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PubMed2005

Total and reactive lysine contents in selected cereal-based food products.

The aim of the study was to determine and compare reactive and total lysine contents in a range of breakfast cereal products. Crude fiber, fat, ash, and crude protein contents of 20 breakfast cereal products ranged from 4 to 38, 14 to 144, 7 to 32, and 52 to 253 g/kg, respectively. The concentrations of glutamic acid (18.7-32.1 g/100 g protein) and proline (4.7-10.8 g/100 g protein) were high while those of the amino acids methionine (1.2-2.0 g/100 g protein) and histidine (1.2-3.3 g/100 g protein) were relatively low. There was a strong relationship between reactive lysine determined using the guanidination and fluorodinitrobenzene methods (R = 0.99). The total lysine content, determined after conventional acid hydrolysis, ranged from 0.8 to 3.7 g/100 g protein, while the reactive lysine content (guanidination) ranged from 0.4 to 2.8 g/100 g protein. Reactive lysine was 20-54% lower than total lysine in the cereal products. The large differences between total and reactive lysine suggest a considerable loss of lysine in the breakfast cereals tested.

Amino Acids↗

PubMed1997

Initial and chronic gastric acid inhibition by lansoprazole and omeprazole in relation to meal administration.

In a placebo-controlled, double-blind, multiple crossover study, the initial and chronic acid-inhibitory effect of lansoprazole 30 mg, orally administered half an hour before breakfast or immediately after breakfast, and of omeprazole 20 mg, administered postprandially, respectively, was investigated in 16 healthy volunteers, using ambulant 24-hr intragastric pH monitoring. On the first day of medication, only preprandially administered lansoprazole reduced acid secretion significantly (median 24-hr pH 3.0; P < 0.05). On day 15, the median 24-hr intragastric pH of lansoprazole preprandial (pH 4.1), lansoprazole postprandial (pH 4.3), and omeprazole postprandial (pH 3.3), respectively, differed significantly (P < 0.05) from placebo (pH 1.2). It is concluded that the interaction between food intake and lansoprazole administration only is important at the start of oral therapy. Lansoprazole taken before breakfast is effective even on the initial day of treatment.

2-Pyridinylmethylsulfinylbenzimidazoles↗

PubMed1998

Health risk assessment for diabetes mellitus based on longitudinal analysis of MHTS database.

This study was designed with a follow up of 16 years to provide the epidemiological model evaluating the risk of developing diabetes mellitus in Japan. A cohort of 2573 subjects (1851 males and 722 females) from a MHTS in Tokyo, who were nondiabetic (fasting blood glucose (FBS) less than 110 mg/dl) in the initial year, were selected. This cohort was followed every year to identify the occurrence of diabetes mellitus. Diabetes Mellitus was defined as fasting blood glucose over 110 mg/dl, or the initiation of diabetic therapy. We compared two prognosis groups (a normal group and a diabetic group) in terms of age, examination findings, and prevalence of health risks (lifestyle, stress, and working form). We also assessed family history of diabetes and past histories including hypertension, hypercholesterolemia, and hyperuricemia. After assessing each variable by univariate analysis (t-test, chi 2 test), we employed Cox's proportional hazards model analysis. We used stepwise model adopting risk factors. The diabetic group had significant differences compared to the normal group in age, BMI (body mass index), FBS, smoking, drinking, not eating breakfast, dairy intake, hypertension, hypercholesterolemia, hyperuricemia, and family history by univariate analysis. According to proportional hazards model analysis, FBS, age, family history, hypertension, smoking, and BMI were incorporated into significant risk factors for diabetes in males, and not eating breakfast, FBS, age, drinking, and hypertension were incorporated in females. Diabetes seemed to be related to fixed factors (age), or genetic factors (family history and FBS) in males. For females, lifestyle (not eating breakfast and drinking habit) seemed to play an important role. It will be worthwhile to assess the risks of developing diabetes mellitus by this epidemiological model.

Adolescent↗

PubMed2001

Effective oral administration of tacrolimus in renal transplant recipients.

