scholarly journals Standardization of the Pharmaceutical Substance of the Drug LCS-1208

2021 ◽  
Vol 10 (3) ◽  
pp. 88-94
Author(s):  
E. V. Ignateva ◽  
I. V. Yartseva ◽  
Z. S. Shprakh ◽  
A. P. Bud'ko ◽  
L. V. Ektova ◽  
...  

Introduction. Indolocarbazole derivatives are of increasing scientific interest for practical oncology. A number of N-glycosides, indolo[2,3-a] carbazole under the laboratory code LCS, were synthesized in the laboratory of chemical synthesis of the National Medical Center of Oncology named after N.N. Blokhin. Currently, one of the most promising compounds in this class is LCS-1208, a representative of the arabinoside class of indolo [2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione. According to the mechanism of biological action, LCS-1208 is a protein kinase C inhibitor and is of great interest for the treatment of malignant neoplasms.Aim. chemical and pharmaceutical standardization of the pharmaceutical substance LCS-1208.Materials and methods. Laboratory samples of pharmaceutical substance LCS-1208. Methods of investigation: gravimetry, spectrophotometry, polarimetry, high-performance liquid chromatography (HPLC), high-resolution nuclear magnetic resonance (NMR) spectroscopy and infrared (IR) spectroscopy.Results and discussion. The quality assessment of LCS-1208 was carried out according to the indicators adopted in the XIV edition of the State Pharmacopoeia of the Russian Federation for quality control of pharmaceutical substances. LCS-1208 - orange amorphous powder, odorless; soluble in dimethylsulfoxide (DMSO) and dimethylformamide (DMF); very slightly soluble in 95 % ethyl alcohol and practically insoluble in water. The authenticity of the substance is confirmed by NMR and IR spectra, as well as electronic absorption spectra. The values of the specific optical rotation of LCS-1208 (1 % solution in DMF) are placed in the range from +58° to +61°. All the studied samples of the substance were free of inorganic impurities, sulphate ash, heavy metals and contained no more than 1.0 % water, determined by the K. Fischer titration method. The content of possible related impurities in the substance LCS-1208 and the content of the main active substance were determined by HPLC. The studied laboratory series of the pharmaceutical substance LCS-1208 contained no more than 1.0 % of any single and no more than 3 % of the total unidentified impurities. The content of the main active substance was more than 97 %.Conclusion. As a result of the work carried out, quality criteria and parameters were selected and methods for their determination were developed, which allow to adequately assess the quality and standardness of the pharmaceutical substance LCS-1208.

2020 ◽  
Vol 22 (Supplement_3) ◽  
pp. iii386-iii386
Author(s):  
Nune Karapetyan ◽  
Samvel Danielyan ◽  
Gevorg Tamamyan ◽  
Armen Tananyan ◽  
Liana Safaryan ◽  
...  

Abstract BACKGROUND Central nervous system (CNS) tumors are the second most common malignant neoplasms among children worldwide. The current paper aims to analyze the situation in pediatric neuro-oncology in Armenia from the neurosurgical perspective. METHODS We have collected data of pediatric patients with CNS tumors treated in the Neurosurgery department of “Surb Astvasamayr” Medical Center from 01.01.2010 till 01.12.2019. Incidence by gender, age at diagnosis, and histopathology results were calculated. Survival rates were calculated based on the follow-up results performed until 30.12.2019. RESULTS Hospital-based data showed that during the previous 10 years 47 patients with CNS tumors received neurosurgical treatment in the unit, among them 66% were females. 38.3%, 31.9% and 29.8% of diagnosed patients were aged 0–4, 5–9, and 10–18 respectively. In 41 cases, the disease was not disseminated at diagnosis. The most common observed malignancies were low-grade gliomas (21.3%) and embryonal tumors (19.1%), followed by high-grade gliomas (14.9%) and ependymal tumors (8.5%). Follow-up information only for 33 patients is available. From them, 14 are dead and 19 alive. Survival rates in most common groups were 62.5%, 80%, 50%, and 50% respectively. The median follow-up time was 18 months (range 1–113 months). CONCLUSION Similar to the data reported in the literature, low-grade gliomas, and embryonal tumors are the most frequent pediatric CNS tumors in Armenia. On the other hand, the pediatric CNS tumor survival rates are lower compared to those reported in developed countries.


