scholarly journals Development of the composition and technology of a combined gel for the treatment of osteoarthritis with a pharmacological rationale for the content of components

2021 ◽  
Vol 10 (4) ◽  
pp. 69-78
Author(s):  
U. V. Nogaeva ◽  
Ju. M. Kotsur ◽  
E. V. Flisyuk ◽  
D. Yu. Ivkin ◽  
E. D. Semivelichenko ◽  
...  

Introduction. Osteoarthritis (OA) is the most common joint disease that affects more than 10 % of the world's population. More than 600 000 people are diagnosed for the first time each year, but these data do not reflect the true prevalence of the disease, since not all patients seek help from hospitals [1, 2].Aim. Pharmaceutical development of the composition and technology of a gel based on meloxicam, a purine derivative and an immunomodulating component for the treatment of OA with pharmacological substantiation of the content of active substances.Materials and methods. A combination of three active pharmaceutical substances was studied: a non-steroidal anti-inflammatory drug – meloxicam, a purine derivative and an original immunomodulator M. Sodium alginate, natrozole and xanthan gum were considered as gelling agents. Were identified two technological modes of obtaining a gel base. The concentrations of active substances were selected based on the results of preclinical studies. OA was modeled by the combined administration of 0.1 ml of a mixture of Freund's complete adjuvant with a 10 % talc suspension in isotonic sodium chloride solution in a ratio of 1 : 10 into the hock (tarsus) joint cavity. The criteria for choosing the optimal composition of the gel were the size of the damaged joint, exercise tolerance and the histological picture in comparison with intact and control animals. For quantitative data, sample mean values (M) and standard deviations (SD) were calculated. The results corresponded to the laws of normal distribution, statistical processing was carried out using one-way analysis of variance (One-Way ANOVA) using the GraphPad Prism 8.0.2 software, USA at the level of statistical significance of differences p < 0,05 и p < 0,001.Results and discussion. The composition was developed and the technology of the topical dosage form based on sodium alginate was proposed. Preclinical data indicate that the highest efficacy is achieved when using a formulation containing 3 % purine derivative, 5 % immunomodulator M and 0.5 % meloxicam. The developed composition for the effectiveness of suppressing the symptoms of OA showed results that exceeded the reference drug.Conclusion. An original combined agent for the treatment of OA has been developed. Due to the selected component composition, with greater efficiency, it was possible to reduce the dosage of meloxicam to 0.5 %, and the use of sodium alginate as a gelling agent contributed to the prolongation of the action of the gel and the subsequent reduction in the number of applications.

Author(s):  
Thomaz R. Mostardeiro ◽  
Ananya Panda ◽  
Robert J. Witte ◽  
Norbert G. Campeau ◽  
Kiaran P. McGee ◽  
...  

Abstract Purpose MR fingerprinting (MRF) is a MR technique that allows assessment of tissue relaxation times. The purpose of this study is to evaluate the clinical application of this technique in patients with meningioma. Materials and methods A whole-brain 3D isotropic 1mm3 acquisition under a 3.0T field strength was used to obtain MRF T1 and T2-based relaxometry values in 4:38 s. The accuracy of values was quantified by scanning a quantitative MR relaxometry phantom. In vivo evaluation was performed by applying the sequence to 20 subjects with 25 meningiomas. Regions of interest included the meningioma, caudate head, centrum semiovale, contralateral white matter and thalamus. For both phantom and subjects, mean values of both T1 and T2 estimates were obtained. Statistical significance of differences in mean values between the meningioma and other brain structures was tested using a Friedman’s ANOVA test. Results MR fingerprinting phantom data demonstrated a linear relationship between measured and reference relaxometry estimates for both T1 (r2 = 0.99) and T2 (r2 = 0.97). MRF T1 relaxation times were longer in meningioma (mean ± SD 1429 ± 202 ms) compared to thalamus (mean ± SD 1054 ± 58 ms; p = 0.004), centrum semiovale (mean ± SD 825 ± 42 ms; p < 0.001) and contralateral white matter (mean ± SD 799 ± 40 ms; p < 0.001). MRF T2 relaxation times were longer for meningioma (mean ± SD 69 ± 27 ms) as compared to thalamus (mean ± SD 27 ± 3 ms; p < 0.001), caudate head (mean ± SD 39 ± 5 ms; p < 0.001) and contralateral white matter (mean ± SD 35 ± 4 ms; p < 0.001) Conclusions Phantom measurements indicate that the proposed 3D-MRF sequence relaxometry estimations are valid and reproducible. For in vivo, entire brain coverage was obtained in clinically feasible time and allows quantitative assessment of meningioma in clinical practice.


