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At least 37 records · Page 2Linked to original sources
PubMed1987

Pharmacokinetics of norethisterone following its oral administration and by spraying it nasally or sublingually to male bonnet monkeys.

Pharmacokinetic parameters of norethisterone (NET) were studied in eight adult male bonnet monkeys following the administration of a single dose of 300 ug. The animals were crossed over between the following three routes of administration: oral ingestion, nasal and sublingual spraying. The results indicate that NET was readily absorbed by all three routes but the Cmax and AUC of NET were significantly greater by the sublingual route. No significant difference in the t 1/2 alpha or t 1/2 beta was observed between the three routes. These findings suggest that the sublingual route offers the possibility of reducing the effective dose of NET, which is widely used for contraceptive purposes.

Administration, Intranasal↗
PubMed1986

[Determination of piperazine in hen eggs with HPLC following oral administration].

After oral administration of piperazine citrate to hens, this antihelmintic agent appeared unchanged in the eggs. After a therapeutic dose of ca. 0.9 g piperazine citrate per hen, a maximum level of 1.5 mg piperazine/kg egg was found two days after the application. The elimination half-life was 29 h and piperazine was found in the eggs up to 17 days after administration (limit of detection: 1 microgram/kg). Piperazine determination was performed by HPLC of the dansylderivative after clean-up by TLC.

Administration, Oral↗
PubMed1984

Investigations on the detection of mutagenic activity of beef extract in rats after oral administration.

After oral administration of beef extract the body fluids of Aroclor-treated and untreated rats were investigated for mutagenicity using the Salmonella/microsome test. In the stomach contents, the bile and the urine of the animals, mutagenic activity was discovered after S-9 activation. Although the mutagenic substances must have been transported by the blood stream to the excreting organs no increased mutagen-induced his+ revertants were observed in venous blood. Direct-acting mutagens were not detected in the tested body fluids, either in the Aroclor-treated rats or in the untreated ones.

Administration, Oral↗
PubMed1989

[Pharmacokinetics of norethindrone-oxime and norethindrone in rabbits after oral administration].

After oral administration of [3H]-labelled norethindrone-oxime (NETO) or norethindrone (NET) to rabbits, the blood concentrations of NETO and NET were determined by measuring the radioactivity after separation with HPLC. The pharmacokinetic parameters of the compounds were also compared. Experimental results indicate that both NETO and NET were quickly absorbed. Their elimination from blood revealed a fast and a slow phase. One portion of NETO was metabolized to NET, and the remainder was excreted in unchanged form. The amount of NETO and its metabolite, NET, in serum were about equal within 24 hours. The serum concentration-time curves of NETO and NET adequately fitted to a two-compartment model. There was significant difference between NETO and NET in Tmax (P less than 0.05). But no significant differences in other parameters (P greater than 0.05) were observed.

Administration, Oral↗
PubMed1987

[Transfer of ofloxacin into suction blister fluid after its oral administration].

After oral administration of 300 mg of ofloxacin (OFLX), the concentration of OFLX in serum peaked at 2 hours and reached 2.88 +/- 0.62 micrograms/ml (mean +/- S.D.). In the fluid of dermal blisters produced by suction, the peak value was 1.74 +/- 0.88 micrograms/ml at 4 hours. Pharmacokinetically, Cmax (maximum concentration), Tmax (time of maximum concentration), Ka (absorption rate constant) and AUC0-8hrs. (area under the concentration-time curve) were calculated as 2.65 micrograms/ml, 2.07 hours, 0.79 hr-1 and 14.5 micrograms.hr/ml in serum, and 1.59 micrograms/ml, 4.49 hours, 0.27 hr-1 and 10.1 micrograms.hr/ml, respectively. Therapeutic AUC (area under the curve above minimum effective concentration) were also calculated as 13.3 micrograms.hr/ml (0.14-12.4 hours) in serum, and 11.5 micrograms.hr/ml (0.42-17.3 hours).

Administration, Oral↗
PubMed2006

Pharmacokinetics of olanzapine after single-dose oral administration of standard tablet versus normal and sublingual administration of an orally disintegrating tablet in normal volunteers.

Olanzapine (OLZ) is a second-generation antipsychotic agent available in 2 solid oral dosage forms, a standard oral tablet (SOT) and an orally disintegrating tablet (ODT). This study assessed the absorption of each by different routes of administration. Secondarily, the influence of P-glycoprotein (P-gp) genotype was assessed. It was hypothesized that more rapid absorption of the OLZ ODT would occur when administered sublingually versus standard oral administration. A randomized, 3-way crossover study assessed the 5-mg OLZ formulations in healthy volunteers (n = 10). Blood was collected (0-8 hours) to assess OLZ pharmacokinetics using liquid chromatography/mass spectrometry. Both routes of ODT administration resulted in more measurable early concentrations relative to SOT. However, there were no statistically significant differences observed between any of the OLZ exposures for observed pharmacokinetic parameters (C(max), T(max), AUC(0-8h)). The homozygous TT genotype for P-gp resulted in an increased AUC of OLZ for SOT administration but not for either condition where sublingual absorption could occur.

