ISRN Pharmaceutics最新文献_第7页

Morphology and release kinetics of protein-loaded porous poly(l-lactic Acid) spheres prepared by freeze-drying technique. 冷冻干燥法制备载蛋白多孔聚乳酸微球的形貌及释放动力学。

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-08-15 DOI: 10.5402/2011/490567

Takashi Sasaki, Kazuki Tanaka, Daisuke Morino, Kensuke Sakurai

{"title":"Morphology and release kinetics of protein-loaded porous poly(l-lactic Acid) spheres prepared by freeze-drying technique.","authors":"Takashi Sasaki, Kazuki Tanaka, Daisuke Morino, Kensuke Sakurai","doi":"10.5402/2011/490567","DOIUrl":"https://doi.org/10.5402/2011/490567","url":null,"abstract":"Freeze-drying a biodegradable polymer, poly(L-lactic acid) (PLLA), from 1,4-dioxane solutions provided very porous spherical particles of ca. 3 mm in radius with specific surface area of 8-13 m(2) g(-1). The surface of the particle was found to be less porous compared with its interior. To apply the freeze-dried PLLA (FDPLLA) to drug delivery system, its morphology and drug releasing kinetics were investigated, bovine serum albumin (BSA) being used as a model drug compound. Immersion of FDPLLA into a BSA aqueous solution gave BSA-loaded FDPLLA, where mass fraction of the adsorbed BSA reached up to 79%. Time-dependent release profile of BSA in water suggested a two-step mechanism: (1) very rapid release of BSA deposited on and near the particle surface, which results in an initial burst, and (2) leaching of BSA from the interior of the particle by the diffusion process. It was suggested that the latter process is largely governed by the surface porosity. The porosity of both the interior and surface was found to decrease remarkably as the concentration of the original PLLA/1,4-dioxane solution increases, C(0). Thus, C(0) is a key parameter that controls the loading and releasing of BSA.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2011 ","pages":"490567"},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2011/490567","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30505769","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: 2

Synthesis, characterization, and antibacterial studies of mixed ligand dioxouranium complexes with 8-hydroxyquinoline and some amino acids. 8-羟基喹啉和一些氨基酸混合配体二氧铀配合物的合成、表征及抗菌研究。

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-09-27 DOI: 10.5402/2011/168539

Sunil S Patil, Ganesh A Thakur, Manzoor M Shaikh

{"title":"Synthesis, characterization, and antibacterial studies of mixed ligand dioxouranium complexes with 8-hydroxyquinoline and some amino acids.","authors":"Sunil S Patil, Ganesh A Thakur, Manzoor M Shaikh","doi":"10.5402/2011/168539","DOIUrl":"https://doi.org/10.5402/2011/168539","url":null,"abstract":"Mixed ligand complexes of dioxouranium (VI) of the type [UO(2)(Q)(L)·2H(2)O] have been synthesized using 8-hydroxyquinoline (HQ) as a primary ligand and amino acids (HL) such as L-threonine, L-tryptophan, and L-isoleucine as secondary ligands. The metal complexes have been characterized by elemental analysis, electrical conductance, magnetic susceptibility measurements, and spectral and thermal studies. The electrical conductance studies of the complexes indicate their nonelectrolytic nature. Magnetic susceptibility measurements revealed diamagnetic nature of the complexes. Electronic absorption spectra of the complexes show intraligand and charge transfer transitions, respectively. Bonding of the metal ion through N- and O-donor atoms of the ligands is revealed by IR studies, and the chemical environment of the protons is confirmed by NMR studies. The thermal analysis data of the complexes indicate the presence of coordinated water molecules. The agar cup and tube dilution methods have been used to study the antibacterial activity of the complexes against the pathogenic bacteria S. aureus, C. diphtheriae, S. typhi, and E. coli.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2011 ","pages":"168539"},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2011/168539","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30505265","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

Preparation of Fluconazole β-Cyclodextrin Complex Ocuserts: In Vitro and In Vivo Evaluation. 氟康唑β-环糊精复合制剂的制备：体外和体内评价。

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-08-25 DOI: 10.5402/2011/237501

Hindustan Abdul Ahad, J Sreeramulu, B Suma Padmaja, M Narasimha Reddy, P Guru Prakash

