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Study of Impurity Profiles in Raw Materials and Tablets of Rutin and Its Production Process: Correlation Analysis 芦丁原材料和片剂中的杂质概况及其生产工艺研究：相关性分析
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03152-8
Xinyu Kuang, Dandan Shen, Qun Wu, Linggao Zeng, Wei Zhang, Jianhua Wang
{"title":"Study of Impurity Profiles in Raw Materials and Tablets of Rutin and Its Production Process: Correlation Analysis","authors":"Xinyu Kuang, Dandan Shen, Qun Wu, Linggao Zeng, Wei Zhang, Jianhua Wang","doi":"10.1007/s11094-024-03152-8","DOIUrl":"https://doi.org/10.1007/s11094-024-03152-8","url":null,"abstract":"<p>An HPLC-UV method with high sensitivity and good resolution, calculated by the principal component external standard method with correction factors and detailed methodological validation according to ICH guidelines, was developed for the accurate detection of impurities in three different extraction processes of rutin raw materials and their tablets, and the determination of impurity profiles by LC-MS/MS. In this study, nine impurities (&gt;0.1%) were mainly isolated and identified, four of which were process impurities, and the other five were degradation products. The results of the correlation between impurity profiles and production processes showed that the impurity content of rutin tablets correlated positively with the impurity level of the raw materials used, which correlated significantly with the extraction process. The finished rutin under the alkali-dissolution and acid-sedimentation refining method had low purity and the highest impurity content. In contrast, the number of impurities and the total amount of impurities detected in rutin by the secondary recrystallization process with methanol washing were the lowest, and were mainly process impurities. This further indicates that generating degradation impurities could be avoided, and a suitable refining process could effectively reduce impurities. This study provides an essential basis for manufacturers to optimize the process parameters of rutin raw materials.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"18 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526671","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of New Conjugates of Edaravone and 1-Aminoadamantanes and Their Interaction with NMDA Receptors in Rats 依达拉奉和 1-氨基金刚烷新共轭物的合成及其与大鼠 NMDA 受体的相互作用
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03134-w
V. V. Grigoriev, A. Yu. Aksinenko, T. V. Goreva, A. V. Gabrelyan, T. A. Epishina
{"title":"Synthesis of New Conjugates of Edaravone and 1-Aminoadamantanes and Their Interaction with NMDA Receptors in Rats","authors":"V. V. Grigoriev, A. Yu. Aksinenko, T. V. Goreva, A. V. Gabrelyan, T. A. Epishina","doi":"10.1007/s11094-024-03134-w","DOIUrl":"https://doi.org/10.1007/s11094-024-03134-w","url":null,"abstract":"<p>New adamantane-containing derivatives of edaravone, one of two drugs used to treat amyotrophic lateral sclerosis, were synthesized. The pyrazolone ring and adamantane moiety in the new edaravone derivatives were conjugated by alkyl and azetidine linkers via amination of the corresponding alcohol mesylates. Some of the new compounds were found to be effective blockers of the allosteric NMDA receptor binding site in rats but exhibited little activity against the intrachannel NMDA receptor binding site. The structure–activity relationship between the ability to block the ifenprodil binding site and the structure of the linkers and substituents on the molecule was analyzed.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"31 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526672","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Variability of the Constituent Composition of Mentha piperita L. Essential Oil 薄荷精油成分的可变性
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03142-w
A. N. Alibegov, A. M. Aliev, G. K. Radjabov, F. A. Vagabova, A. M. Musaev
