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At least 19 recordsLinked to original sources
PubMed2002

Improvement of the enzymatic stability of a cytotoxic T-lymphocyte-epitope model peptide for its oral administration.

Oral administration of peptide antigens, to provide proper mucosal and/or systemic immunity, is largely ineffective. This is mainly due to the very small quantity of antigen that survives degradation in the intestine and that crosses the intestinal absorption membrane. The present study focuses on the improvement of the enzymatic stability of a 13 amino acid long peptide containing a cytotoxic T-lymphocytes (CTL)-epitope. Within this study, it is shown, that simple chemical modification at the N- and C-terminus of the peptide can provide significant stability towards enzymatic attack by intestinal exopeptidases. Around 50% of the modified peptide resisted enzymatic attack on native porcine intestinal mucosa within 3h of incubation at pH 6.8 and 37 degrees C, whereas unmodified control peptide was almost completely degraded within the same time period. Additionally, a mucoadhesive drug carrier matrix with specific inhibitory properties towards luminally secreted endopeptidases has been generated. The incorporation of the simply modified peptide in this delivery system should enhance the amount of biologically active antigen being available at the mucosal site for further presentation to immunomodulating systems. This might open the door for a successful oral immunotherapy.

Administration, Oral↗
PubMed1998

Effect of barbiturate on central pain: difference between intravenous administration and oral administration.

OBJECTIVE: To examine whether the oral administration of barbiturates is of clinical use in a patient with central pain. SETTING: Pain Clinic, Osaka University Medical Hospital, Osaka, Japan. PATIENT: A patient with central pain after loss of his left upper extremity. INTERVENTIONS: A 50-mg dose of intravenous amobarbital, which produced a plasma concentration of 2.5-4.0 microg/ml, was effective in reducing the central pain. Subsequently, doses of 300-400 mg/day were administered orally; these succeeded in achieving similar plasma concentration levels. RESULTS AND CONCLUSIONS: Oral administration of barbiturate did not alleviate central pain, even when the plasma concentration was the same as the effective level in intravenous use. Pharmacokinetic and pharmacodynamic factors more complex than simple plasma concentrations may be involved in producing the difference in the effects.

Administration, Oral↗
PubMed2006

A comparison of effects of sequential transdermal administration versus oral administration of estradiol plus norethisterone acetate on serum NO levels in postmenopausal women.

AIM: To compare the effects of sequential transdermal administration versus oral administration of estradiol plus NETA on serum nitric oxide (NO) levels in postmenopausal women (PMW). MATERIALS AND METHODS: Eighty postmenopausal subjects without any prior hormone replacement therapy (HRT) usage were enrolled in this study. All participants were healthy, ambulatory, non-smoker and had similar life styles with dietary habits. HRT was given to participants according to desired HRT administration, in group A (n=50); oral estradiol hemi-hydrate (2 mg)/norethisterone acetate (1 mg), and in group B (n=30); transdermal combined patch comprising estradiol (0.05 mg) alone and estradiol (0.05 mg)/norethisterone acetate (0.25 mg), were given sequential for 12 months. Serum NO levels were studied using Total Oxide Assay Kit (Assay Designs, Inc.) according to manufacturer's instructions prior to and after 12 months from the HRT treatment. RESULTS: The mean serum NO levels prior to the HRT in groups A and B was 0.48+/-0.46 (range, 0.27-0.76 nmol/mL) nmol/mL and 0.47+/-0.48 nmol/mL (range, 0.29-0.693 nmol/mL) (p>0.05). The mean serum NO levels after the HRT in groups A and B was 0.53+/-0.33 nmol/mL (range, 0.29-2.10 nmol/mL) and 2.91+/-0.50 nmol/mL (range, 2.10-3.67 nmol/mL) (p<0.05). A significant difference was found between mean serum NO levels prior to and after the treatment in group B (p<0.05). CONCLUSIONS: Transdermal sequential combined HRT with estradiol hemi-hydrate/NETA was found to be superior to sequential combined oral HRT in increasing serum NO levels.

Administration, Cutaneous↗
PubMed2002

Pharmacokinetics of the active antifungal enantiomer, SCH 42427 (RR), and evaluation of its chiral inversion in animals following its oral administration and the oral administration of its racemate genaconazole (RR/SS).

