The Open Drug Delivery Journal最新文献_第2页

Can Biorelevant Media be Simplified by using SLS and Tween 80 to Replace Bile Compounds 用SLS和Tween 80替代胆汁化合物可以简化生物相关介质吗

The Open Drug Delivery Journal Pub Date : 2010-04-29 DOI: 10.2174/1874126601004020030

Thomas Taupitz, S. Klein

{"title":"Can Biorelevant Media be Simplified by using SLS and Tween 80 to Replace Bile Compounds","authors":"Thomas Taupitz, S. Klein","doi":"10.2174/1874126601004020030","DOIUrl":"https://doi.org/10.2174/1874126601004020030","url":null,"abstract":"In the scientific literature, the use of a surfactant is recommended for both designing quality control tests for water insoluble or sparingly water soluble drugs and for predicting the bioavailability of drugs from various types of for- mulations. Since the number of poorly soluble drugs is increasing, the selection of adequate dissolution test for these be- comes more and more important. The aim of the present study was to develop predictive and discriminatory test methods based on surfactants that are recommended in the literature. Particular respect was given to the use of sodium lauryl sul- fate and Tween 80, the two most commonly used surfactants for this purpose. Tamoxifen was used as a model drug. Dis- solution experiments were performed using various concentrations of the two surfactants in buffer media typically used to prepare biorelevant test media. Results were then compared with those deriving from the same test formulations in biorelevant and simplified \"biorelevant\" media. Results from this study indicate that the concentration of surfactant has a huge impact on both the rate and extent of drug release from the formulation and also on the discriminatory power of the test. However, they also indicate that a well designed and validated test medium containing SLS or Tween 80 can be useful in terms of establishing a discriminatory test medium that possibly could also be used to assure batch to batch bioequivalence. Therefore, the approach described in the present paper might be very helpful for developing predictive and discriminatory methods in early formulation development for poorly soluble drugs and which could also be adopted for QC.","PeriodicalId":421840,"journal":{"name":"The Open Drug Delivery Journal","volume":"18 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2010-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"133359704","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: 24

Effect of Vehicles on Release of Meloxicam from Various Topical Formulations 不同外用制剂对美洛昔康释放的影响

The Open Drug Delivery Journal Pub Date : 2009-06-30 DOI: 10.2174/1874126600903010019

G. Yener, Özlem Dal, M. Üner

{"title":"Effect of Vehicles on Release of Meloxicam from Various Topical Formulations","authors":"G. Yener, Özlem Dal, M. Üner","doi":"10.2174/1874126600903010019","DOIUrl":"https://doi.org/10.2174/1874126600903010019","url":null,"abstract":"This article evaluates the effect of various vehicles (O/W, W/O and two W/O/W emulsions and a hydrogel) on meloxicam release. One of W/O/W emulsions was named W/O/W-C containing Carbopol ® 934 as a gelling agent in its outer aqueous phase. Release of drug through cellulose acetate membrane was studied by using Franz-type diffusion cells. Hydrogel formulation gave the highest release with a significant difference followed by W/O/W, O/W, W/O/W-C and W/O emulsions. Increase in amount of oil phase resulted in slower drug release strictly indicating importance of lipophility of vehicle on release of lipophilic drugs like MX. Incorporation of MX in hydrogel increased the released amount by up to 20 times when compared with the other formulations. Increase in viscosity of the formulations was also followed the same order. Release study was performed by using UV spectroscopy. Furthermore, the determination method of MX was validated through the following performance criteria: linearity, intra-day and inter-day precision, accuracy, specifity and recovery. This method was proved as precise and accurate determination of MX in multi-component pharmaceutical preparations besides colorimetric methods.","PeriodicalId":421840,"journal":{"name":"The Open Drug Delivery Journal","volume":"3 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2009-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"130443674","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: 15

Characterization of the Ion Exchange Reaction Between Propranolol-H+ or K+ with Amberlite IRP 69 Resin by Both, Isothermal Titration Calorimetry and (Flame) Photometric Equilibrium Analysis 用等温滴定量热法和(火焰)光度平衡分析表征普萘洛尔- h +或K+与安贝石irp69树脂离子交换反应

