INDIAN DRUGS最新文献_第2页

ENHANCING GASTRIC ULCER MANAGEMENT: NOVEL INSIGHTS FROM TERAZOSIN-PANTOPRAZOLE COMBINATION THERAPY 加强胃溃疡管理：特拉唑嗪-泮托拉唑联合疗法的新启示

INDIAN DRUGS Pub Date : 2024-01-28 DOI: 10.53879/id.61.01.14392

Teresa J. Vadakutt, Gaurav M. Doshi

引用次数: 0

FORMULATION AND ASSESSMENT OF A SUNSCREEN CREAM BASED ON GREEN TEA AND MARIGOLD FLOWER EXTRACTS 基于绿茶和金盏花提取物的防晒霜的配方和评估

INDIAN DRUGS Pub Date : 2024-01-28 DOI: 10.53879/id.61.01.14376

Akshay V. Rasal, Amol Kumar A. Kempwade, Madhuri Sankpal

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LIVING WITH THE GHOST: CAN WE EVER ESCAPE COVID-19’S SHADOW? 与幽灵共存：我们能否摆脱科维德-19 的阴影？

INDIAN DRUGS Pub Date : 2024-01-28 DOI: 10.53879/id.61.01.p0005

Pooja A. Chawla

引用次数: 0

DIALKYL ISOMERS OF BENZENESULFONAMIDPHENYLPYRIMIDINE-4(1H)-ONE: SYNTHESIS, STRUCTURE AND PHARMACOLOGICAL STUDIES 苯磺酰胺苯基嘧啶-4(1h)-酮的二烷基异构体：合成、结构和药理研究

INDIAN DRUGS Pub Date : 2024-01-28 DOI: 10.53879/id.61.01.14327

D. Anenko, I. Kodonidi, S. D. Kirik, Tamara N. Glizhova, N. Saidov

{"title":"DIALKYL ISOMERS OF BENZENESULFONAMIDPHENYLPYRIMIDINE-4(1H)-ONE: SYNTHESIS, STRUCTURE AND PHARMACOLOGICAL STUDIES","authors":"D. Anenko, I. Kodonidi, S. D. Kirik, Tamara N. Glizhova, N. Saidov","doi":"10.53879/id.61.01.14327","DOIUrl":"https://doi.org/10.53879/id.61.01.14327","url":null,"abstract":"Interaction of N-acetyl-2-phenylacetamide with sulfanilamide and N-(2-phenylacetyl)propanamide with sulfanilamide led to the preparation of the two isomeric benzenesulfonamidphenylpyrimidin-4(1H)-ones. In positions 2 and 6, the synthesized phenylpyrimidin-4(1H)-ones contained methyl and ethyl as substituents in the first case (IIa), and ethyl and methyl – in the second one (IIb), respectively. The crystal structures of the compounds have been determined by X-ray powder diffraction. It has been established that the positions of substituents significantly affect the conformation of molecules. In molecule IIa, the phenyl ring is rotated to the pyrimidine one by 84°; in IIb, the both rings lie in the same plane. Due to different conformations, the packing of molecules in the crystal lattice changes significantly. Pharmacological properties of isomeric pyrimidinones have been studied in relation to the anti-inflammatory and cerebroprotective activity in chronic traumatic encephalopathy. A comparative analysis of the drug similarity has been carried out. Screening of anti-inflammatory and cerebroprotective activities has shown that compound IIa surpassed its structural isomer in the pharmacological action, which was interpreted as a greater elasticity result of molecule IIa compared to IIb due to the less extended π-system.","PeriodicalId":13409,"journal":{"name":"INDIAN DRUGS","volume":"412 19","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140490433","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

INVESTIGATION OF THE HEPATOPROTECTIVE POTENTIAL OF FRACTIONS AND PHYTOSOMAL COMPLEXES OF TELFAIRIA OCCIDENTALIS HOOK F LEAF EXTRACTS ON ALCOHOL-INDUCED HEPATOTOXICITY IN RAT MODELS 研究西洋接骨木钩叶提取物的馏分和植物体复合物对酒精诱导的大鼠肝毒性模型的保肝潜力

INDIAN DRUGS Pub Date : 2024-01-28 DOI: 10.53879/id.61.01.14224

Romanus C. Omeh, K. Okolo, M. E. Ugwueze, C. C. Mbah, Anthony A. Atamma, M. A. Momoh, J. Ogbonna, L. O. Ugorji

