Al-Azhar Journal of Pharmaceutical Sciences最新文献

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REVIEW ON THE SIGNIFICANCE OF QUINAZOLINONE DERIVATIVES AS POTENT ANTIHYPERGLYCEMIC AGENTS 喹唑啉酮衍生物作为强效降糖药的意义综述
Al-Azhar Journal of Pharmaceutical Sciences Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223768
Helmy M. Sakr
{"title":"REVIEW ON THE SIGNIFICANCE OF QUINAZOLINONE DERIVATIVES AS POTENT ANTIHYPERGLYCEMIC AGENTS","authors":"Helmy M. Sakr","doi":"10.21608/ajps.2022.223768","DOIUrl":"https://doi.org/10.21608/ajps.2022.223768","url":null,"abstract":"Diabetes mellitus is a chronic metabolic disease which is characterized by high blood sugar levels over a prolonged period of time. Uncontrolled hyperglycemia can lead to serious damage to many vital organs in the body, including kidney damage, heart disease, and nerve damage. The goal of treatment of diabetes mellitus is reduction of blood glucose levels and controlling subsequent complications. Different mechanisms are involved in diabetes mellitus treatment. Quinazolinone and its derivatives have been found as effective and versatile pharmacophoric units in medicinal chemistry to design and develop a wide range of bioactive compounds. The present review summarizes the advances in lead compounds of quinazolinone hybrids and their related heterocycles in treatment of diabetes mellitus. Moreover, the review also helps to intensify the drug development process by providing an understanding of the potential role of these hybridized pharmacophoric features in exhibiting the hypoglycemic effect.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"55 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85650066","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
EVALUATION OF ANTIDIABETIC AND ANTI-OBESITY POTENTIAL AND SAFETY OF A POLYHERBAL REMEDY 一种复方中药的抗糖尿病和抗肥胖潜力及安全性评价
Al-Azhar Journal of Pharmaceutical Sciences Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223776
Amal H. Ahmed
{"title":"EVALUATION OF ANTIDIABETIC AND ANTI-OBESITY POTENTIAL AND SAFETY OF A POLYHERBAL REMEDY","authors":"Amal H. Ahmed","doi":"10.21608/ajps.2022.223776","DOIUrl":"https://doi.org/10.21608/ajps.2022.223776","url":null,"abstract":"Objective: To evaluate the antidiabetic and anti-obesity potentials and the safety of a polyherbal remedy. Method: A mixture of polyherbal remedy containing Gymnema sylvestre, Garcinia cambogia, Cleome droserifolia, and Nigella sativa (100 or 200 mg/Kg, p.o.) was subjected to qualitative chemical identification for marker compounds on individual plant extracts using Q-TOF-LC-MS. In addition, the antidiabetic and antiobesity potential were evaluated in streptozotocin-induced diabetic rats using metformin (100 mg/Kg, p.o.) and insulin (10 U/Kg, IP) as standards. The evaluation based on fasting blood glucose level (FBG), insulin level, and change in body weight gain of different treatment groups. Furthermore, the safety profile was assessed by the measurement of certain biochemical, hematological, and histopathological parameters. Results: A total of thirteen marker compounds, (Gymnemoside ND1, Myricetin, Hydroxycitric acid lactone, Garcinol, Garcimangosone D, 5,3`-Dihydroxy-3,6,7,4`,5`pentamethoxyflavone, 5-Hydroxy-3,6,7,3`,4`,5`-hexamethoxyflavone, Magnoflorine, Kaempferol glycoside, Sapindoside B, Alpha-hedrin, Tauroside H2, and Thymoquinone) were identified in the four plant extracts individually. The administration of polyherbal remedy extract (100 or 200 mg/Kg, p.o.)-, metformin-, and insulin-treated diabetic rats resulted in a significant decrease in the FBG by 62, 67, 44 and 73 % respectively, and significant increase in insulin level by 2161, 3433, 2400 and 5658 %, respectively, as compared to vehicle-treated control. Regarding the body weight change, polyherbal remedy extract (100 or 200 mg/Kg, p.o.)-, metformin-, and insulin-treated animals demonstrated a significant decrease by 45, 54, 72 and 65%, respectively, as compared to their initial weight. The results of polyherbal remedy (100 or 200 mg/Kg, p.o.)-treated groups showed a dose-independent potency between that obtained from insulinand metformin-treated groups. Concerning the safety profile; treatment with remedy extracts markedly improved the streptozotocin-induced alteration in the hepatic biochemical, and hematological indices (liver enzymes, total protein, albumin, TC, TG, HDL, LDL, RBCs count, WBCs count, Hb concentration and platelet count) besides preservation of the normal histopathological features of liver, kidney, and pancreas. Conclusion: The polyherbal remedy can be used as an effective and safe treatment of obesity, diabetes, and its complications.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"19 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88039795","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