ATP Binding Cassette Transporter, Subfamily B↗
PubMed2001

Metabolic fate of (-)-[4-(3)H]epigallocatechin gallate in rats after oral administration.

After oral administration of [4-(3)H]EGCg to rats, the radioactivity in blood, major tissues, urine, and feces was measured over time. The radioactivity in blood and most tissues remained low for 4 h postdose, began to increase after 8 h, peaked at 24 h, and then decreased. Major urinary excretion of radioactivity occurred in the 8-24 h period, and the cumulative radioactivity excreted by 72 h was 32.1% of the dose. The radioactivity in the feces was 35.2% of the dose within 72 h postdose. In the case of rats pretreated with antibiotics (antibiotic-pretreated rats), the radioactivity levels of the blood and urine were definitely lower than those in rats not pretreated with antibiotics (normal rats). The radioactivity recovered in the antibiotic-pretreated rat urine was estimated to be only (1)/(100) of that in the normal rat urine. These results clearly demonstrated that the radioactivity detected in the blood and urine of normal rats mostly originated from degradation products of EGCg produced by intestinal bacteria. Furthermore, a main metabolite in the normal rats was purified and identified as 5-(5'-hydroxyphenyl)-gamma-valerolactone 3'-O-beta-glucuronide (M-2). In feces of the normal rats, EGC (40.8% of the fecal radioactivity) and 5-(3',5'-dihydroxyphenyl)-gamma-valerolactone (M-1, 16.8%) were detected. These results suggested that M-1 was absorbed in the body after degradation of EGCg by intestinal bacteria, yielding M-1 with EGC as an intermediate. Furthermore, M-2 was thought to be formed from M-1 in the intestinal mucosa and/or liver, then to enter the systemic circulation, and finally to be excreted in the urine. Taking into account all of the above findings, a possible metabolic route of EGCg orally administered to rats is proposed.

Administration, Oral↗
PubMed1992

Is sublingual nifedipine administration superior to oral administration in the active treatment of hypertension?

Nifedipine, a calcium-channel-blocking agent, was administered orally to 44 untreated patients (Group A) and sublingually to 51 untreated patients (Group B) who had a diastolic blood pressure more than 90 mm Hg and systolic blood pressure more than 140 mm Hg. The mean pretreatment systolic and diastolic blood pressure values were 185.3 +/- 26.0 and 115.1 +/- 13.4 mm Hg in Group A patients and 193.6 +/- 23.1 and 118.1 +/- 14.1 mm Hg in Group B patients respectively (p greater than 0.05). The hypotensive activity of nifedipine was observed at the tenth minute in both groups. Mean systolic and diastolic pressures were 168.9 +/- 23.7 and 101.9 +/- 14.2 mm Hg in Group A and 170.6 +/- 26.2 and 103.0 +/- 15.8 mm Hg in Group B, (p less than 0.001) Diastolic blood pressures dropped under 100 mm Hg at the twentieth minute in both groups. Maximal reduction of blood pressure was observed at the fortieth minute in both groups and the degree of reduction in blood pressure was also the same (mean systolic and diastolic blood pressures: 143.7 +/- 22.1 and 86.9 +/- 11.7 in Group A and 148.7 +/- 21.4 and 91.7 +/- 17.0 in Group B (p less than 0.05). The authors conclude that sublingual nifedipine administration is not superior to oral nifedipine administration (in capsular form) in the acute treatment of hypertension.

Acute Disease↗
PubMed1990

Modulating the microbial colonization of the gastrointestinal tract by oral administration of defined Escherichia coli strains. III. Lipopolysaccharide-specific IgA in the intestine after oral administration of Escherichia coli.

The assumption that local immunologic mechanisms are responsible for findings on the specific microbial colonization of the gastrointestinal tract of mice, is confirmed by results described in the present communication. Quantitative examination of intestinal lavage fluids after oral administration of germs by ELISA showed that (i) there is a critical dose above which a significant increase of IgA synthesis is observable; (ii) low antibody levels could be detected already in the untreated control group. It may be assumed that--regardless of the biological characteristics of the administered strain, namely, substrate and receptor competition--the stimulability of local immunity provides against permanent monocolonization with displacement of the autochthonous Enterobacteriaceae in adult and immunocompetent hosts.