Genaconazole (SCH 39304) is a potent triazole antifungal agent that is active both orally and topically. Genaconazole is a racemic mixture which contains 50% of the RR (SCH 42427) and 50% of the SS (SCH 42426) enantiomers. The RR isomer accounts for most of the antifungal activity of genaconazole. Serum concentrations of the RR and SS enantiomers were analyzed by a chiral HPLC method which involved extraction of serum with organic solvent followed by separation on a Cyclobond I column and quantification by UV absorbance at 205 nm. The bioavailability and pharmacokinetic profiles of the two enantiomers after oral administration of the racemate (genaconazole) were very similar in cynomolgus monkeys. In rats following dosing with genaconazole, the RR enantiomer had a lower C(max) and a longer t(1/2) than the SS enantiomer, while the AUC(I) values of the two enantiomers were similar. Based on chiral HPLC analysis, there was no evidence for the inversion of the RR to the SR isomer, or of the SS to the SR isomer, indicating that there was no chiral inversion of the RR or SS enantiomers in either species. Genaconazole at 20 mg/kg and the RR (SCH 42427) enantiomer at 10 mg/kg had very similar serum concentration-time profiles and C(max), AUC(I), and t(1/2) values for the RR enantiomer in both rats and monkeys, indicating that the two treatments were equivalent with respect to the bioavailability of the RR enantiomer.

Administration, Oral↗
PubMed1985

[A phase II study of etoposide (NK 171) in small cell lung cancer--comparison of results between intravenous administration and oral administration].

A phase II study of Etoposide (NK 171) was carried out in 13 institutions of the National Chest Hospital Lung Cancer Cooperative Study Group. Twenty-two patients (pts.) were treated by intravenous (i.v.) administration of etoposide, 80 mg/m2/day, for 5 consecutive days, and 25 pts. by oral administration of the same drug, 130 mg/m2/day, for 5 consecutive days. Eight (36.4%) out of 22 evaluable pts. given i.v. etoposide showed partial response (PR) while 7 (28%) out of 25 evaluable pts. given oral etoposide showed PR. Thirteen (41%) out of 32 previously untreated pts. were responders, but only 2 (13%) out of 15 previously treated pts. responded. The average total dose of i.v. etoposide was 664 (368-1552) mg/m2 while that of oral etoposide was 1320 mg/m2, or about double the dose of i.v. etoposide. The major dose-limiting factor was leukopenia (less than 3000/mm3). being observed in 63.6% of the i.v. treated pts. and 31.8% of the orally-treated pts. The oral and i.v. etoposide provided equivalent results. Despite the advantage of the reduced myelotoxicity of oral etoposide, we may recommend that all pts. are treated parenterally at present until the problem of erratic absorption of the oral drug is resolved.

Administration, Oral↗
PubMedDate not supplied

[Antidiabetogenic action of heparin during its oral administration].

Oral heparin given to rats was found to neutralize the hyperglycemic and hypoinsulinemic effects of diabetogenic factor and to produce a protective action by preventing the animals from the diabetogenic action of alloxan. The chronic oral heparin use alleviated the course of severe alloxan diabetes in rats, by contributing to the reduction of hyperglycemic levels, to the elevation of blood insulin concentrations, thus promoting their higher survival.

Administration, Oral↗
PubMed2002

Efficacy of oral administration and oral intake of edible vaccines.

To evaluate whether vaccine administration via intragastric gavage is indicative for the outcome of edible vaccines, mice were orally immunised with ovalbumin (OVA) mixed with or without Vibrio cholerae toxin (CT) in various compositions via various routes: (1) OVA dissolved in saline and intragastrically (IG) administered ('IG'); (2) OVA mixed with food extract and administered IG ('food IG'); (3) food chow absorbed with OVA dissolved in saline and fed to the animals ('food'); and (4) OVA dissolved in saline and administered via drinking bottles ('drinking'). When given to naive mice, 'IG' and 'food IG' but not 'food' or 'drinking' induced anti-OVA IgG1 responses in serum, but oral boost immunisations were necessary. Serum IgA was not induced. Oral boosting of subcutaneously (SC) primed mice enhanced the IgG1 and IgA response in serum regardless of the route of immunisation or the vaccine composition. CT did not dramatically enhance the immune response. All immunisation routes except 'drinking' induced antigen-specific IgA antibody secreting cells (ASC) in the lamina propria of naive mice. But antigen-specific antibody responses in faeces were not observed. We concluded that oral (i.e. IG) administration is distinct from oral intake. The composition of the vaccine (food or saline) did not influence oral administration. We thus suggested that the route of administration greatly influenced the outcome of oral immunisation. Although oral administration is a well-accepted route to test the potentials of oral vaccines, our study demonstrated that it is merely indicative for the effectiveness of edible vaccines. Studies on the feasibility of edible vaccines should thus be performed by eating the vaccine.