PRODUCTION OF FATTY ACIDS BY YARROWIA LIPOLYTICA USING AGRO-INDUSTRIAL WASTE AT LOW TEMPERATURE 低温下利用农工废弃物生产脂肪酸的多脂耶氏菌
Al-Azhar Journal of Pharmaceutical Sciences Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223772
Mohamed Al-Hewaily
{"title":"PRODUCTION OF FATTY ACIDS BY YARROWIA LIPOLYTICA USING AGRO-INDUSTRIAL WASTE AT LOW TEMPERATURE","authors":"Mohamed Al-Hewaily","doi":"10.21608/ajps.2022.223772","DOIUrl":"https://doi.org/10.21608/ajps.2022.223772","url":null,"abstract":"Single-cell oil has long been considered an alternative to conventional oil sources. The oil produced can also be used as a feedstock for biodiesel production. In this research, Morphological, microscopical, Biochemical tests and VITEK 2 YST ID card are used to identify most lipid screening yeast isolate named Y4. Many parameters (different Carbone sources, different nitrogen sources, PH, Incubation days, shaking, and statistic incubation) were studied using the optimization of one variable at time (OVAT). On YED agar media, the isolated yeast Yarrowia lipolyticaY4 gave the maximum biomass of 4.15±0.04 g/l, lipid yield of 0.86±0.03 g/l and lipid content of 20.67±0.62 %, respectively. Molasses was utilized as a carbon source and it was supporting both yeast growth and lipid production with two-fold increase biomass of 9.36±0.06 g/l, lipid yield of 1.80±0.18 g/l and lipid content of 19.31±1.81 %. Also, the oil profile by gas chromatography was contain 36.17%, 56.54% and 7.26% of saturated, monounsaturated and polyunsaturated fatty acids after 7 days’ incubation period at refrigerator and, contain 64.21%, 28.40%, and 7.33% of saturated, monounsaturated and polyunsaturated fatty acids after 30 days’ incubation at refrigerator. Consequently, this work study new insights for the economical oil production with valuable profile using cheap agro-industrial waste molasses as a substrate for growth of marine Yarrowia lipolyticaY4 yeast at low temperature 4°C for one week and one month.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"48 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87937444","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
ISOLATION AND CHARACTERIZATION OF CRUDE OIL-DEGRADING BACTERIA FROM PETROLEUM OIL CONTAMINATED EGYPTIAN SOILS 石油污染埃及土壤中原油降解细菌的分离与鉴定
Al-Azhar Journal of Pharmaceutical Sciences Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223771
Sara El-Shennawy
{"title":"ISOLATION AND CHARACTERIZATION OF CRUDE OIL-DEGRADING BACTERIA FROM PETROLEUM OIL CONTAMINATED EGYPTIAN SOILS","authors":"Sara El-Shennawy","doi":"10.21608/ajps.2022.223771","DOIUrl":"https://doi.org/10.21608/ajps.2022.223771","url":null,"abstract":"Eleven bacterial strains were isolated from two different oil contaminated Egyptian soils. They were characterized according to their phenotypic examination as species of the genus Bacillus. These bacterial populations showed counts ranging between 8 and 10 log CFU/g soil on the agar plates. An experimental study was undertaken to assess the efficiency of these bacterial isolates in degradation of the petroleum oil in their culture medium amended with 1% v/v petroleum oil. Results revealed that both CS1.1 and CS1.7 are the most effective isolates to degrade two crude oils from Suez and Agiba Company for the first time by growing the individual isolates separately on oil agar media. In addition, CS1.1and CS1.7 exhibited 55.6% and 53.5%, respectively emulsification activity after 48 hrs. incubation time. Also, isolates CS1.1 and CS1.7 could reduce the surface tension to 36.5 ± 0.25mN/m and 37.5 ± 0.45mN/m, respectively in less than 12 hrs. in glucose based media. The gravimetric analysis revealed that both CS1.1 and CS1.7 isolates were able to degrade the petroleum oil and utilize it as a sole carbon source for growth, energy and reproduction. These isolates, CS1.1 and CS1.7 degraded 65% and 64 % of added petroleum oil respectively, over 15 days incubation time. Also, the change in absorbance values of the tested samples from 0.936 O.D. to 1.832 O.D. compared with the control sample 0.815 O.D. indicates the breakdown of the molecular structure of oil and confirms the degradation of crude oil by bacterial isolates. Physiological and biochemical parameters for those the most potent degrading isolates were determined. They were identified as Bacillus subtilis and Bacillus licheniformis.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"7 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73100871","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