BACKGROUND: Tacrolimus is usually administered orally based on mg/kg or the trough concentration (Cmin) in whole blood. However, it is not easy to determine the optimal oral dose because of considerable variation of tacrolimus bioavailability between patients. In this study, pharmacokinetics of tacrolimus in various conditioning kidney transplant recipients was investigated. METHODS: 1) Thirty-three patients were randomly assigned to participate in two groups. In 17 patients, tacrolimus was administered orally after an overnight fast with breakfast given 1 h later, and in the other 16 patients it was administered orally 1 h after breakfast. 2) In 4 patients, the same dose tacrolimus was given after an overnight fast and 0.5 h after breakfast on two consecutive days. 3) Five patients who underwent continuous ambulatory peritoneal dialysis (CAPD) before transplantation were studied. All patients were investigated in daily profile of tacrolimus blood levels. RESULTS: There was a strong correlation between area under the curve (AUC) and the trough concentration in both preprandial and postprandial oral administration, with correlation coefficients of 0.838 and 0.860, respectively. Significant increases in the peak concentration (Cmax) and AUC were observed in the preprandial oral administration subjects. Absorption of CAPD patients was obviously insufficient. CONCLUSIONS: Since tacrolimus absorption was better under fasted condition than under the presence of food, it is thought that the highest medicine effect with the least dosage is provided by preprandial oral administration. Furthermore, preprandial oral administration is recommended from a respect of economic burden reduction and side effect reduction.

Administration, Oral↗

PubMed1985

Food-induced changes in theophylline absorption from controlled-release formulations. Part II. Importance of meal composition and dosing time relative to meal intake in assessing changes in absorption.

Theo-24 (G. D. Searle & Co.) is an ultra-slow-absorbing formulation of theophylline suitable for once-a-day dosing in slow and normal metabolizers of theophylline. Relative to fasting conditions, increased rate and extent of theophylline absorption occur when this product is administered immediately after a breakfast with a high fat content. Our study demonstrated that factors such as meal composition (fat content) or dosing time relative to meal intake can modify the high fat-induced changes in absorption. For consistent, slow absorption, patients taking high doses (greater than or equal to 900 mg) of Theo-24 once a day should take this product in the morning under fasting conditions or with a breakfast containing less than or equal to 10 gm fat. If a high-fat breakfast (greater than 55 gm fat) is taken, then Theo-24 should be administered at least 1 hour before the meal.

Absorption↗

PubMed1997

Dietary fat reduction achieved by increasing consumption of a starchy food--an intervention study.

OBJECTIVE: To test t he hypothesis that increased consumption of foods in rich in starch, such as breakfast cereals, will enable a substantial reduction in the percentage dietary energy derived from fat. DESIGN: Parallel experimental design, with matched subjects allocated randomly to an intervention or a control group. SETTING: Free-living subjects (mean age 20 y), undergraduate students at a college for higher education. SUBJECTS: Sixty-two enrolled, 59 completed the study; 7 d weighed intakes at baseline, 4 weeks and 12 weeks. INTERVENTION: The intervention group were required to eat 60 g breakfast cereal daily with semi-skimmed milk. Pre-weighed portions of three types of cereal were distributed without charge at the beginning of each week of the study; subjects were reimbursed for the cost of milk used. No other dietary advice was given. RESULTS: At baseline, total energy intake and percentage energy from macronutrients was very similar in both the intervention and control group. After four weeks of intervention there was a significant reduction in % energy from fat (-5.4%) in the experimental group, maintained at the 12 weeks follow-up. There was a corresponding rise in energy from CHO: a significant increase of 5.5% after four weeks had reached 6.5% by 12 weeks. Total energy remained virtually unchanged, indicating a replacement of fat energy by carbohydrate energy. These changes were not found in the control group. CONCLUSIONS: A simple dietary intervention to increase consumption of breakfast cereal led to a 5% reduction in % dietary fat energy, with a beneficial effect on micronutrient intakes. The results support the case for positive advice to increase consumption of complex carbohydrate, as a strategy for dietary fat reduction in the wider population.

Adolescent↗

PubMed1998

Sources of bias in a dietary survey of children.

