Influence of polyvinylpyrrolidone, microcrystalline cellulose and colloidal silicon dioxide on technological characteristics of a high-dose Petiveria alliacea tablet.

PURPOSE: Petiveria alliacea L. (Phytolaccaceae) is a perennial shrub used by its immunomodulatory, anticancerogenic and anti-inflammatory properties. This study determined the influence of polyvinylpyrrolidone (PVP), colloidal silicon dioxide (CSD) and microcrystalline cellulose (MC) on the technological characteristic of a high-dose P. alliacea tablet prepared by the wet granulation method. METHODOLOGY: The botanical and pharmacognostic analysis of the plant material was firstly performed, followed by a 23 factorial design considering three factors at two levels: (a) the binder (PVP) incorporated in formulation at 10% and 15% (w/w); (b) the compacting agent (CSD) added at 10% and 15% (w/w) and; (c) the diluent (MC) included at 7.33% and 12.46% (w/w). The analysis of pharmaceutical performance and the accelerated and long-term stability of the best prototype were also completed. RESULT AND DISCUSSION: The binder, compacting agent and the interaction binder/diluent had a significant impact on breaking force of high-dose P. alliacea tablet. The optimum formula was found to contain 15% (w/w) of CSD, 7.33% (w/w) of MC and 10% (w/w) of PVP. At these conditions, the tablet shows a breaking force of 77.96 N, a friability of 0.39%, a total phenol content of 1.30 mg/tablet and a maximum disintegration time of 6 min. CONCLUSIONS: The use of adequate amounts of PVP, MC and CSD as per the factorial design allowed the preparation of a tablet suitable for administration, despite the inappropriate flow and compressibility properties of the P. alliacea powder.

[Preparation and pharmacokinetics of brucine hydrogel patch].

OBJECTIVE: To investigate the effect of dose on pharmacokinetic properties of brucine hydrogel patch. METHODS: The plasma concentration of brucine was determined by HPLC. Brucine hydrogel patch was prepared and its pharmaceutical characterization was investigated. After transdermal administration of different dose brucine hydrogel patch; Plasma concentration versus time profiles were determined and pharmacokinetic parameters were calculated by DAS program. RESULTS: The pharmaceutical properties of brucine hydrogel patch were satisfactory. The AUC0-1 values were 7.24 +/- 0.61, 16.02 +/- 2.34 and 54.84 +/- 26.59 microg x h/mL after administration of 30, 60 and 180 mg/kg brucine hydrogel patch, respectively. The corresponding C(max) values were 0.73 +/- 0.23, 1.45 +/- 0.28 and 4.59 +/- 1.85 microg/mL, respectively. And the corresponding T(max) values were 8.67 +/- 2.07, 11.67 +/- 2.66 and 8.33 +/- 2.65 h, respectively. CONCLUSION: The pharmacokinetic properties of brucine do not vary with the dose of brucine hydrogel patch.

[Optimization of the matrix formulation of compound Die Da Zhen Tong cataplasm by uniform design].

OBJECTIVE: To optimize the matrix formulation of compound Die Da Zhen Tong cataplasm. METHODS: The optimal preparation was selected by U17 (17(16)) uniform design, independent variables were the percentage ratio of the matrix formulation component part in compound Die Da Zhen Tong cataplasm,and the viscosity, continued viscosity and overall desirability used as indexes were dependent variables. RESULTS: The percentage of the matrix formulation component part in compound Die Da Zhen Tong cataplasm was, NP-700: carbomer 980: PVP K-90: dihydroxy aluminum: tartaric: kaolinite: sorbitol: glycerin = 5: 1. 2: 2.5: 0.25: 0.15:4: 12: 5. CONCLUSION: The optimized cataplasm has good viscosity, continued viscosity and high overall desirability.

A multicenter, double-blind, parallel group, placebo-controlled clinical study to examine the safety and efficacy of T-Clair SPHP700-3 in the management of mild to moderate dry eye in adults.

PURPOSE: To study the safety and efficacy of T-Clair SPHP700-3, a new over-the-counter preservative-free formulation, in the management of mild to moderate dry eye in adults. METHODS: Sixty adult patients with mild to moderate dry eye were consecutively recruited in 2 eye clinics and randomized into 2 groups: treatment and placebo. Signs and symptoms of dry eye were compared along 28 days of treatment. RESULTS: No adverse events were reported during the study. Symptoms and signs of dry eye showed significant differences between the 2 groups after 2 and 4 weeks of treatment. CONCLUSIONS: SPHP700-3 preservative-free formulation showed to be safe and effective in mild to moderate dry eye, improving tear film stability, ocular surface lubrification, and patients' symptomatology.

Formulation and characterization of ternary solid dispersions made up of Itraconazole and two excipients, TPGS 1000 and PVPVA 64, that were selected based on a supersaturation screening study.