{"title":"Variability of the Constituent Composition of Mentha piperita L. Essential Oil","authors":"A. N. Alibegov, A. M. Aliev, G. K. Radjabov, F. A. Vagabova, A. M. Musaev","doi":"10.1007/s11094-024-03142-w","DOIUrl":"https://doi.org/10.1007/s11094-024-03142-w","url":null,"abstract":"<p>Varieties of <i>Mentha piperita</i> L. (peppermint) cultivated at altitudes of 1100 and 1650 m above sea level on identical soils were studied to identify the variability in the accumulation and constituent composition of their essential oils. Essential oils from cultivated samples were obtained by hydrodistillation. The composition of volatile organic substances was determined by GC-MS using a Shimadzu GCMS-QP2010 Plus quadrupole gas chromatograph-mass spectrometer. As a result, up to 58 constituents were identified, including 11 major ones. The quantitative content of the essential oil was found to be highly dependent on the climatic conditions of cultivation, whereas the composition of volatile organic substances varied insignificantly for a certain variety but was highly variable between different varieties.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"21 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526523","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Quality Management System in Production of Reference Materials 标准物质生产质量管理体系
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03150-w
V. S. Pyzhov, V. I. Gegechkori, V. A. Darina, E. A. Pogrebinskaya
{"title":"Quality Management System in Production of Reference Materials","authors":"V. S. Pyzhov, V. I. Gegechkori, V. A. Darina, E. A. Pogrebinskaya","doi":"10.1007/s11094-024-03150-w","DOIUrl":"https://doi.org/10.1007/s11094-024-03150-w","url":null,"abstract":"<p>The article touches the most relevant aspects of the role of quality management systems (QMSs) in the creation and replenishment of universal bases of reference materials (RMs) and harmonization of international standards. The article demonstrates how application of a QMS in this area ensures high-quality RM production by controlling the quality at each stage of the technological process. The publication focuses on the potential of a QMS to minimize errors and risks associated with the production of RMs, which increases their reliability and accuracy when used in scientific and production areas.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"34 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526669","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Effect of Quercetin and its Derivatives on the Excretory Function of Rat Kidneys 槲皮素及其衍生物对大鼠肾脏排泄功能的影响
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI: 10.1007/s11094-024-03135-9
E. N. Zaitseva, A. I. Altareva, A. V. Dubishchev, V. A. Kurkin, O. V. Sharova
{"title":"Effect of Quercetin and its Derivatives on the Excretory Function of Rat Kidneys","authors":"E. N. Zaitseva, A. I. Altareva, A. V. Dubishchev, V. A. Kurkin, O. V. Sharova","doi":"10.1007/s11094-024-03135-9","DOIUrl":"https://doi.org/10.1007/s11094-024-03135-9","url":null,"abstract":"<p>The optimal diuretic doses of quercetin and rutin (5 mg/kg) and dihydroquercetin and hyperoside (1 mg/kg) were determined in experiments on white rats with a single intragastric administration. The mechanism of action of sodium quercetin and its derivatives on glomerular filtration and tubular transport was studied in acute experiments. Quercetin, dihydroquercetin, rutin, and hyperoside with a single intramuscular injection at the above doses contributed to an increase in diuresis, saluresis, creatinine clearance (except for rutin), and excreted sodium fraction by an average of 141%, 203%, 153%, and 189%, respectively (<i>p</i> &lt; 0.05). Rutin also led to a decrease in the creatinine concentration index (by an average of 79%, <i>p</i> &lt; 0.05). The diuretic furosemide with a single intramuscular injection at the threshold dose of 1 mg/kg increased diuresis, saluresis, and excreted sodium fraction (by an average of 187%, <i>p</i> &lt; 0.05), like the effect of the quercetin derivatives; decreased the creatinine concentration index (by an average of 62%, <i>p</i> &lt; 0.05); and did not affect creatinine clearance identically to the effect of rutin.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"13 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141526522","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Effect of Formulation Parameters and Physiological Environment on Amlodipine Release Kinetics Encapsulated in Biodegradable Polymers and Optimized by Design Methodology 可生物降解聚合物包封的配方参数和生理环境对氨氯地平释放动力学的影响及设计方法的优化
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-05-28 DOI: 10.1007/s11094-024-03129-7
Naima Ifourah, Sandrine Cammas-Marion, Hayet Belkacemi
