Enhancement of griseofulvin release from liquisolid compacts

Hentzschel, Christina M; Alnaief, Mohammad; Смирнова, Ирина; Sakmann, Albrecht; Leopold, Claudia

doi:10.1016/j.ejpb.2011.08.001

Cited by 60 publications

(35 citation statements)

References 31 publications

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“…The solvent helps to dissolve or disperse the drug, which plays a significant role in enhancing the dissolution rate 14 . It has been shown that liquisolid technique is one of the most promising tools applied to improve the absorption and bioavailability of BCS class II drugs [15][16][17][18] . As soft gelatin capsules displayed higher bioavailability than other conventional orally administered solid dosage forms due to the solubilizing effect of liquid vehicle presented in the formulations 19 , this principle is also applicable in liquisolid systems for explaining the improved dissolution rate.…”

Section: Introductionmentioning

confidence: 99%

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: Introductionmentioning

confidence: 99%

Dissolution enhancement of tadalafil by liquisolid technique

Xing

Yang

et al. 2016

Pharmaceutical Development and Technology

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“…It was shown that avicel exhibited fast aqueous penetration into compacts, so act as a disintegrant. The disintegration time of tablets containing neusilin was slightly more than tablets containing avicel may be because of more hardness of former and poor disintegration property of silicate 23 . In-vitro Drug Dissolution: As per dissolution study, the concentration of drug in the liquid vehicle has been shown to affect the dissolution rate.…”

Section: Thickness Hardness Friability Drug Content and Disintegramentioning

confidence: 99%

“…Despite such a high liquid load factor, the formulation fulfilled the required flow ability and tablet hardness. The high liquid loading capacity may be explained by its extremely high specific surface area 23 . Pre-compression Study of Liquisolid Tablets Using Avicel and Neusilin as a Carrier: The liquisolid powder systems were subjected to flow property evaluation.…”

Section: Stability Studymentioning

confidence: 99%

“…The type of carrier has affected the hardness of tablets. The larger surface area associated with neusilin than avicel may cause an increase in contact points between particles and consequently increasing binding and crushing strength 23 . Uniform drug content was observed for all these formulations as per the IP specification (90-110%).…”

Section: Thickness Hardness Friability Drug Content and Disintegramentioning

confidence: 99%

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2017

IJPSR

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Olmesartan medoxomil, a BCS class II drug, is an angiotensin-II receptor antagonist used for the treatment of hypertension. A liquisolid tablet of Olmesartan medoxomil was developed to improve its dissolution and flow properties. The commonly used carrier Avicel was compared with Neusilin. Because of higher liquid load factor, Neusilin was selected as a carrier for further optimization study using 3 2 Factorial design. Two independent factors, % drug concentration in a liquid vehicle (X1) and carrier coating ratio (X2) were studied, each with three levels and the systems was assessed for two dependent variables; % drug dissolution and angle of repose. Mathematical equations and response surface plots were used to relate the dependent and independent variables. All prepared liquisolid formulations were characterized for pre-and post-compression parameters. The optimized formulation F7 (15% drug concentration and 30 carrier coating ratio) was tested for X-ray powder diffractometry and FTIR. Results showed that maximum drug dissolution was exhibited by systems with minimum drug concentration in liquid vehicle and optimum carrier to coating ratio. Optimized formulation displayed significantly enhanced dissolution profiles than that of marketed formulation. In conclusion, avicel could be replaced by neusilin for the formulation of low weight liquisolid tablets along with increased dissolution.

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“…The aqueous solubility for poorly water soluble drugs is usually less than 100 μg/ml (4). Especially poorly soluble, highly permeable active pharmaceutical ingredients (BCS Class II drugs) represent the technological challenge, as poor bioavailability is solely caused by poor water solubility resulting in low drug absorption (5). Different techniques have been reported in the literature to achieve better drug dissolution rates.…”

Section: Introductionmentioning

confidence: 99%

Development and characterization of rozuvastatin loaded self emulsifying drug delivery system for the effective management of hypolipidemia

et al. 2017

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The present work was aimed to develop and characterize rosuvastatin loaded self emulsifying drug delivery system for the effective management of hypolipidemia (RSEDDS) for improving bioavailability, to enhance solubility, to prolong residence time and to provide sufficient amount of drug to a target site in a sustained release manner. Self-emulsifying drug delivery system was prepared by simple emulsification technique, six batches i.e. f1 to f6 were prepared by varying the concentration of oils, surfactant, co-surfactant and co-solvent and evaluated for the various parameters, e.g. optical microscopy, assessment of self emulsification, emulsification time, droplet size analysis, zeta potential measurement, transmission electron microscopy, viscosity determination, drug content, percentage transmittance, in vitro dissolution study and stability studies. The RSEDDS was optimized and batch F5 was opted for further studies. The drug content of selected batch F5 was found to be 97.65 ± 1.37%, which suggests that method for encapsulation was effective. The results of in vitro drug release studies showed about 83% of the drug release within 180 minutes, which exhibit sustained release of drug. There were no significant changes observed in the physical appearance, drug content and in vitro release during stability studies. The studies reveal that the RSEDDS is a potential candidate for sustained release drug delivery which can successfully increase bioavailability. increasing efficacy.

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Enhancement of griseofulvin release from liquisolid compacts

Cited by 60 publications

References 31 publications

Dissolution enhancement of tadalafil by liquisolid technique

Dissolution enhancement of tadalafil by liquisolid technique

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Development and characterization of rozuvastatin loaded self emulsifying drug delivery system for the effective management of hypolipidemia

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