Author(s):  
Anna A. Romanyuk ◽  
Dmitry V. Moiseev

Objective: generalization and analysis of scientific data on the component composition, pharmacological properties and standardization of senna leaves. Materials and methods. The article provides an overview of scientific publications in the journals of the search platforms Scopus and PubMed, as well as the databases of the Russian Science Citation Index. The analysis of the range of herbal medicinal products was carried out according to the data of the State Registers of Medicines of the Republic of Belarus, the Russian Federation and the Republic of Kazakhstan using content analysis, comparison and generalization of data. Results. In addition to the laxative effect, determined by the presence of anthracene derivatives in senna leaves, the complex of their biologically active substances has antimicrobial, hypoglycemic, antioxidant, antifungal and antitumor effects. Also, the chemical composition of the plant is represented by fatty acids, triglycerides, flavonoids, macro- and microelements. The analysis of medicinal herbal preparations based on senna leaves registered in the Russian Federation, the Republic of Belarus and the Republic of Kazakhstan has been carried out. The differences in the methods of their standardization, given in the normative documentation on quality, have been revealed. The scientific experience of using the method of high performance liquid chromatography for the determination of anthracene derivatives in senna leaves is generalized. Conclusion. The complex of biologically active substances of senna leaves exhibits various pharmacological effects, which, possibly, will expand the range of combined preparations based on them. The use of a modern and selective method of high-performance liquid chromatography in the analysis of senna leaves is a very promising direction in the field of standardization of this type of medicinal plant material.


Materials ◽  
2021 ◽  
Vol 14 (19) ◽  
pp. 5483
Author(s):  
Enrico Storti ◽  
Marc Neumann ◽  
Tilo Zienert ◽  
Jana Hubálková ◽  
Christos Georgios Aneziris

Full metal-ceramic composite beads containing different amounts of niobium and alumina, particularly 100 vol% alumina, 100 vol% niobium, and 95/5 vol% niobium/alumina, were produced by the alginate gelation process. The suspension for bead fabrication contained sodium alginate as gelling agent and was added dropwise into a calcium chloride solution to trigger the consolidation process. After debinding in air, sintering of the composite beads was performed under inert atmosphere. Samples in green and sintered state were analyzed by digital light microscopy and scanning electron microscopy equipped with energy dispersive X-ray spectroscopy. Investigations by mercury intrusion porosimetry revealed that pure alumina beads featured smaller pores compared to composite beads, although the open porosities were comparable. The fracture strength was evaluated on single beads. Contrary to the pure alumina, the composite beads showed a clear plastic deformation. Pure niobium beads showed a ductile behavior with very large deformations. XRD analyses revealed the presence of calcium hexaluminate and beta-alumina as minor phases in the alumina beads, while the composite ones contained about 25 wt% of impurities. The impurities comprised NbO arising from the oxidation, and β-Nb2C, from the reaction with the residual sodium alginate.


2013 ◽  
Vol 6 (6) ◽  
pp. 10117-10163 ◽  
Author(s):  
P. R. Colarco ◽  
R. A. Kahn ◽  
L. A. Remer ◽  
R. C. Levy

Abstract. We use the Moderate Resolution Imaging Spectroradiometer (MODIS) satellite aerosol optical thickness (AOT) product to assess the impact of reduced swath width on global and regional AOT statistics and trends. Ten different sampling strategies are employed, in which the full MODIS dataset is sub-sampled with various narrow-swath (~400–800 km) and curtain-like (~10 km) along-track configurations. Although view-angle artifacts in the MODIS AOT retrieval confound direct comparisons between averages derived from different sub-samples, careful analysis shows that with many portions of the Earth essentially unobserved, the AOT statistics of these sub-samples exhibit significant regional and seasonal biases. These AOT spatial sampling artifacts comprise up to 60% of the full-swath AOT value under moderate aerosol loading, and can be as large as 0.1 in some regions under high aerosol loading. Compared to full-swath observations, narrower swaths exhibit a reduced ability to detect AOT trends with statistical significance, and for curtain-like sampling we do not find any statistically significant decadal-scale trends at all. An across-track sampling strategy obviates the MODIS view angle artifact, and its mean AOT converges to the full-swath mean values for sufficiently coarse spatial and temporal aggregation. Nevertheless, across-track sampling has significant seasonal-regional sampling artifacts, leading to biases comparable to the curtain-like along-track sampling, lacks sufficient coverage to assign statistical significance to aerosol trends, and is not achievable with an actual narrow-swath or curtain-like instrument. These results suggest that future aerosol satellite missions having significantly less than full-swath viewing are unlikely to sample the true AOT distribution well enough to determine decadal-scale trends or to obtain the statistics needed to reduce uncertainty in aerosol direct forcing of climate.