OBJECTIVE: To compare non-responders and responders to a dietary survey with respect to demographic variables and intention to choose selected breakfast foods, and to examine if there was any systematic change in number of food items reported during a 7 d recording period. DESIGN: Cross-sectional survey. SETTING: Mölndal, Sweden. SUBJECTS: All pupils in 5th, 7th and 9th grades in the municipality were asked to complete a questionnaire during school hours. All those present (n = 1584, 92% of total) answered questions about lifestyle factors and about intentions, attitudes and beliefs concerning high-fibre bread and milk with varying fat content. All subjects in the initial sample were asked to fill in a 7 d record of food consumed. Acceptable food records were completed by 69% of the initial participants. RESULTS: Subjects not completing the food record differed significantly from participants with respect to demographic, lifestyle and dietary factors. Dropout was more common among those who reported not usually eating breakfast and among those intending to drink whole milk for breakfast. A decline in reported food items during the recording period was also observed. CONCLUSIONS: Two sources of bias were observed here, one indicating significant differences between non-participants and participants, the other suggesting the presence of a time-dependent trend in number of recorded foods. It is likely such biases are present in other dietary surveys involving schoolchildren, and should be taken into consideration in the design, analysis and interpretation of such studies.

Adolescent↗

PubMed2002

Depression of the glycemic index by high levels of beta-glucan fiber in two functional foods tested in type 2 diabetes.

OBJECTIVES: To determine the extent to which beta-glucan reduces the glycemic index (GI) of oat products and whether high levels of beta-glucan impair palatability. DESIGN: The study design was an open-label, randomized cross-over study with six treatment segments. SETTING: Free-living outpatients. SUBJECTS: Sixteen volunteers with type 2 diabetes (10 men, six women, 61+/-2 y, body mass index 29+/-2 kg/m(2), HbA1c 7.4+/-0.4%) were recruited from the St Michael's Hospital diabetes clinic. INTERVENTIONS: Volunteers were given, in random order, 50 g available carbohydrate portions of: white bread; a commercial oat bran breakfast cereal (4.4 g% beta-glucan); and a prototype beta-glucan-enriched breakfast cereal and bar, both high in beta-glucan (8.1 and 6.5 g% beta-glucan, respectively) and sweetened with fructose. Capillary blood samples were taken fasting and then 30, 60, 90, 120, 150 and 180 min after the start of the meal. Palatability was recorded using two different methods. RESULTS: The glycemic indices of the prototype beta-glucan cereal (mean+/-s.e.m.; 52+/-5) and beta-glucan bar (43+/-4.1) were significantly lower than the commercial oat bran breakfast cereal (86+/-6) and white bread (100; P<0.05). All foods were highly palatable and not significantly different. It was found that the GI of the test foods used in this study decreased by 4.0+/-0.2 units per gram of beta-glucan compared to our estimate of 3.8+/-0.6 for studies reported in the literature. CONCLUSION: Addition of beta-glucan predictably reduces the GI while maintaining palatability. In a 50 g carbohydrate portion each gram of beta-glucan reduces the GI by 4 units, making it a useful functional food component for reducing postprandial glycemia. SPONSORSHIP: Nestec, Switzerland.

Aged↗

PubMed2003

Hydrothermal treatment and malting of barley improved zinc absorption but not calcium absorption in humans.

OBJECTIVE: To study whether hydrothermal treatment or malting of barley (cv. Blenheim) improves zinc and calcium absorption in humans. DESIGN: : Two groups of 10 and 12 healthy subjects, respectively, were in a period of 2 months in a fasting state, served two single meals each containing porridge or breakfast cereals prepared from processed or unprocessed (control) barley (60 g). The meals included 200 g of milk, extrinsically labelled with (65)Zn and (47)Ca. Whole-body retention of both minerals was measured. SETTING: The study was carried out at the Department of Radiation Physics, Sahlgrenska University Hospital, Göteborg. SUBJECTS: The subjects were recruited among students at the Göteborg University. None dropped out. INTERVENTIONS: The activities of (65)Zn and (47)Ca were measured by whole-body counting four to five times over a 4-week period after each meal. RESULTS: Zinc absorption from hydrothermally treated barley porridge, containing 28 mg P as inositol tri- to hexaphosphates (InsP(3)-InsP(6)), was significantly higher (P<0.001) than from control porridge containing 111 mg P as InsP(3)-InsP(6), 25.2+/-6.9 vs 11.0+/-2.5% (n=12). Calcium absorption did not differ (P>0.05), 21.1+/-6.8 vs 19.5+/-4.7% (n=12). Zinc absorption from breakfast cereals of malted barley with phytase activity and containing 70 mg P as InsP(3)-InsP(6,) was significantly higher (P<0.05) than from flakes of barley, containing 108 mg P as InsP(3)- InsP(6) and no phytase activity, 22.9+/-5.8 vs 14.8+/-4.6% (n=10). The calcium absorption was 21.3+/-6.5 vs 18.5+/-4.3% (n=10) and did not differ significantly (P>0.05). CONCLUSION: Improvements of zinc absorption in breakfast meals can be achieved by optimised hydrothermal treatment or malting of barley. Calcium absorption was not influenced in the meals in this study. SPONSORSHIP: Supported by Semper AB, Sweden, Oy Lahden Polttimo, Finland, the SL-Foundation, Sweden, Swedish National Board for Industrial and Technical Development (NUTEK), the Nordic Industrial Foundation, Swedish Council for Forestry and Agricultural Research (SJFR, project no 50.0306/97).

