scholarly journals Paediatric formulation: budesonide 0.1 mg/mL viscous oral solution for eosinophilic esophagitis using cyclodextrins

2018 ◽  
Vol 0 (0) ◽  
Author(s):  
Caroline Ey ◽  
Christel Hosselet ◽  
Benjamin Villon ◽  
Frédéric Marçon
Keyword(s):  
Degradation Products ◽  
Dose Range ◽  
Oral Solution ◽  
Related Substance ◽  
Cyclodextrin Complexation ◽  
Home Based ◽  
The Stability ◽  
Preservative Free ◽  
Paediatric Formulation

Abstract Background Viscous oral solutions of budesonide (dose range: 1 mg to 2 mg) have long been used to treat eosinophilic oesophagitis in children. The objective of the present study was to provide a convenient paediatric pharmaceutical formulation of a viscous budesonide solution at a dose level of 0.1 mg/mL, using cyclodextrin as a solubilizer. Methods Solubility studies were performed with γ-cyclodextrin and hydroxypropyl-β-cyclodextrin, and viscosity was tested with a Brookfield viscometer. The stability of the final formulation was tested in a climatic chamber. Levels of budesonide, budesonide impurities and degradation products were assayed using the HPLC–UV method described for the budesonide-related substance assay in the European Pharmacopoeia monograph. Results The solubility of budesonide increased linearly with both cyclodextrins. Gamma cyclodextrin (complexation efficiency: 0.147) was preferred to hydroxypropyl-β-cyclodextrin (complexation efficiency: 0.064) as a solubilizing agent. Hydroxypropylcellulose (1 % m/v) was added to increase viscosity, and sucralose was added to improve palatability. The sterilized, filtered, final formulation was stable for at least 3 months when packed aseptically in sterile 15 mL type 1 amber glass vials. Conclusions We have developed a convenient, stable, preservative-free, viscous formulation of a budesonide solution for the hospital- and home-based treatment of paediatric patients.

scholarly journals The traditional experience strategy (TES) and combined ultrasonography examination (CUE) for the treatment of lateral compression type 1 pelvic fractures: a historical control study

2021 ◽  
Vol 22 (1) ◽  
Author(s):  
Hai Huang ◽  
Bin-Fei Zhang ◽  
Ping Liu ◽  
Hong-Li Deng ◽  
Peng-Fei Wang ◽  
...  
Keyword(s):  
Pelvic Fractures ◽  
Definitive Treatment ◽  
Lateral Compression ◽  
Level Of Evidence ◽  
Conservative Group ◽  
Medical Records System ◽  
The Stability ◽  
And Function ◽  
Compression Type

Abstract Background It is difficult to judge the stability of lateral compression type-1 (LC-1) pelvic fracture, as it is often based on static images of the pelvis. Compared with the traditional experience strategy, ultrasonography examination may be able to distinguish operative and conservative patients before definitive treatment. However, in previous studies, we have not compared the outcomes between traditional experience strategy (TES group) and combined ultrasonography examination (CUE group). Thus, the aim of the study is comparing the differences between TES and CUE strategy, to identify the value of ultrasonography examination. Methods Medical records system for patients with LC-1 pelvic fractures who were treated with TES and CUE strategy were included. Patients’ baseline characteristics, treatment strategy, and function were recorded at follow-up. Functional outcomes were evaluated using the Majeed grading system. Results In total, 77 patients with LC-1 pelvic fractures were included in the study. There were 42 and 35 patients in TES and CUE group, respectively. Compared to TES group (69 %), there were less proportion patients chosen the operative treatment in CUE group (43 %, P = 0.021). The volume of intraoperative blood loss in CUE operative group was more than TES operative group (P = 0.037). There were more patients with complete sacral fracture in CUE operative group than TES operative group (P = 0.002). The Majeed scores in CUE conservative group was higher than TES conservative group (P = 0.008). The overall Majeed scores in CUE group was higher than that in TES group (P = 0.039). Conclusions The ultrasonography examination could relatively accurately identify the unstable LC-1 pelvis than the traditional experience strategy, the operative rate could be reduced and the overall function of LC-1 patients could be improved under the ultrasonography examination. Level of evidence Level III.

scholarly journals Quiescent Gap Solitons in Coupled Nonuniform Bragg Gratings with Cubic-Quintic Nonlinearity

2021 ◽  
Vol 11 (11) ◽  
pp. 4833
Author(s):  
Afroja Akter ◽  
Md. Jahedul Islam ◽  
Javid Atai
Keyword(s):  
Numerical Stability ◽  
Bragg Gratings ◽  
Stability Boundaries ◽  
Quintic Nonlinearity ◽  
Numerical Stability Analysis ◽  
Gap Solitons ◽  
The Stability ◽  
Dual Core

We study the stability characteristics of zero-velocity gap solitons in dual-core Bragg gratings with cubic-quintic nonlinearity and dispersive reflectivity. The model supports two disjointed families of gap solitons (Type 1 and Type 2). Additionally, asymmetric and symmetric solitons exist in both Type 1 and Type 2 families. A comprehensive numerical stability analysis is performed to analyze the stability of solitons. It is found that dispersive reflectivity improves the stability of both types of solitons. Nontrivial stability boundaries have been identified within the bandgap for each family of solitons. The effects and interplay of dispersive reflectivity and the coupling coefficient on the stability regions are also analyzed.

