail A, Kamaruddin N, Rahman SA
    Int J Food Sci Nutr, 2010 Mar;61(2):125-37.
    PMID: 19995131 DOI: 10.3109/09637480903348080
    Assessment of calcium bioavailability from non-dairy foods containing moderate amounts of calcium is especially important in populations that have habitually low dairy consumption. Absorption of calcium from milk and tempeh (a traditional fermented soy product) was compared in a sample of Malay subjects. A randomized, crossover design was utilized to assess calcium absorption in 20 postmenopausal women from either a glass of milk (114 g) or from a meal of tempeh (206 g); each containing 130 mg calcium. At each study of Phase 1 (mid-July) and Phase 2 (mid-August), intravenous (42)Ca and oral (44)Ca were administered and calcium absorption was measured in 24-h urine collections post-dosing; with a 1-month washout period between phases. Absorption of calcium from tempeh did not differ significantly from milk (36.9 +/- 10.6% vs. 34.3 +/- 8.6%, respectively). Due to differences in the calcium content of tempeh, four servings of this product would be needed to get the same amount of absorbed calcium as that obtained from a 4-ounce glass of milk. Tempeh may provide readily available calcium for this population of women at risk for low bone mass.
    Matched MeSH terms: Intestinal Absorption*
  9. Fulltext Aqueous Extract of Nypa fruticans Wurmb. Vinegar Alleviates Postprandial Hyperglycemia in Normoglycemic Rats
    Yusoff NA, Ahmad M, Al-Hindi B, Widyawati T, Yam MF, Mahmud R, et al.
    Nutrients, 2015 Aug;7(8):7012-26.
    PMID: 26308046 DOI: 10.3390/nu7085320
    Nypa fruticans Wurmb. vinegar, commonly known as nipa palm vinegar (NPV) has been used as a folklore medicine among the Malay community to treat diabetes. Early work has shown that aqueous extract (AE) of NPV exerts a potent antihyperglycemic effect. Thus, this study is conducted to evaluate the effect of AE on postprandial hyperglycemia in an attempt to understand its mechanism of antidiabetic action. AE were tested via in vitro intestinal glucose absorption, in vivo carbohydrate tolerance tests and spectrophotometric enzyme inhibition assays. One mg/mL of AE showed a comparable outcome to the use of phloridzin (1 mM) in vitro as it delayed glucose absorption through isolated rat jejunum more effectively than acarbose (1 mg/mL). Further in vivo confirmatory tests showed AE (500 mg/kg) to cause a significant suppression in postprandial hyperglycemia 30 min following respective glucose (2 g/kg), sucrose (4 g/kg) and starch (3 g/kg) loadings in normal rats, compared to the control group. Conversely, in spectrophotometric enzymatic assays, AE showed rather a weak inhibitory activity against both α-glucosidase and α-amylase when compared with acarbose. The findings suggested that NPV exerts its anti-diabetic effect by delaying carbohydrate absorption from the small intestine through selective inhibition of intestinal glucose transporters, therefore suppressing postprandial hyperglycemia.
    Matched MeSH terms: Intestinal Absorption/drug effects
  10. Fulltext Microencapsulated Tuna Oil Results in Higher Absorption of DHA in Toddlers
    Ghasemi Fard S, Loh SP, Turchini GM, Wang B, Elliott G, Sinclair AJ
    Nutrients, 2020 Jan 18;12(1).
    PMID: 31963702 DOI: 10.3390/nu12010248
    : Docosahexaenoic acid (DHA) is an essential component for brain and visual acuity development during foetal and early postnatal life. A newly released directive under the European Commission stipulates DHA as a mandatory ingredient in infant formula. This poses challenges to manufacturers in preserving the stability and bioavailability of DHA at levels akin to human breast milk. The aims of this study were (a) to investigate the bioavailability of microencapsulated omega-3 DHA formulations in healthy toddlers compared with high DHA fish oil for a one-month period and (b) to assess the effect of DHA supplementation on children's sleep and cry patterns. Sixty toddlers were randomly