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In silico Prediction of Pyrazoline Derivatives as Antimalarial agents 吡唑啉衍生物抗疟疾药物的计算机预测
Asian Journal of Pharmaceutical Research Pub Date : 2022-05-26 DOI: 10.52711/2231-5691.2022.00018
Sonal Dubey, Sakshi Bhardwaj, Prabitha Parbhakaran, Ekta Singh
{"title":"In silico Prediction of Pyrazoline Derivatives as Antimalarial agents","authors":"Sonal Dubey, Sakshi Bhardwaj, Prabitha Parbhakaran, Ekta Singh","doi":"10.52711/2231-5691.2022.00018","DOIUrl":"https://doi.org/10.52711/2231-5691.2022.00018","url":null,"abstract":"Malaria is one of the toughest health and development challenges faced by tropical countries. The resistance of malarial parasite to available drugs and currently used chemotherapy made its emergence for development of new drugs. Pyrazoline derivatives have shown good antimalarial activity. In present work, our objective is to explore pyrazoline derivatives with in silico methods for their antimalarial activity. A five-point pharmacophore was developed using 80 molecules having logIC50 ranging from 10.39 to 6.72. The pharmacophore yielded a statistically significant 3D-QSAR model with a high correlation coefficient R2= 0.806772, cross validation coefficient Q2= 0.7154 at four component PLS factor. To evaluate the effectiveness of docking protocol, we have selected crystallographic bound compound to validate our docking procedure. Protein selected for our studies with PDB id is 2BMA having resolution 2.7 Å. Further similar orientations were observed between the superpositions of 80 compounds after pharmacophore and 3D-QSAR poses, pharmacophore and XP docking poses, 3D-QSAR and XP docking poses. These present studies will provide insight in designing novel molecules with better antimalarial activity. Results explained that two aromatic rings and two hydrophobic groups are important for the antimalarial activity. The docking studies of all selected inhibitors in the active site of 2BMA showed crucial hydrogen bond interactions with HIS95, SER97, GLN323, ARG93, ALA321, ALA346, ILE166, ILE102 and PRO96 amino acid residues.","PeriodicalId":8537,"journal":{"name":"Asian Journal of Pharmaceutical Research","volume":"154 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77508020","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: 2
Enhancement of Dissolution profile of poorly water soluble drug using Water Soluble Carriers 利用水溶性载体增强难水溶性药物的溶出谱
Asian Journal of Pharmaceutical Research Pub Date : 2022-05-26 DOI: 10.52711/2231-5691.2022.00021
Snehal S Manekar, Ravindra L. Bakal, Manoj S. Charde
{"title":"Enhancement of Dissolution profile of poorly water soluble drug using Water Soluble Carriers","authors":"Snehal S Manekar, Ravindra L. Bakal, Manoj S. Charde","doi":"10.52711/2231-5691.2022.00021","DOIUrl":"https://doi.org/10.52711/2231-5691.2022.00021","url":null,"abstract":"Teneligliptin Hydrobromide is a long-acting, orally bioavailable, pyrolidone anti-diabetic activity with a solubility of 1.7mg/ml in water which also depends upon the pH and temperature of the solvent. So, Solid dispersion of drug with different polymers an attempt was made to improve dissolution of teneligliptin hydrobromide. The aim of this study was to prepare, characterize and compare solid dispersions of poorly water soluble anti diabetic drug by using PVP and HPMC for enhancing the dissolution rate of the drug. The solid dispersions were prepared by physical mixing method and kneading method at 1:1, 1:2 and 2:1 ratios of drug to polymer. The drug-excipient interaction study showed that the drug and polymers were compatible with each other. The formulations were evaluated for percent drug content, micromeritics and in-vitro dissolution studies. In the present study it was seen that there was an increase in in-vitro drug release for solid dispersion as compared to the pure drug taken alone. Based on the pattern of drug release, the kneading method showed more drug release as compared to physical mix method. In physical mix method, the rate of dissolution of teneligliptin hydrobromide was increased in teneligliptin and Polyvinylpyrrolidone (PVP) with the proportion of (1:2) when compared to the other formulations. In kneading method, the rate of dissolution of teneligliptin hydrobromide was increased in drug and Hydroxypropylmethylcellulose (HPMC) with the proportion of (1:2) when compared to the other formulations. Finally, solid dispersion containing HPMC, as a carrier, gave faster dissolution rates among all the formulations and was selected as the optimized formulation inthis study.","PeriodicalId":8537,"journal":{"name":"Asian Journal of Pharmaceutical Research","volume":"54 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84071634","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: 1
A Review on Cleaning Validation-Regulatory Guidelines for The Pharmaceutical Industry 清洁验证-制药行业监管指南综述
Asian Journal of Pharmaceutical Research Pub Date : 2022-05-26 DOI: 10.52711/2231-5691.2022.00026
