Results in pharma sciences最新文献

筛选
英文 中文
Glycosylation improves α-chymotrypsin stability upon encapsulation in poly(lactic-co-glycolic)acid microspheres 糖基化提高了聚乳酸-羟基乙酸微球包封α-凝乳胰蛋白酶的稳定性
Results in pharma sciences Pub Date : 2012-01-01 DOI: 10.1016/j.rinphs.2012.08.001
Giselle M. Flores-Fernández, Kai Griebenow
{"title":"Glycosylation improves α-chymotrypsin stability upon encapsulation in poly(lactic-co-glycolic)acid microspheres","authors":"Giselle M. Flores-Fernández,&nbsp;Kai Griebenow","doi":"10.1016/j.rinphs.2012.08.001","DOIUrl":"10.1016/j.rinphs.2012.08.001","url":null,"abstract":"<div><p>Enhancing protein stability upon encapsulation and release from polymers is a key issue in sustained release applications. In addition, optimum drug dispersion in the polymer particles is critical for achieving release profiles with low unwanted initial “burst” release. Herein, we address both issues by formulating the model enzyme α-chymotrypsin (α-CT) as nanoparticles to improve drug dispersion and by covalently modifying it with glycans to afford improved stability during encapsulation in poly(lactic-co-glycolic) acid (PLGA) microspheres. α-CT was chemically modified with activated lactose (500<!--> <!-->Da) to achieve molar ratios of 4.5 and 7.1 lactose-to-protein. The bioconjugates were co-lyophilized with methyl-β-cyclodextrin followed by suspension in ethyl acetate to afford nanoparticles. Nanoparticle formation did not significantly impact protein stability; less than 5% of the protein was aggregated and the residual activity remained above 90% for all formulations. Using a solid-in-oil-in-water (s/o/w) methodology developed in our laboratory for nanoparticles, we obtained a maximum encapsulation efficiency of 61%. Glycosylation completely prevented otherwise substantial protein aggregation and activity loss during encapsulation of the non-modified enzyme. Moreover, <em>in vitro</em> protein release was improved for glycosylated formulations. These results highlight the potential of chemical glycosylation to improve the stability of pharmaceutical proteins in sustained release applications.</p></div>","PeriodicalId":89718,"journal":{"name":"Results in pharma sciences","volume":"2 ","pages":"Pages 46-51"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.rinphs.2012.08.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31248101","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 19
Polymer excipients enable sustained drug release in low pH from mechanically strong inorganic geopolymers 聚合物赋形剂可以使机械强度高的无机地聚合物在低pH下持续释放药物
Results in pharma sciences Pub Date : 2012-01-01 DOI: 10.1016/j.rinphs.2012.02.001
Erik Jämstorp , Tejaswi Yarra , Bing Cai , Håkan Engqvist , Susanne Bredenberg , Maria Strømme
{"title":"Polymer excipients enable sustained drug release in low pH from mechanically strong inorganic geopolymers","authors":"Erik Jämstorp ,&nbsp;Tejaswi Yarra ,&nbsp;Bing Cai ,&nbsp;Håkan Engqvist ,&nbsp;Susanne Bredenberg ,&nbsp;Maria Strømme","doi":"10.1016/j.rinphs.2012.02.001","DOIUrl":"10.1016/j.rinphs.2012.02.001","url":null,"abstract":"<div><p>Improving acid resistance, while maintaining the excellent mechanical stability is crucial in the development of a sustained and safe oral geopolymer dosage form for highly potent opioids. In the present work, commercially available Methacrylic acid–ethyl acrylate copolymer, Polyethylene-glycol (PEG) and Alginate polymer excipients were included in dissolved or powder form in geopolymer pellets to improve the release properties of Zolpidem, herein acting as a model drug for the highly potent opioid Fentanyl. Scanning electron microscopy, compression strength tests and drug release experiments, in gastric pH 1 and intestinal pH 6.8 conditions, were performed. The polymer excipients, with an exception for PEG, reduced the drug release rate in pH 1 due to their ability to keep the pellets in shape, in combination with the introduction of an insoluble excipient, and thereby maintain a barrier towards drug diffusion and release. Neither geopolymer compression strength nor the release in pH 6.8 was considerably impaired by the incorporation of the polymer excipients. The geopolymer/polymer composites combine high mechanical strength and good release properties under both gastric and intestinal pH conditions, and are therefore promising oral dosage forms for sustained release of highly potent opioids.</p></div>","PeriodicalId":89718,"journal":{"name":"Results in pharma sciences","volume":"2 ","pages":"Pages 23-28"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.rinphs.2012.02.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33116488","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 15
