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At least 19 recordsLinked to original sources
PubMed1998

Assessment of a tablet drug delivery system incorporating nonoxynol-9 coprecipitated with polyvinylpyrrolidone in preventing the onset of pregnancy in rabbits.

OBJECTIVE: To assess the in vivo efficacy of the tablet drug delivery system containing nonoxynol-9 coprecipitated with polyvinylpyrrolidone by delivering the spermicidal agents vaginally and evaluating their ability to prevent the onset of pregnancy in rabbits. DESIGN: Controlled clinical study. SETTING: Division of Laboratory and Animal Resources, College of Pharmacy, University of Kentucky. ANIMAL(S): Forty-two New Zealand White female rabbits. INTERVENTION(S): The rabbits were artificially inseminated at various intervals after vaginal insertion of the tablet drug delivery system containing either polyvinylpyrrolidone only (0 minutes) or nonoxynol-9 coprecipitated with polyvinylpyrrolidone (polyvinylpyrrolidone/nonoxynol-9; 0, 3, 30, 180, and 360 minutes). The rabbits were induced to ovulate 6 hours before insemination by i.m. injection of hCG (200 IU). MAIN OUTCOME MEASURE(S): The onset of pregnancy in the rabbits was evaluated after insertion of the tablet drug delivery system containing polyvinylpyrrolidone only or polyvinylpyrrolidone/nonoxynol-9 at various intervals, followed by artificial insemination. RESULT(S): The onset of pregnancy was not reduced significantly when the tablet drug delivery system containing polyvinylpyrrolidone or polyvinylpyrrolidone/nonoxynol-9 was used and insemination was performed immediately after tablet insertion (time 0). However, pregnancy rates (PRs) were reduced significantly in the rabbits that received the tablet drug delivery system containing polyvinylpyrrolidone/nonoxynol-9 and were inseminated at 3, 30, 180, and 360 minutes after tablet insertion. The highest PR reduction occurred between 30 and 180 minutes after insertion of the tablet drug delivery system containing polyvinylpyrrolidone/nonoxynol-9. CONCLUSION(S): The tablet drug delivery system is an efficient method of delivering the tested spermicidal agents vaginally. The design and dosage used in preparing the tablet drug delivery system provide short- and long-term release of the spermicidal agents, which results in almost immediate and extended enhancement of their contraceptive properties.

Administration, Intravaginal↗
PubMed1982

[Pseudo-tumour after injections of procaine-polyvinylpyrrolidone (author's transl)].

In a 67-year-old woman a tumour-like swelling developed at the site of repeated bilateral injections of procaine solution with polyvinylpyrrolidone as an additive. The histological picture of the removed tumour showed striking similarities to a malignant histiocytic tumour. The diagnosis was histiocytic inflammation due to polyvinylpyrrolidone storage. Retention of polyvinylpyrrolidone increases with increasing molecular weight and is dependent of the form of application. Treatment consists of removal of the storage focus, because polyvinylpyrrolidone maintains foreign-body reaction and absorption and storage in internal organs may cause further complications. Injectable drugs should not be used with polyvinylpyrrolidone as depot-carrier.

Aged↗
PubMed1995

Testing the mutagenic potential of polyvinylpyrrolidone and methyl cellulose by sister chromatid exchange analysis prior to use in intracytoplasmic sperm injection procedures.

