scholarly journals Co-Amorphous Simvastatin-Nifedipine with Enhanced Solubility for Possible Use in Combination Therapy of Hypertension and Hypercholesterolemia

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2161 ◽  
Author(s):  
Cecilia Martínez-Jiménez ◽  
Jorge Cruz-Angeles ◽  
Marcelo Videa ◽  
Luz Martínez
Keyword(s):  
Combination Therapy ◽  
Amorphous State ◽  
Active Pharmaceutical Ingredient ◽  
Molar Ratio ◽  
Amorphous System ◽  
Enhanced Solubility ◽  
Significant Area ◽  
One Year ◽  
The Stability ◽  
Therapy Of Hypertension

The high index of simultaneous incidence of hypertension and hypercholesterolemia in the population of many countries demands the preparation of more efficient drugs. Therefore, there is a significant area of opportunity to provide as many alternatives as possible to treat these illnesses. Taking advantage of the solubility enhancement that can be achieved when an active pharmaceutical ingredient (API) is obtained and stabilized in its amorphous state, in the present work, new drug-drug co-amorphous formulations (Simvastatin SIM- Nifedipine NIF) with enhanced solubility and stability were prepared and characterized. Results show that the co-amorphous system (molar ratio 1:1) is more soluble than the pure commercial APIs studied separately. Aqueous dissolution profiles showed increments of solubility of 3.7 and 1.7 times for SIM and NIF, correspondingly, in the co-amorphous system. The new co-amorphous formulations, monitored in time, (molar fractions 0.3, 0.5 and 0.7 of SIM) remained stable in the amorphous state for more than one year when stored at room temperature and did not show any signs of crystallization when re-heating. Inspection on the remainder of a sample after six hours of dissolution showed no recrystallization, confirming the stability of co-amorphous system. The enhanced solubility of the co-amorphous formulations makes them promising for simultaneously targeting of hypertension and hypercholesterolemia through combination therapy.

scholarly journals Carbidopa Capsules for Insulinoma Diagnostic: Compounding and Stability Study

2020 ◽  
Vol 4 (3-4) ◽  
pp. 99-104
Author(s):  
Christophe Curti ◽  
Fanny Mathias ◽  
Morane Savelli ◽  
Philippe Garrigue ◽  
Edouard Lamy ◽  
...  
Keyword(s):  
Single Dose ◽  
Hospital Pharmacy ◽  
Room Temperature ◽  
Active Pharmaceutical Ingredient ◽  
Oral Formulation ◽  
Stability Study ◽  
Dose Administration ◽  
Disease Associations ◽  
One Year ◽  
The Stability

AbstractBackgroundCarbidopa is a drug mainly used to treat Parkinson’s disease. Associations with levodopa or with levodopa/entacapone are commercialized, but there is no oral formulation of carbidopa alone available in Europe. As carbidopa can also be used as premedication of adult patients for insulinoma diagnosis, it must be compounded as single dose mg capsules. The single dose administration of a magistral preparation implies the compounding of only one capsule, or the loss of consequent quantities of active pharmaceutical ingredient. As an alternative solution, carbidopa capsules could be compounded as batches of hospital preparation.MethodWith this objective, a stability-indicating dosing method for 200 mg carbidopa capsules was developed. Then, the compounding process was assessed according to the European Pharmacopeia requirements. Finally, the stability of carbidopa capsules stored protected from light at room temperature was studied for one year.Results200 mg carbidopa capsules compounding process was validated on three independent batches. The beyond use date was fixed at one year.ConclusionOur work confirms that carbidopa 200 mg capsules can be realized in hospital pharmacy and its stability allows the compounding of large batches.

Destabilizing the Structural Integrity of SARS-CoV2 Receptor Proteins by Curcumin Along with Hydroxychloroquine: An Insilco Approach for a Combination Therapy

2020 ◽  
Author(s):  
Akhileshwar Srivastava ◽  
Divya Singh
Keyword(s):  
Binding Energy ◽  
Combination Therapy ◽  
Receptor Binding ◽  
Structural Integrity ◽  
Binding Domain ◽  
Receptor Binding Domain ◽  
Receptor Proteins ◽  
Main Protease ◽  
The Stability ◽  
Therapeutic Activities