Release behavior of trans,trans-farnesol entrapped in amorphous silica capsules 反式、反式法尼醇在无定形硅胶胶囊中的释放行为
Results in pharma sciences Pub Date : 2012-01-01 DOI: 10.1016/j.rinphs.2012.07.001
Filipa L. Sousa , Sara Horta , Magda Santos , Sílvia M. Rocha , Tito Trindade
{"title":"Release behavior of trans,trans-farnesol entrapped in amorphous silica capsules","authors":"Filipa L. Sousa ,&nbsp;Sara Horta ,&nbsp;Magda Santos ,&nbsp;Sílvia M. Rocha ,&nbsp;Tito Trindade","doi":"10.1016/j.rinphs.2012.07.001","DOIUrl":"10.1016/j.rinphs.2012.07.001","url":null,"abstract":"<div><p>Farnesol, a compound widely found in several agro-food by-products, is an important bioactive agent that can be exploited in cosmetics and pharmaceutics but the direct bioapplication of this compound is limited by its volatility. Here the entrapment of farnesol in silica capsules was investigated to control the release of this bioactive compound in the vapor phase and in ethanol solutions. The preparation of silica capsules with oil cores was obtained by employing a sol–gel method using O/W/O multiple emulsions. Two distinct chemical vehicles for farnesol have been investigated, retinol and oleic acid, that afterwards have been emulsified as internal oil phases. The volatile release of farnesol from the as-prepared SiO<sub>2</sub> capsules was investigated by headspace solid phase microextraction (HS-SPME) followed by gas chromatographic analysis (GC), and the release to ethanol was carried out by direct injection of the ethanolic fraction into the GC system. It is demonstrated that these capsules are efficient for the long controlled release of farnesol and that the respective profiles depend on the chemical parameters employed in the synthesis of the capsules.</p></div>","PeriodicalId":89718,"journal":{"name":"Results in pharma sciences","volume":"2 ","pages":"Pages 52-56"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.rinphs.2012.07.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33116491","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 11
Applying terahertz technology for nondestructive detection of crack initiation in a film-coated layer on a swelling tablet 应用太赫兹技术无损检测溶胀片膜包覆层起裂
Results in pharma sciences Pub Date : 2012-01-01 DOI: 10.1016/j.rinphs.2012.04.001
Wataru Momose , Hiroyuki Yoshino , Yoshifumi Katakawa , Kazunari Yamashita , Keiji Imai , Kazuhiro Sako , Eiji Kato , Akiyoshi Irisawa , Etsuo Yonemochi , Katsuhide Terada
{"title":"Applying terahertz technology for nondestructive detection of crack initiation in a film-coated layer on a swelling tablet","authors":"Wataru Momose ,&nbsp;Hiroyuki Yoshino ,&nbsp;Yoshifumi Katakawa ,&nbsp;Kazunari Yamashita ,&nbsp;Keiji Imai ,&nbsp;Kazuhiro Sako ,&nbsp;Eiji Kato ,&nbsp;Akiyoshi Irisawa ,&nbsp;Etsuo Yonemochi ,&nbsp;Katsuhide Terada","doi":"10.1016/j.rinphs.2012.04.001","DOIUrl":"10.1016/j.rinphs.2012.04.001","url":null,"abstract":"<div><p>Here, we describe a nondestructive approach using terahertz wave to detect crack initiation in a film-coated layer on a drug tablet. During scale-up and scale-down of the film coating process, differences in film density and gaps between the film-coated layer and the uncoated tablet were generated due to differences in film coating process parameters, such as the tablet-filling rate in the coating machine, spray pressure, and gas–liquid ratio etc. Tablets using the PEO/PEG formulation were employed as uncoated tablets. We found that heat and humidity caused tablets to swell, thereby breaking the film-coated layer. Using our novel approach with