Adolescent↗

PubMed2006

Determination of glycaemic index; some methodological aspects related to the analysis of carbohydrate load and characteristics of the previous evening meal.

OBJECTIVES: To determine the possible differences in glycaemic index (GI) depending on (1) the analytical method used to calculate the 'available carbohydrate' load, that is, using carbohydrates by difference (total carbohydrate by difference, minus dietary fibre (DF)) as available carbohydrates vs available starch basis (total starch minus resistant starch (RS)) of a food rich in intrinsic RS and (2) the effect of GI characteristics and/or the content of indigestible carbohydrates (RS and DF) of the evening meal prior to GI testing the following morning. DESIGN: Blood glucose and serum insulin responses were studied after subjects consuming (1) two levels of barley kernels rich in intrinsic RS (15.2%, total starch basis) and (2) after a standard breakfast following three different evening meals varying in GI and/or indigestible carbohydrates: pasta, barley kernels and white wheat bread, respectively. SUBJECTS: Healthy adults with normal body mass index. RESULTS: (1) Increasing the portion size of barley kernels from 79.6 g (50 g 'available carbohydrates') to 93.9 g (50 g available starch) to adjust for its RS content did not significantly affect the GI or insulin index (11). (2) The low GI barley evening meal, as opposed to white wheat bread and pasta evening meals, reduced the postprandial glycaemic and insulinaemic (23 and 29%, respectively, P < 0.05) areas under the curve at a standardized white bread breakfast fed the following morning. CONCLUSION: (1) Increasing portion size to compensate for the considerable portion of RS in a low GI barley product had no significant impact on GI or II. However, for GI testing, it is recommended to base carbohydrate load on specific analyses of the available carbohydrate content. (2) A low GI barley evening meal containing high levels of indigestible carbohydrates (RS and DF) substantially reduced the GI and II of white wheat bread determined at a subsequent breakfast meal.

Adult↗

PubMed2006

Oligofructose promotes satiety in healthy human: a pilot study.

OBJECTIVE: The administration of a fermentable dietary fibre (oligofructose) in rats increases satietogenic gut peptides and lowered spontaneous energy intake. The aim of the study was to assess the relevance of those effects of oligofructose on satiety and energy intake in humans. DESIGN: Single-blinded, crossover, placebo-controlled design, pilot study. SUBJECTS: Volunteers included five men and five women aged 21-39 years, BMI ranging from 18.5 to 27.4 kg/m(2), were randomly assigned as described below. INTERVENTIONS: Subjects were included in two 2-week experimental phases during which they received either fibre (oligofructose (OFS)) or placebo (dextrine maltose (DM)); a 2-week washout period was included between crossover phases. In total, 8 g OFS or 8 g DM were ingested twice daily (16 g/day in total). Energy intake, hunger, satiety, fullness and prospective food consumption were assessed with analogue scales at the end of each experimental phase. RESULTS: During breakfast, OFS significantly increases the satiety (P=0.04) without any difference on other sensations as compared to DM treatment periods. After lunch, no significant differences are observed between treatment period. At dinner, OFS significantly increases satiety (P=0.04), reduces hunger (P=0.04) and prospective food consumption (P=0.05). The energy intake at breakfast and lunch are significantly lower (P=0.01, 0.03, respectively) after OFS treatment than after DM treatment. Total energy intake per day is 5% lower during OFS than in DM period. CONCLUSION: Oligofructose treatment increases satiety following breakfast and dinner, reduces hunger and prospective food consumption following dinner. This pilot study presents a rationale to propose oligofructose supplements in the management of food intake in overweight and obese patients.