Administration, Oral↗
PubMed1984

[Fundamental studies on the introduction of chemotherapy of uterine cervical carcinoma--tissue level of 5-FU after oral administration].

In Japan, oral 5-FU has been popularly used as an adjuvant chemotherapy to surgical operation mainly gastrointestinal carcinomas. This drug is generally administered consecutively at a low dose over a long term, because of its distribution at high levels in the upper gastrointestinal organs after oral administration. The authors have attempted to introduce the oral administration of 5-FU as an adjuvant chemotherapy in the treatment of uterine cervical carcinoma, and the results of a preliminary trial are reported in this paper; that is, the 5-FU level in target organs was measured after oral administration of 5-FU in 44 cases of uterine cervical carcinoma. Judging from the 5-FU level in organs removed about 2 hours after preoperative administration of 5-FU at 300 mg, the distribution of the drug to bilateral lymph nodes and the uterine cervix was good, and when calculated on the basis of the trace as 0, the average tissue level was 0.0432 microgram/g in the left lymph node, 0.0104 microgram/g in the right lymph node and 0.0190 microgram/g in the uterine cervix. From the above, it was concluded that, in the application of oral 5-FU as an adjuvant chemotherapy to treatment of uterine cervical carcinoma, a different manner application procedure should be established from that used to treat gastrointestinal carcinoma; that is, 5-FU should be administered intermittently at a moderate dose.

Administration, Oral↗
PubMed1996

Neonatal vitamin K prophylaxis in Denmark: three years' experience with oral administration during the first three months of life compared with one oral administration at birth.

A Danish surveillance group established after the introduction of oral vitamin K prophylaxis monitored Danish cases with late onset vitamin K deficiency bleeding by regular questionnaires to all paediatric departments. Six cases were reported, one of whom died and three are severely handicapped. All cases occurred among an estimated 134,500 infants given a single oral 1 mg vitamin K dose at birth. No cases have been reported so far during the existent regimen: 2 mg at birth and 1 mg weekly orally administered vitamin K during the first 3 months of life, given to at least 163,000 infants. The present study is concordant with the only other study on weekly peroral prophylaxis published. We consider the mentioned weekly regimen safe and appropriate.

Administration, Oral↗
PubMed2006

Modulation of immunity-related gene expression in small intestines of mice by oral administration of lactoferrin.

Oral administration of lactoferrin (LF), an antimicrobial and immunomodulatory protein, shows a protective effect against infectious diseases, possibly via immunomodulation of the host. Initially, we confirmed an immunomodulatory effect of LF by observing changes in the number of cells in the leukocyte subsets in the peripheral blood and spleens of mice 1 day after oral administration of LF. Then we developed a quantitative reverse transcription-PCR method for 20 immunity-related genes of antimicrobial proteins, pattern recognition receptors, cytokines, and lymphocyte mobilization-related proteins, and we assessed the expression of these genes in the small intestines of mice 2 h after administration of water, bovine serum albumin (BSA), or LF. Expression of the LF gene was lower in mice administered LF than in mice administered water or BSA, implying a negative-feedback control. Expression of gamma interferon (IFN-gamma) and interleukin-10 (IL-10) was lower in both BSA- and LF-administered mice than in water administered mice, suggesting a nonspecific effect of protein ingestion. Expression of NOD2, IFN-beta, and IL-12p40 was higher with LF administration than with water or BSA administration. The expression levels of these three genes were correlated. This study indicated that oral administration of LF modulates the small intestinal expression of genes closely related to the host defense in a specific or a nonspecific manner.

Administration, Oral↗
PubMed1975

[Action of acebutolol on heart rate and FEV1 in asthmatic patients. Single intravenous administration and long term oral administration].

In 7 asthmatic patients, intravenous injection of acebutolol resulted in a slowing of the heart rate by blocking the cardiac beta-receptors. An aerosol of isoprenaline, which accelerated the heart, is without effect after intravenous injection of acebutolol. On the contrary, isoprenaline caused similar changes in the FEV1 before and after acebutolol injection in the same patients. This effect confirms the slight action of the compound on the beta2-adrenergic receptors. Prolonged oral administration did not cause any adverse clinical effects in 6 asthmatic patients.

Acebutolol↗
PubMed1993

Pharmacokinetics and biochemical efficacy after single and multiple oral administration of losartan, an orally active nonpeptide angiotensin II receptor antagonist, in humans.