The treatment of infertility due to severe oligoasthenoteratozoospermia has been revolutionized by the introduction of the technique of intracytoplasmic sperm injection. However, techniques which involve injection into the oocyte of polyvinylpyrrolidone solution as a vehicle for the selected spermatozoon have caused concern since the possible harmful effects of polyvinylpyrrolidone have not been fully investigated. This study was performed to investigate the potential mutagenic effect of polyvinylpyrrolidone on cultured human somatic cells, at the concentration used for intracytoplasmic sperm injection, in addition to a possible alternative vehicle, methyl cellulose, using the technique of sister chromatid exchange analysis. The results showed no increase in the basal frequency of sister chromatid exchanges with polyvinylpyrrolidone (median 5.0, 95% interval 5.00-6.00) or with methyl cellulose (median 6.0, 95% interval 4.22-6.00) in comparison with the negative control (saline: median 6.0, 95% interval 5.00-7.00), and in contrast to the positive control (mitomycin C: median 25.0, 95% interval 22.23-28.77). This finding suggests that polyvinylpyrrolidone and methyl cellulose do not cause DNA lesions resulting in sister chromatid exchanges, and provides reassuring evidence concerning their use in sperm injection procedures.

Cytoplasm↗
PubMed1984

Effect of aging on hydrocortisone-polyethylene glycol 4000 and hydrocortisone-polyvinylpyrrolidone dispersions.

Dispersions containing 40% hydrocortisone were prepared by the solvent method in polyethylene glycol 4000. Dispersions in polyvinylpyrrolidone were prepared by slow evaporation of solvent (type A) and by fast evaporation of solvent (type B). These dispersions were stored at 25 degrees C for 30 d. Plots of time required for 50% (t50%) and 70% (t70%) of the hydrocortisone dispersion to dissolve (beaker method) versus time were obtained. Hydrocortisone-polyethylene glycol showed no apparent significant change in either dissolution rate, X-ray spectra, or scanning electron micrographs. Type A dispersions showed an increase in dissolution rate up to 8 d. Type B dispersions showed an initial decrease followed by an increase in dissolution rate. The initial decrease in dissolution rate of type B dispersions is due to hydrocortisone crystallizing out of the polyvinylpyrrolidone matrix. The increased dissolution for both types of polyvinylpyrrolidone dispersions was not expected and is for both types of polyvinylpyrrolidone dispersions was not expected and is explained by an increased proportion of the high-energy amorphous component, based on X-ray spectra. Other possibilities such as the presence of polymorphic forms of hydrocortisone and/or reduction in particle aggregation could not be discounted.

Chromatography, Thin Layer↗
PubMed1981

Uptake by rat peritoneal macrophages of 125I-labelled polyvinylpyrrolidone entrapped within liposomes.

Rat peritoneal macrophages in vitro capture 125I-labelled polyvinylpyrrolidone entrapped within either negatively or positively charged liposomes more rapidly than they do the free macromolecule. The uptake of negatively charged liposomes was linear with time over 10 h, whilst the uptake of positively charged ones, although more rapid, was more transient. Neither type of liposome was taken up in the presence of 2,4-dinitrophenol (100 microgram/ml), and 5 mM calcium chloride increased the uptake of negatively charged liposomes. The enhanced uptake of 125I-labelled polyvinylpyrrolidone when presented in liposomes must have been a consequence of entrapment rather than of a simple interaction between lipid and polyvinylpyrrolidone since the presence of the lipids employed or of empty liposomes had no effect on the uptake of unentrapped 125I-labelled polyvinylpyrrolidone.

Animals↗
PubMed1975

The teratogenic effects in rabbits of doxycycline, dissolved in polyvinylpyrrolidone, injected into the yolk sac.

A technique was developed for injecting agents into the yolk sac of rabbits to study their teratogenic effects. On the 9th day of gestation the rabbits were laparotomized during ether-oxygen narcosis. The test substance was injected into the yolk sacs in one horn of the uterus, and as control the corresponding solvent was injected into the other horn. On the 28th day of gestation the rabbits were killed, resorptions counted, and fetuses examined for malformations. Three series of studies were made: physiological saline; polyvinylpyrrolidone; and doxycycline dissolved in polyvinylpyrrolidone (DIP). The rate of resorptions and malformations significantly increased after injection of Vibravenos. As polyvinylpyrrolidone was not teratogenic it is concluded that the teratogenic effects of DIP were probably caused by doxycycline.