{"title":"INVESTIGATION OF THE HEPATOPROTECTIVE POTENTIAL OF FRACTIONS AND PHYTOSOMAL COMPLEXES OF TELFAIRIA OCCIDENTALIS HOOK F LEAF EXTRACTS ON ALCOHOL-INDUCED HEPATOTOXICITY IN RAT MODELS","authors":"Romanus C. Omeh, K. Okolo, M. E. Ugwueze, C. C. Mbah, Anthony A. Atamma, M. A. Momoh, J. Ogbonna, L. O. Ugorji","doi":"10.53879/id.61.01.14224","DOIUrl":"https://doi.org/10.53879/id.61.01.14224","url":null,"abstract":"The aim of this work was to evaluate the hepatoprotective potential of fractions and phytosomal complexes of Telfairia occidentalis leaf extracts on ethanol-induced hepatotoxicity in rat models. Phytosomal complexes of ethanol extract fractions were prepared by the thin film hydration technique. Hepatoprotective activities were evaluated by biochemical assays and histopathological examination of liver sections. Intoxication of animals with pure ethanol significantly (p < 0.05) elevated their liver enzyme titers, whereas co-administration with various extracts and phytosomal complexes reversed the increases. Histopathological findings revealed liver tissue protective effects of the extracts with the phytosomal complexes exhibiting greater effects (p < 0.05). Significant differences at p ≤ 0.05 were observed in the liver indices of animals treated with co-administered ethanol and extract fractions or phytosomes complexes versus the positive control group. T. occidentalis leaf extract formulated as phytosomes, therefore, has good potential of enhancing the hepatoprotective activities of the extract.","PeriodicalId":13409,"journal":{"name":"INDIAN DRUGS","volume":"396 8","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140490688","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

FORMULATION AND DEVELOPMENT OF BIOADHESIVE PELLETS FOR MANAGEMENT OF HELICOBACTER PYLORI INFECTION 配制和开发用于治疗幽门螺旋杆菌感染的生物胶丸

INDIAN DRUGS Pub Date : 2024-01-28 DOI: 10.53879/id.61.01.13983

Raj Khatri, Munira M. Momin, Sankalp Gharat, M. Damani

{"title":"FORMULATION AND DEVELOPMENT OF BIOADHESIVE PELLETS FOR MANAGEMENT OF HELICOBACTER PYLORI INFECTION","authors":"Raj Khatri, Munira M. Momin, Sankalp Gharat, M. Damani","doi":"10.53879/id.61.01.13983","DOIUrl":"https://doi.org/10.53879/id.61.01.13983","url":null,"abstract":"Helicobacter pylori, a gram-negative bacterium, is a group I carcinogen which is responsible for duodenal ulcer, gastric ulcer, and gastric cancer. The existing treatment is based on the use of proton pump inhibitors, but is inadequate owing to factors such as low concentration of drug reaching the target site, short residence time, and resistance to activity. Intending to mitigate these limitations, bioadhesive pellets of tinidazole and pantoprazole sodium sesquihydrate for the management of H. pylori infection were developed. Tinidazole-loaded pellets will act on gastric mucosa and pantoprazole-loaded pellets will release the drug in the intestine. Readily dispersible bioadhesive pellets were formulated by extrusion spheronization using Noveon® AA and hydroxypropyl methyl cellulose (HPMC) as the matrix-forming polymers and microcrystalline cellulose as the core-forming agent. The size of placebo pellets was 1.192±0.017mm. Pantoprazole pellets were coated with Eudragit® S100 to achieve sustained drug release in the intestine. In vitro release studies of pellets showed that 98.331±0.456% and 99.438±0.465% of tinidazole and pantoprazole, respectively were released by the end of 8 h. Ex vivo mucoadhesion study on the gastric mucosa of goat demonstrated a mucoadhesive force of 2.3544±0.02 N. The study thus indicates that the developed formulation sustains the release of tinidazole as well as pantoprazole sodium and could prove to be efficacious and promising for H. pylori eradication at lower doses, reduced adverse effects, and enhanced bioavailability.","PeriodicalId":13409,"journal":{"name":"INDIAN DRUGS","volume":"225 3","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140491314","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

OPTIMIZATION AND CHARACTERIZATION OF FAST DISSOLVING TABLETS OF CANDESARTAN CILEXETIL PREPARED FROM SPHERICAL AGGLOMERATES 用球形团聚体制备坎地沙坦西来替酯快速溶解片的优化和表征

INDIAN DRUGS Pub Date : 2024-01-28 DOI: 10.53879/id.61.01.13910

Swapnil S. Patil, Rohan D. Patil, Prakash V. Chavan, Nisha M. Jagtap, Harshad P. Khade, S. Upadhye, Suraj J. Patil, Sandip M. Honmane