allocated to four groups: 1. unfortified formula, 2. unfortified formula plus high DHA tuna oil, 3. fortified formula with dairy-based microencapsulated high DHA tuna oil powder, and 4. fortified formula with allergenic-free microencapsulated high DHA tuna oil powder. Bioavailability was assessed from both blood and faecal fatty acid levels. The results showed an enhanced bioavailability with significantly greater concentrations of blood DHA levels in formulas with microencapsulated powders. There were no significant effects of treatment on sleep and cry patterns. Application and delivery of microencapsulated DHA tuna oil powder in toddlers' formula provided better bioavailability of the active DHA.
    Matched MeSH terms: Intestinal Absorption*
  11. Enhancing biopharmaceutical performance of an anticancer drug by long chain PUFA based self-nanoemulsifying lipidic nanomicellar systems
    Khurana RK, Beg S, Burrow AJ, Vashishta RK, Katare OP, Kaur S, et al.
    Eur J Pharm Biopharm, 2017 Dec;121:42-60.
    PMID: 28887099 DOI: 10.1016/j.ejpb.2017.09.001
    The aim of this study was to develop polyunsaturated fatty acid (PUFA) long chain glyceride (LCG) enriched self-nanoemulsifying lipidic nanomicelles systems (SNELS) for augmenting lymphatic uptake and enhancing oral bioavailability of docetaxel and compare its biopharmaceutical performance with a medium-chain fatty acid glyceride (MCG) SNELS. Equilibrium solubility and pseudo ternary phase studies facilitated the selection of suitable LCG and MCG. The critical material attributes (CMAs) and critical process parameters (CPPs) were earmarked using Placket-Burman Design (PBD) and Fractional Factorial Design (FFD) for LCG- and MCG-SNELS respectively, and nano micelles were subsequently optimized using I- and D-optimal designs. Desirability function unearthed the optimized SNELS with Temul <5min, Dnm <100nm, Rel15min >85% and Perm45min >75%. The SNELS demonstrated efficient biocompatibility and energy dependent cellular uptake, reduced P-gp efflux and increased permeability using bi-directional Caco-2 model. Optimal PUFA enriched LCG-SNELS exhibited distinctly superior permeability and absorption parameters during ex vivo permeation, in situ single pass intestinal perfusion, lymphatic uptake and in vivo pharmacokinetic studies over MCG-SNELS.
    Matched MeSH terms: Intestinal Absorption/drug effects
  12. Fulltext Preparation and characterization of nano liposomes of Orthosiphon stamineus ethanolic extract in soybean phospholipids
    Aisha AF, Majid AM, Ismail Z
    BMC Biotechnol, 2014;14:23.
    PMID: 24674107 DOI: 10.1186/1472-6750-14-23
    O. stamineus is a medicinal herb with remarkable pharmacological properties. However, poor solubility of the active principles limits its medicinal value. This study sought to prepare nano liposomes of OS ethanolic extract in unpurified soybean phospholipids in order to improve its solubility and permeability. OS liposomes were prepared by the conventional film method, and were characterized for solubility, entrapment efficiency, Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), particle size and zeta potential, release, absorption in everted rat intestinal sacs, and DPPH scavenging effect.
    Matched MeSH terms: Intestinal Absorption
  13. Knowledge, attitude and practice towards dietary iron among patients with thalassemia and their caregivers in Peninsular Malaysia
    Chin DM, Kader Maideen SF, Rashid A
    Med J Malaysia, 2019 Oct;74(5):365-371.
    PMID: 31649210
    INTRODUCTION: Thalassemias are the most common human monogenic disorders in the world. Regular blood transfusion and increased intestinal absorption of iron among thalassemia patients will lead to iron overload, which will not only markedly decrease their life expectancy but also pose a heavy burden to the healthcare system. The objective of this study was to evaluate the level of knowledge, attitude and practice towards dietary iron among thalassemia patients and their caregivers.