The Open Drug Delivery Journal Pub Date : 2009-02-09 DOI: 10.2174/1874126600903010010

D. Zeiss, M. Wagner, A. Bauer-Brandl

引用次数: 3

Sertaconazole-Loaded Cyclodextrin–Polysaccharide Hydrogels as Antifungal Devices§ 塞他康唑-负载环糊精-多糖水凝胶作为抗真菌设备§

The Open Drug Delivery Journal Pub Date : 2009-01-14 DOI: 10.2174/1874126600903010001

E. Lopez-Montero, J. F. D. Santos, J. Torres-Labandeira, A. Concheiro, C. Alvarez‐Lorenzo

{"title":"Sertaconazole-Loaded Cyclodextrin–Polysaccharide Hydrogels as Antifungal Devices§","authors":"E. Lopez-Montero, J. F. D. Santos, J. Torres-Labandeira, A. Concheiro, C. Alvarez‐Lorenzo","doi":"10.2174/1874126600903010001","DOIUrl":"https://doi.org/10.2174/1874126600903010001","url":null,"abstract":"The aim of the present work was to develop novel hydrogels for delivering sertaconazole based on cyclodex- trins and various biocompatible polysaccharides. Sertaconazole is an antifungal agent very effective for treatment of Can- dida albicans infections. However its poor aqueous solubility is still a challenging issue for developing suitable formula- tions. Complexation with cyclodextrins is a very attractive route to overcome this limitation, simultaneously enhancing its antifungal effectiveness. Hydroxypropyl-￻-cyclodextrin (HP￻CD) hydrogels prepared by direct cross-linking in presence of methylcellulose (MC), hydroxypropyl cellulose (HPC), hydroxypropyl methylcellulose (HPMC), carboxymethyl cellu- lose (CMCNa), or dextran were transparent and swelled in water without dissolving, which enables the formation of mi- croenvironments very rich in cyclodextrin cavities responsible for hosting the drug and control its release rate. HP￻ CD hydrogels showed a high capability to load sertaconazole (with partition coefficients from 22 to 470) while still combining high water affinity (superabsorbency), versatile biomechanical properties (hardness and compressibility) and sustained re- lease behavior (up to 4 days). Importantly, sertaconazol-loaded hydrogels showed effectiveness against Candida albicans in culture medium. HPCD-polysaccharide hydrogels could be useful as sertaconazole delivery systems for the treatment of mucosal infections.","PeriodicalId":421840,"journal":{"name":"The Open Drug Delivery Journal","volume":"72 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2009-01-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128374579","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: 17

Hydrazone, Amide, Carbamate, Macromolecular and Other Prodrugs of Doxorubicin 阿霉素的腙类、酰胺类、氨基甲酸酯类、大分子类及其他前药

The Open Drug Delivery Journal Pub Date : 2008-10-22 DOI: 10.2174/1874126600802010077

S. Rollas,, S. G. Kucukguzel

引用次数: 17

Effect of 5-Fluorouracil Pretreatment on the In Vitro Drug Release from Colon-Targeted Guar Gum Matrix Tablets 5-氟尿嘧啶预处理对结肠靶向瓜尔胶基质片体外释药的影响

The Open Drug Delivery Journal Pub Date : 2008-09-04 DOI: 10.2174/1874126600802010071