Administration, Oral↗
PubMed2006

Effects of dopamine transporter selective 3-phenyltropane analogs on locomotor activity, drug discrimination, and cocaine self-administration after oral administration.

Several studies suggest that a dopamine transporter uptake inhibitor that has a slower onset and longer duration of action than cocaine in animal behavioral measures and decreases cocaine self-administration would be useful as an indirect dopamine agonist pharmacotherapy to treat cocaine addiction. In the present study, we compared five 3-phenyltropane analogs administered orally in locomotor activity in mice and drug discrimination in rats to gain information concerning relative potency, onset, and duration of action. The compounds were also evaluated for reduction of cocaine self-administration in rats after oral administration. In general, the compounds had a slower onset of action than cocaine and reduced cocaine self-administration. 3beta-(4-Chlorophenyl)-2beta-(3-(4'-methylphenyl)-isoxazol-5-yl)tropane (RTI-336) was the most potent in locomotor activity and drug discrimination; it was less stimulatory than cocaine in the first hour and had the slowest onset and longest duration of action. It also reduced self-administration of two infusion doses of cocaine in the rat.

Administration, Oral↗
PubMed1985

[UFT concentration in serum and tissues of patients with gynecologic malignant tumors following oral administration].

Oral UFT was given to patients with genital carcinoma prior to surgery. 5-FU, FT and uracil levels in the tumor site were then measured in the surgical specimens obtained. Simultaneous estimates of tissues and plasma 5-FU indicated that the amount of drug in the tumor site (0.227 +/- 0.117 micrograms/g wet weight) had a 6.3-fold increase in concentration compared with that in normal tissues (0.036 +/- 0.019 micrograms/g wet weight) and was approximately 13.4 times that of the peripheral circulation (0.017 +/- 0.007 micrograms/ml). The rate of increase in concentration of tissue 5-FU rose especially in carcinoma of the cervix (0.394 +/- 0.215 micrograms/g), corpus uteri (0.116 +/- 0.042 micrograms/g) and ovary (0.171 +/- 0.047 micrograms/g). In the case of carcinoma of the cervix, the concentration of 5-FU in the tumor site was found to be about 14.1 times higher in invasive carcinoma than in carcinoma in situ. 5-FU concentration in the tumor site showed a still higher level compared with normal tissue after the drug was administered, suggesting an accumulation of 5-FU within the tumor.

Antineoplastic Combined Chemotherapy Protocols↗
PubMed2006

High-performance liquid chromatographic method for the determination and pharmacokinetic study of wogonoside in rat serum after oral administration of traditional Chinese medicinal preparation Huang-Lian-Jie-Du decoction.

A high-performance liquid chromatographic method for the determination of wogonoside in plasma of rats administrated orally with the traditional Chinese medicinal preparation Huang-Lian-Jie-Du decoction was developed. Sample preparation was carried out by protein precipitation with a mixture of acetonitrile and methanol (1:1, v/v). The extracted sample was separated on a Hypersil C(18) (150 x 5 mm i.d., 5 microm) analytical column by linear gradient elution using 0.05% (v/v) phosphoric acid (containing 5 mm sodium dihydrogen phosphate) and acetonitrile as mobile phase at a flow rate of 1.5 mL/min. The eluate was detected using a UV detector at 276 nm. The assay was linear over the range 0.109-7.0 microg/mL (R(2) = 0.9999, n = 5). Mean recovery was determined as 98.39%. Intra- and inter-day precisions (RSD) were < or =7.59%. The limit of quantitation was 0.109 microg/mL. After validation, the HPLC method developed was applied to investigate the preliminary pharmacokinetics of wogonoside in rat after oral administration of Huang-Lian-Jie-Du decoction.

Administration, Oral↗
PubMed1995

Transfer of methyl chloroform, trichloroethylene and tetrachloroethylene to milk, tissues and expired air following intraruminal or oral administration in lactating goats and milk-fed kids.