Author(s):  
Sanket Kumar ◽  
Mahesh Singh ◽  
Babulal Patel

Peptic ulcer, it is the most common type of stomach disease, according to the American Gastroenterology Association. “We know that ulcers occur because there has been a disruption in the balance of factors that injure the digestive tract and those factors that protect it from injury,” The present investigation deal with the formulation, optimization and evaluation of sodium alginate based in situ gel of ranitidine hydrochloride (R-HCl) in ulcer treatment. The in-situ formulation are homogenous liquid when administration orally and become gel at the contact site. The evaluation of the formulation is dependent upon accurate results obtained by analytical method used during the study. Accurate results require the use of standard and a calibration procedure. Hence, standard plots of Ranitidine hydrochloride were prepared in (0.1N HCL, pH 1.2) solutions. Two, sodium alginate and calcium carbonate used as a polymer and cross-linking agent respectively in the formulation of in-situ gel. From the IR studies it may be concluded that the drug and carriers used undergo physical interaction there is no chemical change, and thus the gelling agent, cross-linking agent and other excipient is suitable for formulation of in-situ gel of ranitidine hydrochloride. Indicate that the formulation, DKF9 which was prepared by the Sodium alginate (2 gm) with Ranitidine Hydrochloride showed minimum drug release (sustained drug release) after 8 hrs. It can be concluded that the In-situ gel was beneficial for delivering the drug which needs sustained release to achieve the slow action. Keywords: In-situ gel, Peptic Ulcer, Ranitidine Hydrochloride (R-HCl), Sodium alginate.


2020 ◽  
Vol 21 (2) ◽  
pp. 254-262
Author(s):  
Koval Inna

The content, component composition, and main directions of the use of monoterpenes of wild rose petals compounds are considered in the research. The study on six wild rose species was carried out in the collection of M.M. Gryshko National Botanical Garden of the National Academy of Sciences of Ukraine. Volatile organic compounds were isolated by steam distillation, and their determination was performed by means of gas chromatography. R. rugosa petals contained the highest number of monoterpenoids, while R. canina petals – the lowest. In our research twentyone different (acyclic, monocyclic, bicyclic) monoterpenoids were identified, including alcohols, aldehydes, ethers, and ketones. All groups of monoterpenoids are biologically active substances and have a significant effect on the aroma of the studied plants.


2020 ◽  
Vol 100 (4) ◽  
pp. 52-59
Author(s):  
А.S. Kishkentayeva ◽  
◽  
S.N. Mantler ◽  
М.М. Zhakanov ◽  
S.М. Adekenov ◽  
...  

The review summarizes data on biologically active compounds of Achillea nobilis L. and methods of their isolation. From Achillea nobilis L., collected in different places of growth, the following have been isolated: essential oil, the main components of which are monoterpene compounds; sesquiterpene lactones estafiatin, hanphyllin, anobin, chrysartemine A, canin, anolide and tanapartin-β-peroxide; the steroid acetyleucanbin; flavonoids: 3,5-dihydroxy-6,7,8-trimethoxyflavone, 5-hydroxy-3,6,7,4’-tetramethoxyflavone and 5,3’-di-hydroxy-3,6,7,4’-tetramethoxyflavone. It has been determined that the component composition of the essen-tial oil of Achillea nobilis L. largely depends on the soil and climatic factors in the places of its growth, the phase of the growing season and the method of its extraction from plant raw materials, and the extractant used (chloroform, ethanol, hot water, diethyl ether). Antibacterial, antimicrobial, antioxidant, antiparasitic activi-ties are characteristic both for the sums of extractive substances from Achillea nobilis L. and for individual compounds isolated from them. Methods for the isolation of biologically active substances from Achillea nobilis L. for the development of new drug substances are described. The main aim of this work was a com-parative analysis of the available research results on the phytochemical study of Achillea nobilis L.