{"title":"Preparation of Fluconazole β-Cyclodextrin Complex Ocuserts: In Vitro and In Vivo Evaluation.","authors":"Hindustan Abdul Ahad, J Sreeramulu, B Suma Padmaja, M Narasimha Reddy, P Guru Prakash","doi":"10.5402/2011/237501","DOIUrl":"10.5402/2011/237501","url":null,"abstract":"The main purpose of the present study was to develop ocuserts of Fluconazole β-CD (beta-cyclodextrin) complex and to evaluate both in vitro and in vivo. Fluconazole was made complex with β-CD, and the release rate was controlled by HPMC K(4)M and ethyl cellulose polymers using dibutyl Phthalate as permeability enhancer. Drug-polymer interactions were studied by Fourier transform infrared spectroscopic studies. The formulated ocuserts were tested for physicochemical parameters of in vitro release and in vivo permeation in rabbits. The optimized formulations (F-5 and F-8) were subjected to stability studies. The formulated ocuserts were found to have good physical characters, thickness, diameter, uniformity in weight, folding endurance, less moisture absorption, and controlled release of drug both in vitro and in vivo. The optimized formulations retained their characteristics even after stability studies. The study clearly showed that this technique was an effective way of formulating ocuserts for retaining the drug concentration at the intended site of action for a sufficient period of time and to elicit the desired pharmacological response.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2011 ","pages":"237501"},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2011/237501","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30505765","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: 9

Enhancement or Suppression of ACE Inhibitory Activity by a Mixture of Tea and Foods for Specified Health Uses (FOSHU) That Are Marketed as "Support for Normal Blood Pressure". 以“支持正常血压”销售的茶和特定保健用途食品(FOSHU)的混合物增强或抑制ACE抑制活性

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-08-04 DOI: 10.5402/2011/712196

Isao Murakami, Hiroyuki Hosono, Shigeto Suzuki, Junichi Kurihara, Fumio Itagaki, Machiko Watanabe

{"title":"Enhancement or Suppression of ACE Inhibitory Activity by a Mixture of Tea and Foods for Specified Health Uses (FOSHU) That Are Marketed as \"Support for Normal Blood Pressure\".","authors":"Isao Murakami, Hiroyuki Hosono, Shigeto Suzuki, Junichi Kurihara, Fumio Itagaki, Machiko Watanabe","doi":"10.5402/2011/712196","DOIUrl":"https://doi.org/10.5402/2011/712196","url":null,"abstract":"The ACE inhibitory activities of mixtures of FOSHUs (Healthya, Goma-Mugicha, Lapis Support and Ameal) were examined in order to identify any antihypertensive interactions. Among combinations of Healthya with other samples that contain active peptides, only that with Ameal was found to have no inhibitory activity. Enhanced activity was observed in 2 other mixtures. The activity of a mixture of tea polyphenols and the whey component extracted from an Ameal solution was significantly decreased, thus demonstrating that whey protein lowered the ACE inhibitory activity of Healthya. Although oral administration of tea polyphenols alone significantly decreased SBP in SHR at 2 and 4 hr, combined administration with Ameal failed to decrease SBP at the same time points. In conclusion, the simultaneous intake of tea and FOSHUs that contain active peptides might affect daily self-antihypertensive management via enhancement or suppression of ACE inhibitory activity.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2011 ","pages":"712196"},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2011/712196","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30506742","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: 2

Human tissue in the evaluation of safety and efficacy of new medicines: a viable alternative to animal models? 人体组织在新药安全性和有效性评估中的应用:动物模型的可行替代方案?

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-07-06 DOI: 10.5402/2011/806789

Robert A Coleman

{"title":"Human tissue in the evaluation of safety and efficacy of new medicines: a viable alternative to animal models?","authors":"Robert A Coleman","doi":"10.5402/2011/806789","DOIUrl":"https://doi.org/10.5402/2011/806789","url":null,"abstract":"The pharma Industry's ability to develop safe and effective new drugs to market is in serious decline. Arguably, a major contributor to this is the Industry's extensive reliance on nonhuman biology-based test methods to determine potential safety and efficacy, objective analysis of which reveals poor predictive value. An obvious alternative approach is to use human-based tests, but only if they are available, practical, and effective. While in vivo (phase 0 microdosing with high sensitivity mass spectroscopy) and in silico (using established human biological data), technologies are increasingly being used, in vitro human approaches are more rarely employed. However, not only are increasingly sophisticated in vitro test methods now available or under development, but the basic ethically approved infrastructure through which human cells and tissues may be acquired is established. Along with clinical microdosing and in silico approaches, more effective access to and use of human cells and tissues in vitro provide exciting and potentially more effective opportunities for the assessment of safety and efficacy of new medicines.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2011 ","pages":"806789"},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2011/806789","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30506745","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

Solubility and dissolution enhancement of etoricoxib by solid dispersion technique using sugar carriers. 糖载体固体分散技术增强依托昔布的溶解度和溶出度。

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-09-05 DOI: 10.5402/2011/819765