A New, Rapid and Simple RP-HPLC Method for Stability Quantification of a Protease Inhibitor in Tablets

2021 ◽  
Author(s):  
Rochele Cassanta Rossi ◽  
Josué Guilherme Lisbôa Moura ◽  
Vanessa Mossmann ◽  
Patrícia Weimer ◽  
Pedro Eduardo Fröehlich
Keyword(s):  
Quality Control ◽  
Protease Inhibitor ◽  
Degradation Products ◽  
Gradient Elution ◽  
Hplc Method ◽  
Array Detector ◽  
Forced Degradation ◽  
Control Analysis ◽  
Quality Control Laboratory ◽  
The Stability

Abstract Fosamprenavir calcium is a protease inhibitor widely used in the treatment and prevention of human immunodeficiency virus and acquired immunodeficiency syndrome. This protease inhibitor serves as a prodrug of amprenavir, offering better oral bioavailability. Although this drug was approved by the FDA in 2003, there are few methods established for quantifying the stability for quality control analysis of fosamprenavir-coated tablets. The purpose of the study was to develop and validate a method for determining the stability of fosamprenavir-coated tablets (Telzir®) that may be applied by any quality control laboratory. Chromatographic separation was performed using a Vertical RP-18 column programmed to run a gradient elution with sodium acetate buffer and acetonitrile. Flow rate was 1.2 mL min−1 for a total run time of 15 min. Ultraviolet detection was set at 264 nm and the use of a photodiode array detector in scan mode allowed selectivity confirmation by peak purity evaluation. The analyte peak was found to be adequately separated from degradation products generated during forced degradation studies. Thus, the proposed method was found to accurately indicate stability and was sufficient for routine quantitative analysis of fosamprenavir in coated tablets without interference from major degradation products and excipients.

Temperature Dependence of Degradation of Colored Oxo-Biodegradable Low-Density Polyethylene Films under Accelerated Thermal Aging

2017 ◽  
Vol 890 ◽  
pp. 82-85 ◽  
Author(s):  
Reymark D. Maalihan ◽  
Bryan B. Pajarito
Keyword(s):  
Thermal Aging ◽  
Degradation Products ◽  
Low Density Polyethylene ◽  
Effect Of Temperature ◽  
Low Density ◽  
Polyethylene Films ◽  
Hot Air ◽  
Taguchi Design Of Experiments ◽  
Oxidant Concentration ◽  
The Stability

This work reports the effect of temperature on degradation of colored low-density polyethylene (PE) films during thermal aging. Film samples were formulated according to Taguchi design of experiments where colorant, thickness, and pro-oxidant concentration were varied accordingly. Tensile properties of films were monitored with time during heat aging in a hot air oven at 50, 70, and 90 °C. Likewise, surfaces of aged films were analyzed to evaluate the degree of oxidation of PE during thermal aging. The Arrhenius equation was then used to predict the lifetime of PE at an in-use temperature of 30 °C. Results indicate that increasing the temperature reduces the tensile strength and modulus of films. Formation of carbonyl groups as degradation products is also observed at higher temperatures. Consequently, thermal aging at 90 °C offers the highest extent of degradation of exposed films. Regression analysis reveals that white films degrade at a higher rate than yellow and non-colored films. The presence of TiO2 in white films shortens the lifetime of PE while amine stabilizer in yellow films enhances the stability of PE during thermal aging.

scholarly journals The Instability of Dimeric Fc-Fusions Expressed in Plants Can Be Solved by Monomeric Fc Technology

2021 ◽  
Vol 12 ◽  
Author(s):  
Pia Gattinger ◽  
Shiva Izadi ◽  
Clemens Grünwald-Gruber ◽  
Somanath Kallolimath ◽  
Alexandra Castilho
Keyword(s):  
Monoclonal Antibodies ◽  
Fusion Proteins ◽  
Degradation Products ◽  
Therapeutic Proteins ◽  
Cost Effective ◽  
Full Length ◽  
Peptide Sequence ◽  
Reporter Protein ◽  
The Stability