    METHODS: An analytical cross-sectional study using purposive sampling method was conducted at eight thalassemia societies in Peninsular Malaysia. 260 respondents comprised of patients and caregivers were assessed with two separate sets of questionnaires.

    RESULTS: Knowledge on dietary iron among the respondents was unsatisfactory, despite them having good knowledge on thalassemia disorder. Female patients were found to have better dietary knowledge, attitude and practice compared to males. The percentage of caregivers with good attitude and good practice were significantly higher compared to adult patients. Caregivers with children on iron chelators were noted to have better dietary attitude and practice. Thalassemia knowledge and children on vitamins were found to be the predictors of dietary knowledge among the patients and caregivers respectively.

    CONCLUSION: The level of knowledge on dietary iron among the patients and caregivers was unsatisfactory in spite of their attitude and practice towards dietary iron were good. Effective delivery of dietary information to the patients and caregivers is essential to enable them to choose a healthy diet for their condition.

    Matched MeSH terms: Intestinal Absorption
  14. Pharmacokinetic and bioequivalent study of a generic Metoprolol tablet preparation
    Yuen KH, Peh KK, Chan KL, Toh WT
    Drug Dev Ind Pharm, 1998 Oct;24(10):955-9.
    PMID: 9876550
    A study was conducted to compare the in vivo bioavailability of a generic metoprolol tablet preparation (Metoprolol) with that of the innovator product, Betaloc. Both preparations have a labeled dose of 100 mg metoprolol tartrate. Twelve healthy adult male volunteers participated in the study, which was conducted according to a standard two-way crossover design with a washout period of 1 week. The bioavailability was compared using the total area under the plasma level versus time curve (AUC0-infinity), peak plasma concentration (Cmax), and time to reach peak plasma concentration (Tmax). No statistically significant difference was observed between the logarithmically transformed AUC0-infinity values or the logarithmically transformed Cmax values of the two preparations. However, a statistically significant difference was observed between the Tmax values, but may not be therapeutically significant or important. Moreover, the 90% confidence interval (CI) for the ratio of the logarithmically transformed AUC0-infinity values of Metoprolol over those of Betaloc was calculated to be between 0.94 and 1.02, while that of Cmax was between 0.98 and 1.01, both of which are within the acceptable limit of 0.80-1.25. From the data obtained, it was also observed that a high proportion of our volunteers of Asian origin appeared to be poor metabolizers of metoprolol, which was consistent with what had been observed in our previous study of another preparation of metoprolol.
    Matched MeSH terms: Intestinal Absorption
  15. Fulltext PEGylated Lipid Polymeric Nanoparticle-Encapsulated Acyclovir for In Vitro Controlled Release and Ex Vivo Gut Sac Permeation
    Mahmood S, Kiong KC, Tham CS, Chien TC, Hilles AR, Venugopal JR
    AAPS PharmSciTech, 2020 Oct 14;21(7):285.
    PMID: 33057878 DOI: 10.1208/s12249-020-01810-0
    Currently, pharmaceutical research is directed wide range for developing new drugs for oral administration to target disease. Acyclovir formulation is having common issues of short half-life and poor permeability, causing messy treatment which results in patient incompliance. The present study formulates a lipid polymeric hybrid nanoparticles for antiviral acyclovir (ACV) agent with Phospholipon® 90G (lecithin), chitosan, and polyethylene glycol (PEG) to improve controlled release of the drugs. The study focused on the encapsulation of the ACV in lipid polymeric particle and their sustained delivery. The formulation developed for the self-assembly of chitosan and lecithin to form a shell encapsulating acyclovir, followed by PEGylation. Optimisation was performed via Box-Behnken Design (BBD), forming nanoparticles with size of 187.7 ± 3.75 nm, 83.81 ± 1.93% drug-entrapped efficiency (EE), and + 37.7 ± 1.16 mV zeta potential. Scanning electron microscopy and transmission electron microscopy images displayed spherical nanoparticles formation. Encapsulation of ACV and complexity with other physical parameters are confirmed through analysis using Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. Nanoparticle produced was capable of achieving 24-h sustained release in vitro on gastric and intestinal environments. Ex vivo study proved the improvement of acyclovir's apparent permeability from 2 × 10-6 to 6.46 × 10-6 cm s-1. Acyclovir new formulation was achieved to be stable up to 60 days for controlled release of the drugs. Graphical abstract.
    Matched MeSH terms: Intestinal Absorption
  16. A 1-h time interval between a meal containing iron and consumption of tea attenuates the inhibitory effects on iron absorption: a controlled trial in a cohort of healthy UK women using a stable iron isotope
    Ahmad Fuzi SF, Koller D, Bruggraber S, Pereira DI, Dainty JR, Mushtaq S
    Am J Clin Nutr, 2017 Dec;106(6):1413-1421.
    PMID: 29046302 DOI: 10.3945/ajcn.117.161364
