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The bioavailability of oral penicillin V. A comparative study of the absorption of different salts of penicillin V in children.

Different salts of penicillin V (pc-V): potassium pc-V (Calciopen and Kåvepenin), calcium pc-V (Penicals) and benzathine pc-V (Meropenin) were given to 37 children (age 2 months to 4 years) with upper respiratory infections. The gastro-intestinal absorption of the drug given in a mixture was followed for three hours after administration by determination of the serum levels from capillary samples. Administration of the mixtures containing the potassium pc-V resulted in a more rapid absorption and in significantly higher plasma concentrations at 30 min than did administration of the preparations containing the calcium and benzathine salts. In four children with coeliac disease, verified by intestinal biopsy, the absorption of potassium pc-V (Calciopen) was compared with that of calcium pc-V (Penicals). A decreased absorption was found and this was most pronounced when the calcium salt was given.

Calcium

A new product of rearrangement of penicillin V (S)-sulphoxide.

Penicillin V (S)-sulphoxide (I), treated with methanesulphonic acid in benzene and dimethylacetamide, gives the decarboxylated increment3-cephem compound (IV) and a new product of rearrangement to which the structure of the 4-[N-(1'-carboxy-2'-methylenepropyl)carbamoyl]-2-phenoxymethylthiazole (VIII) is ascribed.

Magnetic Resonance Spectroscopy

Influence of diarrhea on the oral absorption of penicillin V and ampicillin in children.

Oral ampicillin and penicillin V was given to 23 and 42 children, respectively, with upper respiratory infections. The absorption of the drugs was followed on one of the first days of treatment for 3 hours after administration by taking capillary samples and determining the serum levels. Approximately 60% of the children were tested for oral absorption during convalescence, 6-8 days after the initiation of the treatment. Diarrhea was evident in more than 60% of the children during treatment with both ampicillin and penicillin V. Diarrhea of short duration did not have influence on the absorption of the antibiotics. Only when persistent diarrhea over the whole therapy period existed, absorption of penicillin V was decreased.

Administration, Oral

The comparative efficacy of minocycline and penicillin-V in Staphylococcus aureus skin and soft tissue infections.

The antistaphylococcal properties of orally administered minocycline and penicillin-V were compared for one hundred and fifteen patients receiving minocycline and one hundred and twenty-eight receiving penicillin-V for various types of cutaneous infections. The majority of bacterial isolates were staphylococcal organisms. Of these 82 percent showed initial in vitro sensitivity to minocycline while only 20 percent did to penicillin-V. The percentage of clinical cures was higher with minocycline (74 percent) than with penicillin-V (54 percent), however, most patients, in both groups, showed clinical improvement. The rate of clinical improvement appeared to be significantly faster with minocycline. There was a higher percentage of adverse, chiefly vestibular, effects in the minocycline group (16 percent vs 7 percent). The study clearly demonstrates the superior antistaphylococcal properties of minocycline as compared with penicillin-V.

Adolescent

High-performance liquid chromatographic analysis of penicillin V benzathine oral suspensions.

A rapid high-performance liquid chromatographic assay for penicillin V content of penicillin V benzathine bulk drug and oral suspensions is described. Dilution of the oral suspension with methanol containing 1,3,5-trimethoxybenzene as the internal standard allowed for direct analysis on a reversed-phase column with a mobile phase of 53% methanol in 0.05 M aqueous pH 3.5 phosphate buffer. A relative standard deviation of less than 1% was obtained on commercial formulations, and the system was linear over a range 10-40 microgram injected.

Chromatography, High Pressure Liquid

Penicillin V therapy for streptococcal pharyngitis: comparison of dosage schedules.

Two dosage regimens of penicillin V were compared in 327 patients with mild to moderately severe streptococcal pharyngitis. Patients fulfilling study criteria were randomly assigned to a b.i.d. or a t.i.d. dosage schedule. Those in the b.i.d. group were given 500 mg twice daily; those in the t.i.d. group were given 250 mg three times daily. Duration of therapy was ten days for both groups. Cure was based on prompt symptomatic improvement, subsidence of clinical signs, and negative throat cultures for group A beta-hemolytic streptococci. Both dosage schedules yielded similar cure rates, indicating that with penicillin V, a b.i.d. regimen is as effective as a t.i.d. regimen in treating streptococcal pharyngitis.

Acute Disease

[Penicillin V potassium in tonsillar tissue and serum (author's transl)].

