RESUMO
This study investigated the interaction between polydeoxyribonucleotide (PDRN) and several ionic and nonionic isotonic agents, thickeners and a preservative that were employed as excipients in ophthalmic preparations. Interaction of each individual excipient and PDRN aqueous solution was evaluated by analyzing their rheological properties. Rheological properties of PDRN solutions were evaluated by dynamic oscillatory shear tests and values of elastic modulus (G'), viscous modulus (Gâ³) and loss tangent (tan δ) were used to assess the relative changes in viscoelastic properties. At given concentrations, sodium chloride was found to show alteration in viscoelastic properties of PDRN solution while nonionic isotonic agents like d-glucose and d-sorbitol did not alter them. Similarly, nonionic water soluble polymers like polyvinylpyrrolidone (PVP) and hydroxypropyl methylcellulose (HPMC) also did not interact with PDRN to alter the viscoelastic properties. However, there were changes observed when carbopol 940 was used as a thickener. Therefore, PDRN was found to interact with ionic excipients and the interactions were negligible when nonionic materials were examined, which suggests that nonionic excipients are suitable to be formulated with PDRN.
Assuntos
Química Farmacêutica/métodos , Excipientes/química , Polidesoxirribonucleotídeos/química , Polímeros/química , Composição de Medicamentos/métodos , Módulo de Elasticidade , Soluções Oftálmicas , Reologia , Cloreto de Sódio/química , Substâncias Viscoelásticas/químicaRESUMO
The oxygen reduction reaction (ORR) activity of a Cu-doped Ba0.5Sr0.5FeO3-δ (Ba0.5Sr0.5Fe1-xCuxO3-δ, BSFCux, x = 0, 0.05, 0.10, 0.15) perovskite cathode was investigated in terms of oxygen vacancy formation and valence band structure. The BSFCux (x = 0, 0.05, 0.10, 0.15) crystallized in a cubic perovskite structure (Pm3¯m). By thermogravimetric analysis and surface chemical analysis, it was confirmed that the concentration of oxygen vacancies in the lattice increased with Cu doping. The average oxidation state of B-site ions decreased from 3.583 (x = 0) to 3.210 (x = 0.15), and the valence band maximum shifted from -0.133 eV (x = 0) to -0.222 eV (x = 0.15). The electrical conductivity of BSFCux increased with temperature because of the thermally activated small polaron hopping mechanism showing a maximum value of 64.12 S cm-1 (x = 0.15) at 500 °C. The ASR value as an indicator of ORR activity decreased by 72.6% from 0.135 Ω cm2 (x = 0) to 0.037 Ω cm2 (x = 0.15) at 700 °C. The Cu doping increased oxygen vacancy concentration and electron concentration in the valence band to promote electron exchange with adsorbed oxygen, thereby improving ORR activity.
RESUMO
The oxygen vacancy formation behavior and electrochemical and thermal properties of Ba0.5Sr0.5Fe1-xMnxO3-δ (BSFMnx, x = 0-0.15) cathode materials were investigated. For thermogravimetric analysis, the weight decreased from 1.98% (x = 0) to 1.81% (x = 0.15) in the 400-950 °C range, which was due to oxygen loss from the lattice. The average oxidation state of the B-site increased, the Oads/Olat ratio decreased, and the binding energy of the Olat peak increased with Mn doping. These results indicate that Mn doping increases the strength of the metal-oxygen bond and decreases the amount of oxygen vacancies in the lattice. The electrical conductivity of BSFMnx increased with the temperature due to the thermally activated small-polaron hopping mechanism showing a maximum value of 10.4 S cm-1 (x = 0.15) at 450 °C. The area-specific resistance of BSFMn0.15 was 0.14 Ω cm2 at 700 °C and the thermal expansion coefficient (TEC) gradually decreased to 12.7 × 10-6 K-1, which is similar to that of Ce0.8Sm0.2O2 (SDC) (12.2 × 10-6 K-1). Mn doping increased the metal-oxygen bonding energy, which reduced the oxygen reduction reaction activity but improved the electrical conductivity and thermal stability with SDC.
RESUMO
MnO2 and CeO2 were doped to improve the corrosion resistance of CSZ (calcia-stabilized zirconia), and we studied the phase formation, mechanical properties, and corrosion resistance by molten mold flux. The volume fraction of the monoclinic phase gradually decreased as the amount of MnO2 doping increased. The splitting phenomenon of the t(101) peak was observed in 2Mn_CSZ, and in 4Mn_CSZ, it was completely split, forming a cubic phase. The relative density increased and the monoclinic phase decreased as the doping amount increased, leading to an increase in Vickers hardness and flexural strength. However, in 3Mn_CSZ and 4Mn_CSZ, where cubic phase formation occurred, the tetragonal phase decreased, leading to a reduction in these properties. MnO2-doped CSZ exhibited a larger fraction of the monoclinic phase compared to the original CSZ after the corrosion test, indicating worsened corrosion resistance. These results are attributed to the predominant presence of Mn3+ and Mn2+ forms, rather than the Mn4+ form, which has a smaller basicity difference with SiO2, and due to the low melting point. The monoclinic phase fraction decreased as the doping amount of CeO2 increased in CeO2-doped CSZ, but the rate of decrease was lower compared to MnO2-doped CSZ. The monoclinic phase decreased as the doping amount increased, but the Vickers hardness and flexural strength showed a decreasing trend due to the low relative density. The destabilization behavior of Ca in SEM-EDS images before and after corrosion was difficult to identify due to the presence of Ca in the slag, and the destabilization behavior of Ce due to slag after corrosion was not observed. In the XRD data of the specimen surface after the corrosion test, the fraction of the monoclinic phase increased compared to before the test but showed a lower monoclinic phase fraction compared to CSZ. It is believed that CeO2 has superior corrosion resistance compared to CaO because Ce predominantly exists in the form of Ce4+, which has a smaller difference in basicity within the zirconia lattice.