Both d-alpha-tocopheryl polyethylene glycol 1000 (TPGS 1000) and polyvidone-vinylacetate 64 (PVPVA 64) provided an increase in the degree of supersaturation and stability of supersaturated Itraconazole solutions, compared to a blanc without excipient. Therefore, both components were combined as carrier in order to make ternary solid dispersions of Itraconazole by spray drying. This way, TPGS 1000 could be incorporated into a powder. Dissolution experiments on the ternary solid dispersions revealed that during the first hour the release was much higher than for the binary Itraconazole/PVPVA 64 solid dispersions. For some compositions a release of more than 80% was reached after 10min. However, after the first hour the drug started to precipitate. The ternary solid dispersions were all XRD amorphous, but MDSC revealed the coexistence of multiple amorphous phases and a crystalline Itraconazole phase, depending on the composition. Therefore the burst effect during the first hour can be ascribed to an accelerated dissolution of the amorphous Itraconazole fraction in the presence of TPGS 1000. The precipitation after 1h, however, is probably due to the combination of the surfactant properties of TPGS and the small crystalline Itraconazole fraction.

[Preparation of Zhongjiefeng dispersible tablets].

OBJECTIVE: To prepare Zhongjiefeng dispersible tablets. METHODS: The formulation of Zhongjiefeng dispersible tablets were optimized as index of disintegration time by orthogonal design test. RESULTS: The optimized Zhongjiefeng dispersible tablets, which were prepared by selecting 16% PVPP and 3% L-HPC as disintegrants, 40% MCC as filler, can disintegrate in 3 mins. CONCLUSIONS: The above formulation is reasonable and the disintegration time is suitable, so it can provide theoretic support for industrialization.

The targeting of anionized polyvinylpyrrolidone to the renal system.

We reported that the co-polymer composed of vinylpyrrolidone and maleic acid selectively distributed into the kidneys after i.v. injection. To further optimize the renal drug delivery system, we assessed the renal targeting capability of anionized polyvinylpyrrolidone (PVP) derivatives after intravenous administration in mice. The elimination of anionized PVP derivatives from the blood decreased with increasing anionic groups, and the clearance of carboxylated PVP and sulfonated PVP from the blood was almost similar. But carboxylated PVP efficiently accumulated in the kidney, whereas sulfonated PVP was rapidly excreted in the urine. The renal levels of carboxylated PVP were about five-fold higher than sulfonated PVP. Additionally, carboxylated PVP was effectively taken up by the renal proximal tubular epithelial cells in vivo after i.v. injection. These anionized PVP derivatives did not show any cytotoxicity against renal tubular cells and endothelial cells in vitro. Thus, these carboxylated and sulfonated PVPs may be useful polymeric carriers for drug delivery to the kidney and bladder, respectively.

Studies on the effect of polyvinyl pyrrolidone on the activity of chlorhexidine mouthrinses: plaque and stain.

BACKGROUND, AIMS: Polyvinyl pyrrolidone (PVP) was shown in vitro to reduce chlorhexidine induced, dietary staining without affecting the uptake of the antiseptic to the test substrate. The aim of these studies in vivo was to determine whether PVP affected plaque and dietary staining by a low concentration chlorhexidine rinse. METHODS: The plaque and stain studies used a double blind, randomised 6, treatment crossover design involving healthy subjects with a high standard of oral hygiene and gingival health. The rinse formulations under test were: (A) aqueous alcohol (placebo control), (B) 0.03% chlorhexidine, (C) 0.06% chlorhexidine, (D) 0.06% chlorhexidine+1.2% PVP, (E) 0.06% chlorhexidine+5% PVP, (F) 0.06% chlorhexidine+10% PVP. In the plaque study, on day 1 of each period, subjects were rendered plaque free and then rinsed with 15 ml of the test rinse for 60 s. No further tooth cleaning was performed and subjects returned 24 h later for plaque scoring by area. In the stain study, on day 1 of each period, the tongue and teeth of each subject were rendered stain free. Subjects then rinsed under supervision for 60 s with 15 ml of the allocated rinse 8 x a day between 09:00 h and 17:00 h for 3 days. Immediately after each rinse with the test formulation, subjects rinsed for 120 s with 15 ml of warm black tea. Subjects were requested to also drink at least 5 cups of tea or coffee per day. On day 4, stain was scored by area and intensity from designated teeth and dorsum of the tongue. Washout periods were at least 7 days in both studies. RESULTS: Plaque areas were greatest with placebo and least with 0.06% chlorhexidine. Plaque scores increased with increasing concentrations of PVP in the 0.06% chlorhexidine rinse and were significantly higher than 0.06% chlorhexidine without PVP rinse. Tooth stain areas were comparable for placebo, 0.03% and 0.06% chlorhexidine rinses, but significantly reduced with the PVP/chlorhexidine rinses compared to the 0.06% chlorhexidine rinse. Tooth stain intensity was significantly increased with 0.06% chlorhexidine rinses compared to placebo and chlorhexidine/PVP rinses. Tongue stain area and intensity were significantly reduced with 5% and 10% PVP/chlorhexidine rinses compared to 0.06% chlorhexidine rinse. CONCLUSION: PVP, at the concentrations tested, reduced the stain propensity of a 0.06% chlorhexidine rinse but at the expense of some loss of plaque inhibition.