1.2 mega U Penicillin V potassium was given to 20 patients 2 hours (group 1) and another 19 patients 3 hours (group 2) before tonsillectomy. After the operation biological determinations of the levels of active principle were made from tonsillar tissue and serum with statistical evaluation of the results (Spearman's rank correlation). There was a significant connection between the serum and tonsillar tissue concentrations (in children and adults) in both groups. The level of the active principle in group 2 was only slightly lower than in group 1. Many of the micro-organisms responsible for tonsillitis can be influenced by the concentrations found here, so that application of Penicillin V can often be expected to have a good therapeutic effect.

Adolescent

The gastrointestinal absorption of penicillin V in children with suspected coeliac disease.

The gastrointestinal absorption of penicillin V (pc-V) was investigated in 6 children, 6-12 months old, with suspected coeliac disease. The diagnosis was set after small bowel biopsy and absorption tests of vitamin A and d-xylose. As control groups served 7 children with diarrhoea but with normal small bowel biopsy and/or absorption tests and a group of 9 children with upper respiratory tract infection of the same ages as the children in the test group. The absorption of calcium pc-V in oil suspension (Penicals) was impaired in the patients with suspected coeliac disease compared to that of the control groups. There was no significantly different absorption of pc-V between the control children with diarrhoea and those with upper respiratory tract infection. After 6-8 months of gluten free diet in the children with suspected coeliac disease their absorptive ability of oral calcium pc-V in suspension form was equal with that of a control group.

Biopsy

Stability of penicillin V potassium in unit dose oral syringes.

The stability of reconstituted penicillin V potassium (PVK) when stored in 6-ml plastic oral syringes at various temperatures and protected from light was studied. One batch of PVK was reconstituted with distilled water according to manufacturer's directions (label claim: 125 mg/ml). Samples of 5 ml were stored in plastic oral syringes at 4 C, 25 C, 41 C, 60 C or 75 C and assayed spectrophotometrically and microbiogically at various times. From an initial concentration of 113% of label claim, PVK stored at 4 C (refrigerated) reached 90% of manufacturer's label claim in 11.5 days (95% confidence level). PVK stored at 25 C (room temperature) was unstable after storage for less than 37 hours. PVK degradation followed a first-order process. No significant difference was found between the spectrophotometric and microbiological assay (p less than 0.05). Manufacturer's stability data for storage of reconstituted PVK in the original bulk container should not be applied to PVK repackaged in plastic oral syringes. The pharmacy department developed guideliness designed to prevent the administration of subpotent PVK.

Drug Stability

[Aqueous-and serum levels of cephalexin and penicillin V after oral application in man (author's transl)].

This clinical study implies orally administered cephalexin and penicillin V as agents with effective aqueous homor penetration in noninfected human eyes. Aqueous humor concentration of cephalexin increases up to 15% of the serum level 2 h after application. Administration of 1 g or 2 g cephalexin revealed no significant difference in aqueous humor concentration. So penetration of blood-aqueous-humor barrier can be regarded as a saturation process. Individual results of 92 cephalexin determinations are variant and not related to body weight or age of the patients.

Aged

Serum levels of penicillin v after oral administration of pediatric preparations to healthy subjects.

The bioavailability of nine commercial pediatric preparations of penicillin V was tested in a double-blind, cross-over fashion on ten healthy student nurses who were given 1 mill I.U. of the various preparations. The serum concentrations were determined using the paper disc method of "AB Biodisc" Sweden. The preparations could be divided into two different groups: (1) the mixtures (2) the effervescent tablets, substance for drops and granulate. This classification is based upon the mean peak serum levels obtained. With one exception the peak serum levels in group 2 were significantly higher than in group 1. 2,4 and 6 hours after ingestion there were no differences in the serum levels, indicating that none of the preparations gave sustained high serum levels. The results presented indicate that the preparations in group 2 should be preferred.

Administration, Oral

Stability of several brands of ampicillin and penicillin V potassium oral liquids following reconstitution.

The stability-time profiles of the active ingredient of five generically equivalent brands of penicillin V potassium for oral solution, and of five generically equivalent brands of ampicillin for oral suspension, were studied. Three controlled conditions were employed-refrigerated, room and elevated temperature-and all the samples were assayed chemically for drug remaining at specific time intervals after reconstitution. The results showed that considerable variations in the initial concentrations of active component existed among the various ampicillin and penicillin products. In one penicillin product the official content requirement was not met. The data also showed that although the labels on each of the commerical penicillin products tested indicate that the reconstituted products may be stored in a refrigerator for 14 days without significant loss of potency, only one penicillin product still met 90% of label claim (minimal potency requirement of the United States Pharmacopeia for dry powder). All ampicillin products tested were stable when stored at the conditions recommended by the manufacturers, but the trihydrate forms exhibited greater stability than the anhydrous forms, probably because of the more rapid dissolution rate of anhydrous ampicillin.

Ampicillin

[Penicillin V].

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