SPECTROPHOTOMETRIC METHODS FOR DETREMINATION OF TOLTRAZURIL IN PRESENCE OF ITS ALKALI-INDUCED DEGRADATION PRODUCT 用分光光度法测定妥曲祖利碱致降解产物的含量
Al-Azhar Journal of Pharmaceutical Sciences Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223769
Amr M. Abdelfatah
{"title":"SPECTROPHOTOMETRIC METHODS FOR DETREMINATION OF TOLTRAZURIL IN PRESENCE OF ITS ALKALI-INDUCED DEGRADATION PRODUCT","authors":"Amr M. Abdelfatah","doi":"10.21608/ajps.2022.223769","DOIUrl":"https://doi.org/10.21608/ajps.2022.223769","url":null,"abstract":"Toltrazuril is a veterinary antiprotozoal drug. In this work, four different simple, accurate, and sensitive spectrophotometric methods have been developed to determine toltrazuril in the presence of its alkali-induced degradation product. Two of these methods depend on selection of two wavelengths at zero order spectrum these methods include (A) dual wavelength method at 239.60 and 257.40 nm, (B) simultaneous equation method at 242.4 nm (λmax of toltrazuril) and 249.8 nm (λmax of toltrazuril degradation product),while the another two methods are (C) area under the curve method at (235245)nm and ( 247-257) nm of toltrazuril and its degradation product and (D) ratio derivative method the absorption spectra of toltrazuril were divided by a suitable absorption spectrum of its degradation product (divisor) and the amplitudes of the first derivative of the ratio spectra at 219 nm were recorded. These methods have been validated for linearity, accuracy and precision and found to be rapid, precise to applied for determination of toltrazuril in Yoserzoril ® suspension.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84730258","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
MICROBIOLOGICAL AND MOLECULAR STUDIES OF SOME GRAM NEGATIVE PATHOGENS CAUSING BLOOD STREAM INFECTIONS IN INTENSIVE CARE UNITS 一些引起重症监护病房血流感染的革兰氏阴性病原体的微生物学和分子研究
Al-Azhar Journal of Pharmaceutical Sciences Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223773
Mohab Sayed
{"title":"MICROBIOLOGICAL AND MOLECULAR STUDIES OF SOME GRAM NEGATIVE PATHOGENS CAUSING BLOOD STREAM INFECTIONS IN INTENSIVE CARE UNITS","authors":"Mohab Sayed","doi":"10.21608/ajps.2022.223773","DOIUrl":"https://doi.org/10.21608/ajps.2022.223773","url":null,"abstract":"Bloodstream infections (BSIs) and especially central line associated bloodstream infections (CLABSIs), are increasing globally as an important cause of morbidity and mortality. The condition can be life threatening in critically ill patients in the intensive care units (ICUs) of the hospitals. There are serious concerns about the rapid increase of multidrug resistant Gram negative bacteria (MDR-GNB) such as Escherichia coli, Klebsiella pneumonia and Acinetobacter baumannii as the major causes of bloodstream infections. The aim of the study was to emphasize on the significance of MDR-GNB, determine their antibiotic susceptibility pattern, genotypic identification as well as the detection of some virulence genes. Blood specimens were collected from 231 bacteremic patients admitted to different ICUs at three tertiary care hospitals in Egypt. Recovered bacterial isolates were subjected to biochemical identification using conventional methods. Antimicrobial susceptibility testing was performed on Gram negative isolates using both Kirby-Bauer disc diffusion method and Vitek-2 system. Thirty MDR-GNB isolates were selected and screened for the presence of 16S-23S rRNA, UIDA and OMPA genes using PCR assays to confirm their identification. Also, the thirty isolates were screened for the presence of East-1, Cnf-1, IutA and FyuA genes. A total of 185 clinical isolates were recovered from 185 positive blood specimens. Laboratory examination of the positive blood culture specimens revealed that 120 (64.4%), 56 (30.2 %) and 9 (4.8%) were Gram negative, Gram positive and Candida spp., respectively. Thirty MDR-GNB were selected and their antimicrobial susceptibility was compared