Adult↗

PubMed2000

Orlistat fails to alter postprandial plasma lipid excursions or plasma lipases in normal-weight male volunteers.

OBJECTIVES: After 10 d of orlistat administration (120 mg three times/day), the primary objective was to determine the drug's effect on postprandial plasma lipoprotein lipase (LPL) and hepatic triglyceride lipase (HTGL) activities on day 10 after an oral fat-load. The secondary objectives were to determine the effects of orlistat on 12 h postprandial measures of: (1) preheparin HTGL and LPL; and (2) serum triglycerides, very-low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, low-density lipoprotein cholesterol and free fatty acids. METHODS: Twenty-four normal-weight, healthy male volunteers were randomized to either 120 mg orlistat (n=12) or placebo (n=12) three times a day with meals for 10 d. Preheparin LPL and HTGL activities and LPL specific activity were measured in the fasted state on days 1, 5, and 10. On days 5 and 10 the study medication (orlistat or placebo) was taken at the beginning of a fat-rich breakfast and serum lipid and lipoprotein levels monitored for 12 h postprandially. On day 10, 15 min postheparin HTGL activity was measured 8 h after the fat-rich breakfast. RESULTS: No differences were found between groups in fasting levels of preheparin LPL or HTGL activity or in LPL-specific activity on days 1, 5 and 10. No difference was found between the two treatment groups in postheparin HTGL activity 8 h after the fat-rich breakfast. Also, no differences were found between the two groups in plasma triglycerides or lipoproteins. CONCLUSION: The results indicate that the oral administration of orlistat (120 mg t. i.d.) does not significantly alter plasma triglycerides or lipoproteins, and that the inhibitory effect of orlistat on lipases is limited to the gastrointestinal tract and is not manifested systemically.

Adult↗

PubMed2000

The effect of glucagon-like peptide-1 on energy expenditure and substrate metabolism in humans.

OBJECTIVE: To investigate the effects of a near-physiological peripheral glucagon-like peptide-1 (GLP-1) infusion, during and after a breakfast of fixed energy content, on resting energy expenditure, substrate oxidation and metabolism and the desire to eat specific types of food in humans. DESIGN: A placebo-controlled, randomized, blinded, cross-over study. Infusion (GLP-1, 50 pmol/kg x h or saline) was started simultaneously with initiation of the test meals. SUBJECTS: 20 healthy, normal weight (body mass index 20.3-25.7 kg/m2) men of 20-31 y of age. MEASUREMENTS: Energy expenditure and substrate oxidations were measured before and for 4 h after standard breakfast (20% of calculated daily energy requirements, 50% of energy from carbohydrates, 37% of energy from fat and 13% of energy from protein) using a ventilated hood system. Visual analogue scales were used throughout the experiment to assess the desire to eat specific types of food and the palatability of the test meals. Blood was sampled throughout the day for analysis of plasma hormone and substrate concentrations. RESULTS: Diet-induced thermogenesis (DIT) was lower (47%) on the GLP-1 infusion than on the saline infusion (P < 0.0001). This was due to a lower carbohydrate oxidation (P < 0.01). No differences in fat oxidation or total 4 h protein oxidation were observed. All hormone and substrate profiles except non-esterified fatty acids (NEFA) and cholecystokinin (CCK) were significantly suppressed (GLP-2 completely suppressed) during the GLP-1 infusion, whereas profiles of NEFA and CCK differed in time course during the two treatments (treatment x time effect), P < 0.0001). GLP-1 infusion also suppressed the desire to eat all food types following the breakfast (treatment effect: P < 0.05). CONCLUSION: Peripheral GLP-1 decreased DIT and carbohydrate oxidation, probably secondary to a delayed absorption of nutrients, since substrate and hormone concentrations in plasma were suppressed during GLP-1 infusion. Endogenous secretion of GLP-1 and GLP-2 was completely suppressed by GLP-1 infusion. Finally, the desire to eat any type of food was decreased by exogenous administrated GLP-1.

