Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407

Vyas, Vikrant; Sancheti, Pankajkumar; Karekar, Poonam; Shah, Manali; Pore, Yogesh

doi:10.2478/v10007-009-0037-4

Cited by 75 publications

(43 citation statements)

References 12 publications

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“…Further increase in concentration of poloxamer retarded the drug release due to gel forming property. [23] The SD formulations prepared by kneading method and MM showed higher dissolution compared to PD and PM prepared. This may be due to partial to complete dispersion of drug in hydrophilic carrier poloxamer 407.…”

Section: In Vitro Drug Release Studies Of Sdsmentioning

confidence: 99%

“…[22] Solubility of pure drug (PD) was found to be increased 5.3 folds with 1.5% poloxamer 407 [ Table 2] and above 1.5% solubility was found to be decreased due to its gel forming property. [23] The values of Gibbs-free energy (ΔG°tr) associated with the aqueous solubility of OLM in polymeric solution of poloxamer 407 are given in Table 2. The ΔG°tr values were negative at the different concentrations of the polymers, which showed the spontaneous nature of the OLM solubilization.…”

Section: Phase Solubility Studymentioning

confidence: 99%

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Mali

2017

AJP

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Aim: Olmesartan medoxomil (OLM) is a poorly soluble drug and its low aqueous solubility leads to poor dissolution and bioavailability. The aim of this work was to improve the solubility of poorly aqueous soluble drug OLM by solid dispersion (SD) technique. Materials and Methods: A phase solubility study was performed to determine the effect of various polymers on aqueous solubility of drug. The binary SD of OLM was prepared by using poloxamer 407. The SDs were prepared by kneading, melting and solvent evaporation (SE) method by varying drug to carrier ratio. The optimized SD formulations were characterized by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and powder X-ray diffraction (XRD). Fast disintegrating tablets (FDTs) of OLM were formulated using optimized SD. The in vitro evaluation of FDTs was done including stability studies. Results: Phase solubility study indicated 5.3 fold increase in solubility of OLM by Poloxamer 407. The results of FTIR, DSC, SEM, and XRD study showed the conversion of crystalline form of OLM to amorphous form. The results revealed that SD prepared by SE method showed rapid dissolution as compared to other methods. The FDTs of optimized SD containing croscarmellose sodium showed faster and complete in vitro drug release within 20 min. Formulation M6 was found to be optimized formulation owing to its 84.09 dissolution efficiency, 4.82 min mean dissolution time and 100% drug release. Optimized formulation was found to be stable for 3-month period. Conclusion: The results conclusively confirmed successful improvement in dissolution of poorly water-soluble drug OLM.

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Section: In Vitro Drug Release Studies Of Sdsmentioning

confidence: 99%

Section: Phase Solubility Studymentioning

confidence: 99%

Untitled

Mali

2017

AJP

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“…However, the detailed 111 impact of these factors on the apparent solubility of drug has not 112 been clearly defined and requires further study. Td solid disper-113 sions have been described several times to date but they were 114 based on block polyethylene and polypropylene glycol copolymer 115 (Pluronic, Poloxamer) as a polymeric matrix [23,11]. Since this sub- 116 stance is known to be capable of forming micelles in a solution, an 117 increase in apparent solubility in this case is a result of an addi-118 tional solubilizing effect visible even for physical mixtures.…”

mentioning

confidence: 98%

Physicochemical properties of tadalafil solid dispersions – Impact of polymer on the apparent solubility and dissolution rate of tadalafil

Wlodarski

Sawicki

Haber

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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“…However, poor solubility in water limits the development of new dosage forms. Thus, microporous silicate carriers, preparing inclusion complexes with modified β-cyclodextrines or solid dispersions with poloxamer, PEGs and PVP, have been proposed to enhance dissolution of TA (7)(8)(9)(10).…”

Section: Introductionmentioning

confidence: 99%

Physicochemical Properties of Bosentan and Selected PDE-5 Inhibitors in the Design of Drugs for Rare Diseases

et al. 2016

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Abstract.The study provides the physicochemical characteristic of bosentan (BOS) in comparison to tadalafil (TA) and sildenafil citrate (SIL). Despite some reports dealing with thermal characteristic of SIL and TA, physicochemical properties of BOS have not been investigated so far. Recent clinical reports have indicated that the combination of bosentan and PDE-5 inhibitor can improve the effectiveness of pharmacotherapy of pulmonary arterial hypertension (PAH). However, in order to design personalized medicines for therapy of chronic rare diseases, detailed information on the thermal behaviour and solubility of each drug is indispensable. Thus, XRD, DSC and TGA-QMS analyses were applied to compare the properties of the drugs, their thermal stability as well as to identify the products of thermal degradation. The dehydration of BOS started at 70°C and was followed by the chemical degradation with the onset at 290°C. The highest thermal stability was stated for TA, which decomposed at ca. 320°C, whereas the lowest onset of the thermal decomposition process was stated for SIL, i.e. 190°C. The products of the drug decomposition were identified. FT-FIR was applied to study intra-and intermolecular interactions between the drug molecules. FT-MIR and Raman spectroscopy were used to examine the chemical structure of the drugs. Chemoinformatic tools were used to predict the polar surface area, pKa, or logP of the drugs. Their results were in line with solubility and dissolution studies.

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Physicochemical characterization of solid dispersion systems of tadalafil with poloxamer 407

Cited by 75 publications

References 12 publications

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Physicochemical properties of tadalafil solid dispersions – Impact of polymer on the apparent solubility and dissolution rate of tadalafil

Physicochemical Properties of Bosentan and Selected PDE-5 Inhibitors in the Design of Drugs for Rare Diseases

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