{"title":"OPTIMIZATION AND CHARACTERIZATION OF FAST DISSOLVING TABLETS OF CANDESARTAN CILEXETIL PREPARED FROM SPHERICAL AGGLOMERATES","authors":"Swapnil S. Patil, Rohan D. Patil, Prakash V. Chavan, Nisha M. Jagtap, Harshad P. Khade, S. Upadhye, Suraj J. Patil, Sandip M. Honmane","doi":"10.53879/id.61.01.13910","DOIUrl":"https://doi.org/10.53879/id.61.01.13910","url":null,"abstract":"The primary objective of this study was to develop a rapidly dissolving tablet containing an antihypertensive drug, candesartan cilexetil (CAND). The research work focused on improving solubility and in vitro dissolution of drugs using spherical agglomeration technique. Spherical agglomerates of CAND were developed using PVPK-30 as polymer and dichloromethane as bridging liquid. A spherical agglomerate of CAND was used to formulate fast dissolving tablet (FDT) with different superdisintegrants like Crospovidone and Cross carmellose sodium. The prepared powder blend was evaluated for different pre-compression parameters like solubility, compressibility index, Hausner’s ratio and flow property and post-compression parameters including in vitro dissolution study. The solubility of prepared agglomerates was found to be 0.15 to 0.91 mg mL-1, and it was higher than the pure drug (0.00071 mg mL-1). In vitro drug release study of optimized batch of FDT has shown 95.47 % of drug release. From the results, it was revealed that the prepared FDT using the agglomeration technique might be used to enhance the solubility and bioavailability of CAND to augment acute and chronic hypertension therapy.","PeriodicalId":13409,"journal":{"name":"INDIAN DRUGS","volume":"266 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140491094","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

TECHNIQUES AND ALGORITHMS FOR STRUCTURE-BASED VIRTUAL SCREENING (SBVS): AN OVERVIEW 基于结构的虚拟筛选（SBVS）的技术和算法：概述

INDIAN DRUGS Pub Date : 2024-01-28 DOI: 10.53879/id.61.01.13346

Raksha K. Rao, Somdatta Y. Chaudhari, Shailaja B. Jadhav, Pravin D. Chaudhari, Ujwala B. Yedake

引用次数: 0

EVALUATION OF IN VITRO CYTOTOXIC POTENTIAL OF DIFFERENT CARMUSTINE FORMULATIONS AGAINST U-87 MG HUMAN GLIOBLASTOMA CELL LINE 评估不同卡莫司汀制剂对 U-87 mg 人胶质母细胞瘤细胞系的体外细胞毒性潜力

INDIAN DRUGS Pub Date : 2024-01-28 DOI: 10.53879/id.61.01.14427

A. Mali, Anil S. Bhanwase

引用次数: 0

MOLECULAR FIELD ANALYSIS AND DYNAMIC SIMULATION STUDIES OF 1,5-DISUBSTITUTED PYRAZOLINE-BASED MAO-A INHIBITORS FOR THE MANAGEMENT OF DEPRESSION 用于治疗抑郁症的 1,5-二取代吡唑啉基 mao-a 抑制剂的分子场分析和动态模拟研究

INDIAN DRUGS Pub Date : 2024-01-28 DOI: 10.53879/id.61.01.14236

Abhimannu Shome, Pooja A. Chawla, N. K. Rangra, V. Eyupoglu, Ravi Rawat

{"title":"MOLECULAR FIELD ANALYSIS AND DYNAMIC SIMULATION STUDIES OF 1,5-DISUBSTITUTED PYRAZOLINE-BASED MAO-A INHIBITORS FOR THE MANAGEMENT OF DEPRESSION","authors":"Abhimannu Shome, Pooja A. Chawla, N. K. Rangra, V. Eyupoglu, Ravi Rawat","doi":"10.53879/id.61.01.14236","DOIUrl":"https://doi.org/10.53879/id.61.01.14236","url":null,"abstract":"Depression, along with grief and anxiety, is currently one of the most common mental illnesses. It was placed 25th among the major diseases. QSAR (CoMFA) of 37 compounds with MAO-A inhibitory activity yielded the most significant QSAR model, m.3, with r2 = 0.963, SDEC= 0.129, q2 = 0.742, SDEP= 0.34. Using the lead likeness matrix, thirty-seven 1,5-disubstituted MAO-A inhibitors were developed and tested based on the QSAR models. The top 13 compounds were identified. Furthermore, compound 2B (ΔG: -10.3 kcal mol-1, RMSD: 0.151 Å) was selected among the top 13 hits obtained from molecular docking experiments. Significant interactions were also observed, including π-π contacts with Phe208, Tyr444, Trp407, and hydrogen bond interactions with Ala68 and Tyr69. Furthermore, dynamic modelling demonstrated that compound 2B (0.11 nm) has higher overall stability than clorgyline, with a lower RMSD value, and may reach equilibrium in the final 20-25 ns. In terms of RMSF, 2B produced around 0.34 nm with less variation than clorgyline. Throughout the simulation, 2B (No. of H-bond: 6) had more hydrogen bonding than clorgyline (No. of H-bond: 3) with the highest occupancy, i.e. 117.39% for GLU216, 29% for TYR444, and 49% for PRO72, and so on. Compound 2B was proven to be the most essential throughout the experiments. These new chemicals will be optimized in vitro and in vivo in the future. This study will surely contribute to the development of novel MAO-A inhibitors for the treatment of depression.","PeriodicalId":13409,"journal":{"name":"INDIAN DRUGS","volume":"405 11","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140490553","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0