The distribution of methyl chloroform was determined (MCF), trichloroethylene (TRI) and tetrachloroethylene (PCE) in milk, tissues and expired air by intraruminally administering 0.625 ml kg(-0.75) of an equal-volume mixture of the three compounds to lactating goats. The milk secreted during 24 h after the intraruminal administration contained 1.42 mg of MCF, 1.87 mg of TRI, 6.43 mg of PCE and 0.33 mg of trichloroethanol (TCE). MCF, TRI and PCE appeared in the blood less than 30 min after administration. Oral administration of these chemicals to milk-fed kids showed that at 3.5 h post-administration, the liver contained these chemicals in greatest abundance. The adaptation of milk-fed kids to 3 weeks administration of small amounts of propylene glycol stimulated the metabolic conversion of TRI to TCE. There were linear relationships between the blood concentrations of these chemicals and the expiration rates after oral administration of 0.4 ml kg(-1) of each chemical to milk-fed kids. The expiration rates of MCF, TRI and PCE were 605, 122 and 46 microg min(-1) kg(-1) at 2 microg ml(-1) blood concentrations of MCF, TRI and PCE, respectively. These results suggested that MCF is little metabolized, being most readily exhaled in expired air, while PCE demonstrates the greatest tissue-partitioning, being largely secreted into the milk or retained in the liver. TRI can be extensively metabolized to other compounds such as TCE in milk-fed kids.

Journal Article↗
PubMed1992

[The effect of preoperative oral administration of ranitidine on pH and volume of gastric juice].

The effect of ranitidine, administrated 2 or 4 hours prior to induction of anesthesia, on volume and pH of gastric juice was investigated in patients undergoing elective surgery. Three-hundred mg of ranitidine was administrated orally in 54 patients 2 hours prior to anesthesia and in 50 patients 4 hours prior to anesthesia. The volume and pH of gastric juice were measured immediately after induction of anesthesia. In more than 90% of patients of both groups, volume of gastric juice was smaller than 25 ml and its pH was more than 2.5. Ranitidine 450 mg was administrated orally in 7 patients, and its plasma concentration was measured 2, 4 and 6 hours after administration. In one patient, volume of gastric juice was larger than 25 ml and its pH was less than 2.5. Ranitidine concentration in this patient was below the effective level 2 hours after administration and it was above the level after 4 hours. We concluded that oral administration of ranitidine 300 mg, 4 hours preoperatively, could be more effective to prevent aspiration pneumonitis than when it is given 2 hours preoperatively.

Administration, Oral↗
PubMed2005

Pharmacokinetics and bioavailability of mycophenolic acid after intravenous administration and oral administration of mycophenolate mofetil to heart transplant recipients.

The aim of this prospective study was to characterize the multiple-dose pharmacokinetics of mycophenolic acid (MPA) after administration of a 3-hour intravenous (IV) infusion of mycophenolate mofetil (MMF, CellCept) at a dose level of 1.5 g every 12 hours for 5 full days to cardiac allograft recipients and to compare the bioavailability of MPA after a switch from the IV infusion to an oral dose of 1.5 g every 12 hours from day 6. In addition to MMF, patients received cyclosporine and prednisolone. Blood (EDTA) samples for full pharmacokinetic profiles were obtained for 9 patients on days 3 and 5 (IV MMF) and on days 6 and 10 (oral MMF). They were centrifuged within 45 minutes of collection, and plasma was stabilized by addition of ortho-phosphoric acid to prevent in vitro conversion of MMF to MPA. Plasma concentrations of MPA were determined using a validated HPLC procedure. The median MPA AUC on day 6 (29.7 mg.h/L) after the first oral dose was slightly lower than the AUCs on the other study days (34.2, 33.8, and 33.8 mg.h/L on days 3, 5, and 10, respectively). Pairwise comparison of the individual days revealed statistically significant (P<0.05) differences between day 6 and day 3 and between day 5 and day 3. The Cmax on day 6 was significantly lower than that on study days 3 and 5. The bioavailability of MPA from the oral MMF formulation was estimated as the ratio of the AUC on day 6 or 10 to the AUC on day 5 when steady state was presumed to have been reached with the IV formulation. The mean ratios (expressed as percentage) for the log-transformed AUCs were 91.6% and 107.8% on days 6 and 10, respectively, relative to day 5. The 90% confidence interval (CI) on day 6 (79.3% to 105.8%) was marginally below the range (80%-125%) required to conclude that the formulations are bioequivalent, whereas on day 10 the 90% CI (93.3% to 124.7%) was within this range. In the case of the Cmax values, however, the 90% confidence intervals fell outside of this range (day 6, 57.2% to 92.8%; day 10, 70.6% to 114.9%). The results of this study show that heart transplant recipients receiving the IV formulation of MMF (1.5 g BID) are not subject to a greater drug exposure than that seen with the oral formulation (1.5 g BID) and that the oral MMF formulation shows excellent, high, and consistent bioavailability (mean 95%) based on comparison with the IV formulation.

Administration, Oral↗
PubMed2005

Pharmacokinetics of azathioprine following single-dose intravenous and oral administration and effects of azathioprine following chronic oral administration in horses.