2020 ◽  
Vol 10 (4) ◽  
pp. 301-307
Author(s):  
Ekaterina V. Kul’chavenya ◽  
Denis P. Kholtobin ◽  
Alexander I. Neymark

Introduction. In March 2020, the World Health Organization declared the outbreak of the novel coronavirus infection (COVID-19) a pandemic. The pandemic also significantly affected all academic, scientific and educational activities. Material and methods. We compared the work of the urological departments of the private (Medical Center Avicenna, Novosibisk) and municipal (City Clinical Hospital No. 11, Barnaul) clinics, as well as the urogenital department of the Novosibirsk Research Institute of Tuberculosis of the Ministry of Healthcare of Russia for 6 months of calm 2019, and the first half of 2020, which coincided with the start of the COVID-19 coronavirus pandemic. Results. In March 2020, the urogenital department of the Novosibirsk Research Institute of Tuberculosis of the Ministry of Healthcare of Russia was redesigned into an observational one. In the first half of 2020, patients with malignant neoplasms, varicocele, chronic pyelonephritis, hydronephrosis, dropsy of the testicular membranes and with phimosis/paraphimosis were admitted to the urology department of the City Hospital No. 11 in Barnaul in the first half of 2020. On the contrary, statistically significant in 2020 the number of patients admitted for kidney abscess and acute prostatitis prevailed. It can be assumed that, due to the tense epidemic situation, patients postponed seeking medical attention until their condition required emergency intervention. In the Medical Center Avicenna (Novosibirsk) in the first half of 2020 the number of visits to the pediatric urologist significantly decreased, the inpatient and average bed-day decreased. On the contrary the total duration of the patients' stay in the day hospital has significantly increased, which is logically explained by the epidemic situation; there was a statistically significant decrease in the number of most operations and outpatient procedures. Conclusion. The new coronavirus infection has affected all spheres of human life, to a maximum extent on medicine. In the first six months, no unified approaches to the management of urological patients in epidemic conditions were developed; clinics worked according to internal standards. Our analysis showed that strict adherence to sanitary and hygienic standards and the implementation of anti-epidemic measures allows us to provide urological care to patients in full-even in such unfavorable conditions.


1976 ◽  
Vol 143 (2) ◽  
pp. 422-436 ◽  
Author(s):  
M E Pereira ◽  
E A Kabat

The purified lectins from Lotus tetragonolobus and Dolichos biflorus were coupled to Sepharose 2B to make insoluble adsorbents for purification and fractionation of blood group A and H active glycoproteins. With both adsorbents, hog gastric mucin A + H blood substance (HGM), purified by phenol-ethanol precipitation, yielded fractions showing only A, only H, or AH activities. The AH fraction was obtained when the adsorbent column was overloaded with HGM and its A and H specificities seem to be carried on the same molecules since they were not separable by chromatography on either column. However A and H specificities of blood group substance from the stomach of a presumably heterozygous individual hog were both on the same molecules as they too could not be fractionated on either column. Analytical properties of the isolated fractions were generally similar to those of the unfractionated material, the purfied A substances had a higher galactosamine/fucose ratio than did the H substances. Although the original A + H showed very little specific optical rotation, the separated A and H substances rotated positively and negatively, respectively. The lectin-Sepharose adsorbents have also proven useful in isolating A or H substances directly from the crude commercial hog gastric mucin. Blood group A2 substance from a human ovarian cyst yielded two fractions on the Lotus-Sepharose column; the effluent did not interact with the Lotus lectin but precipitated the Ulex and Dolichos lectins and anti-A, and appears to contain type 1 H determinants. The other fraction reacted with Lotus and Ulex lectin as well as with Dolichos and anti-A.


