Journal of Pharmacology & Pharmaceutical Research最新文献

Effect of Capsaicin on the Barrier Functions of Porcine Intestinal Epithelial Cells (IPEC-J2) 辣椒素对猪肠上皮细胞(IPEC-J2)屏障功能的影响

Journal of Pharmacology & Pharmaceutical Research Pub Date : 2021-12-05 DOI: 10.31038/jppr.2021444

B. España, D. L. Guern, Camille Rozier, C. Prouillac

引用次数: 0

Accommodating Evidence of Traditional Use for Medicines Within Risk-Based Regulation in Australia

Journal of Pharmacology & Pharmaceutical Research Pub Date : 2021-11-26 DOI: 10.31038/jppr.2021442

D. Graham

引用次数: 0

Soybean Phosphatidylcholine-based Nanovesicular Topical Formulation for Non-invasive Treatment of Localized Obesity 基于大豆磷脂酰胆碱的纳米囊泡局部配方用于非侵入性治疗局部肥胖

Journal of Pharmacology & Pharmaceutical Research Pub Date : 2021-09-10 DOI: 10.31038/jppr.2021434

引用次数: 0

Dual Arginine and Glutamic Amino Acids Delivery Effectiveness of Injectable Chitosan-Poloxamer P407 towards Wound Healing Application 壳聚糖-波洛沙姆P407在伤口愈合中的双重精氨酸和谷氨酸递送效果

Journal of Pharmacology & Pharmaceutical Research Pub Date : 2021-09-05 DOI: 10.31038/jppr.2021435

D. Nguyen, L. Dang, Bich Tram Nguyen, N. Tran

引用次数: 0

Rivaroxaban Failure in a SARS-CoV-2 (COVID-19) Positive Patient SARS-CoV-2 (COVID-19)阳性患者利伐沙班治疗失败

Journal of Pharmacology & Pharmaceutical Research Pub Date : 2021-08-30 DOI: 10.31038/jppr.2021433

S. Gopal, K. Kurpad, Geethika Earthineni

引用次数: 0

Utilization of Co-evaporation Technique for Enhancement the Solubility and Dissolution Rate of Etodolac 利用共蒸发技术提高乙酸乙dolac的溶解度和溶出速率

Journal of Pharmacology & Pharmaceutical Research Pub Date : 2021-07-10 DOI: 10.31038/jppr.2021422

Ahmed M Mohammed, Saud Almawash, S. Osman

{"title":"Utilization of Co-evaporation Technique for Enhancement the Solubility and Dissolution Rate of Etodolac","authors":"Ahmed M Mohammed, Saud Almawash, S. Osman","doi":"10.31038/jppr.2021422","DOIUrl":"https://doi.org/10.31038/jppr.2021422","url":null,"abstract":"Etodolac (ETD), a member of non-steroidal anti-inflammatory drugs (NSAIDs), has a poor aqueous solubility. Long term administration of ETD causes severe gastrointestinal disturbances such as peptic ulcer and bleeding. The enhancement of its solubility and dissolution profile is expected to improve its bioavailability and reduce its side effects. In the present study, we tried to enhance the aqueous solubility and dissolution rate of ETD by two co-evaporation techniques. The first one is the formation of solid dispersion with different hydrophilic carriers, including polyethelene glycol (PEG 4000), polyvinyl pyrrolidones (PVP K25 and PVP K90) and urea. The second method is the formation of solid adsorbates using inert carriers such as avecil PH 101, bentonite and aerosil 200 as adsorbents. Co-evaporates were prepared at (1:1 w/w), (1:3 w/w) and (1:5 w/w) ETD to carrier ratios and the corresponding physical mixtures were also prepared. The solubility and dissolution studies of all formulations were measured. Moreover, the physicochemical properties of the modified co-evaporates were characterized using different techniques including, differential scanning calorimetry (DSC), infrared spectroscopy and X-ray diffractometry (XRD) analysis. The results showed that the co-evaporates exhibited higher dissolution rate than the corresponding physical mixtures and both showed higher dissolution rate than the unmodified drug. Increase polymer concentration led to increase in the dissolution rate of drug. Plus, the dissolution rate was enhanced by increasing the temperature of the dissolution medium. Avecil PH 101 exhibited the highest dissolution rate over all other polymers. Infrared studies showed no interaction between the drug and the investigated carrier. The DSC and XRD studies indicated the conversion of ETD to an amorphous state. The enhancement of the drug solubility may be attributed to the increase of drug surface area, the wettability, formation of hydrogen bonds and the conversion to amorphous state.","PeriodicalId":285318,"journal":{"name":"Journal of Pharmacology & Pharmaceutical Research","volume":"455 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2021-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"133846644","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

Cenobamate: New Antiseizure Medication with High Seizure Freedom and Dual Mechanisms of Action 新抗癫痫药物，具有高癫痫发作自由度和双重作用机制

Journal of Pharmacology & Pharmaceutical Research Pub Date : 2021-07-07 DOI: 10.31038/jppr.2021424

