Effect of Some Commercial Grades of Microcrystalline Cellulose on Flowability, Compressibility, and Dissolution Profile of Piroxicam Liquisolid Compacts

Javadzadeh, Yousef; Shariati, Hesam; Movahhed-Danesh, Elmira; Nokhodchi, Ali

doi:10.1080/03639040802277672

Cited by 46 publications

(16 citation statements)

References 33 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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“…When the drug within the liquisolid system is completely dissolved in the liquid vehicle, it is located in the powder substrate still in a solubilized state. The accelerated release in zolmitriptan liquisolid ODTs (F11) is due to its markedly increased wettability and surface area available to the dissolution medium [34]. fig.…”

Section: Wetting Time (Wt) and In Vitro Disintegration Time (Dt)mentioning

confidence: 99%

Design Zolmitriptan Liquisolid Orodispersible Tablets and Their in Vitro Evaluation

Egla

Hammid

2016

Int J Pharm Pharm Sci

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Objective: The objective of present study is to develop orodispersible tablets (ODTs) of zolmitriptan by liquisolid technique using different types of super disintegrants to enhance the disintegration and dissolution of zolmitriptan to improve the bioavailability of the drug.Methods: Liquisolid ODTs of zolmitriptan were prepared from; microcrystalline cellulose (Avicel PH-102) as carrier, colloidal silicon dioxide (Aerosil 200) as a coating material, croscarmellose sodium (CSS), sodium starch glycolate (SSG), and crospovidone (CP) as super disintegrants, and propylene glycol as liquid vehicle. The ratio of carrier to coating material was kept constant in all formulations at 35:1, this ratio was chosen after testing the ratios 10:1, 15:1, 20:1, 25:1,30:1, and 35:1. The ratio 35:1 give optimal results relative to other ratios. The pre-compression evaluation includes: flow properties were measured using the angle of repose and the compressibility index and FT-IR. The prepared liquid-solid system compacts were evaluated for their post-compression evaluation which includes: hardness, friability, wetting time, in vitro disintegration time, drug content and in vitro drug release. Results:The tabletting properties of the liquid-solid ODTs were within the acceptable limits. Among the three super disintegrants, CP found to be the best in term of showing the fastest disintegration time. The optimized selected formula (F11) was prepared using 5% w/w crospovidone, by direct compression showed the shortest disintegration time (24 s), superior drug release profile [ the time required for 80% of the drug to be released (T80%) and percent drug dissolved in 2 min (D2 Conclusion:The overall results showed that CP was the best super disintegrant of showing the shortest disintegration time while loading factor of 0.125 was the best in the preparing of zolmitriptan liquid-solid ODTs, and this suggested the possibility of utilizing the selected best formula (F11) in the preparation of zolmitriptan ODTs as a new dosage form for oral administration. min) 1.84 min and 87.59%, respectively]. In addition to that, the selected formula had an acceptable hardness and friability, so it was selected as the best formula.

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“…Also, these authors observed that the drug release superiority of liquisolid tablets is inversely proportional to the aqueous solubility of the contained drug. Liquisolid tablets demonstrated significantly faster drug dissolution patterns in small volumes of dissolution media such as 450 mL and 300 mL Studies by Javadzadeh Y., et al (2009) provide evidence that among the different grades of MCC evaluated, compacts containing MCC ® PH 101 and 102 showed better hardness, friability and dissolution profile. Aging had no effect on hardness or dissolution profile of liquisolid tablets prepared from MCC PH 101.…”

Section: Pre Compression Studiesmentioning

confidence: 99%

The Liquisolid technique: an overview

Burra¹,

Yamsani²,

Venkateswarlu³

2011

Braz. J. Pharm. Sci.

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A novel "Powder Solution Technology" involves absorption and adsorption efficiency which makes use of liquid medications, drug suspensions admixed with suitable carriers, coating materials and formulated into free flowing, dry looking, non adherent and compressible powder forms. Based upon a new mathematical model expression, improved flow characteristics and hardness of the formulation has been achieved by changing the proportion of Avicel ® PH 200 and Aerosil ® PH 200 from 50:1 ratio to 5:1 and in which the drug is dispersed in an almost molecularly state. Due to their significantly improved wetting properties a greater drug surface area is exposed to the dissolution media, resulting in an increased dissolution rate and bio availability. By using the Liquisolid technique, sustained drug delivery systems were developed for the water soluble drugs in which hydrophobic non-volatile solvents are used as vehicles.Uniterms: Liquisolid. Solubility. Bioavailability. Flow properties. Load factor. Powder solution technology.A nova "Tecnologia da Solução Sólida" envolve eficiência de absorção e de adsorção, faz uso de medicações líquidas, suspensões de fármacos e misturas com transportadores adequados, materiais de cobertura e é formulada em formas sólidas em fluxo livre, secas, não aderentes e compressíveis. Com base em novo modelo matemático, características aprimoradas de fluxo e dureza da formulação foram alcançadas modificando-se a proporção de Avicel ® PH 200 e Aerosil ® PH 200 de 50:1 para 5:1, na qual o fármaco é disperso quase que no estado molecular. Devido às propriedades de umidificação significativamente aprimoradas e à área do fármaco exposta ao meio de dissolução, que resulta na velocidade de dissolução, a biodisponibilidade foi aumentada. Utilizando a técnica Liquisólido, desenvolveram-se sistemas de liberação controlada de fármacos solúveis em água, nos quais solventes hidrofóbicos não voláteis foram usados como veículos.Unitermos: Liquisólido. Solubilidade. Biodisponibilidade. Propriedades de fluxo. Fator de carga. Tecnologia de solução sólida.

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Effect of Some Commercial Grades of Microcrystalline Cellulose on Flowability, Compressibility, and Dissolution Profile of Piroxicam Liquisolid Compacts

Cited by 46 publications

References 33 publications

Dissolution enhancement of tadalafil by liquisolid technique

Dissolution enhancement of tadalafil by liquisolid technique

Design Zolmitriptan Liquisolid Orodispersible Tablets and Their in Vitro Evaluation

The Liquisolid technique: an overview

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