RESUMO
The degradation behavior of yttria-stabilized zirconia by thermal aging was investigated in terms of phase transformation, local atomic structure, and electrical conductivity. The average grain size of 8YSZ was increased from 20.83 µm to 25.81 µm with increasing aging temperature. All 8YSZ samples degraded at different temperatures had a predominantly cubic structure. The (400) peak of 8YSZ deteriorated at 1300 and 1400 °C shifted to a high angle, and the peak of tetragonal was not indexed. For 8YSZ degraded at 1500 °C, the (400) peak shifted to a lower angle, and the peak of tetragonal was identified. Analysis of the local microstructure of aged 8YSZ using extended X-ray absorption fine structure showed that the intensity of the Zr-O peak gradually increased and that the intensity of the peak of cationic Zr decreased as the aging temperature increased. The changes in the peaks indicate that the oxygen vacancies were reduced and Y3+ ions escaped from the lattice, leading to the destabilization of 8YSZ. The activation energies of 8YSZ at 1300 °C and 1400 °C were derived to be 0.86 and 0.87 eV, respectively, and the activation energy of 8YSZ at 1500 °C increased significantly to 0.92 eV. With the thermal deterioration of 8YSZ, the cation (Y3+) escaped from the lattice and the number of oxygen vacancies decreased, resulting in the formation of a tetragonal structure and high activation energy at 1500 °C.
RESUMO
Given the increasingly serious nature of environmental problems, many countries have recently declared carbon neutrality policies and expended efforts to implement them. The domestic building industry aims to reduce its environmental impact using life-cycle assessments (LCAs) of buildings according to the Green Standard for Energy and Environmental Design. However, it is difficult to perform efficient LCAs because the required quantity takeoff process is complex, and the quantity takeoff sheet may not exist during the building's design phase. In this study, 21 building LCAs were used to simplify and improve the efficiency of the proposed method and enable building LCAs even when there was no quantity takeoff sheet. Furthermore, a standard quantity database of building materials was constructed based on the analysis of the input quantities of building materials per unit area, and the apartment buildings LCA method was proposed using this database. The input quantities of building materials were analyzed using the probabilistic analysis technique. The probability distribution was derived using Monte Carlo simulations, and the goodness-of-fit was verified. Finally, the reliability of the proposed building LCA method was verified using a case study.
RESUMO
The therapeutic potential of saquinavir, a specific inhibitor of human immunodeficiency virus (HIV)-1 and HIV-2 protease enzymes, has been largely limited because of a low solubility and consequnt low bioavailability. Thus, we aimed to design a supersaturated self-microemulsifying drug delivery system (S-SMEDDS) that can maintain a high concentration of saquinavir in gastro-intestinal fluid thorugh inhibiting the drug precipitation to enhance the lymphatic transport of saquinavir and to increase the bioavailability of saquinavir considerably. Solubilizing capacity of different oils, surfactants, and cosurfactants for saquinavir was evaluated to select optimal ingredients for preparation of SMEDDS. Through the construction of pseudo-ternary phase diagram, SMEDDS formulations were established. A polymer as a precipitation inhibitor was selected based on its viscosity and drug precipitation inhibiting capacity. The S-SMEDDS and SMEDDS designed were administered at an equal dose to rats. At predetermined time points, levels of saquinavir in lymph collected from the rats were assessed. SMEDDS prepared presented a proper self-microemulsification efficiency and dispersion stability. The S-SMEDDS fabricated using the SMEDDS and hydroxypropyl methyl cellulose 2910 as a precipitation inhibitor exhibited a signficantly enhanced solubilizing capacity for saquinavir. The drug concentration in a simulated intestinal fluid evaluated with the S-SMEDDS was also maintained at higher levels for prolonged time than that examined with the SMEDDS. The S-SMEDDS showed a considerably enhanced lymphatic absoprtion of saquinavir in rats compared to the SMEDDS. Therefore, the S-SMEDDS would be usefully exploited to enhance the lymphatic absorption of hydrophobic drugs that need to be targeted to the lymphatic system.