terahertz wave nondestructively detect film surface density (<em>FSD</em>) and interface density differences (<em>IDD</em>s) between the film-coated layer and an uncoated tablet. We also found that a reduced <em>FSD</em> and <em>IDD</em> between the film-coated layer and uncoated tablet increased the risk of crack initiation in the film-coated layer, thereby enabling us to nondestructively predict initiation of cracks in the film-coated layer. Using this method, crack initiation can be nondestructively assessed in swelling tablets after the film coating process without conducting accelerated stability tests, and film coating process parameters during scale-up and scale-down studies can be appropriately established.</p></div>","PeriodicalId":89718,"journal":{"name":"Results in pharma sciences","volume":"2 ","pages":"Pages 29-37"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.rinphs.2012.04.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33116489","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 23
Moxifloxacin in situ gelling microparticles–bioadhesive delivery system 莫西沙星原位胶凝微颗粒-生物胶粘剂给药系统
Results in pharma sciences Pub Date : 2012-01-01 DOI: 10.1016/j.rinphs.2012.09.002
Qiongyu Guo , Ahmed Aly , Oliver Schein , Morgana M. Trexler , Jennifer H. Elisseeff
{"title":"Moxifloxacin in situ gelling microparticles–bioadhesive delivery system","authors":"Qiongyu Guo ,&nbsp;Ahmed Aly ,&nbsp;Oliver Schein ,&nbsp;Morgana M. Trexler ,&nbsp;Jennifer H. Elisseeff","doi":"10.1016/j.rinphs.2012.09.002","DOIUrl":"10.1016/j.rinphs.2012.09.002","url":null,"abstract":"<div><p>Antibiotic use for ocular treatments has been largely limited by poor local bioavailability with conventional eyedrops formulations. Here, we developed a controlled delivery system composed of moxifloxacin-loaded poly(lactic-co-glycolic acid) (PLGA) microparticles encapsulated in a chondroitin sulfate-based, two-component bioadhesive hydrogel. Using a simple and fast electrohydrodynamic spray drying (electrospraying) technique, surfactant-free moxifloxacin-loaded microparticles were fabricated with diameters on the order of 1<!--> <!-->μm. A mixed solvent system of methanol/dichloromethane (MeOH/DCM) was employed to prepare the microparticles for the electrospraying processing. Extended release of moxifloxacin using a series of MeOH/DCM mixed solvents was accomplished over 10 days with release concentrations higher than the minimum inhibitory concentration (MIC). In contrast, moxifloxacin loaded directly in hydrogels was released rapidly within 24<!--> <!-->h. We observed a decrease of the drug release rate from the microparticles when using an increased percentage of methanol in the mixed solvent from 10% to 30% (v/v), which can be explained by the mixed solvent system providing a driving force to form a gradient of the drug concentrations inside the microparticles. In addition, the delivery system developed in this study, which incorporates a bioadhesive to localize drug release by <em>in situ</em> gelling, may potentially integrate antibiotic prophylaxis and wound healing in the eye.</p></div>","PeriodicalId":89718,"journal":{"name":"Results in pharma sciences","volume":"2 ","pages":"Pages 66-71"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.rinphs.2012.09.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"33116493","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 14
Two-step nanoprecipitation for the production of protein-loaded PLGA nanospheres 两步纳米沉淀法制备载蛋白PLGA纳米球
Results in pharma sciences Pub Date : 2012-01-01 DOI: 10.1016/j.rinphs.2012.11.001
Moraima Morales-Cruz, Giselle M. Flores-Fernández, Myreisa Morales-Cruz, Elsie A. Orellano, José A. Rodriguez-Martinez, Mercedes Ruiz, Kai Griebenow