The potential therapeutic value of many proteins is ultimately limited by their rapid in vivo clearance. One strategy to limit clearance by metabolism and excretion, and improving the stability of therapeutic proteins, is their fusion to the immunoglobulin fragment crystallizable region (Fc). The Fc region plays multiple roles in (i) dimerization for the formation of “Y”-shaped structure of Ig, (ii) Fc-mediated effector functions, (iii) extension of serum half-life, and (iv) a cost-effective purification tag. Plants and in particular Nicotiana benthamiana have proven to be suitable expression platforms for several recombinant therapeutic proteins. Despite the enormous success of their use for the production of full-length monoclonal antibodies, the expression of Fc-fused therapeutic proteins in plants has shown limitations. Many Fc-fusion proteins expressed in plants show different degrees of instability resulting in high amounts of Fc-derived degradation products. To address this issue, we used erythropoietin (EPO) as a reporter protein and evaluated the efforts to enhance the expression of full-length EPO-Fc targeted to the apoplast of N. benthamiana. Our results show that the instability of the fusion protein is independent from the Fc origin or IgG subclass and from the peptide sequence used to link the two domains. We also show that a similar instability occurs upon the expression of individual heavy chains of monoclonal antibodies and ScFv-Fc that mimic the “Y”-shape of antibodies but lack the light chain. We propose that in this configuration, steric hindrance between the protein domains leads to physical instability. Indeed, mutations of critical residues located on the Fc dimerization interface allowed the expression of fully stable EPO monomeric Fc-fusion proteins. We discuss the limitations of Fc-fusion technology in N. benthamiana transient expression systems and suggest strategies to optimize the Fc-based scaffolds on their folding and aggregation resistance in order to improve the stability.

scholarly journals Role of Vif in Stability of the Human Immunodeficiency Virus Type 1 Core

2000 ◽  
Vol 74 (23) ◽  
pp. 11055-11066 ◽  
Author(s):  
Åsa Öhagen ◽  
Dana Gabuzda
Keyword(s):  
Human Immunodeficiency Virus ◽  
Dna Synthesis ◽  
Virus Entry ◽  
Wild Type ◽  
The Core ◽  
Immunodeficiency Virus ◽  
The Stability ◽  
Hiv 1

ABSTRACT The Vif protein of human immunodeficiency virus type 1 (HIV-1) is important for virion infectivity. Previous studies have shown thatvif-defective virions exhibit structural abnormalities in the virus core and are defective in the ability to complete proviral DNA synthesis in acutely infected cells. We developed novel assays to assess the relative stability of the core in HIV-1 virions. Using these assays, we examined the role of Vif in the stability of the HIV-1 core. The integrity of the core was examined following virion permeabilization or removal of the lipid envelope and treatment with various triggers, including S100 cytosol, deoxynucleoside triphosphates, detergents, NaCl, and buffers of different pH to mimic aspects of the uncoating and disassembly process which occurs after virus entry but preceding or during reverse transcription.vif mutant cores were more sensitive to disruption by all triggers tested than wild-type cores, as determined by endogenous reverse transcriptase (RT) assays, biochemical analyses, and electron microscopy. RT and the p7 nucleocapsid protein were released more readily from vif mutant virions than from wild-type virions, suggesting that the internal nucleocapsid is less stably packaged in the absence of Vif. Purified cores could be isolated from wild-type but not vif mutant virions by sedimentation through detergent-treated gradients. These results demonstrate that Vif increases the stability of virion cores. This may permit efficient viral DNA synthesis by preventing premature degradation or disassembly of viral nucleoprotein complexes during early events after virus entry.

scholarly journals Isolation and Structural Characterization of Degradation Products of Aceclofenac by HPLC, HRMS and 2D NMR

2019 ◽  
Vol 31 (4) ◽  
pp. 851-854
Author(s):  
Santhosh Guduru ◽  
V.V.S.R.N. Anji Karun Mutha ◽  
B. Vijayabhaskar ◽  
Muralidharan Kaliyaperumal ◽  
Raghu Babu Korupolu ◽  
...  
Keyword(s):  
Degradation Product ◽  
Degradation Products ◽  
Acid Stress ◽  
2D Nmr ◽  
Stress Conditions ◽  
Preparative Hplc ◽  
Mass Spectral ◽  
2D Nmr Spectra ◽  
The Stability

The stability of aceclofenac under stress conditions was assessed to identify the degradation products. So, it was subjected to stress conditions like acid, base and oxidation, according to ICH guideline Q1A (R2). One degradation product formed when the drug was subjected to acid stress. Three degradation products were formed during the basic stress condition. The drug substance was found to be stable to oxidative stress. The degradants formed during the stress were separated on a C-18 column using gradient preparative HPLC elution. The only product (DP-2) formed during the acid stress and this one is same as of one of the three degradation products (DP-1, DP-2, DP-3) were formed during base stress. 1D and 2D NMR spectra and mass spectral analysis supported the proposed structures for the products. The products DP-2 and DP-3 have been reported earlier but this is the first report of product DP-1 as a degradation product of aceclofenac.

