The Liquisolid technique: an overview

Burra, Shashidher; Yamsani, Madhusudhanrao; Venkateswarlu, Vobalaboina

doi:10.1590/s1984-82502011000300005

Cited by 22 publications

(10 citation statements)

References 17 publications

(14 reference statements)

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“…As for the dissolution rate, it was reported that dissolution rate was affected by the excipients ratio (R). More specifically, dissolution rate could be increased proportionally as excipients ratio R was increased until an apparent maximum plateau was reached at R value greater than 20 37 , thus three excipients ratios (10, 15 and 20) were selected to analyze the effect of excipients ratio R on the dissolution rate. Avicel PH 102 is one of the most commonly used carriers.…”

Section: Solubility Studymentioning

confidence: 99%

“…However, only small amount of dissolution fluid was involved in the formation of the stagnant diffusion layer around the drug particle. Consequently, at such a micro-environment of diffusion layer, the infinite amounts of liquid vehicle may act as a cosolvent, leading to the enhancement of saturated solubility (C S ) of tadalafil 37 . An increase in C S would undoubtedly increase the drug concentration gradient (C S À C), and thus improved the dissolution rate according to the Noyes-Whitney equation 54 .…”

Section: In Vitro Dissolution Studymentioning

confidence: 99%

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Dissolution enhancement of tadalafil by liquisolid technique

Xing

Yang

et al. 2016

Pharmaceutical Development and Technology

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This study aimed to enhance the dissolution of tadalafil, a poorly water-soluble drug by applying liquisolid technique. The effects of two critical formulation variables, namely drug concentration (17.5% and 35%, w/w) and excipients ratio (10, 15 and 20) on dissolution rates were investigated. Pre-compression tests, including particle size distribution, flowability determination, Fourier transform infrared (FT-IR), differential scanning calorimetry (DSC), X-ray diffractometry (XRD) and scanning electron microscopy (SEM), were carried out to investigate the mechanism of dissolution enhancement. Tadalafil liquisolid tablets were prepared and their quality control tests, dissolution study, contact angle measurement, Raman mapping, and storage stability test were performed. The results suggested that all the liquisolid tablets exhibited significantly higher dissolution rates than the conventional tablets and pure tadalafil. FT-IR spectrum reflected no drug-excipient interactions. DSC and XRD studies indicated reduction in crystallinity of tadalafil, which was further confirmed by SEM and Raman mapping outcomes. The contact angle measurement demonstrated obvious increase in wetting property. Taken together, the reduction of particle size and crystallinity, and the improvement of wettability were the main mechanisms for the enhanced dissolution rate. No significant changes were observed in drug crystallinity and dissolution behavior after storage based on XRD, SEM and dissolution results.

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Section: Solubility Studymentioning

confidence: 99%

Section: In Vitro Dissolution Studymentioning

confidence: 99%

Dissolution enhancement of tadalafil by liquisolid technique

Xing

Yang

et al. 2016

Pharmaceutical Development and Technology

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“…The method employed for tableting in this study was direct compression for which the drug should possess good flow properties in order to get a uniform feed as well as reproducible filling of tablet dies, the failing of which may lead to high dose variations. In order to ensure the flow properties of the liquisolid systems for direct compression into tablets, angle of repose measurements, Carr's index and Hausner's ratios were adopted for further evaluation [27][28][29][30] . Pure drug lornoxicam exhibited high angle of repose value (45.07 ± 0.73) indicating extremely poor flow property.…”

Section: Micromeritic Propertiesmentioning

confidence: 99%

Untitled

2020

IJPSR

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The present study is undertaken with an aim to improve the dissolution profile and availability of a poorly soluble drug, Lornoxicam, through the development of liquisolid tablets. Liquisolid compacts were prepared by employing PEG 400, Avicel PH 112, and Aerosil 200 as solvent, carrier and coating materials, respectively. The flow properties of the drug improved significantly after formulating it into the liquisolid compacts. The post-compressional parameters of prepared tablets revealed the uniformity and maintenance of standards within the different batches. In-vitro drug release studies showed significant improvement in the dissolution of lornoxicam in its liquisolid form compared to a commercial product. The effect of formulation parameters, such as drug concentration and carrier to coat ratio, on enhancing drug dissolution, was also explored. FT-IR, DSC and XRD techniques were employed for the physical characterization of the drug in the liquisolid systems. The drug release from the optimized liquisolid compacts (F8) followed first-order release kinetics. INTRODUCTION: Solubility is one of the important parameters to achieve the desired concentration of drug in systemic circulation for achieving required pharmacological response. Poorly water-soluble drugs often require high doses in order to reach the therapeutic plasma concentrations after oral administration. Most of the drugs are either weakly acidic or weakly basic, having poor aqueous solubility, thus producing major problems with formulation development of new chemical entities. Hence, a significant number of new and possibly beneficial chemical entities do not have suitable pharmaceutical dosage form because of their poor solubility and poor dissolution rate 1, 2 .

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“…Generally, the solid liquid compacts with high R-value comprised of the relatively large amount of powder admixture (carrier and coating materials) and the amount of non-volatile solvent available per powder substrate is relatively larger. Hence the solid liquid compacts with high R values showed a better dissolution profile [29,30].…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

Cinnarizine Liquid Solid Compacts: Preparation Evaluation

Sisinthy

Selladurai

2019

Int J App Pharm

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Objective: The objective of this research was to formulate cinnarizine tablets using the liquid-solid compact technique to enhance its solubility and dissolution rate.Methods: Cinnarizine liquid-solid compacts were formulated using propylene glycol as the non-volatile solvent, Neusilin US2 as the carrier material, Aerosil 200 as the coating material and croscarmellose sodium as the disintegrant. The interaction between drug and excipients were characterized by Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) studies. Different batches of liquid, solid compacts were prepared by using varying carrier-coating excipient ratio and different concentration of liquid medication. Flow parameters such as bulk density, tapped density, Carr’s Index, Hausner’s Ratio as well as an angle of repose were used to test the flowability of the powder blend. The liquid-solid compacts were produced by direct compression method and were evaluated for tests such as weight variation, drug content, hardness, thickness, friability, wetting time, disintegration time as well as the in vitro dissolution studies.Results: The results of the preformulation studies of liquisolid compacts showed acceptable flow properties. The results of FTIR and DSC studies showed that there is no drug-excipient interactions. The different R values and concentrations were found to have a marked effect on the dissolution profile. Formulations with higher carrier: coating ratio (R-value) and lower drug concentrations displayed a better dissolution profile. The percentage of drug release of F3 with an R-value of 20 and a drug concentration of 10% was found to be 88.11% when compared to the conventional marketed tablet which released only 44.07% at the end of 2 h.Conclusion: From this research, it is inferred that liquid-solid technique is a promising and effective approach that can be used to enhance the dissolution rate of cinnarizine.

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The Liquisolid technique: an overview

Cited by 22 publications

References 17 publications

Dissolution enhancement of tadalafil by liquisolid technique

Dissolution enhancement of tadalafil by liquisolid technique

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Cinnarizine Liquid Solid Compacts: Preparation Evaluation

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