{"title":"Two-step nanoprecipitation for the production of protein-loaded PLGA nanospheres","authors":"Moraima Morales-Cruz,&nbsp;Giselle M. Flores-Fernández,&nbsp;Myreisa Morales-Cruz,&nbsp;Elsie A. Orellano,&nbsp;José A. Rodriguez-Martinez,&nbsp;Mercedes Ruiz,&nbsp;Kai Griebenow","doi":"10.1016/j.rinphs.2012.11.001","DOIUrl":"10.1016/j.rinphs.2012.11.001","url":null,"abstract":"<div><p>One of the first methods to encapsulate drugs within polymer nanospheres was developed by Fessi and coworkers in 1989 and consisted of one-step nanoprecipitation based on solvent displacement. However, proteins are poorly encapsulated within polymer nanoparticles using this method because of their limited solubility in organic solvents. To overcome this limitation, we developed a two-step nanoprecipitation method and encapsulated various proteins with high efficiency into poly(lactic-<em>co</em>-glycolic)acid (PLGA) nanospheres (NP). In this method, a protein nanoprecipitation step is used first followed by a second polymer nanoprecipitation step. Two model enzymes, lysozyme and α-chymotrypsin, were used for the optimization of the method. We obtained encapsulation efficiencies of &gt;70%, an amount of buffer-insoluble protein aggregates of typically &lt;2%, and a high residual activity of typically &gt;90%. The optimum conditions identified for lysozyme were used to successfully encapsulate cytochrome <em>c</em>(Cyt-c), an apoptosis-initiating basic protein of similar size, to verify reproducibility of the encapsulation procedure. The size of the Cyt-c loaded-PLGA nanospheres was around 300–400<!--> <!-->nm indicating the potential of the delivery system to passively target tumors. Cell viability studies, using a human cervical cancer cell line (HeLa), demonstrate excellent biocompatibility of the PLGA nanoparticles. PLGA nanoparticles carrying encapsulated Cyt-c were not efficient in causing apoptosis presumably because PLGA nanoparticles are not efficiently taken up by the cells. Future systems will have to be optimized to ascertain efficient cellular uptake of the nanoparticles by, e.g., surface modification with receptor ligands.</p></div>","PeriodicalId":89718,"journal":{"name":"Results in pharma sciences","volume":"2 ","pages":"Pages 79-85"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.rinphs.2012.11.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"31158884","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 77
The differences between the branded and generic medicines using solid dosage forms: In-vitro dissolution testing 使用固体剂型的品牌药和仿制药之间的差异:体外溶出度测试
Results in pharma sciences Pub Date : 2012-01-01 DOI: 10.1016/j.rinphs.2011.12.001
Mubarak Nasser Al Ameri , Nanda Nayuni , K.G. Anil Kumar , David Perrett , Arthur Tucker , Atholl Johnston
{"title":"The differences between the branded and generic medicines using solid dosage forms: In-vitro dissolution testing","authors":"Mubarak Nasser Al Ameri ,&nbsp;Nanda Nayuni ,&nbsp;K.G. Anil Kumar ,&nbsp;David Perrett ,&nbsp;Arthur Tucker ,&nbsp;Atholl Johnston","doi":"10.1016/j.rinphs.2011.12.001","DOIUrl":"10.1016/j.rinphs.2011.12.001","url":null,"abstract":"<div><h3>Introduction</h3><p>Dissolution is the amount of substance that goes into solution per unit time under standardised conditions of liquid/solid interface, solvent composition and temperature. Dissolution is one of the most important tools to predict the <em>in-vivo</em> bioavailability and in some cases to determine bioequivalence and assure interchangeability.</p></div><div><h3>Aim</h3><p>To compare the differences in dissolution behaviour of solid dosage forms between innovators (reference products) and their generic counterparts (tested products).</p></div><div><h3>Methods</h3><p>Four replicates for each batch of 37 tested medicines was carried out using A PT-DT70 dissolution tester from Pharma Test. A total of 13 branded medicines and 24 generic counterparts were obtained locally and internationally to detect any differences in their dissolution behaviour. They were tested according to the British Pharmacopeia, European Pharmacopeia and the US Pharmacopeia with the rate of dissolution determined by ultra-violet Spectrophotometery.</p></div><div><h3>Results</h3><p>Most tested medicines complied with the pharmacopoeial specifications and achieved 85% dissolution in 60<!--> <!-->min. However, some generic medicines showed significant differences in dissolution rate at 60 and 120<!--> <!-->min. Many generic medicines showed a slower dissolution rate than their branded counterparts such as the generic forms of omeprazole 20<!