Preparation and physicochemical characterization of binary and ternary ground mixtures of carvedilol with PVP and SLS aimed to improve the drug dissolution

Bolourchian, Noushin; Talamkhani, Zohreh; Nokhodchi, Ali

doi:10.1080/10837450.2019.1641516

Cited by 9 publications

(6 citation statements)

References 35 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The DSC thermograms of the intact drug and prepared samples are depicted in Figure 4. A characteristic endotherm appeared at the onset temperature of 113.6°C, which may have been attributed to the melting of carvedilol form II (20). No distinct peak observed for form III of the intact drug was attributable to the very small amount of this form in the sample.…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 93%

“…The availability of this drug for absorption from small intestine might be prohibited due to its poor solubility and low dissolution rate, which along with high degree of first-pass metabolism results in poor oral bioavailability of 25 -30% (16,17). Different approaches have been applied to enhance CA dissolution rate based on nanosuspensions (16,18), adsorption onto porous silica (19), co-grinding (20), self-emulsification and liquisolid techniques (21), complexation with cyclodextrins (22,23), and solid dispersions (24)(25)(26).…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

The Effect of Surfactant Type and Concentration on Physicochemical Properties of Carvedilol Solid Dispersions Prepared by Wet Milling Method

Bolourchian

Panah

2022

Iran J Pharm Res

Self Cite

View full text Add to dashboard Cite

: The present study mainly aimed to prepare solid dispersions (SDs) of a poorly water-soluble compound, carvedilol (CA), in the presence of pluronic F68 (F68) and myrj 52 by adopting wet milling technique in order to enhance drug dissolution. The process enabled the preparation of SDs without using any toxic organic solvents. SDs with different CA, surfactant ratios were prepared by adopting wet milling followed by freeze-drying method and evaluated for their particle size and dissolution. They were also characterized based on/using X-ray diffraction (XRD), differential scanning calorimetry (DSC), fourier transform infrared (FTIR) spectroscopy, scanning electron microscope (SEM), and saturated solubility. The effect of cryoprotectant type on the dissolution and particle size of SDs was also investigated. Wet milling process resulted in the reduced particle size depending on the type of surfactant. The significant drug dissolution and saturated solubility enhancement were recorded for milled SD formulations. In this regard, Myrj had a greater impact compared to F68. Dissolution efficiencies (DE30) obtained for the myrj-included SDs were up to 8.2-fold higher than that of untreated CA. The type of cryoprotectant was also found to affect the drug dissolution. According to the results, partial amorphization occurred in wet-milled samples, as confirmed by XRD and DSC analysis. It was concluded that using an appropriate surfactant along with wet-milling method may have been an effective approach for improving the dissolution rate of CA, a poorly soluble compound.

show abstract

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 93%

Section: Introductionmentioning

confidence: 99%

The Effect of Surfactant Type and Concentration on Physicochemical Properties of Carvedilol Solid Dispersions Prepared by Wet Milling Method

Bolourchian

Panah

2022

Iran J Pharm Res

Self Cite

View full text Add to dashboard Cite

show abstract

“…A physical mixture (PM) of ENZ and polymers was prepared by a simple triturating method using mortar and pestle. The PM was sifted through an 80# sieve (Bolourchian, N., 2019).…”

Section: Preparation Of Physical Mixturementioning

confidence: 99%

Dissolution enhancement of Enzalutamide by solid dispersion approach

Bagul¹,

Mundada²

2022

ijhs

View full text Add to dashboard Cite

Enzalutamide (ENZ) is a BCS class II, fast crystallizing, a hydrophobic compound that has solubility limited absorption in vivo. Ternary solid dispersion of Enzalutamide was prepared with water-soluble polymers Soluplus (SOL) and Poloxamer P 188 (POL) by solvent evaporation spray drying technique. Initially, different ratios of Soluplus: Poloxamer and solvents were used to prepare Ternary solid dispersions of Enzalutamide and evaluated for the dissolution enhancement property. The prepared solid dispersion was characterized by FTIR spectroscopy, Differential scanning calorimetry (DSC), X-ray diffraction (XRD) analysis, Scanning electron microscopy (SEM), Particle size distribution (PSD) by Malvern and Physico-chemical analysis. FTIR spectroscopy shows that there was no interaction between the ENZ and polymers. DSC and XRD analysis show that conversion to amorphous form of ENZ in ternary SD, which enhances the dissolution rate. In vitro dissolution studies and Ex-vivo intestinal absorption studies clearly show that the prepared solid dispersion enhanced the dissolution and ex-vivo intestinal absorption of ENZ compared with pure ENZ.

show abstract

“…By breaking down the medication into smaller pieces, the ASD enhances the drug's surface area and speeds up its breakdown. 10,11…”

Section: Dissolution Profile Studymentioning

confidence: 99%

Stable Amorphous Solid Dispersion of Eplerenone Prepared with Water Soluble Polymer by Spray Drying Technique

Bagul¹,

Mundada²

2022

IJPQA

View full text Add to dashboard Cite

Class II in the Biopharmaceutical Classification System, eplerenone (EPL) is a selective aldosterone antagonist. Due to its poor solubility, EPL has limited bioavailability. Here, an innovative spray-drying method was used to transform a water soluble polymer into an amorphous dispersion of the EPL. Different polymer SOL/EPL ratios were tested to determine EPL’s solubility and dissolution enhancement properties. In order to learn more about the physical and chemical properties of this novel amorphous solid dispersion (ASD), methods like powder X-ray diffraction spectroscopy (PXRD), differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), particle size distribution (PSD) using a Malvern instrument, and scanning electron microscopy (SEM) were used. There was no chemical interaction between the binary mixture of EPL and SOL which was confirmed from the FTIR spectra obtained. The enhancement in the solubility and dissolution of EPL and binary mixture prepared were due to the amorphous conversion of EPL in the SOL polymer (amorphous solid dispersion), which was confirmed from DSC thermogram, PXRD spectra obtained and was also confirmed from the solubility study, in-vitro dissolution study. Finally, ex-vivo intestinal absorption study performed on the goat intestine using amorphous solid dispersion and pure EPL, also improved intestinal absorption of EPL through amorphous solid dispersion prepared.

show abstract

Preparation and physicochemical characterization of binary and ternary ground mixtures of carvedilol with PVP and SLS aimed to improve the drug dissolution

Cited by 9 publications

References 35 publications

The Effect of Surfactant Type and Concentration on Physicochemical Properties of Carvedilol Solid Dispersions Prepared by Wet Milling Method

The Effect of Surfactant Type and Concentration on Physicochemical Properties of Carvedilol Solid Dispersions Prepared by Wet Milling Method

Dissolution enhancement of Enzalutamide by solid dispersion approach

Stable Amorphous Solid Dispersion of Eplerenone Prepared with Water Soluble Polymer by Spray Drying Technique

Contact Info

Product

Resources

About