    Background: Tea has been shown to be a potent inhibitor of nonheme iron absorption, but it remains unclear whether the timing of tea consumption relative to a meal influences iron bioavailability.Objective: The aim of the study was to investigate the effect of a 1-h time interval of tea consumption on nonheme iron absorption in an iron-containing meal in a cohort of iron-replete, nonanemic female subjects with the use of a stable isotope (57Fe).Design: Twelve women (mean ± SD age: 24.8 ± 6.9 y) were administered a standardized porridge meal extrinsically labeled with 4 mg 57Fe as FeSO4 on 3 separate occasions, with a 14-d time interval between each test meal (TM). The TM was administered with water (TM-1), with tea administered simultaneously (TM-2), and with tea administered 1 h postmeal (TM-3). Fasted venous blood samples were collected for iron isotopic analysis and measurement of iron status biomarkers. Fractional iron absorption was estimated by the erythrocyte iron incorporation method.Results: Iron absorption was 5.7% ± 8.5% (TM-1), 3.6% ± 4.2% (TM-2), and 5.7% ± 5.4% (TM-3). Mean fractional iron absorption was found to be significantly higher (2.2%) when tea was administered 1 h postmeal (TM-3) than when tea was administered simultaneously with the meal (TM-2) (P = 0.046). An ∼50% reduction in the inhibitory effect of tea (relative to water) was observed, from 37.2% (TM-2) to 18.1% (TM-3).Conclusions: This study shows that tea consumed simultaneously with an iron-containing porridge meal leads to decreased nonheme iron absorption and that a 1-h time interval between a meal and tea consumption attenuates the inhibitory effect, resulting in increased nonheme iron absorption. These findings are not only important in relation to the management of iron deficiency but should also inform dietary advice, especially that given to those at risk of deficiency. This trial was registered at clinicaltrials.gov as NCT02365103.
    Matched MeSH terms: Intestinal Absorption/drug effects*
  17. Biowaiver monograph for immediate-release solid oral dosage forms: bisoprolol fumarate
    Charoo NA, Shamsher AA, Lian LY, Abrahamsson B, Cristofoletti R, Groot DW, et al.
    J Pharm Sci, 2014 Feb;103(2):378-91.
    PMID: 24382794 DOI: 10.1002/jps.23817
    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate-release (IR) solid oral dosage forms containing bisoprolol as the sole active pharmaceutical ingredient (API) are reviewed. Bisoprolol is classified as a Class I API according to the current Biopharmaceutics Classification System (BCS). In addition to the BCS class, its therapeutic index, pharmacokinetic properties, data related to the possibility of excipient interactions, and reported BE/bioavailability problems are taken into consideration. Qualitative compositions of IR tablet dosage forms of bisoprolol with a marketing authorization (MA) in ICH (International Conference on Harmonisation) countries are tabulated. It was inferred that these tablets had been demonstrated to be bioequivalent to the innovator product. No reports of failure to meet BE standards have been made in the open literature. On the basis of all these pieces of evidence, a biowaiver can currently be recommended for bisoprolol fumarate IR dosage forms if (1) the test product contains only excipients that are well known, and used in normal amounts, for example, those tabulated for products with MA in ICH countries and (2) both the test and comparator dosage form are very rapidly dissolving, or, rapidly dissolving with similarity of the dissolution profiles demonstrated at pH 1.2, 4.5, and 6.8.
    Matched MeSH terms: Intestinal Absorption
  18. The effect of cassava leave intake on thyroid hormone and urinary iodine
    Osman BA, Ng ML, Bakar AA, Khalid BA
    East Afr Med J, 1993 May;70(5):314-5.
    PMID: 8306912
    The effect of consuming large amounts of cassava leaves on thyroid function and urinary iodine was studied. Twenty volunteers were given 200 gm of boiled cassava leaves twice a day for 12 consecutive days. Thyroid hormones triiodothyronine and thyroxine were significantly lower by 9 days. Urinary iodine excretion was also significantly decreased. Cassava leaves, consumed in large amounts by aborigines, probably caused goitres by decreasing iodine absorption.
    Matched MeSH terms: Intestinal Absorption
  19. Death by 'ice': fatal methamphetamine intoxication of a body packer case detected by postmortem computed tomography (PMCT) and validated by autopsy
    Bin Abdul Rashid SN, Rahim AS, Thali MJ, Flach PM
    Forensic Sci Med Pathol, 2013 Mar;9(1):82-7.
    PMID: 23404531 DOI: 10.1007/s12024-012-9395-1
    Fatal acute methamphetamine (MA) poisoning in cases of internal drug trafficking is rarely described in the literature. This case study reports an MA 'body packer' who died from fatal methamphetamine intoxication due to leaking drug packages in the alimentary tract. The deceased was examined by postmortem computed tomography (PMCT), and the results were correlated to subsequent autopsy and toxicological findings. The deceased was arrested by the police when he was found disoriented in the city of Kuala Lumpur. He was transferred to the emergency department on suspicion of drug abuse. The initial drug screening was reactive for amphetamines. Shortly after admission to the hospital, he died despite rigorous resuscitation attempts. The postmortem plain chest and abdominal radiographs revealed multiple suspicious opacities in the gastrointestinal tract attributable to body packages. An unenhanced whole body PMCT revealed twenty-five drug packages, twenty-four in the stomach and one in the transverse colon. At least two were disintegrating, and therefore leaking. The autopsy findings were consistent with the PMCT results. Toxicology confirmed the diagnosis of fatal methamphetamine intoxication.
    Matched MeSH terms: Intestinal Absorption
  20. Fulltext Rabbit as an Animal Model for Pharmacokinetics Studies of Enteric Capsule Contains Recombinant Human Keratinocyte Growth Factor Loaded Chitosan Nanoparticles
    Kumar PV, Maki MAA, Wei YS, Tatt LM, Elumalai M, Cheah SC, et al.
    Curr Clin Pharmacol, 2019;14(2):132-140.
    PMID: 30457053 DOI: 10.2174/1574884714666181120103907
    BACKGROUND: Recombinant human keratinocyte growth factor (rHuKGF) has gained considerable attention by researchers as epithelial cells proliferating agent. Moreover, intravenous truncated rHuKGF (palifermin) has been approved by Food and Drug Administration (FDA) to treat and prevent chemotherapy-induced oral mucositis and small intestine ulceration. The labile structure and short circulation time of rHuKGF in-vivo are the main obstacles that reduce the oral bioactivity and dosage of such proteins at the target site.