Abnormalities, Drug-Induced↗
PubMed2002

Characterization and solubility study of solid dispersions of flunarizine and polyvinylpyrrolidone.

Flunarizine is a selective calcium entry blocker poorly water-soluble. In this report, the interactions of this drug with polyvinylpyrrolidone in solid dispersions, prepared according to the dissolution method using methanol as the solvent, have been investigated. For purposes of comparison physical mixtures were prepared by simple mixture and homogeneization of the two pulverized components. Combinations of flunarizine/polyvinylpyrrolidone of the following percentage proportions were prepared: 10/90, 20/80, 30/70, 40/60, 50/50, 60/40 and 80/20 (mean particle size of 0.175 mm). The physicochemical properties of solid dispersions were investigated with X-ray diffraction, infrared spectroscopy, differential scanning calorimetry and solubility in equilibrium. X-ray patterns and differential scanning calorimetry have shown that polyvinylpyrrolidone inhibits the crystallization of flunarizine when percentages drug/polymer are 10/90, 20/80 and 30/70. The infrared spectra suggest that there was no chemical interaction between flunarizine and polyvinylpyrrolidone. Equilibrium solubility studies showed that drug solubility was enhanced as the polymer content increased. In general, the solubility increase was greater in solid dispersions than in physical mixtures and the solubility in equilibrium for solid dispersions and physical mixtures at the same drug/polymer proportion showed significant differences (P < 0.05).

Calcium Channel Blockers↗
PubMed2003

Anaphylaxis to polyvinylpyrrolidone after vaginal application of povidone-iodine.

A 59-year-old woman who had had several episodes of contact urticaria after hair treatment, developed anaphylaxis after vaginal application of povidone-iodine solution for disinfection. Prick tests showed wheal-and-flare responses to both povidone-iodine (0.1% aqueous) and polyvinylpyrrolidone (povidone, PVP) (0.001% aq.), but not to iodine or polyoxy-ethyrenenonylphenyl ether, both of which are also contained in povidone-iodine solution. We confirmed that basophils from her peripheral blood released considerable amounts of histamine on stimulation by PVPs. It appeared that both the shampoo and the permanent-wave solution contained polyvinylpyrrolidone N, N-dimethyl aminoethyl methacrylic acid copolymer diethyl sulphate solution and polyvinylpyrrolidone styrene-copolymer emulsion. Both these agents in the hair care products provoked an immediate skin response on prick testing. We speculate that sensitization to PVP had been established by these hair care products at a beauty parlor. She was recommended to avoid PVP-containing products and remained free from symptoms thereafter.

Administration, Intravaginal↗
PubMed1998

Cytokine expression is downregulated by collagen-polyvinylpyrrolidone in hypertrophic scars.

We evaluated the in situ expression of adhesion molecules (E-selectin and vascular cell-adhesion molecule) and proinflammatory/fibrogenic cytokines (IL-1beta, TNF-alpha, TGF-beta1, and PDGF) in sections of normal skin, hypertrophic scar, and hypertrophic scar previously treated with an irradiated mixture of collagen-polyvinylpyrrolidone and completely resolved. Expression of these proteins was detected by indirect immunoperoxidase staining. The hypertrophic scar group displayed an increased amount of IL-1beta, TNF-alpha, TGF-beta1, and PDGF compared with the normal skin and treated scar groups. Values were statistically significant when cytokines in hypertrophic scar and hypertrophic treated sections were compared. Surprisingly, no differences were detected between normal skin and treated scars. On the other hand, differences in levels of E-selectin and vascular cell-adhesion molecule were not statistically significant between the groups, except for vascular cell-adhesion molecule, which decreased in treated scars. Also, supernatants from fibroblast cultures derived from treated hypertrophic scar, showed a reduction in TGF-beta1 and PDGF expression, although apparently collagen synthesis was not affected. Based on previous data from clinical studies in human dermal fibrosis remodeling, and the results presented here, we suggest that collagen-polyvinylpyrrolidone modulates extracellular matrix turnover, mainly of collagen, because expression levels of IL-1beta, TNF-alpha, TGF-beta1, and PDGF were diminished. We infer that collagen-polyvinylpyrrolidone participation could also modify the inflammatory process observed in hypertrophic scarring, by diminishing the expression of adhesion molecules, as a consequence of lower levels of proinflammatory cytokines, mainly IL-1beta and TNF-alpha.