S. Beula, S. R, R. Y., V. M., V. G.
{"title":"A Review on Cleaning Validation-Regulatory Guidelines for The Pharmaceutical Industry","authors":"S. Beula, S. R, R. Y., V. M., V. G.","doi":"10.52711/2231-5691.2022.00026","DOIUrl":"https://doi.org/10.52711/2231-5691.2022.00026","url":null,"abstract":"Manufacturing of Pharmaceutical products shall demonstrate a control to reproduce consistently the desired quality of product, wherein the control of cross-contamination plays an important role. An effective cleaning shall be in place to provide documented evidence that the cleaning methods employed within a facility consistently controls potential carryover of product (including intermediates and impurities), cleaning agents and extraneous material into subsequent product to a level which is below predetermined levels. Pharmaceutical manufacturers must validate their cleaning process to ensure compliance with cGMP regulations. So it is necessary to validate the cleaning procedures to ensure safety, efficacy, quality of the subsequent batches of drug product and regulatory requirements in Pharmaceutical product manufacture. In this article cleaning validation and cleaning validation program discussed in brief.","PeriodicalId":8537,"journal":{"name":"Asian Journal of Pharmaceutical Research","volume":"38 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75487110","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: 2
Recent Advance in Gastroretantive Drug Delivery System (GRDDS) 胃保留给药系统(GRDDS)研究进展
Asian Journal of Pharmaceutical Research Pub Date : 2022-05-26 DOI: 10.52711/2231-5691.2022.00022
Ashwini A Zanke, Hemant H Gangurde, Ananta B Ghonge, Praful S. Chavan
{"title":"Recent Advance in Gastroretantive Drug Delivery System (GRDDS)","authors":"Ashwini A Zanke, Hemant H Gangurde, Ananta B Ghonge, Praful S. Chavan","doi":"10.52711/2231-5691.2022.00022","DOIUrl":"https://doi.org/10.52711/2231-5691.2022.00022","url":null,"abstract":"The drug delivery system is most important and preferable drug delivery system. This route has high patient acceptability, primarily due to easy of administration. Effective oral drug delivery depends upon the factors such as gastric emptying process, the gastrointestinal transit time of the dosage form drug release from the dosage form, and site of absorption of drug. In recent years, scientific and technological advancements have been made in the research and development of gastro retentive drug delivery systems. Hence forth a wide spectrum of dosage forms has been developed for the drugs which have narrow absorption window, unstable at intestinal pH, are soluble in acidic pH, and have a site of action specific to stomach. The purpose of writing this review was to investigate, compile and present the recent as well as past literature in a more concise way with a special focus on approaches that are currently utilized in the prolongation of gastric residence time. These include floating system, swelling and expanding system, bio/mucoadhesive system, high-density system, and other delayed gastric emptying devices. The present review addresses briefly the classification, formulation consideration for Gastroretantive drug delivery system (GRDDS), factors controlling gastric retention, merits, demerits, and applications of gastro retentive drug delivery systems.","PeriodicalId":8537,"journal":{"name":"Asian Journal of Pharmaceutical Research","volume":"99 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78389906","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: 1
Mobocertinib is an Oral kinase inhibitor targeted against EGFR and used in the treatment of Non-small cell Lung cancer: A Review Mobocertinib是一种靶向EGFR的口服激酶抑制剂，用于治疗非小细胞肺癌
Asian Journal of Pharmaceutical Research Pub Date : 2022-05-26 DOI: 10.52711/2231-5691.2022.00029
Mayur S. Jain, Shashikant D. Barhate, Rahul D. Shimpi