Steve S. Chung

引用次数: 0

Inhibition of the Dimerization of SARS-COV-2 Encoded Nucleocapsid Protein by Chlorophyll A, Halothane and Tetraethylene Glycol Monooctyl Ether 叶绿素A、氟烷和四乙二醇单辛基醚对SARS-COV-2编码核衣壳蛋白二聚化的抑制作用

Journal of Pharmacology & Pharmaceutical Research Pub Date : 2020-12-17 DOI: 10.31038/jppr.2020334

Pierre Limtung, H.Y. Lim Tung

{"title":"Inhibition of the Dimerization of SARS-COV-2 Encoded Nucleocapsid Protein by Chlorophyll A, Halothane and Tetraethylene Glycol Monooctyl Ether","authors":"Pierre Limtung, H.Y. Lim Tung","doi":"10.31038/jppr.2020334","DOIUrl":"https://doi.org/10.31038/jppr.2020334","url":null,"abstract":"SARS-COV-2 is the etiologic agent of COVID-19. There is currently no effective remedy for SARS-COV-2 infections or COVID-19. Dimerization of SARS-COV-2 encoded Nucleocapsid protein (NCp) is a prerequisite step for it to act as an essential co-factor for the replication, transcription and packaging of SARS-COV-2 genome. Molecules that prevent the dimerization of NCp are potential prophylactics and therapeutics for the control of SARS-COV-2 infections and virulence. Here, through interrogation of chemical ligand data banks and thermodynamic calculations, we show that Chlorophyll A, Halothane and Tetraethylene glycol monooctyl ether (TGME) are inhibitors of the dimerization of NCp. Chlorophyll A is the most potent inhibitor of NCp dimerization with dissociation constant (K D ) of ~28 pM. Chlorophyll A binding caused the dissociation constant (K D ) for NCp-NCp interaction to increase from ~7.2 pM to ~1000000 pM. Chlorophyll A also bound to NCp mutated at phosphorylation sites S186, S197 and S202 (S186F, S197L and S202N) and phosphorylation recognition sites RNpSTP, (S197L) and RGTpSP (RG203/204KR and RG203/204KT) with dissociation constants of ~12 pM, ~6.1 pM, ~27.8. pM, ~27.8 pM and ~2.2 pM respectively. These results show that Chlorophyll A, a chemical ligand that is present in high abundance with good absorption properties and near-zero toxicity is a potential very potent prophylactic and therapeutic that acts via disruption of NCp dimerization.","PeriodicalId":285318,"journal":{"name":"Journal of Pharmacology & Pharmaceutical Research","volume":"16 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2020-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"127807076","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 of Rivastigmine, a Liquid Drug Substance, for Use in a Simulating Study of Hollow Microstructured Transdermal Delivery System 用于中空微结构透皮给药系统模拟研究的液体原料药利瓦斯他明的配方

Journal of Pharmacology & Pharmaceutical Research Pub Date : 2020-12-08 DOI: 10.31038/jppr.2020333

引用次数: 3

PI3K Signaling Pathway Regulates the Caspase-9 in Renal Tubular Epithelial Cells PI3K信号通路调控肾小管上皮细胞Caspase-9

Journal of Pharmacology & Pharmaceutical Research Pub Date : 2020-11-30 DOI: 10.31038/jppr.2020331

Pei-Fung Wu, Cheng-tse Lee

{"title":"PI3K Signaling Pathway Regulates the Caspase-9 in Renal Tubular Epithelial Cells","authors":"Pei-Fung Wu, Cheng-tse Lee","doi":"10.31038/jppr.2020331","DOIUrl":"https://doi.org/10.31038/jppr.2020331","url":null,"abstract":"Background: To evaluate how resveratrol regulates the IL-6 signaling in renal cell, pCMV6-IL-6 was overexpressed in the renal tubular epithelial cell line NRK-52E. Methods: IHC and TUNEL assay were used to identify the localization and apoptosis detection of the overexpression of IL-6 in NRK-52E cells. To identify the effect of overexpressed IL-6, the mitochondrial fraction was isolated and caspase activities and western blotting were performed. Results: Our results revealed that pCMV6-IL-6 was overexpressed in the nucleus and around the nuclear membrane of the cells. Moreover, the cell membrane showed no IL-6 overexpression, which may be suggest absence of the IL-6/IL-6R binding effect on the cell membrane. Furthermore, the results of the TUNEL assay demonstrated that pCMV6-IL-6-transfected cells showed features of apoptotic cells. The results of the caspase activity assay revealed that resveratrol significantly attenuated IL-6-induced caspase-3 activity but not attenuated IL-6-induced caspase-9 activity, indicating the antiapoptotic ability of resveratrol response on caspase-3 activity. The PI3K inhibitor could decrease the caspase-9 level, suggesting that the reduction of the caspase-9 level mediate by through the PI3K signaling pathway. Conclusions: Taken together, our results demonstrated that IL-6 expression not only in the cytosol but also in the nucleus of renal tubular epithelial cells. The PI3K signaling pathway regulates the caspase-9 in renal tubular epithelial cells.","PeriodicalId":285318,"journal":{"name":"Journal of Pharmacology & Pharmaceutical Research","volume":"15 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2020-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"133537404","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