{"title":"Effect of Formulation Parameters and Physiological Environment on Amlodipine Release Kinetics Encapsulated in Biodegradable Polymers and Optimized by Design Methodology","authors":"Naima Ifourah, Sandrine Cammas-Marion, Hayet Belkacemi","doi":"10.1007/s11094-024-03129-7","DOIUrl":"https://doi.org/10.1007/s11094-024-03129-7","url":null,"abstract":"<p>In this study, two polyelectrolytes, chitosan and propyl methyl cellulose carbonate, were associated by crosslinking with tripolyphosphate (TPP), to prepare microspheres loaded with amlodipine besylate (Aml). The formulations were optimized by Box–Behnken experimental design, in which three factors, four responses were studied to check the effect of independent variables (concentration of TPP, pH of TPP solution, and pH of a polymer mixture) on responses: zeta potential, particle size, polydispersity index and entrapment efficiency. The optimal encapsulation efficiency was around 92.43%, the zeta potential on average 41.75 mV, and the minimum mean particle size was 310 nm. The effects of the parameters on changes in structure, crystallinity, and surface charges of polymers, by crosslinking in microparticles, were identified by FT-IR, XRD, and dynamic light scattering analyses. The encapsulation parameters and the environment media influenced the mechanism of release and the kinetics model, which was greater in the duodenal medium at pH 5.5 (<i>Q</i> = 100%). The microencapsulation by nontoxic polymers in water is a good method of preparing amlodipine-loaded microspheres, which are intended for the oral route, with optimal dose release in the duodenal medium. This represents the target site for absorption of the drug, in the pulmonary sphere.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"132 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141166912","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design, Synthesis and Biological Evaluation of 7-Azaindole Analogues as Novel Antiproliferative Agent and Tyrosine Protein Kinase SRC Inhibitors 作为新型抗增殖剂和酪氨酸蛋白激酶 SRC 抑制剂的 7-氮杂吲哚类似物的设计、合成和生物学评价
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-05-17 DOI: 10.1007/s11094-024-03120-2
Neha Sharma, Anurag, Monika Sachdeva
{"title":"Design, Synthesis and Biological Evaluation of 7-Azaindole Analogues as Novel Antiproliferative Agent and Tyrosine Protein Kinase SRC Inhibitors","authors":"Neha Sharma, Anurag, Monika Sachdeva","doi":"10.1007/s11094-024-03120-2","DOIUrl":"https://doi.org/10.1007/s11094-024-03120-2","url":null,"abstract":"<p>A new series of SRC inhibitors based on 7-azaindole core were designed, synthesized and evaluated for antiproliferative and antioxidant activities. All synthesized analogues of 7-azindole were characterized through <sup>1</sup>H and <sup>13</sup>C NMR and Mass Spectrometry. Synthesized analogues were screened <i>in vitro</i> antiproliferative activity on the MCF-7 breast cancer cell line. Compounds <b>5a</b>, <b>5b</b>, <b>5d</b>, <b>5g</b>, and <b>5h</b> showed significant results. Compound <b>5b</b> was the most active in the series with a GI50 of 2.19 mM. Molecular docking studies of the most active analogues were performed to reveal the structural features responsible for their interaction with the active site of SRC. The synthesized analogues were also screened for antioxidant activity by the DPPH method. In conclusion, for the creation of novel drugs, these compounds offer promising potential.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"43 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-05-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141059161","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Prospects for Production of Microencapsulated Medicines Based on Plant Extracts (Review) 基于植物提取物的微囊药物的生产前景（综述）
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-05-13 DOI: 10.1007/s11094-024-03121-1
O. A. Semkina, O. M. Beloshapkina, M. A. Dzhavakhyan