{"title":"Mobocertinib is an Oral kinase inhibitor targeted against EGFR and used in the treatment of Non-small cell Lung cancer: A Review","authors":"Mayur S. Jain, Shashikant D. Barhate, Rahul D. Shimpi","doi":"10.52711/2231-5691.2022.00029","DOIUrl":"https://doi.org/10.52711/2231-5691.2022.00029","url":null,"abstract":"Mobocertinib is a kinase inhibitor targeted against human epidermal growth factor receptor (EGFR). It is used particularly in the action of non-small cell lung cancer (NSCLC) caused by exon 20 placing mutations in the EGFR gene, which are classically linked through a poorer prognosis (as compared to \"classical\" EGFR mutants causing NSCLC) and are linked with opposition to standard targeted EGFR inhibitors. Mobocertinib appears to be an effective means of treating this otherwise treatment-resistant NSCLC, exerting an inhibitory effect on EGFR exon 20 insertion mutant variants at concentrations 1.5- to 10-fold lower than those required to inhibit wild-type EGFR.2 Mobocertinib, below the brand name Exkivity (Takeda Pharmaceuticals Inc.), was granted accelerated agreement by the FDA in September 2021 for the action of locally advanced or metastatic NSCLC in patients with EGFR exon 20 insertion mutations who have failed previous therapies.1","PeriodicalId":8537,"journal":{"name":"Asian Journal of Pharmaceutical Research","volume":"136 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88918779","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
Preparation, Reactions and Medical Applications of Chalcone Intermediate - A Review 查尔酮中间体的制备、反应及医学应用综述
Asian Journal of Pharmaceutical Research Pub Date : 2022-05-26 DOI: 10.52711/2231-5691.2022.00027
Hambirrao Chetan S., Thorat Shubhangi S., Dhaygude Vishwajit D., Sandeep R. Kane
{"title":"Preparation, Reactions and Medical Applications of Chalcone Intermediate - A Review","authors":"Hambirrao Chetan S., Thorat Shubhangi S., Dhaygude Vishwajit D., Sandeep R. Kane","doi":"10.52711/2231-5691.2022.00027","DOIUrl":"https://doi.org/10.52711/2231-5691.2022.00027","url":null,"abstract":"Chalcone is an unsaturated aromatic ketone a central core for a several of important biological compounds, are communally known as chalcones. Chalcone are -unsaturated ketone, 2 aromatic rings are attached by a 3 carbon α, β-unsaturated carbonyl. This survey provides information on (synthesis processes, reactions, implementations of medical and biological activities, their uses and their source as a source of information) (whether natural or synthetic). Data on the chemistry of chalcones appeared on its preparation methods, reaction methods and medical application. This are different activities like Antiviral Activity, Anti hepatotoxic activity, Anti malarial Activity, Anti cancer Activity, Immunosuppressive Activity, Ant platelet Activity, Hypoglycemic activity, Anti inflammatory, Antibacterial Activity.","PeriodicalId":8537,"journal":{"name":"Asian Journal of Pharmaceutical Research","volume":"23 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75757242","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
Recent Updates on Psoriasis: A Review 牛皮癣最新进展:综述
Asian Journal of Pharmaceutical Research Pub Date : 2022-03-05 DOI: 10.52711/2231-5691.2022.00012
Tejasavi Mahajan, Navdeep Singh, Kamya Goyal, Shammy Jindal, V. Pandit, M. Ashawat
{"title":"Recent Updates on Psoriasis: A Review","authors":"Tejasavi Mahajan, Navdeep Singh, Kamya Goyal, Shammy Jindal, V. Pandit, M. Ashawat","doi":"10.52711/2231-5691.2022.00012","DOIUrl":"https://doi.org/10.52711/2231-5691.2022.00012","url":null,"abstract":"In the past 15 years, breakthroughs in the understanding towards the pathogenesis of psoriasis have been translated into highly and targeted effective therapies which provides fundamental insights into the pathogenesis of chronic inflammatory diseases. In this article we understand the mechanisms involved in the initiation and development of psoriasis, as well as the therapeutic options that arises from the dissection of the inflammatory psoriatic pathways. The whole discussion begins by addressing the inflammatory pathways and key cell types which initiating and perpetuating the psoriatic inflammation. Also, we discuss the role of genetics, associated epigenetic mechanisms, and the interaction of the skin flora in the pathophysiology of psoriasis. So, we the purpose of our study is to understand psoriasis comprehensively, and this review is well-established to explain the therapies, and other novel targeted drugs that are mostly used in the effective treatment of psoriasis.","PeriodicalId":8537,"journal":{"name":"Asian Journal of Pharmaceutical Research","volume":"29 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84369322","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: 3
Immunity Management Post Cancer Therapy 癌症治疗后的免疫管理
Asian Journal of Pharmaceutical Research Pub Date : 2022-03-05 DOI: 10.52711/2231-5691.2022.00005
Pavan Konde, Rahul Game, Mayuri Urhe, Akanksha Shinde