Abhisekh Das, Amit Kumar Nayak, Biswaranjan Mohanty, Satyabrata Panda

{"title":"Solubility and dissolution enhancement of etoricoxib by solid dispersion technique using sugar carriers.","authors":"Abhisekh Das, Amit Kumar Nayak, Biswaranjan Mohanty, Satyabrata Panda","doi":"10.5402/2011/819765","DOIUrl":"https://doi.org/10.5402/2011/819765","url":null,"abstract":"The aim of the present study was to improve solubility and dissolution of the poorly aqueous soluble drug, etoricoxib by solvent evaporation technique using various sugar carriers, such as lactose, sucrose, and mannitol. Etoricoxib solid dispersions and their respective physical mixtures using lactose, sucrose, and mannitol were prepared in different ratios by solvent evaporation technique. The percent yield, drug content, saturation solubility, and in vitro dissolution of etoricoxib solid dispersions and physical mixtures were analyzed. Etoricoxib solid dispersions were characterized by FTIR spectroscopy, XRD, and DSC analysis. The FTIR spectroscopic analysis revealed the possibility of intermolecular hydrogen bonding in various solid dispersions. The XRD and DSC studies indicated the transformation of crystalline etoricoxib (in pure drug) to amorphous etoricoxib (in solid dispersions) by the solid dispersion technology. Both the aqueous solubility and dissolution of etoricoxib were observed in all etoricoxib solid dispersions as compared with pure etoricoxib and their physical mixtures. The in vitro dissolution studies exhibited improved dissolution in case of solid dispersion using lactose than the solid dispersions using both sucrose and mannitol. The in vitro dissolution of etoricoxib from these solid dispersions followed Hixson-Crowell model.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2011 ","pages":"819765"},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2011/819765","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30506746","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: 54

Synthesis and Inhibiting Activity of Some 4-Hydroxycoumarin Derivatives on HIV-1 Protease. 一些4-羟基香豆素衍生物的合成及其对HIV-1蛋白酶的抑制活性

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-07-26 DOI: 10.5402/2011/137637

Stancho Stanchev, Frank Jensen, Anton Hinkov, Vasil Atanasov, Petia Genova-Kalou, Radka Argirova, Ilia Manolov

引用次数: 12

Preparation of carboxymethylchitosan nanoparticles with Acid-sensitive bond based on solid dispersion of 10-hydroxycamptothecin. 基于10-羟基喜树碱固体分散体的酸敏键羧甲基壳聚糖纳米颗粒的制备。

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-07-27 DOI: 10.5402/2011/624704

Risheng Yao, Lu Liu, Shengsong Deng, Weitao Ren

{"title":"Preparation of carboxymethylchitosan nanoparticles with Acid-sensitive bond based on solid dispersion of 10-hydroxycamptothecin.","authors":"Risheng Yao, Lu Liu, Shengsong Deng, Weitao Ren","doi":"10.5402/2011/624704","DOIUrl":"https://doi.org/10.5402/2011/624704","url":null,"abstract":"Solid dispersions were prepared by a conventional solvent evaporation method from the water-insoluble model drug 10-hydroxycamptothecin (HCPT) and monomethoxypoly(ethylene glycol) 2000 (mPEG 2000). And then one type of novel biodegradable nanoparticles, the solid dispersion (HCPT/mPEG-CHO) grafted with carboxymethylchitosan (HCPT/mPEG-g-CMCTS) was synthesized. The increase in HCPT solubility of solid dispersion was up to 21-fold compared with the original drug. With the increasing of the amount of mPEG-CHO, solubility of HCPT was from 7.71 μg/mL to 25.82 μg/mL. Colloid systems based on solid dispersion were stable in aqueous medium at 5°C. After 5 months storage at 25°C, the solid dispersions do not change at all. HCPT/mPEG-g-CMCTS was synthesized by grafting reaction of carboxymethylchitosan with mPEG-CHO to form Schiff base which is sensitive to acid environment. The release rate of HCPT from this conjugate in pH 5.4 was much higher than that in the environment of pH 7.4 and p H 4.5. The cumulative release percentages are 45%, 25%, and 15%, respectively. The cumulative release percentage of HCPT in conjugate was only 15% within 85 h while the original drug was up to 70% in pH 7.4, showing a significant slow-release property. This drug model can be attractive candidates as delivery biosystems in tumor therapy.","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2011 ","pages":"624704"},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2011/624704","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30506739","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: 7

Development and evaluation of microemulsions for transdermal delivery of insulin. 胰岛素透皮微乳的研制与评价。

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-07-07 DOI: 10.5402/2011/780150

Jadupati Malakar, Suma Oomen Sen, Amit Kumar Nayak, Kalyan Kumar Sen

引用次数: 57

Ex vivo evaluation of insulin nanoparticles using chitosan and arabic gum. 壳聚糖和阿拉伯胶制备胰岛素纳米颗粒的体外评价。

ISRN Pharmaceutics Pub Date : 2011-01-01 Epub Date: 2011-07-10 DOI: 10.5402/2011/860109

M R Avadi, A M M Sadeghi, Naser Mohamadpour Dounighi, R Dinarvand, F Atyabi, M Rafiee-Tehrani

引用次数: 42