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Registros recuperados: 7
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Solid dispersion-based pellet for colon delivery of tacrolimus through time- and pH-dependent layer coating: preparation, in vitro and in vivo studies BJPS
Guo,Jian; Fang,Huihui; Gui,Shuangying; Huang,Yuzhe.
The intent of the present investigation is to develop and evaluate colon-specific coated tacrolimus solid dispersion pellet (SDP) that retards drug release in the stomach and small intestine but progressively releases in the colon. Tacrolimus-SDP was prepared by extrusion-spheronization technology and optimized by the micromeritic properties including flowability, friability, yields and dissolution rate. Subsequently, the pH-dependent layer (Eudragit L30D55) and time-dependent layer (Eudragit NE30D and L30D55) were coated on the SDP to form tacrolimus colon-specific pellets (CSP) using a fluidized bed coater. Under in vitro gradient pH environment, tacrolimus only released from CSP after changing pH to 6.8 and then quickly released in the phosphate buffer...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Tacrolimus; Solid dispersion; Pellet; Oral colon-specific; Biodistribution.
Ano: 2019 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100557
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Characterization of gliclazide-polyethylene glycol solid dispersion and its effect on dissolution BJPS
Patil,Moreshwar Pandharinath; Gaikwad,Naresh Janardan.
The present study was initiated with the objective of studying the in vitro dissolution behavior of gliclazide from its solid dispersion with polyethylene glycol 6000. In this work, a solid dispersion of gliclazide with polyethylene glycol was prepared by the fusion method. In vitro dissolution study of gliclazide, its physical mixture and solid dispersion were carried out to demonstrate the effect of PEG 6000. Analytical techniques of FT-IR spectroscopy, differential scanning calorimetry and X-ray diffractometry were used to characterize the drug in the physical mixtures and solid dispersions. The dissolution studies of solid dispersion and physical mixture showed greater improvement compared to that of the pure drug. The mechanisms for increased...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Gliclazide; Polyethylene glycol 6000; Solid dispersion; In vitro dissolution.
Ano: 2011 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502011000100020
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Enhancement of solubility and dissolution rate of poorly water soluble raloxifene using microwave induced fusion method BJPS
Patil,Payal Hasmukhlal; Belgamwar,Veena Sailendra; Patil,Pratibha Ramratan; Surana,Sanjay Javerilal.
The objective of the present work was to enhance the solubility and dissolution rate of the drug raloxifene HCl (RLX), which is poorly soluble in water. The solubility of RLX was observed to increase with increasing concentration of hydroxypropyl methylcellulose (HPMC E5 LV). The optimized ratio for preparing a solid dispersion (SD) of RLX with HPMC E5 LV using the microwave-induced fusion method was 1:5 w/w. Microwave energy was used to prepare SDs. HPMC E5 LV was used as a hydrophilic carrier to enhance the solubility and dissolution rate of RLX. After microwave treatment, the drug and hydrophilic polymer are fused together, and the drug is converted from the crystalline form into an amorphous form. This was confirmed through scanning electron microscopy...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Raloxifene HCl; Microwave-induced fusion method; Solid dispersion; Solubility enhancement; HPMC E5 LV.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502013000300019
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A novel approach in mucoadhesive drug delivery system to improve zidovudine intestinal permeability BJPS
Pedreiro,Liliane Neves; Cury,Beatriz Stringhetti Ferreira; Chaud,Marco Vinícius; Gremião,Maria Palmira Daflon.
ABSTRACT Zidovudine (AZT) mucoadhesive solid dispersions (SD) were prepared using a sodium starch glycolate (SSG) and hypromellose phthalate (HPMCP) mixtures as carrier to enhance the intestinal permeability and bioavailability of zidovudine. SDs were prepared using the co-precipitation method followed by solvent evaporation and characterized according to their physicochemical properties such as particle size, crystallinity, thermal behavior, and liquid uptake ability. In vitro drug dissolution, mucoadhesiveness and AZT intestinal permeability were also determined. Thermal behavior and X-ray diffraction patterns demonstrated the amorphous state of AZT in SD systems. The HPMCP polymer restricted the liquid uptake ability in the acid medium; however, this...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Zidovudine; Solid dispersion; Mucoadhesion; P-glycoprotein; Intestinal permeability..
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000400715
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Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel BJPS
Chaud,Marco Vinicius; Tamascia,Pollyanna; Lima,Andréa Cristina de; Paganelli,Maria Ondina; Gremião,Maria Palmira Daflon; Freitas,Osvaldo de.
The solubility behavior of drugs remains one of the most challenging aspects in formulation development. Solid Dispersion (SD) has tremendous potential for improving drug solubility. Although praziquantel (PZQ) is the first drug of choice in the treatment of schistosomiasis, its poor solubility has restricted its delivery oral route. In spite of its poor solubility, PZQ is well absorbed in the gastrointestinal tract, but large doses are required to achieve adequate concentration at the target sites. The aim of this study was to improve the solubility and dissolution rate of PZQ and to evaluate its intestinal absorption. SDs were formulated with PEG-60 castor oil hydrogenated (CR-60) using a fusion and evaporation method. Pure PZQ and physical mixtures (PM)...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Solid dispersion; Praziquantel/dissolution rates; Praziquantel/solubility; Praziquantel/intestinal absorption.
Ano: 2010 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502010000300010
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Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate BJPS
Adeli,Ehsan.
ABSTRACT Azithromycin is a water-insoluble drug, with a very low bioavailability. In order to increase the solubility and dissolution rate, and consequently increase the bioavailability of poorly-soluble drugs (such as azithromycin), various techniques can be applied. One of such techniques is "solid dispersion". This technique is frequently used to improve the dissolution rate of poorly water-soluble compounds. Owing to its low solubility and dissolution rate, azithromycin does not have a suitable bioavailability. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of azithromycin by preparing its solid dispersion, using different Polyethylene glycols (PEG). Preparations of solid dispersions and physical...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Azithromycin/solubility; Azithromycin/dissolution; Solid dispersion; Polyethylene glycols..
Ano: 2016 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000100002
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Preparation and characterization of cefuroxime axetil solid dispersions using poloxamer 188 BJPS
Sankari,Thaeer; Al-Hariri,Sahar.
The main objective of the present work was to enhance the solubility and dissolution rate of poorly water-soluble drug cefuroxime axetil (CA) by formulating it into solid dispersions (SDs) with water soluble carrier poloxamer 188. Different methods were employed to prepare the dispersion, such as: Solvent method (SM), Kneading method (KM), Melt evaporation method (MEM) and Physical mixture (PM) in different drug: carrier ratios 1:1, 1:2 and 1:3 (cefuroxime axetil: poloxamer 188). The physical mixture(s) and solid dispersion(s) were characterized for drug carrier interaction, drug content, solubility, dissolution rate, differential scanning calorimetry (DSC) and FT-IR study. The dissolution rate of the prepared solid dispersion systems was determined in...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Cefuroxime axetil/dissolution; Poloxamer 188; Solid dispersion.
Ano: 2018 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502018000400622
Registros recuperados: 7
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