RESUMO
Ginsenosides, the major active ingredients of ginseng and other plants of the genus Panax, have been used as natural medicines in the East for a long time; in addition, their popularity in the West has increased owing to their various beneficial pharmacological effects. There is therefore a wealth of literature regarding the pharmacological effects of ginsenosides. In contrast, there are few comprehensive studies that investigate their pharmacokinetic behaviors. This is because ginseng contains the complicated mixture of herbal materials as well as thousands of constituents with complex chemical properties, and ginsenosides undergo multiple biotransformation processes after administration. This is a significant issue as pharmacokinetic studies provide crucial data regarding the efficacy and safety of compounds. Moreover, there have been many difficulties in the development of the optimal dosage regimens of ginsenosides and the evaluation of their interactions with other drugs. Therefore, this review details the pharmacokinetic properties and profiles of ginsenosides determined in various animal models administered through different routes of administration. Such information is valuable for designing specialized delivery systems and determining optimal dosing strategies for ginsenosides.
RESUMO
This study aimed to design phosphatidylcholine (PC)-based solid dispersion (SD) systems for enhancing the apparent aqueous solubility and dissolution of celecoxib (CLC), a selective cyclooxygenase-2 inhibitor with a highly hydrophobic property. Although PC-based dispersion formulations considerably increased solubilities of CLC, the lipidic texture of PC was not appropriate as a solid dosage form for oral administration of CLC. To mask the lipidic texture of PC-based matrices, Neusilin® US2, an adsorbent material with a porous structure and large surface area widely used in the pharmaceutical industry, was employed and thereby fully powderized PC-based dispersion formulations could be fabricated. However, PC matrices containing CLC strongly adsorbed to the pores of Neusilin® US2 was not able to be rapidly released. To address this problem, different hydrophilic materials were examined to promote the release of the CLC-dispersed PC matrices from Neusilin® US2. Among tested hydrophilic materials, croscarmellose sodium was the most suitable to facilitate fast drug dissolution from Neusilin® US2 particles, showing significantly enhanced apparent aqueous solubility and dissolution behavior of CLC. Through differential scanning calorimetry, X-ray diffraction, and Fourier transform infrared spectroscopy (FT-IR) analysis, a considerably reduced crystallinity of CLC dispersed in the PC-based dispersion formulations was demonstrated. The PC-based SD formulations developed in this study would be useful for improving the oral bioavailability of poorly soluble drugs such as CLC.
RESUMO
This study evaluated the moisturizing effect of serine-loaded solid lipid nanoparticles (serine-SLN) and polysaccharide-rich reed (Phragmites communis) root extract (RRE) incorporated in hydrogel bases. The hydrogels with serine-SLN and/or RRE were carefully applied on the volar forearm of human volunteers. Their moisturizing efficacy was evaluated by monitoring conductance values using a skin surface hygrometer. The values of the area under the normalized conductance-time curve (AUCC) were developed and compared as a parameter for the water holding capacity of the skin. Hydrogels with serine-SLN did not significantly moisturize the skin, while hydrogel containing 0.25% RRE produced a significant increase in the moisture content of the skin. However, adding more than 0.25% of RRE into the hydrogel base decreased the moisturizing effect due to the marked reduction of viscosity. Significantly enhanced moisturizing effect was observed with the hydrogel containing 0.25% RRE and 3% serine-SLN, with AUCC increased 2.21 times compared to than blank hydrogel. The results imply that effective delivery of serine into the skin is possible using lipid-based nanocarriers and RRE, which could be a promising strategy to moisturize the skin effectively.
Assuntos
Extratos Vegetais/farmacologia , Poaceae/química , Polissacarídeos/farmacologia , Serina/farmacologia , Pele/efeitos dos fármacos , Administração Cutânea , Adulto , Área Sob a Curva , Cosméticos/administração & dosagem , Cosméticos/farmacologia , Portadores de Fármacos , Feminino , Humanos , Hidrogéis/química , Lipídeos/química , Nanopartículas/química , Tamanho da Partícula , Extratos Vegetais/administração & dosagem , Raízes de Plantas/química , Polissacarídeos/administração & dosagem , Serina/administração & dosagem , Absorção Cutânea , Viscosidade , Adulto JovemRESUMO
ß-Lapachone has drawn increasing attention as an anti-inflammatory and anti-cancer drug. However, its oral bioavailability has not been yet assessed, which might be useful to develop efficient dosage forms possibly required for non-clinical and clinical studies and future market. The aim of the present study was thus to investigate pharmacokinetic properties of ß-lapachone as well as its first-pass metabolism in the liver, and small and large intestines after oral administration to measure the absolute bioavailability in rats. A sensitive HPLC method was developed to evaluate levels of ß-lapachone in plasma and organ homogenates. The drug degradation profiles were examined in plasma to assess the stability of the drug and in liver and intestinal homogenates to evaluate first-pass metabolism. Pharmacokinetic profiles were obtained after oral and intravenous administration of ß-lapachone at doses of 40 mg/kg and 1.5 mg/kg, respectively. The measured oral bioavailability of ß-lapachone was 15.5%. The considerable degradation of ß-lapachone was seen in the organ homogenates but the drug was quite stable in plasma. In conclusion, we suggest that the fairly low oral bioavailability of ß-lapachone may be resulted from the first-pass metabolic degradation of ß-lapachone in the liver, small and large intestinal tracts and its low aqueous solubility.