Development of Microemulsions Containing Carthamus tinctorius Extract for 5α-Reductase Inhibition

2019 ◽  
Vol 819 ◽  
pp. 92-97
Author(s):  
Sitthiphong Soradech ◽  
Khaunnapa Panapong ◽  
Surada Soonthornsatitwong ◽  
Somkamol Manchun ◽  
Sirinan Tubtimted ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Reductase Activity ◽  
Skin Permeation ◽  
Carthamus Tinctorius ◽  
Permeation Rate ◽  
Du145 Cells ◽  
Thai Medicinal Plants ◽  
The Stability ◽  
Stability Results

The purpose of this study was to develop micromeulsion consisting of Carthamus tinctorius floret extract (CT) as an ingredient to inhibit 5α-reductase activity. CT was extracted using a simple maceration technique with ethanol and inhibition of 5α-reductase activities was determined. Solutions of 2% CT extract were loaded into four microemulsion (ME) formulas (F1, F2, F3 and F4) and investigated for their physical properties, skin permeation and stability. Results showed that crude CT extract had no toxic effects on DU145 cells at concentrations of 0.0001-1.0 mg/mL. For reduction of 5α-reductase activities, concentration of CT extract at 0.05 mg/mL exhibited highest 5-reductase type-1 inhibition activity on the DU-145 cell line at 89.96% of the control, higher than standard finasteride (31.39%) and dutasteride (38.58%). The results indicated that a thermodynamically stable microemulsion improved the stability and permeation rate of CT extract. Among the ME formula, F3 was most appropriate for ME formulation with highest permeation rate and good stability during 30 days of storage. Therefore, using nanotechnology for stable transdermal delivery systems of bioactive compounds from Thai medicinal plants is one approach to improve skin and hair follicle permeation.

scholarly journals Development and Validation of a Novel Stability-Indicating Reversed-Phase Ion-Pair Chromatographic Method for the Quantitation of Impurities in Marbofloxacin Tablets

2018 ◽  
Vol 101 (4) ◽  
pp. 1021-1029
Author(s):  
Priyanka Maheshwari ◽  
Neelima Shukla ◽  
Manish Kumar Dare
Keyword(s):  
Mobile Phase ◽  
Chromatographic Method ◽  
Degradation Products ◽  
Reversed Phase ◽  
Ion Pair ◽  
Stress Conditions ◽  
Main Peak ◽  
Stability Indicating ◽  
Photolytic Degradation ◽  
The Stability

Abstract A stability-indicating isocratic reversed-phase ion-pair chromatographic method was designed for the separation of impurities in the presence of degradation products. Marbofloxacin tablets and a placebo were exposed to the stress conditions of oxidative, acid, base, humidity, thermal, and photolytic degradation. Significant and moderate degradation was observed in acidic and oxidative stress conditions, respectively. The degradation products were well resolved from the main peak and its impurities, thus proving the stability-indicating analytical method. The method was developed by using an XTerra RP18 3.5 μm (150 × 4.6 mm) column, with the mobile phase containing a mixture of buffer (pH 2.5)–methanol–glacial acetic acid (77 + 23 + 0.5, v/v). The flow rate of the mobile phase was 1.2 mL/min, with a column oven temperature of 40°C and a detection wavelength of 315 nm. The proposed method met Veterinary International Conference on Harmonization requirements and was successfully used for impurity quantitation in marbofloxacin tablets.

Stability-Indicating Liquid Chromatographic Procedure for Determination of Allantoin in Cosmetic Lotion

1988 ◽  
Vol 71 (2) ◽  
pp. 290-294
Author(s):  
Ramesh J Trivedi
Keyword(s):  
Degradation Products ◽  
Glyoxylic Acid ◽  
Uv Detector ◽  
Stability Indicating ◽  
Assay Procedure ◽  
Relative Standard ◽  
The Stability ◽  
Chromatographic Parameters ◽  
Liquid Chromatographic

Abstract A sensitive, specific liquid chromatographic (LC) procedure was developed for determination of allantoin [(2,5-dioxo-4--imidaazolidinyl) urea or 5-ureidohydantion] in cosmetic lotion. A reverse-phase, ionsuppression mechanism separated allantoin from interfering constituents of the sample matrix, and the compound was determined with a UV detector at 240 nm with a sensitivity limit of ((.20 mg/mL. The chromatographic parameters were optimized for retention time, efficiency, and relative response to the analyte. The assay procedure was validated with spiked laboratory-prepared samples at 100 ± 15% levels. An average recovery of 99.4% with a relative standard deviation of 1.5% (n = 7) was obtained. The stability-indicating characteristics of the method were established by recovery study (99.8%) of samples spiked with known degradation products (urea, allantoic acid, and glyoxylic acid).

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