[Effects of infusion therapy on immunity and calcium contents in patients with stomach cancer]. / Vliianie infuzionnoi terapii na sostoianie immuniteta i soderzhanie kal'tsiia u bol'nykh rakom zheludka.

The humoral factor of non-specific immunity was shown to be inhibited significantly in gastric cancer patients. According to an analysis of immunologic status, phagocytic activity and blood plasma level of lysozymes increased during treatment of stomach cancer, thus pointing to favorable course of postoperative period.

The effect of 3 mouthrinses on plaque and gingivitis development.

The aim of this study was to evaluate the effect of 3 mouthrinses, Listerine Antiseptic (thymol), Peridex (chlorhexidine), Perimed (povidone iodine and hydrogen peroxide), and a placebo (water) on the development of dental plaque and gingivitis, when used as the only oral hygiene procedure for 14 days. 71 subjects were entered into a randomized, double-blind study. At the baseline examination, papillary bleeding score (PBS), and plaque index (PI) were registered, after which subjects received supragingival prophylaxis and were assigned to 1 of 4 study cells. Subjects were asked to refrain from all oral hygiene procedures except for the supervised 14-day 2 x daily rinsing with the assigned preparation. At day 14, the same clinical parameters were again registered. Statistical analysis was performed by a one-way analysis of variance (ANOVA) to compare the 4 groups, followed by Duncan's multiple range test to determine specific group differences. At baseline, average PBS and PI scores were similar for all 4 groups. After 14 days, the average PBS for Peridex and Perimed was significantly lower than for Listerine Antiseptic and water. The frequency of interdental units with a PBS greater than 2 was significantly lower for Peridex and Perimed than for Listerine Antiseptic and water. We concluded that both Peridex and Perimed were effective in reducing plaque and gingivitis when used as a 2 x daily mouthrinse by subjects refraining from other oral hygiene procedures. In vitro, a synergistic effect was assumed when inhibition was achieved with Perimed at the same or greater dilution than was achieved with povidone-iodine alone.

[Artificial synovial fluid for the joints]. / Iskusstvennaia sinovia'lnaia zhidkos't dlia sustavov.

The author presents the results of his biomechanical, experimental and clinical studies to produce an artificial synovial fluid for therapeutic correction when administered intraarticularly in inflammatory and degenerative diseases, traumas and operations on the joints. According to the results of the rheologic investigations, the 15% aqueous solution of mean molecular polyvinylpyrrolidone (PVP) and its complex with a biopolymer (PVP-hyaluronate) turned out to be most similar to the natural synovial fluid of the joints. The experimental studies (201 rabbits) revealed a suppression of the inflammatory process in the joints and an antiadhesive action of the artificial synovia which improved the metabolism of the acetabular cartilage and the functions of the joints. In the clinical part of the study (514 patients) the preparations of the artificial synovial fluid and its complexes with other drugs were administered intraarticularly to the patients with rheumatoid arthritis and deforming osteoarthrosis. An improvement in many values of the function of the joints and of the laboratory and biochemical data has been revealed. There have been no side effects in the patients under study; an improvement in the working ability has been noted, including the evaluation of the long-term results (1 to 10 years).

[Pharmacokinetics of anthracycline antibiotics deposited by polymers]. / Izuchenie farmakokinetiki antratsiklinovykh antibiotikov deponirovannykh polimerami.

An increase of doxorubicin concentration in different organs and tissues and its decrease in the peripheral blood were observed when studying pharmacokinetics of this drug administered in the 10% solution of polyvinylpyrrolidone. A prolonged and stable release of carminomycin from glue composition MK-10-0 "carminacryl" confirms an expediency of alpha-cyanoacrylate use for deposition of anthracycline antibiotics with the aim of loco-regional chemotherapy.

[Anorexia nervosa as a manifestation of endogenous depression in puberty]. / Nervnaia anoreksiia ka proiavlenie éndogennoi depressii v pubertatnom vozraste.

Possible interrelation between anorexia nervosa and affective pathology is discussed. The authors present an analysis of clinical observations where the anorexia nervosa syndrome was developing in the presence of endogenous circulatory depression. It is noted that in some cases of latent depression, this syndrome may present the most prominent feature in the clinical picture of the disease, which makes its diagnosis and treatment rather difficult. Differential diagnostic signs permitting the differentiation between "depressive" anorexia nervosa and its other nosologic variants are discussed.