Presently, an emerging disease (COVID-19) has been spreading across the world due to coronavirus (SARS-CoV2). For treatment of SARS-CoV2 infection, currently hydroxychloroquine has been suggested by researchers, but it has not been found enough effective against this virus. The present study based on in silico approaches was designed to enhance the therapeutic activities of hydroxychloroquine by using curcumin as an adjunct drug against SARS-CoV2 receptor proteins: main-protease and S1 receptor binding domain (RBD). The webserver (ANCHOR) showed the higher protein stability for both receptors with disordered score (<0.5). The molecular docking analysis revealed that the binding energy (-24.58 kcal/mol) of hydroxychloroquine was higher than curcumin (-20.47 kcal/mol) for receptor main-protease, whereas binding energy of curcumin (<a>-38.84</a> kcal/mol) had greater than hydroxychloroquine<a> (-35.87</a> kcal/mol) in case of S1 receptor binding domain. Therefore, this study suggested that the curcumin could be used as combination therapy along with hydroxychloroquine for disrupting the stability of SARS-CoV2 receptor proteins

Evaluation of Mandibular Arch Width Changes following Fixed Retention in Post Orthodontic Patients - a Randomized Clinical Trial

2020 ◽  
Author(s):  
Nasreen Iqbal Nagani
Keyword(s):  
Stainless Steel ◽  
Steel Wire ◽  
P Value ◽  
Chi Square ◽  
Mandibular Arch ◽  
Arch Width ◽  
Orthodontic Patients ◽  
Mean Differences ◽  
One Year ◽  
The Stability

Background: Retention is an integral phase in which teeth are maintained in their newly adapted position for which retainers are inserted. Retainers are generally of two types: removable and fixed. Fixed retainers are indicated in the mandibular arch for an indefinite period specifically in the non-extraction cases. Changes in intercanine and intermolar widths are valuable parameters to evaluate the stability. The objectives of this study were to assess and compare the mandibular intercanine and intermolar width changes following orthodontic treatment after insertion of two types of fixed lingual retainers for one year. Methods: Total 54 subjects were recruited in which two types of fixed lingual retainers were inserted in the mandibular arch randomly. Intercanine and intermolar arch widths were measured by digital caliper of 0.01 mm accuracy. Data was analyzed by using Statistical Package of Social Sciences (SPSS V-21). Chi-square and independent t tests were used to compare baseline characteristics. Intercanine and intermolar widths were assessed and compared using independent t test, p-value ≤ 0.05 is considered as statistically significant. Results: Intercanine width increased from baseline to T4 in both retainers. When mean differences of intercanine width were compared between two retainers significant differences were observed at T1, T2, T3 and T4 with significant p-values (< 0.05) and increased intercanine width with multistranded stainless steel wire (MSW) retainers. Conclusion: Mandibular intercanine width increases significantly in post retention phase with multistranded stainless steel retainers. Thus, fiber reinforced composite retainers are more effective in preserving the arch width changes.

scholarly journals Effects of serpentinite fertilizer on the chemical properties and enzyme activity of young spruce soils

2016 ◽  
Vol 30 (4) ◽  
pp. 401-414 ◽  
Author(s):  
Ewa Błońska ◽  
Kazimierz Januszek ◽  
Stanisław Małek ◽  
Tomasz Wanic
Keyword(s):  
Enzyme Activity ◽  
Chemical Properties ◽  
Molar Ratio ◽  
Tree Roots ◽  
Forest Zone ◽  
Negative Effect ◽  
Phosphorus And Potassium ◽  
One Year ◽  
Nitrogen Phosphorus ◽  
Experimental Plots

AbstractThe experimental plots used in the study were located in the middle forest zone (elevation: 900-950 m a.s.l.) on two nappes of the flysch Carpathians in southern Poland. The aim of this study was to assess the effects of serpentinite in combination with nitrogen, phosphorus, and potassium fertilizers on selected chemical properties of the soil and activity of dehydrogenase and urease in the studied soils. All fertilizer treatments significantly enriched the tested soils in magnesium. The use of serpentinite as a fertilizer reduced the molar ratio of exchangeable calcium to magnesium, which facilitated the uptake of magnesium by tree roots due to competition between calcium and magnesium. After one year of fertilization on the Wisła experimental plot, the pH of the Ofh horizon increased, while the pH of the mineral horizons significantly decreased. Enrichment of serpentinite with nitrogen, phosphorus, and potassium fertilizers stimulated the dehydrogenase activity in the studied organic horizon. The lack of a negative effect of the serpentinite fertilizer on enzyme activity in the spruce stand soil showed that the concentrations of the heavy metals added to the soil were not high enough to be toxic and indicated the feasibility of using this fertilizer in forestry.