using the conventional and the Vitek-2 system. For the K. pneumoniae isolates 100% Categorical agreement (CA) was detected for Ceftriaxone, Cefepime, Gentamicin, Amikacin and Tetracycline. For the E. coli CA of (100%) was seen for Ampicillin+Sulbactam, Cefepime, Amikacin, Ciprofloxacin and Tigecycline. categorical agreement (100%) was seen with the tested antibiotics for A. baumannii. Genotypic confirmation of the selected MDR isolates indicated the presence of genes used for identification in all of them. As for the harboring of virulence genes, EAST-1 gene has only been found in 13.3% of the isolates. CNF-1 gene has been identified in 66.6% of the isolates, IutA gene has been found in 96.6% of the isolates and FyuA has been found in 90% of the isolates. Gram negative pathogens were found to be the major bacteria causing bloodstream infection. Vitek-2 system provide accurate antimicrobial susceptibility testing results. CNF-1 toxin production related gene was found to be Az. J. Pharm Sci. Vol. 65, March, 2022. 149 prevalent in most of the isolates. IutA and FyuA siderophore formation related genes were found to be prevalent in most of the isolates.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"12 1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80404692","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
EFFECT OF DIFFERENT PLANT GROWTH REGULATORS ON PLANT REGENERATION AND CALLUS INDUCTION OF PLUMBAGO AURICULATA AND SOME SECONDARY METABOLITES CONTENT 不同植物生长调节剂对木丹植株再生和愈伤组织诱导及次生代谢产物含量的影响
Al-Azhar Journal of Pharmaceutical Sciences Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223767
Abdelrahman Nabil
{"title":"EFFECT OF DIFFERENT PLANT GROWTH REGULATORS ON PLANT REGENERATION AND CALLUS INDUCTION OF PLUMBAGO AURICULATA AND SOME SECONDARY METABOLITES CONTENT","authors":"Abdelrahman Nabil","doi":"10.21608/ajps.2022.223767","DOIUrl":"https://doi.org/10.21608/ajps.2022.223767","url":null,"abstract":"Plumbago becomes one of the essential medicinal, and decorative plants belonging to the family plumbaginaceae due to the present of plumbagin a secondary metabolite. In this study, the nodal segments of shoots of Plumbago auriculata were used as an explant in establishing in vitro cultures. In vitro callus initiation and shoot regeneration was studied using mixtures of auxins, antiauxins (pChlorophenoxyisobutyric acid and 2,3,5-triiodobenzoic acid), and cytokinins. The medium comprising one mg/l PCIB and 0.5 mg/l BA produced the most significant outcomes in the case of callus induction. However, the best shooting number was given (11.18) with the same combination after eight weeks. According to the data, the leaves extract had the highest level of polyphenols (742.6 mg/100g.d. w) and flavonoids (563.9 mg/100g.d. w).","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75305595","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 DIHYDROCHALCONE AND SGLT2 INHIBITOR ABATE METHOTREXATE HEPATOTOXICITY IN MALE RATS; A COMPARATIVE STUDY 二氢查尔酮和sglt2抑制剂对甲氨蝶呤肝毒性的影响比较研究
Al-Azhar Journal of Pharmaceutical Sciences Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223775
Adel T Osman
{"title":"A DIHYDROCHALCONE AND SGLT2 INHIBITOR ABATE METHOTREXATE HEPATOTOXICITY IN MALE RATS; A COMPARATIVE STUDY","authors":"Adel T Osman","doi":"10.21608/ajps.2022.223775","DOIUrl":"https://doi.org/10.21608/ajps.2022.223775","url":null,"abstract":"1 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Assiut 71524, Egypt. 2 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt. 3 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Nahda University, Beni-Suef 62514, Egypt. 4 Department of Pharmacology & Toxicology, Faculty of Pharmacy, Deraya University, Minya 61519, Egypt. Corresponding author E-mail: adelosman.45@azhar.edu.eg ABSTRACT","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88153914","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
TWO DIFFERENT CHROMATOGRAPHIC METHODS FOR SIMULTANEOUS DETERMINATION OF COMMON COLD DRUGS AMBROXOL HYDROCHLORIDE, PSEUDOEPHEDRINE HYDROCHLORIDE, LEVOCETERIZINE DIHYDROCHLORIDE AND DESLORATADINE, IN PURE FORMS, AND IN PHARMACEUTICAL DOSAGE FORMS. 常用感冒药盐酸氨溴索、盐酸伪麻黄碱、盐酸左西替嗪和地氯雷他定纯剂型和制剂剂型的两种不同色谱法同时测定。
Al-Azhar Journal of Pharmaceutical Sciences Pub Date : 2022-03-01 DOI: 10.21608/ajps.2022.223770
Amany Morsi