Adolescent↗
PubMed1975

Application of polyvinylpyrrolidone as a carrier for kallikrein.

Kallikrein covalently attached to polyvinylpyrrolidone was prepared. The kinetic parameters, the molecular weight and the blood pressure depressor effect of kallikrein and kallikrein bound to polyvinylpyrrolidone are compared. Analytical ultracentrifugation showed a mean molecular weight of 110 000 dalton for kallikrein bound to polyvinylpyrrolidone. The specific activity of kallikrein-PVP was 4.6 times lower when compared with native kallikrein, however K-M was only slightly different. The maximal reduction and the duration of the decrease of mean arterial blood pressure were statistically not different from each other when kallikrein and kallikrein-PVP were injected in amounts of the same esterolytic activity.

Animals↗
PubMed2001

[Uncommon fluorescent properties of nano-structured terbium (III)-phthalic acid complex in polyvinylpyrrolidone].

Nano-sized terbium(III)-phthalic acid complex was prepared in polyvinylpyrrolidone. It's fluorescent spectrum has been investigated, compared to that of common terbium(III)-phthalic acid complex and terbium(III)-polyvinylpyrrolidone complex. The results show that fluorescent characterizations of Nano-sized terbium(III)-phthalic acid complex is obviously different from that of common terbium(III)-phthalic acid complex and terbium(III)-polyvinylpyrrolidone. The relative intensity and half-height width of main emission peaks are obviously varied, two splitting peaks are displayed.

Chelating Agents↗
PubMed1990

[A new chondroprotector--polyvinylpyrrolidone for treating osteoarthrosis patients].

The authors demonstrate the role of chondroprotector therapy in the management of patients with osteoarthrosis (OA). They suggest the use of the polymeric drug polyvinylpyrrolidone as artificial synovial fluid. The drug is administered intra-articularly and is capable of replacing pathological synovial fluid. It has been established that 10 and 20% polyvinylpyrrolidone solutions possess high viscosity and low compressibility, they are isolated from the articular cavity for 6 to 7 days and manifest antiarthrosis action in chondrocytic cultures. The short- and long-terms results of the clinical trials of polyvinylpyrrolidone solutions allow recommending them for the treatment of OA.

Animals↗
PubMed1982

[Simulation of malignant tumors by undeclared polyvinylpyrrolidone in drugs].

Numerous drugs are available containing polyvinylpyrrolidone as a carrier and retard substance. Repeated intramuscular or subcutaneous injections of polyvinylpyrrolidone over a long time can lead to tumor-like foreign body reactions mimicking true malignant tumors by clinical and histological features. Additionally, a storage of polyvinylpyrrolidone in visceral organs is possible in such patients.

Diagnosis, Differential↗
PubMed1980

Model of interaction of ajmaline with polyvinylpyrrolidone.

The chemical shifts in the Fourier transform 13C-NMR spectrum of ajmaline were assigned from consideration of the acetylation shifts and multiplet splitting in the off-resonance decoupled spectrum. On the basis of the assigned signals, the changes of chemical shifts in ajmaline induced by polyvinylpyrrolidone were investigated, and an interaction model of ajmaline with polyvinylpyrrolidone in chloroform was proposed.

Ajmaline↗
PubMed1981

Sorption properties of cross-linked insoluble polyvinylpyrrolidone.