Adult↗

PubMed2006

Determinants of short-term variation in arterial flow-mediated dilatation in healthy young men.

Brachial artery FMD (flow-mediated dilatation) is widely used as a marker of systemic arterial endothelial function. FMD, however, shows considerable 25% day-to-day variation that hinders its clinical use. The reasons for this variability are poorly characterized. Therefore the present study was designed to clarify factors responsible for the hourly variation in endothelial function, including consuming a low-fat meal and circadian rhythms in endogenous hormonal levels. Brachial artery FMD, along with serum glucose, triacylglycerols (triglycerides) and levels of several hormones were measured six times per day on two separate days 1 week apart. On one day, the subjects (healthy males: n=12, mean age, 24 years) ate a light breakfast and a standardized lunch (23.5% fat, 48.7% carbohydrate and 27.8% protein). On the other day, they had a similar breakfast after which they fasted. Postprandial FMD values (both after breakfast and after lunch) were similar to baseline FMD. FMD showed a 28% hourly variation and 27% weekly variation. Variation in plasma levels of insulin (P=0.02) associated negatively and DHPG (3,4-dihydroxyphenylglycol) (P=0.001), a marker of sympathetic nervous activation, associated positively with variation in FMD. The effects of DHPG and insulin on FMD were independent of changes in baseline brachial artery diameter, although DHPG was also inversely associated with baseline diameter. Eating a regular low-fat meal does not have any measurable effects on brachial artery endothelial function. These data suggest that strict requirements for fasting conditions may be unnecessary when measuring peripheral endothelial function using the ultrasound technique. Circadian variation in serum insulin and sympathetic tone are physiological determinants of endothelial function.

Adult↗

PubMed1998

Nocturnal gastric acidity and acid breakthrough on different regimens of omeprazole 40 mg daily.

BACKGROUND: On chronic intake of omeprazole, most healthy volunteers and patients still have nocturnal acid breakthrough (NAB), defined as night-time periods with gastric pH < 4.0 lasting for longer than 1 h. Gastro-oesophageal reflux during NAB may be particularly injurious to the oesophageal mucosa, contributing to the chronic lesions complicating the condition. AIM: To compare the effect of three different dosing regimens of omeprazole 40 mg daily with regard to suppressing nocturnal gastric acidity and avoiding NAB. METHODS: Eighteen healthy volunteers were given three different regimens of omeprazole for 7 days each in randomized order: 40 mg before breakfast (qAM), 40 mg before dinner (qPM) and 20 mg before breakfast and dinner (b.d.). On day 7, 24-h intragastric and intraoesophageal pH-metry was performed. Tracings were analysed for the period from 22.00 h until 06.00 h with regard to the percentage of time at which gastric pH was below 4.0, 3.0 and 2.0, and also the occurrence and duration of NAB. RESULTS: Nocturnal acid breakthrough was significantly more common on qAM than on qPM and b.d. (P < 0.05) dosing. The percentage of time gastric pH was less than 4.0 overnight was significantly lower on qPM (median 31.3) and b.d. (median 20.5) than on qAM (median 66.3) dosing (P=0.01 and P < 0.02, respectively). A pH threshold of 3 and 4 showed the same differences, as did median 24-h gastric pH. Daytime acidity was not significantly different. CONCLUSIONS: In healthy volunteers, dinner time or split dosing of omeprazole 40 mg daily is significantly more effective than dosing before breakfast in preventing NAB and controlling gastric acidity. These regimens should be preferred in patients in whom suppression of nocturnal gastric acidity is desirable.

Adult↗

PubMed1998

Effect of food on the bioavailability of triclabendazole in patients with fascioliasis.