Y. Krishnaiah, B. Srinivas

{"title":"Effect of 5-Fluorouracil Pretreatment on the In Vitro Drug Release from Colon-Targeted Guar Gum Matrix Tablets","authors":"Y. Krishnaiah, B. Srinivas","doi":"10.2174/1874126600802010071","DOIUrl":"https://doi.org/10.2174/1874126600802010071","url":null,"abstract":"The aim of the investigation was to assess the effect of oral 5-flourouracil pre-treatment on the in vitro drug re- lease from a model colon-targeted guar gum matrix tablet formulation of mebendazole. Guar gum matrix tablets of me- bendazole were subjected to in vitro drug release studies in simulated colonic fluids (4%w/v of rat caecal contents) ob- tained after oral treatment of rats either with varying doses of 5-fluorouracil (0.3, 1, 3 or 6 mg kg -1 once daily for 5 days) and 1 ml of 2%w/v of guar gum dispersion or with 1 ml of 2%w/v of guar gum dispersion alone (control study) after completing the dissolution study in 0.1 M HCl (2 h) and pH 7.4 Sorensen's phosphate buffer (3 h). The mebendazole tab- lets disintegrated in the presence of simulated colonic fluids releasing about 97% of the drug (control study) at the end of 24 h. However, the release of mebendazole decreased when drug release studies were carried out in caecal contents of rats pretreated with both 5-fluorouracil and guar gum dispersion. The release of mebendazole significantly decreased when pretreated with 1, 3 or 6 mg kg -1 dose levels of 5-fluorouracil (oral). However, there was no significant effect of 5- fluorouracil on the release of mebendazole when pretreated at a dose level of 0.3 mg kg -1 (oral). It was concluded that multiple administration of 5-fluorouracil at a dose of 0.3 mg kg -1 did not affect the drug release from colon-targeted guar","PeriodicalId":421840,"journal":{"name":"The Open Drug Delivery Journal","volume":"47 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2008-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"125628405","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: 14

Designing of a Thermosensitive Chitosan/Poloxamer In Situ Gel for OcularDelivery of Ciprofloxacin 热敏壳聚糖/波洛沙姆原位凝胶眼给药环丙沙星的设计

The Open Drug Delivery Journal Pub Date : 2008-08-21 DOI: 10.2174/1874126600802010061

J. Varshosaz, M. Tabbakhian, Z. Salmani

{"title":"Designing of a Thermosensitive Chitosan/Poloxamer In Situ Gel for OcularDelivery of Ciprofloxacin","authors":"J. Varshosaz, M. Tabbakhian, Z. Salmani","doi":"10.2174/1874126600802010061","DOIUrl":"https://doi.org/10.2174/1874126600802010061","url":null,"abstract":"To increase the low bioavailability and short ocular residence time of ciprofloxacin eye drops, aqueous solu- tions of drug in chitosan/ Pluronic (poloxamer) were prepared to identify suitable compositions with regard to gel forming properties and drug release behavior. Mixtures of solutions of Pluronic (10-25% w/w) with chitosan (0.1-0.3% w/w) of different molecular weights (Mw) were prepared. Ciprofloxacin release was determined using a membraneless dissolution model in artificial tear solution up to 8 hours and the samples were analyzed spectrophotometrically at 272.4nm. The rheological behavior of solutions in response to dilution or temperature changes and also the phase change temperature (PCT) were determined using a Cup & Bob viscometer. Antimicrobial effect of the solutions was studied in nutrient agar in comparison to marketed solutions of ciprofloxacin using Pseudomonas aueroginosa and Staphylococcus aureus by the agar diffusion test using the cup-plate technique. The formulation consisted of 15% Pluronic and 0.1% low Mw chitosan, with the highest release efficiency (46.61 ± 0.41%) and an acceptable mean release time (1.94 ± 0.27 hr), is suggested as a suitable ophthalmic preparation for sustained release of ciprofloxacin. This in situ gel released the drug by a Higuchi model and Fickian mechanism. It was liquid in non-physiologic conditions (pH 4 and 25oC) and transferred to the gel form upon physiologic conditions (pH 7.4 and 37oC). The PCT of this in situ gel did not change upon dilution and the zone of inhibition of the growth of both studied bacteria was significantly greater for it than the marketed eye drop of ciprofloxacin.","PeriodicalId":421840,"journal":{"name":"The Open Drug Delivery Journal","volume":"50 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2008-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"122542886","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: 127

A New Oil-Based Antigen Delivery Formulation for both Oral and Parenteral Vaccination 一种用于口服和肠外疫苗接种的新型油基抗原递送制剂

The Open Drug Delivery Journal Pub Date : 2008-06-24 DOI: 10.2174/1874126600802010052