1975 ◽  
Vol 58 (3) ◽  
pp. 585-594
Author(s):  
Stanley R Ames ◽  
Emma-Jane E Drury

Abstract A collaborative study was conducted to evaluate a method for identifying d- or dl-∝-tocopherol in pharmaceuticals, food supplements, or feed supplements. The sample is extracted and saponified, the extraneous color is removed by chromatography, and the sample is assayed for vitamin E. Optical rotations are determined before and after formation of the ferricyanide oxidation product. The specific optical rotation of the oxidation product is negligible for the dJ-form and +25.5° for the d-form. Statistical analysis of the data reported by 8 collaborators for the standard d-∝-tocopheryl acetate and for 6 unknown samples indicates a significant interaction between laboratories and samples. The mean coefficients of variation among laboratories for the determinations of the corrected specific optical rotation of the standard and the rotation ratio for the unknown samples containing d-∝-tocopherol were 11.7 and 21.6%, respectively, for all laboratories and 5.8 and 11.8%, respectively, for experienced laboratories. This identification test for vitamin E is acceptable for determining the form of vitamin E as either d or dl, but is not acceptable for accurately determining mixtures of the 2 forms. The method has been adopted as official first action for the identification of d- or dl-∝-tocopherol.


2018 ◽  
Vol 67 (11) ◽  
pp. 2155-2156
Author(s):  
A. V. Orlova ◽  
N. N. Kondakov ◽  
Yu. F. Zuev ◽  
L. O. Kononov

2015 ◽  
Vol 2015 ◽  
pp. 1-5 ◽  
Author(s):  
Qi Jia ◽  
Nana Xu ◽  
Pengqian Mu ◽  
Bo Wang ◽  
Shuming Yang ◽  
...  

Tau-fluvalinate (TFLV) is one of the most potent chiral synthetic pyrethroids to control a wide range of pests in agricultural fields, especially in apiary. In this study, two stereoisomers of TFLV were fully separated by high-performance liquid chromatography (HPLC) with a semipreparative chiral column using cellulose-tris(3,5-dimethylphenylcarbamate) as chiral stationary phase andn-hexane and 2-propanol (96/4, v/v) as mobile phase at a flow rate of 2.5 mL min−1. The (+)-stereoisomer was first eluted by detecting with an optical rotation detector. After obtaining pure single stereoisomer of TFLV, acute toxicities of each isomer and TFLV standard to zebrafish were evaluated. The results showed that the (+)-stereoisomer exhibited 273.4 times higher toxicity than the (−)-stereoisomer and 6.7 times higher than TFLV standard, according to their LC50values at 96 h after exposure. This indicates that the toxicity of TFLV mainly originates from (+)-stereoisomer. These results are very helpful to prepare single stereoisomer of chiral pesticides and evaluate their different toxicological effects to aquatic organisms.


1987 ◽  
Vol 65 (1) ◽  
pp. 1-7 ◽  
Author(s):  
Malcolm B. Perry ◽  
Leann L. MacLean

The cellular lipopolysaccharide produced by Yersinia enterocolitica serotype O:5,27 was of the S-type and composed of an antigenic O-chain polysaccharide linked through a core oligosaccharide region, which in turn was linked through 3-deoxy-D-manno-octulonosyl units to a lipid A moiety. The O-chain polysaccharide was composed of equal molar amounts of L-rhamnose and D-xylulose. By partial hydrolysis, periodate oxidation, methylation, specific optical rotation, and 13C and 1H nuclear magnetic resonance studies, the structure of the O-chain was established as being a linear backbone of alternating 1,3-linked α-L-rhamnopyranosyl and β-L-rhamnopyranosyl units, to which 2,2-linked β-D-threo-pent-2-ulofuranoside (D-xylulofuranoside) units were present on every L-rhamnopyranosyl residue, as shown below.[Formula: see text]


Sign in / Sign up

Export Citation Format

Share Document