{"title":"Immunity Management Post Cancer Therapy","authors":"Pavan Konde, Rahul Game, Mayuri Urhe, Akanksha Shinde","doi":"10.52711/2231-5691.2022.00005","DOIUrl":"https://doi.org/10.52711/2231-5691.2022.00005","url":null,"abstract":"Immunity is the capacity or power of the body and Cancer is uncontrolled growth of abdominal cells in the body. Cancer is second stage of death. The several measures such as surgical resection of tumors, Chemotherapy and radiotherapy used to cure the cancer. The therapeutics can minimize and inhibit cancer cells, They not able to effectively defeat cancers. Hence we use the Immunotherapy process to post cancer therapy for better immunity booster. Immunotherapy is treatment of disease by activating for biological therapy in suppressing of immune system. Cancer immunotherapy called as immune-oncology from of a cancer treatment that used the power of body immune system to removed, control and prevent cancer. There are mainly 4 type of Immunotherapy Checkpoint inhibitors Chimeric antigen receptor, T - cell therapy Cancer vaccines, And Monoclonal antibodies. There are lots of advantages of Immunotherapy which are described in this paper.","PeriodicalId":8537,"journal":{"name":"Asian Journal of Pharmaceutical Research","volume":"11 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76478993","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
A Review on Covid 19 Pandemic and its Global Effects 新冠肺炎疫情及其全球影响研究综述
Asian Journal of Pharmaceutical Research Pub Date : 2021-11-27 DOI: 10.52711/2231-5691.2021.00042
Kandra Naga Vishnu, Praveen Kumar Uppala, Y. Vangoori, Siva Naga Koteswara Rao Gudhanti
{"title":"A Review on Covid 19 Pandemic and its Global Effects","authors":"Kandra Naga Vishnu, Praveen Kumar Uppala, Y. Vangoori, Siva Naga Koteswara Rao Gudhanti","doi":"10.52711/2231-5691.2021.00042","DOIUrl":"https://doi.org/10.52711/2231-5691.2021.00042","url":null,"abstract":"The novel Corona Virus Disease popularly known as COVID-19 brought all sectors to a temporary standstill since its first outbreak in Wuhan China in 2019. The rapid spread of this disease to all countries of the world made it to be declared a pandemic by the world health organization in the first quarter of the year 2020. This pandemic exposed the world population to the understanding of immunity since that was the only remedy at present to this new pandemic. The morbidity and mortality of this new virus were estimated across the globe by many institutions and organizations. The tropical regions where malaria epidemic is more pronounced is less affected by COVID-19 probably due to high immunity already developed by the population as a result of frequent malaria disease and regular use of anti-malarial drug.","PeriodicalId":8537,"journal":{"name":"Asian Journal of Pharmaceutical Research","volume":"31 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-11-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84165429","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: 9
Analgesic activity of Hydroalcholic extract of Achyranthes aspera leaves on animal model 牛膝水醇提取物对动物模型的镇痛作用
Asian Journal of Pharmaceutical Research Pub Date : 2021-11-27 DOI: 10.52711/2231-5691.2021.00041
K. Shukla, Sourabh Jain, Narendra B. Patil, K. Patil, Kalpesh S. Wagh
{"title":"Analgesic activity of Hydroalcholic extract of Achyranthes aspera leaves on animal model","authors":"K. Shukla, Sourabh Jain, Narendra B. Patil, K. Patil, Kalpesh S. Wagh","doi":"10.52711/2231-5691.2021.00041","DOIUrl":"https://doi.org/10.52711/2231-5691.2021.00041","url":null,"abstract":"Achyranthes aspera L. (Family: Amaranthaceae) is widely used as a medicinal plant. The hydroalcholic extract of Achyranthes aspera L. leaves was screened for its analgesic activity. The dose (200 mg/kg) was tested for analgesic activity using hot plate and Tail flick test in albino mice. The hydroalcholic extract of Achyranthes aspera L. leaves showed maximum analgesic activity in hot plate at reaction time 120 min (7.40±0.08) and tail flick method at reaction time 120 min (6.9±0.06). These study suggest that the hydroalcholic extract of Achyranthes aspera L. could be considered as potential analgesic agent.","PeriodicalId":8537,"journal":{"name":"Asian Journal of Pharmaceutical Research","volume":"78 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-11-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89834570","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
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