AIMS: Preliminary results indicate higher absorption of triclabendazole (TCBZ) administered postprandially. Therefore, the influence of food on the pharmacokinetics of TCBZ and its active sulphoxide (TCBZ-SO) and sulphone (TCBZ-SO2) metabolites was investigated. METHODS: Two single doses (10 mg kg(-1)) of TCBZ were administered to 20 patients with fascioliasis. Ten patients were first given the drug after a high energy breakfast and then, 48 h later, after an overnight fast. The other 10 patients first received the drug in fasting state and then, 48 h later, after breakfast. A low energy breakfast was served 2 h after drug administration for fasting state. RESULTS: Compared with the fasting state, an increased AUC and Cmax after food intake (significant, P < 0.0001) was shown from the values of TCBZ, TCBZ-SO and TCBZ-SO2. The mean AUC for TCBZ (fasting: 1.55, fed: 5.72 micromol l(-1) h), TCBZ-SO (fasting: 177, fed: 386 micromol l(-1) h) and TCBZ-SO2 (fasting: 13.9, fed: 30.5 micromol l(-1) h) indicated a large availability increase with food and the strong systemic predominance of the active sulphoxide metabolite over the unchanged drug. (All patients were cured at the end of the trial except one who required a second course of two postprandial doses of triclabendazole (10 mg kg(-1) each). Tolerability to the treatment among the patients was good. CONCLUSIONS: The administration of triclabendazole with food is recommended for improved systemic availability in patients with fascioliasis or paragonimiasis.

Adolescent↗

PubMed1999

The effect of dosing regimen on the pharmacokinetics of risedronate.

AIMS: To examine the effect of timing of a risedronate dose relative to food intake on the rate and extent of risedronate absorption following single-dose, oral administration to healthy male and female volunteers. METHODS: A single-dose, randomized, parallel study design was conducted with volunteers assigned to four treatment groups (31 or 32 subjects per group, 127 subjects total). Each subject was orally administered 30 mg risedronate. Group 1 was fasted for 10 h prior to and 4 h after dosing (fasted group); Groups 2 and 3 were fasted for 10 h and were dosed 1 and 0.5 h, respectively, before a high-fat breakfast; and Group 4 was dosed 2 h after a standard dinner. Blood and urine samples were collected for 168 h after dosing. Pharmacokinetic parameters were estimated by simultaneous analysis of risedronate serum concentration and urinary excretion rate-time data. RESULTS: Extent of risedronate absorption (AUC and Ae ) was comparable (P=0.4) in subjects dosed 2 h after dinner and 0.5 h before breakfast; however, a significantly greater extent of absorption occurred when risedronate was given 1 or 4 h prior to a meal (1.4- to 2.3-fold greater). Administration 0.5, 1, or 4 h prior to a meal resulted in a significantly greater rate of absorption (Cmax 2.8-, 3.5-, and 4.1-fold greater, respectively) when compared with 2 h after dinner. CONCLUSIONS: The comparable extent of risedronate absorption when administered either 0.5-1 h before breakfast or 2 h after an evening meal support previous clinical studies where risedronate was found to have similar effectiveness using these dosing regimens. This flexibility in the timing of risedronate administration may provide patients an alternative means to achieve the desired efficacy while maintaining their normal daily routine.

Absorption↗

PubMed1997

Suppression of the nocturnal free fatty acid levels by bedtime cornstarch in NIDDM subjects.

The aim of the present study was to examine the effects of a large dose of slow-release carbohydrates (CHOs) at bedtime on the nocturnal glucose, insulin and free fatty acid (FFA) levels, and to assess the putative effects on morning fasting and post-prandial glucose levels in patients with moderately controlled non-insulin-dependent diabetes mellitus (NIDDM). Unheated cornstarch (106 g of CHO) or a mixed equicaloric meal (58 g of CHO) was given at 22.00 hours to 10 NIDDM patients. For comparison, the patients were also given a smaller mixed meal at 22.00 hours on a third occasion (17 g of CHO). Compared with the mixed meals, cornstarch led to a slightly elevated early-morning plasma insulin level and a suppression of the nocturnal FFA level (P < 0.05), as well as to a reduced incremental glucose level (IAUC) after breakfast the next morning by approximately 30% (P < 0.05). There was a significant and linear relationship between the nocturnal FFA level and the glucose IAUC after breakfast (r = 0.44, P < 0.02), indicating that the effect may have been mediated by the suppressive effect of cornstarch on nocturnal lipolysis. In summary, bedtime intake of unheated cornstarch in NIDDM subjects is associated with a suppression of the nocturnal FFA levels and a reduced glucose IAUC after breakfast. As the treatment did not improve overall glucose control, studies of the effects of an individually titrated amount of cornstarch are proposed to further explore the putative favourable effects of bedtime cornstarch in the treatment of NIDDM.

Administration, Oral↗