--> <!-->mg. Some showed an incomplete dissolution such as the generic form of nifedipine 10<!--> <!-->mg. Other generics showed faster dissolution rate than their branded counterpart such as the generic forms of meloxicam 15<!--> <!-->mg. Moreover, some generics from different batches of the same manufacturer showed significant differences in their dissolution rate such as the generic forms of meloxicam 7.5<!--> <!-->mg. Nevertheless, some generic medicines violated the EMA and the FDA guidelines for industry when they failed to achieve 85% dissolution at 60<!--> <!-->min, such as the generic form of diclofenac sodium 50<!--> <!-->mg.</p></div><div><h3>Conclusion</h3><p>Most medicines in this study complied with the pharmacopeial limits. However, some generics dissolved differently than their branded counterparts. This can clearly question the interchangeability between the branded and its generic counterpart or even among generics.</p></div>","PeriodicalId":89718,"journal":{"name":"Results in pharma sciences","volume":"2 ","pages":"Pages 1-8"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.rinphs.2011.12.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32998628","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 47
Oil-in-water emulsion lotion providing controlled release using 2-methacryloyloxyethyl phosphorylcholine n-butyl methacrylate copolymer as emulsifier 以2-甲基丙烯酰氧乙基磷酸胆碱正甲基丙烯酸丁酯共聚物为乳化剂,具有控释效果的水包油乳液
Results in pharma sciences Pub Date : 2012-01-01 DOI: 10.1016/j.rinphs.2012.01.001
Akiko Ishikawa, Makiko Fujii, Kumi Morimoto, Tomomi Yamada, Naoya Koizumi, Masuo Kondoh, Yoshiteru Watanabe
{"title":"Oil-in-water emulsion lotion providing controlled release using 2-methacryloyloxyethyl phosphorylcholine n-butyl methacrylate copolymer as emulsifier","authors":"Akiko Ishikawa,&nbsp;Makiko Fujii,&nbsp;Kumi Morimoto,&nbsp;Tomomi Yamada,&nbsp;Naoya Koizumi,&nbsp;Masuo Kondoh,&nbsp;Yoshiteru Watanabe","doi":"10.1016/j.rinphs.2012.01.001","DOIUrl":"10.1016/j.rinphs.2012.01.001","url":null,"abstract":"<div><p>Lotion is a useful vehicle for active ingredients used to treat skin disease because it can be applied to the scalp, can cover large areas of skin, and it is easy to spread due to low viscosity. An emulsion lotion (EL) containing 2-methacryloyloxyethyl phosphorylcholine n-butyl methacrylate copolymer (PMB) as an emulsifier that provides controlled-release was developed. Diphenhydramine (DPH) was used as a model drug. Formulation with 5% DPH, 5% soybean oil, and 4% PMB in water was emulsified using a high-pressure homogenizer. Polysorbate 80 (TO) was used instead of PMB for comparison. They were applied <em>in vitro</em> to Yucatan micropig intact or stripped skin at a practical dose (2<!--> <!-->μL/cm<sup>2</sup>). For stripped skin, penetration of DPH from 4% PMB EL was slower than that from 1% TO EL; results for intact skin were similar. The same phenomenon was observed with application to rabbit skin <em>in vivo</em>. When 4% PMB EL dried on the skin, it made a thin film matrix incorporating the oil phase, which controlled the release of DPH. The release rate could be controlled by the ratio of oil phase to PMB. The EL with PMB shows promise as a vehicle for long-acting treatment of skin diseases.</p></div>","PeriodicalId":89718,"journal":{"name":"Results in pharma sciences","volume":"2 ","pages":"Pages 16-22"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.rinphs.2012.01.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32998630","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 8
Inclusion complex of a new propiconazole derivative with β-cyclodextrin: NMR, ESI–MS and preliminary pharmacological studies 新型丙环唑衍生物与β-环糊精包合物的NMR、ESI-MS及初步药理研究
Results in pharma sciences Pub Date : 2011-05-01 DOI: 10.1016/j.rinphs.2011.07.001
Narcisa Marangoci , Mihai Mares , Mihaela Silion , Adrian Fifere , Cristian Varganici , Alina Nicolescu , Calin Deleanu , Adina Coroaba , Mariana Pinteala , Bogdan C. Simionescu