2011 ◽  
Vol 10 (5) ◽  
pp. 86-90
Author(s):  
N. A. Pulina ◽  
A. I. Krasnova ◽  
F. V. Sobin ◽  
T. A. Yushkova ◽  
V. V. Yushkov

The paper deals with directed synthesis and study of hypoglycemic activity of N-heterylamides of 4-aryl-2-hydroxy-4-oxo-2- butenoic and 4-aryl-3-bromo-2, 4-dioxobutanoic acids. Hypoglycemic activity of 28 compounds was under research. Some regularities of the influence of the heterocyclic moiety structure and the bromine atom on the activity of the compounds were obtained. Two low-toxic and highly active substances comparable in potency with the reference drug were identified.


2021 ◽  
Vol 28 (10) ◽  
pp. 1513-1518
Author(s):  
Munawar Aziz Khattak ◽  
Sana Arbab ◽  
Syed Amjad Shah

Objective: To determine the frequency of the number of roots and root canals in a sample of 250 extracted maxillary first premolar teeth of patients visiting Peshawar Dental College and Hospital Khyber Pakhtunkhwa. Study Design: Cross Sectional. Setting: Department of Oral Biology, Peshawar Dental College and Hospital Khyber Pakhtunkhwa. Period: April 2016 to December 2016. Material & Methods: A total of 250 extracted human maxillary first premolars were collected from the Department of Oral & Maxillofacial Surgery, Peshawar Dental College, and Hospital Khyber Pakhtunkhwa. All teeth were visually inspected to count the number of roots. Subsequently, the access cavity was prepared, and pulp extirpated from each tooth. Endodontic explorer was used to locating the canal orifice(s) at the pulp chamber floor. Later the root canal orifices were injected with India ink to stain the canals. After that roots of teeth were sectioned at different levels to note down the number of canals. Data were analyzed using SPSS version 19. The statistical significance of the variations from mean values was considered significant if the p-value was less than 0.05. Results: Out of 250 maxillary first premolar teeth, 44.8% had one root, 40.4% had two separate and 12.8% had two fused roots. Three roots were seen in 2.0% teeth. Two root canals were present in the vast majority (70.4%), whereas one and three root canals were seen in 27.6% and 2.0% teeth, respectively. The correlation between the number of roots and root canals of maxillary first premolar teeth was highly significant. Conclusions: There was a high frequency of maxillary first premolars with two roots and two root canals.


2019 ◽  
Vol 44 (1) ◽  
pp. 6-12
Author(s):  
Natacha Oyarzo ◽  
María Riveros ◽  
Constanza Andaur ◽  
Jessica Liberona ◽  
Víctor Cortés

Background: diabetes and periodontitis are common comorbidities; however, the clinical implications of this association remain only partially known. This study was aimed to characterize the periodontal status of type 2 diabetic (T2D) patients and its correlation with metabolic and inflammatory parameters. Methods: patients (n = 30) with 5 or less years since the diagnosis of T2D (18 – 65 years old) were recruited. Anthropometric (Body Mass Index, BMI), metabolic (fasting glucose, glycated hemoglobin, insulin, HOMA-IR, HDL, LDL and total cholesterol, triglycerides) and inflammatory parameters (ultrasensitive C reactive protein, usCRP) were quantified. Periodontal evaluation included clinical attachment level (CAL), probing depth (PD), gingival level (GL) and bleeding on probing (BOP) average. Statistical significance was assessed by Mann-Whitney and Spearman correlation tests. Results: mean values of BOP, CAL, PD and GL were 39.3, 2.8, 2.8, and 0.1, respectively. BOP significantly correlated with BMI and HOMA-IR and was higher in patients with elevated usCRP >3 mg/L (p<0.05). Age and duration of T2D directly and inversely correlated with CAL and GL, respectively. BOP correlated with HOMA-IR and usCRP but not with patients´age, duration of T2D or BMI. Conclusions: in patients with recent diagnosis of T2D, BOP is associated with usCRP and HOMA-IR levels, suggesting that periodontal inflammation promotes insulin resistance possibly by increasing systemic inflammation.


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