    OBJECTIVE: Formulation of methacrylic acid-methyl methacrylate copolymer-coated capsules filled with chitosan nanoparticles loaded with rHuKGF for oral delivery.

    METHODS: We report on chitosan nanoparticles (CNPs) with diameter < 200 nm, prepared by ionic gelation, loaded with rHuKGF and filled in methacrylic acid-methyl methacrylate copolymercoated capsules for oral delivery. The pharmacokinetic parameters were determined based on the serum levels of rHuKGF, following a single intravenous (IV) or oral dosages using a rabbit model. Furthermore, fluorescent microscope imaging was conducted to investigate the cellular uptake of the rhodamine-labelled rHuKGF-loaded nanoparticles. The proliferation effect of the formulation on FHs 74 Int cells was studied as well by MTT assay.

    RESULTS: The mucoadhesive and absorption enhancement properties of chitosan and the protective effect of methacrylic acid-methyl methacrylate copolymer against rHuKGF release at the stomach, low pH, were combined to promote and ensure rHuKGF intestinal delivery and increase serum levels of rHuKGF. In addition, in-vitro studies revealed the protein bioactivity since rHuKGFloaded CNPs significantly increased the proliferation of FHs 74 Int cells.

    CONCLUSION: The study revealed that oral administration of rHuKGF-loaded CNPs in methacrylic acid-methyl methacrylate copolymer-coated capsules is practically alternative to the IV administration since the absolute bioavailability of the orally administered rHuKGF-loaded CNPs, using the rabbit as animal model, was 69%. Fluorescent microscope imaging revealed that rhodaminelabelled rHuKGF-loaded CNPs were taken up by FHs 74 Int cells, after 6 hours' incubation time, followed by increase in the proliferation rate.

    Matched MeSH terms: Intestinal Absorption
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