{"title":"TWO DIFFERENT CHROMATOGRAPHIC METHODS FOR SIMULTANEOUS DETERMINATION OF COMMON COLD DRUGS AMBROXOL HYDROCHLORIDE, PSEUDOEPHEDRINE HYDROCHLORIDE, LEVOCETERIZINE DIHYDROCHLORIDE AND DESLORATADINE, IN PURE FORMS, AND IN PHARMACEUTICAL DOSAGE FORMS.","authors":"Amany Morsi","doi":"10.21608/ajps.2022.223770","DOIUrl":"https://doi.org/10.21608/ajps.2022.223770","url":null,"abstract":"Two chromatographic methods were developed for simultaneous determination of some drugs used in common cold. First method is TLC-Densitometric method for the simultaneous estimation of Ambroxol hydrochloride (AMB), Pseudoephedrine hydrochloride (PSE) and Desloratadine (DES) in pure form and in pharmaceutical dosage form, the best resolution was obtained by the use of mobile phase (Ethyl acetate: methanol: ammonia), (14: 0.8: 0.5, v/v/v), the scanning of spots was performed at 254 nm in concentration range (1-40 ug/spot), (5-35 ug/spot),(0.2-2) ug/spot for AMB, PSE and DES, respectively. With LOD 0.262, 0.358 and 0.006 ug/ml. And LOQ 0.793, 1.09 and 0.018 ug /ml for AMB, PSE and DES, respectively. Second method is HPLC-UV Method for the Simultaneous determination of Ambroxol hydrochloride(AMB),Pseudoephedrine hydrochloride(PSE), Desloratadine (DES) and levoceterizine dihydrochloride (LVC) in quaternary mixture by using mobile phase consisted of acetonitrile: 0.01 M phosphate buffer (PH 5.5) (50:50, v/v) in an isocratic mode through inertsil C8 (250mm x 4.6mm, 5 μ) column at a flow rate of 1.3 ml/min. UV detection was carried out at 215 nm in concentration range (1.6-40), (3.2-40) , (0.69), (2.4-8.4 ) ug/ml for AMB, PSE , DES and LVC, respectively .With LOD 0.428, 0.180, 0.125 and 0.124, ug/ml And LOQ 1.299 , 0.550, 0.379, and 0.375ug/ml for AMB, PSE , DES and LVC, respectively The validation of the proposed methods was done according to ICH guidelines.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"14 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82584799","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
SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL PYRAZOLO[3,4-D]PYRIMIDINE DERIVATIVES OF EXPECTED ANTICANCER ACTIVITY 具有抗癌活性的新型吡唑[3,4- d]嘧啶衍生物的合成及生物学评价
Al-Azhar Journal of Pharmaceutical Sciences Pub Date : 2021-03-01 DOI: 10.21608/AJPS.2021.153563
Farag F. Sherbiny
{"title":"SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL PYRAZOLO[3,4-D]PYRIMIDINE DERIVATIVES OF EXPECTED ANTICANCER ACTIVITY","authors":"Farag F. Sherbiny","doi":"10.21608/AJPS.2021.153563","DOIUrl":"https://doi.org/10.21608/AJPS.2021.153563","url":null,"abstract":"A series of novel pyrazolo[3,4-d]pyrimidine derivatives have been designed based on chemical modifications on the general features of the reported and clinically used EGFR-TKIs such as repalcing of quinazoline moiety of reported EGFR-TKIs as erlotinib by pyrazolo[3,4-d]pyrimidine nucleus,introducing different hydrophobic moieties including phenyl, aromatic heterocyclic, fused aromatic or aliphatic structures , introducing different linkers which may be one atom , two atoms, three atoms, four atoms and five atoms and introducing of phenyl ring at position-3 of 1H-pyrazolo[3,4d]pyrimidine nucleus to occupy the hydrophobic region II of ATP binding site. All the new synthesized compounds were biologically screened in vitro for their cytotoxic activities against four cancer cell lines namely, HepG-2, MCF-7, HCT-116, and Hela. The results of cytotoxic evaluation indicated that compound VI was found to be the most prominent broad-spectrum cytotoxic activity and significantly more potent than doxorubicin with IC50 values of 6.18, 6.48, 4.03, and 5.82μM against tested cell lines. In addition, compounds IXa,b displayed promising cytotoxic effect against all tested cell lines with IC50 values less than 30 μM compared with doxorubicin as a control drug. Besides, compound X possessed excellent anti-proliferative activities against the four cell lines with IC50 values ranging from 18 μM to 39.5 μM. Structural pharmacophoric features indicated that pyrazolo[3,4-d]pyrimidine scaffold having a four atoms linker as thiosemicarbazide moiety as compounds IXa,b which substituted with aliphatic moiety at the 4-position was more potent than those possessing one atom, two atoms, three atoms and five atoms linkers which lead to significant decrease in cytotoxic","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"34 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76170698","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
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