1. The pharmacokinetics and biochemical efficacy of losartan, an orally active nonpeptide angiotensin II (AII) receptor antagonist, were evaluated in healthy male volunteers after single and multiple oral administration. 2. Plasma and urinary concentrations of losartan and its active metabolite, E-3174, were determined by a specific high performance liquid chromatographic (h.p.l.c.) method. 3. Plasma concentrations of losartan were proportional to dose over the range of 25 to 200 mg and the terminal half-lives (t1/2,z) ranged from 1.5 to 2.5 h. The mean values of Cmax and AUC0-infinity increased in a dose-dependent manner. 4. Plasma concentrations of E-3174 were higher than those of losartan at all dose levels. The values of Cmax and AUC0-infinity for E-3174 were approximately 2 and 5-8 times higher than those for losartan, respectively. Also the value of t1/2,z was 2 times longer than that of losartan. 5. After multiple dosing for 7 days, the pharmacokinetics of losartan and E-3174 each did not change significantly between day 1 and day 7. 6. Plasma renin activity (PRA) and plasma concentrations of AII increased markedly at all dose levels. Plasma aldosterone levels were slightly reduced, but a similar decrease was also observed with placebo. 7. No clinically significant adverse reaction was observed in any of the volunteers during either study. Blood counts, routine laboratory tests, urine analyses, and electrocardiograms were also not modified by losartan. 8. Losartan appears to be a potent orally active angiotensin II antagonist with a relatively long duration of action.

Administration, Oral↗
PubMed1996

Oral administration of glycine and polyamine receptor antagonists blocks ethanol withdrawal seizures.

Cessation of chronic administration of orally administered large amounts of ethanol for 7 days resulted in a markedly increased frequency of audiogenic seizures in Sprague-Dawley rats. Oral administration of the novel glycine receptor antagonist, L-701,324, produced a dose-dependent (2.5 and 5.0 mg/kg; -30 min) inhibition of ethanol withdrawal signs when measured about 12 h after withdrawal of the ethanol treatment. Similarly, using the same experimental paradigm, oral administration of the specific polyamine receptor antagonist, eliprodil, caused a dose-related (2.0 and 5.0 mg/kg; -30 min) inhibition of ethanol withdrawal-induced audiogenic seizure activity. The inhibition of ethanol withdrawal seizures produced by L-701,324 and eliprodil, respectively, was obtained at doses which by themselves did not change the locomotor activity in naive Sprague-Dawley rats. The findings that L-701,324 and eliprodil are potent inhibitors of seizure activity induced by cessation of chronic ethanol administration and the fact that they, in contrast to currently available NMDA receptor antagonists, do not produce psychotomimetic and/or sedative effects, suggest that these drugs may represent a new class of therapeutically useful pharmacological agents for the treatment of ethanol withdrawal seizures. Furthermore, since there is evidence that eliprodil produces its pharmacological actions through a specific inhibition of NMDAR1 and/or NMDAR2B subunits, these data may indicate that certain NMDA receptor subunits may be of particular importance for the mediation of seizure activity following the discontinuation of chronic ethanol exposure.

Acoustic Stimulation↗
PubMed2004

Pharmacokinetics of DA-7867, a new oxazolidinone, after intravenous or oral administration to rats: intestinal first-pass effect.

Pharmacokinetic parameters of DA-7867 were dose independent after both intravenous administration and oral administration (at doses of 1 to 20 mg/kg of body weight) to rats. After oral administration of DA-7867 to rats at a dose of 10 mg/kg, approximately 8.27% of oral dose was not absorbed from the gastrointestinal tract, F was 70.8%, and approximately 21.8% of the oral dose was eliminated by the intestine (intestinal first-pass effect).

Administration, Oral↗
PubMed1994

Brain content of glycosphingolipids after oral administration of monosialogangliosides GM1 and LIGA20 to rats.

Natural (GM1) and semisynthetic [113-Neu-5-AcGgOse4-2-D-erythro-1,3- dihydroxy-2-dichloroacetylamide-4-trans-octadecene (LIGA20)] glycosphingolipids, given parenterally, protect neurones against glutamate-induced death without producing the side effects typical of glutamate receptor antagonists. Chronic glutamate-related neurotoxicity (e.g., in recurring strokes in elderly hypertensive patients, and in Parkinson disease) could be prevented also by glycosphingolipids treatment, but this therapeutic intervention will require a protracted administration of orally active glycosphingolipids. Here we demonstrate that 3-6 h after oral administration of 68 mumol/kg of LIGA20 and GM1 to rats, the brain content of LIGA20 is 50-fold higher than that of GM1. The brain concentration of LIGA20 remains elevated for at least 12-24 h. Because the LIGA20 that reaches the brain is slowly metabolized, repeated oral administrations of this glycosphingolipid can yield to its accumulation in brain, and can yield various brain levels depending on the dose and frequency of drug administration. In contrast this is not possible with GM1, which given orally for 7 d, cannot accumulate in brain in pharmacologically significant concentrations.

Administration, Oral↗