The interaction of 32 drugs of diverse chemical structure with cross-linked insoluble polyvinylpyrrolidone (crospovidone) was studied. By using a polymer to drug ratio of 10:1, the sorbed amount for 20 compounds was found to be less than 5%. After a 10-fold decrease of the polymer concentration, the sorbed amount of eight other compounds fell to or below the 5% level. Only tannic acid and hexylresorcinol exhibited a significantly stronger sorption tendency. The interaction appeared to be controlled by phenolic groups in the active ingredient. The binding can be quantified by an interaction constant Ks, whose definition is based on a bulk phase model of interaction via independent binding sites. The exceptionally strong binding of hexylresorcinol, however, apparently was caused by cooperative interacting of the hexyl groups in the bound state. Desorption studies revealed that the binding was fully reversible in all cases. Therefore, the presence of cross-linked polyvinylpyrrolidone as a disintegrant in pharmaceutical preparations is not expected to interfere with GI drug absorption.

Adsorption↗
PubMed1982

Chromatographic study of interactions between polyvinylpyrrolidone and drugs.

A chromatographic technique for the study of possible interactions of drugs with soluble or insoluble polymer additives is proposed. Crospovidone was used as a stationary phase. The method allowed the rapid determination of interaction constants in the range of greater than 1 M-1 as relevant for applications in practice. The interaction of 39 drugs and model compounds of diverse chemical structure with povidone and crospovidone was studied. The results closely agreed with data obtained from conventional equilibrium dialysis and sorption studies. The complexation reaction was found to be dominated by hydrogen binding. A close correspondence between the strength of interaction and the nature, number, and position of hydrogen-donating functional groups in the active ingredient was observed. The binding tendency was enhanced when the functional groups were connected with aromatic residues. The carboxyl group was more effective than the hydroxide or amino groups. The binding can be quantified by the binding constants, Kp and Ks, respectively, describing the interaction with polyvinylpyrrolidone via independent binding sites. At pH 1, with the exception of tannic acid, all investigated drugs exhibited Kp and/or Ks values well below an upper limit of 10 M-1. Hence, with additive-drug ratios commonly used in pharmaceutical preparations, the bound amount of drug after oral administration can hardly exceed 3%. In view of this already low degree of potential binding and considering its reversible character and its decreasing tendency with increasing pH during GI passage, the presence of polyvinylpyrrolidone in pharmaceutical preparations is not expected to interfere with GI drug absorption.

Adsorption↗
PubMed1984

Modulation of RNA transport by polyvinylpyrrolidone.

A number of studies have documented substantial loss of nuclear protein during aqueous nuclear isolation procedures. This loss can, to some extent, be counteracted by addition of impermeable macromolecules like polyvinylpyrrolidone, which prevent nuclear swelling. While nucleic acids appear to be much less susceptible to leakage during isolation, the effects of these additives on RNA release during in vitro incubation have not been examined. Here we show that addition of polyvinylpyrrolidone results in significant decreases in RNA transport; inhibition becomes maximal at 50-75 microM addition.

Animals↗
PubMed1980

Rapid quantitation of neutrophil chemotaxis: use of a polyvinylpyrrolidone-free polycarbonate membrane in a multiwell assembly.

A neutrophil chemotaxis assay was developd which permits rapid, quantitative assessment of migration across a membrane filter. The critical factor in the assay was the use of a 10 microns thick polycarbonate membrane without the usual polyvinylpyrrolidone coating. Migrated neutrophils remain adherent to the uncoated membrane, whereas 20-50% fall off polyvinylpyrrolidone-coated membranes. A major advantage of the method is that neutrophil chemotaxis can be readily quantified, since the migrated cells adhere to the membrane surface and are in one optical plane for counting. A 25 mm x 80 mm membrane sheet was used in a 48-well micro chemotaxis assembly, which requires only 20,000 neutrophils and 25 microliters of attractant per assay well. Neutrophil chemotaxis was complete within 10-20 min at 37 degrees C, with 20-30% of the cells migrating to N-formyl-methionyl-leucyl-phenylalanine and 40-50% migrating to complement derived C5a.

Carbonates↗