scholarly journals Charge Transfer Complexes of Ketotifen with 2,3-Dichloro-5,6-dicyano-p-benzoquinone and 7,7,8,8-Tetracyanoquodimethane: Spectroscopic Characterization Studies

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 2039
Author(s):  
Gamal A. E. Mostafa ◽  
Ahmed Bakheit ◽  
Najla AlMasoud ◽  
Haitham AlRabiah
Keyword(s):  
Charge Transfer ◽  
Spectroscopic Characterization ◽  
Molar Ratio ◽  
Charge Transfer Complexes ◽  
Physical Parameters ◽  
Spectrophotometric Methods ◽  
Theoretical Approaches ◽  
The Stability ◽  
Ct Complexes

The reactions of ketotifen fumarate (KT) with 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ) and 7,7,8,8-tetracyanoquinodimethane (TCNQ) as π acceptors to form charge transfer (CT) complexes were evaluated in this study. Experimental and theoretical approaches, including density function theory (DFT), were used to obtain the comprehensive, reliable, and accurate structure elucidation of the developed CT complexes. The CT complexes (KT-DDQ and KT-TCNQ) were monitored at 485 and 843 nm, respectively, and the calibration curve ranged from 10 to 100 ppm for KT-DDQ and 2.5 to 40 ppm for KT-TCNQ. The spectrophotometric methods were validated for the determination of KT, and the stability of the CT complexes was assessed by studying the corresponding spectroscopic physical parameters. The molar ratio of KT:DDQ and KT:TCNQ was estimated at 1:1 using Job’s method, which was compatible with the results obtained using the Benesi–Hildebrand equation. Using these complexes, the quantitative determination of KT in its dosage form was successful.

scholarly journals Comparison between selective caudal fixed screw construct and all variable screw construct in anterior cervical discectomy and fusion

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Jae Jun Yang ◽  
Sehan Park ◽  
Seongyun Park
Keyword(s):  
Fusion Rate ◽  
Anterior Cervical Discectomy ◽  
Disc Space ◽  
Cervical Discectomy ◽  
Locking Mechanism ◽  
Adjacent Disc ◽  
One Year ◽  
The Stability ◽  
Retrospective Comparative Study ◽  
Caudal Level

AbstractThis retrospective comparative study aimed to compare the efficacy of selective caudal fixed screw constructs with all variable screw constructs in anterior cervical discectomy and fusion (ACDF). Thirty-five patients who underwent surgery using selective caudal fixed screw construct (SF group) were compared with 44 patients who underwent surgery using all variable constructs (AV group). The fusion rate, subsidence, adjacent level ossification development (ALOD), adjacent segmental disease (ASD), and plate-adjacent disc space distance were assessed. The one-year fusion rates assessed by computed tomography bone bridging and interspinous motion as well as the significant subsidence rate did not differ significantly between the AV and SF groups. The ALOD and ASD rates and plate-adjacent disc space distances did not significantly differ between the two groups at both the cranial and caudal adjacent levels. The number of operated levels was significantly associated with pseudarthrosis in the logistic regression analysis. The stability provided by the locking mechanism of the fixed screw did not lead to an increased fusion rate at the caudal level. Therefore, the screw type should be selected based on individual patient’s anatomy and surgeon’s experience without concern for increased complications caused by screw type.

Does perianal disease influence the efficacy of combination therapy in Crohn’s disease?

2020 ◽  
Author(s):  
Rui de Sousa Magalhães ◽  
Sofia Xavier ◽  
Tiago Cúrdia Gonçalves ◽  
Francisca Dias de Castro ◽  
Bruno Rosa ◽  
...  
Keyword(s):  
Combination Therapy ◽  
Clinical Remission ◽  
Odds Ratio ◽  
Perianal Disease ◽  
Outcome Variable ◽  
P Value ◽  
Disease Relapse ◽  
Endoscopic Remission ◽  
Remission Rates ◽  
One Year