{"title":"Inclusion complex of a new propiconazole derivative with β-cyclodextrin: NMR, ESI–MS and preliminary pharmacological studies","authors":"Narcisa Marangoci ,&nbsp;Mihai Mares ,&nbsp;Mihaela Silion ,&nbsp;Adrian Fifere ,&nbsp;Cristian Varganici ,&nbsp;Alina Nicolescu ,&nbsp;Calin Deleanu ,&nbsp;Adina Coroaba ,&nbsp;Mariana Pinteala ,&nbsp;Bogdan C. Simionescu","doi":"10.1016/j.rinphs.2011.07.001","DOIUrl":"10.1016/j.rinphs.2011.07.001","url":null,"abstract":"<div><p>A novel inclusion complex of the propiconazole nitrate (NO<sub>3</sub>PCZ) with β-cyclodextrin (β-CD) was prepared by treatment of propiconazole (PCZ) with an acidic nitrating agent. The formation of NO<sub>3</sub>PCZ and its inclusion complex with β-CD has been studied by NMR, ESI–MS, TGA, DSC methods. Using the undecoupled signal in the HMBC correlation spectra, almost identical coupling constants of CH from trizolic ring of PCZ and NO<sub>3</sub>PCZ compounds (<sup>1</sup>J(HC)3=207<!--> <!-->Hz, <sup>1</sup>J(CH)5=214<!--> <!-->Hz, for PCZ; <sup>1</sup>J(HC)3=208<!--> <!-->Hz and <sup>1</sup>J(CH)5=215<!--> <!-->Hz, for NO<sub>3</sub>PCZ) were determined, confirming that the geometry of the heterocyclic skeleton is identical in both the forms. The 1:1 stoichiometry of the complex was determined by ESI–MS and was confirmed using Scott's equation in DMSO and Higuchi and Connors equation in water. The solubility curve obtained for NO<sub>3</sub>PCZ in presence of β-CD in distilled water was constructed, resulting in a solubility diagram of AL type. Solubility of NO<sub>3</sub>PCZ in water was determined by DLS studies. The results showed that NO<sub>3</sub>PCZ was encapsulated within the β-CD cavity with a binding constant of 330 M-1 in DMSO and 975 M-1 in water. Preliminary pharmacological studies showed higher antifungal activities for NO<sub>3</sub>PCZ and its inclusion complex, compared with its PCZ analog. The acute toxicity of the complex is smaller than the pure or modified drug, recommending the inclusion complex as future promising therapeutic agents.</p></div>","PeriodicalId":89718,"journal":{"name":"Results in pharma sciences","volume":"1 1","pages":"Pages 27-37"},"PeriodicalIF":0.0,"publicationDate":"2011-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.rinphs.2011.07.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32992937","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 34
Oral bioavailability of a poorly aqueous drug from three different SBE7-β-cyclodextrin based formulations in beagle dogs 三种不同SBE7-β-环糊精配方的差水药物在比格犬中的口服生物利用度
Results in pharma sciences Pub Date : 2011-05-01 DOI: 10.1016/j.rinphs.2011.09.001
René Holm , Lene Andresen , Claus Strange
{"title":"Oral bioavailability of a poorly aqueous drug from three different SBE7-β-cyclodextrin based formulations in beagle dogs","authors":"René Holm ,&nbsp;Lene Andresen ,&nbsp;Claus Strange","doi":"10.1016/j.rinphs.2011.09.001","DOIUrl":"10.1016/j.rinphs.2011.09.001","url":null,"abstract":"<div><p>Oral administration of Lu 35-138, a low aqueous soluble compound, was investigated in three different formulations containing sulfobutylether β-cyclodextrin (SBE<sub>7</sub>βCD) in fasted beagle dogs. The evaluated formulations was (i) a SBE<sub>7</sub>βCD solution, (ii) a spray dried solution filled into hard gelatine capsules, and (iii) a direct compressible tablet containing SBE<sub>7</sub>βCD. The three formulations did not lead any significant differences in the obtained AUCs, though a trend was observed for the highest absorption when Lu 35-138 was dosed in the cyclodextrin solution. These results demonstrate that a solid formulation with a relative low content of cyclodextrins can be used to increase the bioavailability of a low water soluble compound to a relative high level when compared to a cyclodextrin solution.</p></div>","PeriodicalId":89718,"journal":{"name":"Results in pharma sciences","volume":"1 1","pages":"Pages 57-59"},"PeriodicalIF":0.0,"publicationDate":"2011-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.rinphs.2011.09.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32992940","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 4
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信