M. O. Domingos, D. Lewis, T. Jansen, D. Zimmerman, E. Williamson, R. New

{"title":"A New Oil-Based Antigen Delivery Formulation for both Oral and Parenteral Vaccination","authors":"M. O. Domingos, D. Lewis, T. Jansen, D. Zimmerman, E. Williamson, R. New","doi":"10.2174/1874126600802010052","DOIUrl":"https://doi.org/10.2174/1874126600802010052","url":null,"abstract":"The ability of an oil-based carrier vehicle to act as an antigen delivery system via the oral and/or parenteral routes was investigated. The formulation consists of hydrophilic macromolecules (antigens) solubilised in oil phase, in the absence of water, by virtue of being wrapped in a sheath of phospholipid amphiphile. Results obtained demonstrate that the level of mucosal IgA antibodies detected in the stools of mice immunised orally with cholera toxin B fragment (CTB) or E. coli heat-labile toxin (LT) in oil is much higher than the level of IgA produced by mice immunised with CTB or LT alone. In addition, mice immunised orally with Y. pestis antigens (F1 and V) and CTB as immunostimulant in oil produce a significantly increased (p<0.02) systemic IgG response against both antigens (F1 and V) than mice orally immunised with F1, V and CTB without oil. Six out of ten mice immunised with F1 and V antigens in oil survived an aerosol chal- lenge of 100 LD50 doses of virulent Y. pestis. Furthermore, animals immunised sub-cutaneously with the HIV antigen (HGP-30) in oil induced much stronger humoral and cellular responses against the antigen than mice immunised with the antigen alone. Taken together, these findings indicate that oil can be used successfully as an antigen delivery system in vaccine formulations without the necessity of an aqueous phase or an emulsification process. This greatly enhances the stability and ease of production of a formulation manufactured for commercial use.","PeriodicalId":421840,"journal":{"name":"The Open Drug Delivery Journal","volume":"29 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2008-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"127108391","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: 17

Solid Dispersions of Chitosan Glutamate for the Local Delivery of Miconazole: Characterization and In Vitro Activity 谷氨酸壳聚糖局部递送咪康唑的固体分散体:表征和体外活性

The Open Drug Delivery Journal Pub Date : 2008-06-13 DOI: 10.2174/1874126600802010044

R. Mangiafico, V. Pantó, G. Puglisi, P. Furneri

{"title":"Solid Dispersions of Chitosan Glutamate for the Local Delivery of Miconazole: Characterization and In Vitro Activity","authors":"R. Mangiafico, V. Pantó, G. Puglisi, P. Furneri","doi":"10.2174/1874126600802010044","DOIUrl":"https://doi.org/10.2174/1874126600802010044","url":null,"abstract":"The incorporation of miconazole nitrate (MCN) in mucoadhesive microparticles made of a water-soluble chito- san salt, chitosan glutamate (CHG) was studied. These solid systems may be proposed for buccal or vaginal applications against mycotic infections, taking advantage of the muco-adhesive and permeation enhancing properties of this polymer. Two series of solid dispersions were obtained by either spray-drying and lyophilization, under different formulation vari- ables. The in vitro release of MCN from both the series of microparticles was analyzed at pH simulating the mouth or vaginal environments. A high amount (60 to 85%) of the loaded MCN was released quickly within the first 30 min both at pH 5.0 and 6.6 from all the systems, while the release did not further increase in the following 4 h. These results suggest that the released drug was the fraction of drug desorbed from the CHG particle surface, while a residual amount of drug remained associated or entrapped within them. An in vitro microbiological assay was carried out against different strains of Candida. MCN- CHG lyophilized solid dis- persions gave enhanced inhibitory activity on yeast growth compared to the free drug, whereas the inclusion of MCN in spray-dried microparticles generally did not improve the activity of the drug. The different physical properties of the two kinds of dispersions seemed to be at the basis of the observed different in vitro antimycotic activity.","PeriodicalId":421840,"journal":{"name":"The Open Drug Delivery Journal","volume":"2 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2008-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131725667","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: 8

Improvement of Antiamoebic Activity of Rokitamycin Loaded in Chitosan Microspheres 壳聚糖微球负载罗基他霉素抗阿米巴活性的提高

The Open Drug Delivery Journal Pub Date : 2008-05-23 DOI: 10.2174/1874126600802010038

G. Rassu, E. Gavini, A. Mattana, P. Giunchedi

引用次数: 9