Background: Perianal disease is associated with a disabling course of CD. We aim to study the impact of perianal disease on CD remission rates, after a one-year course of infliximab in combination therapy with azathioprine. Methods: Cohort, retrospective, single centre study, including consecutive CD patients on combination therapy, followed for one year since induction. The outcome variable was split into clinical and endoscopic remission. The correlation towards the outcome variable was assessed with univariate and multivariate analysis, and a survival assessment, using SPSS software. Results: We assessed 74 CD patients, of whom 41 (55.4%) were female, with a mean age of 36 years-old. Thirty-nine percent of the patients presented perianal disease at diagnosis (n=29). We documented 70.3% clinical and 47.2% endoscopic remissions. Several variables had statistical significance towards the outcomes (endoscopic and clinical remission) in the univariate analysis. After adjusting for confoundment, patients with perianal disease presented an odds ratio of 0.20 for achieving endoscopic remission (odds ratio 0.201 CI [0.054-0.75] p-value 0.017) and an odds ratio of 0.203 for achieving clinical remission (OR 0.203 CI [0.048-0.862] p-value 0.031). Sixty-six patients (89.2%) presented an initial response to treatment, from whom, 20 (30.3%) exhibited at least one disease relapse (clinical and/or endoscopic). Patients with perianal disease presented higher probability of disease relapse, displaying statistically significant difference on Kaplan-Meyer curves (Breslow p-value 0.043). Conclusion: In the first year of combination therapy, perianal disease is associated with an 80% decrease in endoscopic and clinical remission rates and higher ratio of disease relapse.

Do Current Measures of Dimensions of Source Credibility Produce Stable Outcomes in Replicated Tests?

1995 ◽  
Vol 81 (2) ◽  
pp. 675-687 ◽  
Author(s):  
F. C. Powell ◽  
J. W. Wanzenried
Keyword(s):  
University Students ◽  
Source Credibility ◽  
Hillary Clinton ◽  
George Bush ◽  
Credibility Scale ◽  
One Year ◽  
The Stability

Over a period of one year, data were obtained from four groups of university students to compare the stability of scores on the McCroskey and Jenson Source Credibility Scale and the Leathers Personal Credibility Scale in repeated tests. Using pre- and posttest scores, perceptions of President Clinton were obtained at four intersections while perceptions of Hillary Clinton, Jerry Brown, George Bush, and Ross Perot were obtained on a single date. The two scales used in the test yield approximate explanations of variance and coefficients a across the 16 analyses. The results suggest that current conceptualization and measurement of source credibility do not provide consistent dimensions on repeated tests.

Dronedarone HCl—Quercetin Co-Amorphous System: Characterization and RP—HPLC Method Development for Simultaneous Estimation

2021 ◽  
Author(s):  
Navya Sree K S ◽  
Swapnil J Dengale ◽  
Srinivas Mutalik ◽  
Krishnamurthy Bhat
Keyword(s):  
Method Development ◽  
Hplc Method ◽  
Molar Ratio ◽  
Simultaneous Estimation ◽  
Content Uniformity ◽  
Amorphous System ◽  
Simultaneous Quantification ◽  
Linearity Range ◽  
Rp Hplc ◽  
Economic Method

Abstract Background Dronedarone HCl is an anti-arrhythmic drug indicated for atrial fibrillation. Dronedarone HCl(DRN) has a low solubility of 2 µg/mL and 4% bioavailability, thus it is formulated as co-amorphous system to enhance its solubility by using Quercetin(QCT) as coformer. Literature lacks a sensitive, accurate and economic method for simultaneous quantification of DRN and QCT in formulation. Objective To develop a RP-HPLC method for simultaneous estimation of DRN and QCT in DRN-QCT co-amorphous system. Method Co-amorphous system was prepared using solvent evaporation technique using DRN and QCT in 1:1 molar ratio. The separation was achieved on Purospher® STAR C18 (250 mm × 4.6 mm × 5 μm) column with mobile phase comprising of Acetonitrile and 25 mM phosphate buffer pH 3.6 (60:40, % v/v). Results DRN and QCT retained at 6.7 and 3.5 min, respectively. For both molecules, method was developed with a wide linearity range of 0.2–500 µg/mL. LOD for DRN was found to be 0.0013 and 0.0026 µg/mL for QCT. Also, LOQ for DRN was found to be 0.0041 and 0.0078 µg/mL for QCT. Conclusion Method was validated as per ICHQ2R1 guidelines for linearity, precision, accuracy, and robustness. The method was used in simultaneous quantification of DRN and QCT in co-amorphous samples. Highlights The method developed was used for the analysis of content uniformity and solubility samples of co-amorphous system, where the method was able to successfully quantify DRN and QCT. Low detection and quantification limits contribute to sensitivity of the method and wide linearity range assures the robust and precise quantification of molecules.

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