Dissolution properties of control released solid dispersion of carvedilol with HPMC and Eudragit RS

Shim, Jung Bo; Kim, Min Jeong; Kim, Seul Ji; Kang, Su Ji; Lee, Ji Hye; Kim, Hyeong Seok; Lee, Dongwon; Khang, Gilson

doi:10.1007/s40005-012-0037-0

Cited by 16 publications

(14 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It is a weakly basic drug with a pKa value 6.8 and practically insoluble in water (4.4 μg/mL) [ 7 ]. The absorption of CAR after oral administration is rapid with an elimination half-life of 6–10 h and low absolute bioavailability (BA) (25% or less) [ 8 , 9 ]. Therefore, poor solubility and short biological half-life limit its clinical application as multiple dosing required to maintain optimum plasma concentration.…”

Section: Introductionmentioning

confidence: 99%

Impact of drying on dissolution behavior of carvedilol-loaded sustained release solid dispersion: development and characterization

Halder

Ahmed

Shuma

et al. 2020

Heliyon

View full text Add to dashboard Cite

Purpose The present study aimed to develop carvedilol (CAR)-loaded (25% w/w) sustained release solid dispersion (SRSD), for enhanced dissolution and to explore the applicability of different industrially accessible drying techniques. Methods SRSD-CAR containing different ratios of polymers were prepared and physicochemically characterized. Dissolution study was carried out in both sink and supersaturated conditions to identify the possible enhancement in dissolution behavior. Results Based on the solubility study, Kolliphor® P188 and Eudragit® RSPO (50:25, % w/w) ratio exhibited the highest solubility among the samples and was chosen as the optimal composition of SRSD-CAR for further characterization. The crystallinity assessments of the optimized formulation indicated amorphization of CAR in the formulation, bring about improved solubility of CAR. The infrared spectroscopic study revealed minor transitions; demonstrating the absence of significant interactions between drug and carrier. Furthermore, the SRSD-CAR exhibited immediate formation of nano particles when dispersed in water. Dissolution study revealed significant improvement in dissolution behavior, with a release of CAR in a gradual manner compared to crystalline CAR. From the dissolution kinetics analysis, the Korsmeyer Peppas model fit the best and diffusion was predominant in release of CAR. The drug release pattern showed insignificant differences between the SRSD-CAR formulations prepared by rotary vacuum drying and freeze drying. Conclusion From these experimental findings, SRSD approach might be a favorable dosage option for CAR, offering improved biopharmaceutical properties.

show abstract

Section: Introductionmentioning

confidence: 99%

Impact of drying on dissolution behavior of carvedilol-loaded sustained release solid dispersion: development and characterization

Halder

Ahmed

Shuma

et al. 2020

Heliyon

View full text Add to dashboard Cite

show abstract

“…Solid dispersion by spray drying method improves the dissolution property of a drug by combining a poorly soluble drug and a hydrophilic carrier [35] . This method was found to be effective in the preparation of Carvedilol-HPMC solid dispersion [61] . Carvedilol and HPMC, at different ratios were dissolved in a co-solvent of methylene chloride and methanol with the volume ratio 1:1.…”

Section: Spray Drying Methodmentioning

confidence: 98%

“…Carvedilol and HPMC, at different ratios were dissolved in a co-solvent of methylene chloride and methanol with the volume ratio 1:1. The suspension was prepared as solid dispersion using spray dryer under the condition showed in (table 2) [61] . In-vitro dissolution test showed a sustained release of Carvedilol during 120mn of dissolution period.…”

Section: Spray Drying Methodmentioning

confidence: 99%

“…These results might be explained by the fact that HPMC was swelled by water and slowly released Carvedilol [62] . [61] .Parameters of spray drying.  Fourier Transform InfraRed spectroscopy (FTIR) [63] identifies chemical bonds in a molecule by producing an infrared absorption spectrum.…”

Section: Spray Drying Methodmentioning

confidence: 99%

“…Other investigations used different polymers (PVP K-30 [32,37] , Poloxamer 407 [32] , HPMC [38] , Gelucire [39] , some Eudragits [38] , PEG 4000, porous silica [40] , Soluplus ® [41] ) alone or in combination also showed a solubility enhancement of the drug. After plotting Carvedilol solubility versus carrier concentration, the apparent complexation constant (K c ) of the solid dispersions can be calculated using the equation:…”

Section: Saturation Solubilitymentioning

confidence: 99%

See 2 more Smart Citations

Carvedilol Solubility Enhancement by Inclusion Complexation and Solid Dispersion: Review

Zoghbi¹,

Wang

2015

J. Drug Delivery Ther.

View full text Add to dashboard Cite

Carvedilol is an effective nonselective alpha-1 and beta blocker discovered by Fritz Wiedemann [1]. It is an antihypertensive drug indicated for the treatment of mild to severe congestive heart failure (CHF), angina pectoris, cardiac arrhythmias and myocardial infarction [2]. Water solubility of Carvedilol is a fundamental property that affects the drug absorption after oral administration. Moreover, its dissolution and gastrointestinal permeability are the parameters that control its bioavailability [3]. The most frequent causes of low oral bioavailability is attributed to poor solubility and low permeability [4]. Carvedilol is categorized as class II drug with low solubility and reasonable membrane permeability. Cyclodextrins are cyclic (α-1,4)-linked oligosaccharides of α-D-glucopyranose, containing a relatively hydrophobic central cavity and hydrophilic outer surface [5]. Drug solubility enhancement using Cyclodextrin and

show abstract

Production of polystyrene-based scintillation microspheres for the measurement of radioactivity by spray-drying

Santiago

Tarancón

Bagán

et al. 2015

J Radioanal Nucl Chem

View full text Add to dashboard Cite

Dissolution properties of control released solid dispersion of carvedilol with HPMC and Eudragit RS

Cited by 16 publications

References 15 publications

Impact of drying on dissolution behavior of carvedilol-loaded sustained release solid dispersion: development and characterization

Impact of drying on dissolution behavior of carvedilol-loaded sustained release solid dispersion: development and characterization

Carvedilol Solubility Enhancement by Inclusion Complexation and Solid Dispersion: Review

Production of polystyrene-based scintillation microspheres for the measurement of radioactivity by spray-drying

Contact Info

Product

Resources

About