{"title":"Prospects for Production of Microencapsulated Medicines Based on Plant Extracts (Review)","authors":"O. A. Semkina, O. M. Beloshapkina, M. A. Dzhavakhyan","doi":"10.1007/s11094-024-03121-1","DOIUrl":"https://doi.org/10.1007/s11094-024-03121-1","url":null,"abstract":"<p>Material devoted to the peculiarities of plant extract microencapsulation used for the development and production of drugs and active substances with pharmacological activity is reviewed. The advantages of some microencapsulation methods of plant extracts are shown: emulsification (dispersion), coacervation, ionic gelation, spray and freeze drying, solvent evaporation, extrusion, fluidized bed microencapsulation. The parameters for choosing an encapsulation method for plant extracts were determined. Possible prospects for microencapsulation technology of plant extracts were described. Domestic and foreign literature sources in the public domain were analyzed using the electronic databases PubMed, e-Library, and CyberLeninka and Google Scholar search engine.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"16 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140929854","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Impact of Ultrasonic Vibrations on the Stability of Bovhyaluronidase Azoximer in Solution 超声波振动对溶液中牛醛酸酶氮氧化物稳定性的影响
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-05-13 DOI: 10.1007/s11094-024-03127-9
A. E. Krasheninnikov, V. V. Sepp, K. S. Bakulin, O. I. Arefieva, A. A. Karsanov
{"title":"Impact of Ultrasonic Vibrations on the Stability of Bovhyaluronidase Azoximer in Solution","authors":"A. E. Krasheninnikov, V. V. Sepp, K. S. Bakulin, O. I. Arefieva, A. A. Karsanov","doi":"10.1007/s11094-024-03127-9","DOIUrl":"https://doi.org/10.1007/s11094-024-03127-9","url":null,"abstract":"<p>Changes in the quantitative content and specific activity of hyaluronidase enzyme after ultrasonic treatment of solutions of bovhyaluronidase azoximer were studied. Solutions of the finished dosage form of bovhyaluronidase azoximer (Longidase<sup>®</sup> lyophilizate for preparation of solution for injection, 3000 IE) and bovhyaluronidase azoximer drug substance (Longidase<sup>®</sup> substance-lyophilizate) were studied. The aim of the study was to determine the effect of ultrasound (US) on the stability of bovhyaluronidase azoximer determined from the measured quantitative content and enzymatic activity of the substance in solution. US at a radiation intensity of 61.4 W/L during treatment in an ultrasonic bath did not significantly affect the quantitative content of the bovhyaluronidase azoximer drug substance in solution, while the decrease in the enzymatic activity of the active substance in Longidase solution after 20 and 30 min of ultrasonic treatment was statistically significant. At the same time, the enzymatic activity of the active substance determined by a biochemical method differed significantly (residual activity from 99.70% to 59.27%) depending on the design features of the nebulizers and the nebulization time after nebulization of the bovhyaluronidase azoximer solution in mesh nebulizers from various manufacturers. Nebulization times of min were least associated with the risk of significant loss of stability of bovhyaluronidase azoximer.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"2014 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140929628","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Formulating GML-1 Tablets Using the Harrington Desirability Function 利用哈灵顿可取函数配制 GML-1 药片
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-05-13 DOI: 10.1007/s11094-024-03126-w
D. I. Gavrilov, E. V. Blynskaya, S. V. Tishkov, K. V. Alekseev
{"title":"Formulating GML-1 Tablets Using the Harrington Desirability Function","authors":"D. I. Gavrilov, E. V. Blynskaya, S. V. Tishkov, K. V. Alekseev","doi":"10.1007/s11094-024-03126-w","DOIUrl":"https://doi.org/10.1007/s11094-024-03126-w","url":null,"abstract":"<p>Features of using the generalized Harrington desirability function for the selection of a binder and lubricant for GML-1 (<i>N</i>-benzyl-<i>N</i>-methyl-1-phenylpyrrolo[1,2-<i>a</i>]pyrazine-3-carboxamide) tablets are considered. The factors affecting the characteristics of the finished dosage form are evaluated. Model formulations with different qualitative and quantitative compositions of disintegrant and lubricant excipients were developed. Their pharmaceutical and technological properties were studied. The factors having the greatest impact on indicators such as the mass loss on drying, strength, disintegration, and solubility of the tablets were identified. The type and amount of disintegrant and lubricant in the tablet that could produce a dosage form with the optimal pharmaceutical and technological characteristics were determined.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"24 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140929564","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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