OBJECTIVE: To determine pharmacokinetics of azathioprine (AZA) and clinical, hematologic, and serologic effects of i.v. and oral administration of AZA in horses. ANIMALS: 6 horses. PROCEDURE: In study phase 1, a single dose of AZA was administered i.v. (1.5 mg/kg) or orally (3.0 mg/kg) to 6 horses, with at least 1 week between treatments. Blood samples were collected for AZA and 6-mercaptopurine (6-MP) analysis 1 hour before and at predetermined time points up to 4 hours after AZA administration. In study phase 2, AZA was administered orally (3 mg/kg) every 24 hours for 30 days and then every 48 hours for 30 days. Throughout study phase 2, blood samples were collected for CBC determination and serum biochemical analysis. RESULTS: Plasma concentrations of AZA and its metabolite, 6-MP decreased rapidly from plasma following i.v. administration of AZA, consistent with the short mean elimination half-life of 1.8 minutes. Oral bioavailability of AZA was low, ranging from 1% to 7%. No horses had abnormalities on CBC determination or serum biochemical analysis, other than 1 horse that was lymphopenic on day 5 and 26 of daily treatment. This horse developed facial alopecia from which 1 colony of a Trichophyton sp was cultured; alopecia resolved within 1 month after the study ended. CONCLUSIONS AND CLINICAL RELEVANCE: Overall, no adverse effects were observed with long-term oral administration of AZA to horses, although 1 horse did have possible evidence of immunosuppression with chronic treatment. Further investigation of the clinical efficacy of AZA in the treatment of autoimmune diseases in horses is warranted.

Administration, Oral↗
PubMed2000

Prevention of nephrotoxicity of cisplatin by repeated oral administration of ebselen in rats.

The ability of ebselen, which exhibits glutathione peroxidase (GSH-Px)-like activity, to prevent cisplatin (CDDP)-induced nephrotoxicity was examined in rats. CDDP (6 mg/kg [20 micromol/kg] body weight) was injected intraperitoneally. In subgroups, daily ebselen doses of 2.75 (10 micromol), 5.5 (20 micromol), or 11.0 mg (40 micromol)/kg body weight were administrated orally 1 hour prior to CDDP treatment. Treatment with CDDP alone resulted in significantly increased plasma creatinine (Cr) and blood urea nitrogen (BUN) levels. Repeated administration of 5.5 and 11.0 mg/kg ebselen prevented the CDDP-induced elevation of plasma Cr and BUN levels and protected against kidney damage. Relative to controls, rat that received CDDP treatment displayed a decreased ratio of reduced glutathione (GSH) to oxidized glutathione (GSSG), an indicator directly related to oxidative stress, and elevated malondialdehyde (MDA) levels in the kidney. In comparison with controls, activity of GSH-Px activity, which antioxidant enzyme, was also reduced in the kidney of rats treated with CDDP. Repeated administration of 5.5 or 11.0 mg/kg ebselen prevented CDDP-induced alteration of GSH/GSSG ratios, MDA levels, and GSH-Px activity; however, no protection against CDDP was observed with administration of 2.75 mg/kg ebselen. Effective protection of CDDP-induced nephrotoxicity with ebselen was observed only when the molar amount of each daily ebselen treatment equaled or exceeded

Administration, Oral↗
PubMed1983

Early stages of chemically induced liver carcinogenesis by oral administration of the antihistaminic methapyrilene hydrochloride.

The antihistaminic drug methapyrilene hydrochloride, which induces liver tumors in rats, was administrated orally to female Wistar rats. The animals were killed after 21, 38, 77, 119, 181, and 196 days. The activities of adenosine-5-triphosphatase (ATPase) and gamma-glutamyltranspeptidase (gamma-GT) in the liver were investigated histochemically. At 21 days, a homogeneous decrease of ATPase activity as well as a slight increase of gamma-GT activity was found in the periportal zone. Additionally, after 38 days hepatocellular foci with reappearance of gamma-GT occurred mainly in the periportal zone. After 119 days, foci with increased gamma-GT activity as well as a significant reduction of ATPase activity could be observed predominantly in the periportal region. The size and number of these putative preneoplastic foci were increased according to the time of administration of methapyrilene hydrochloride. After 181 days of methapyrilene hydrochloride treatment three of five animals developed hyperplastic nodules with corresponding alterations of enzyme activities. Methapyrilene hydrochloride-a carcinogen with an unknown mechanism of reaction-produces preneoplastic changes that are analogous to the well known preneoplastic lesions in the liver observed after administration of other carcinogenic agents.

Adenosine Triphosphatases↗