Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine)

Javadzadeh, Yousef; Jafari-Navimipour, Baharak; Nokhodchi, Ali

doi:10.1016/j.ijpharm.2007.03.034

Cited by 175 publications

(144 citation statements)

References 17 publications

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“…Hence, the drug is available in a solubilized, molecularly dispersed state, which in turn extremely increases surface of the drug available for dissolution. In contrast, conventional MC tablets are just exposing micronized drug particles Javadzadeh et al, 2007a). Second, it is expected that the solubility of the MC might be increased with liquisolid systems, but the small amount of glycerol formal in a liquisolid compact is not sufficient to increase the overall solubility of the MC in the dissolution medium.…”

Section: Dissolution Studiesmentioning

confidence: 99%

“…While, the liquisolid tablets with low R-values have poor dissolution . In such cases, even though drug diffusion out of the primary particles may be rapid, oversaturation might occur resulting in local precipitation/ recrystallization of the drug and thus decreased release rate (Spireas et al, 1999;Javadzadeh et al, 2007a). Moreover, as silica is a hydrophobic material, high amounts of it can cause retardation of drug release.…”

Section: Dissolution Studiesmentioning

confidence: 99%

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Use of biorelevant media for assessment of a poorly soluble weakly basic drug in the form of liquisolid compacts: in vitro and in vivo study

Badawy¹,

Kamel

Sammour³

2014

Drug Delivery

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The purpose of this work is to use biorelevant media to evaluate the robustness of a poorly water soluble weakly basic drug to variations along the gastrointestinal tract (GIT) after incorporation in liquisolid compacts and to assess the success of these models in predicting the in vivo performance. Liquisolid tablets were prepared using mosapride citrate as a model drug. A factorial design experiment was used to study the effect of three factors, namely: drug concentration at two levels (5% and 10%), carriers at three levels (avicel, mannitol and lactose) and powder excipients ratio (R) of the coating material at two levels (25 and 30). The in vitro dissolution media utilized were 0.1 N HCl, hypoacidic stomach model and a transfer model simulating the transfer from the stomach to the intestine. All compacts released above 95% of drug after 10 min in 0.1 N HCl. In the hypoacidic model, the compacts with R 30 were superior compared to R 25, where they released 490% of drug after 10 min compared to 80% for R 25. After the transfer of the optimum compacts from Simulated gastric fluid fast (SGFfast) to fasted state simulated intestinal fluid, slight turbidity appeared after 30 min, and the amount of drug dissolved slightly decreased from 96.91% to 90.59%. However, after the transfer from SGFfast to fed state simulated intestinal fluid, no turbidity or precipitation occurred throughout time of the test (60 min). In vivo pharmacokinetic study in human volunteers proved the success of the in vitro models with enhancement of the oral bioavailability (121.20%) compared to the commercial product.

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Section: Dissolution Studiesmentioning

confidence: 99%

Section: Dissolution Studiesmentioning

confidence: 99%

Use of biorelevant media for assessment of a poorly soluble weakly basic drug in the form of liquisolid compacts: in vitro and in vivo study

Badawy¹,

Kamel

Sammour³

2014

Drug Delivery

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“…This could increase the mass of each tablet over the limit for easy application (21,25). Nevertheless, Javadzadeh et al (26) have proven that it is possible to load a large amount of drug into a liquisolid system using additives (such as polyvinylpyrrolidone, hydroxypropyl methylcellulose and polyethylene glycol 35 000), which can be added to the drug in liquid state to reduce the amount of carrier and coating material. Singh et al (27) have shown that higher viscosity of the additives leads to smaller amounts of carrier and coating material needed to produce flowable powder.…”

Section: Advantages Limitations and Application Of Liquisolid Systemsmentioning

confidence: 99%

“…Polysorbate 80 was successfully used to dissolve the drug in several liquisolid systems containing carbamazepine (26,45), indomethacin (46,47), piroxicam (48), propranolol hydrochloride (35), etc.…”

Section: Excipients For Liquisolid Systemsmentioning

confidence: 99%

Liquisolid systems and aspects influencing their research and development

Vraníková¹,

Gajdziok²

2013

Acta Pharmaceutica

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“…Other methods used to improve drug solubility include complexation [17], liquisolid techniques [18,19] and salt formation [20,21]. Several authors have classed the solid dispersion approach as one of the most effective method of improving dissolution of drugs [5,8,22].…”

Section: Introductionmentioning

confidence: 99%

Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

Adebisi

Kaialy

Hussain

et al. 2016

Colloids and Surfaces B: Biointerfaces

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Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions, Colloids and Surfaces B: Biointerfaces http://dx.doi.org/10. 1016/j.colsurfb.2016.07.032 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. 4. GLU improved the handling of PXM as it significantly reduced its charge in all the spray dried formulations. Technique could be used to determine appropriate formulations that improve handling AbstractThis work explores the use of both spray drying and D-glucosamine HCl (GLU) as a hydrophilic carrier to improve the dissolution rate of piroxicam (PXM) whilst investigating the electrostatic charges associated with the spray drying process. Spray dried PXM:GLU solid dispersions were prepared and characterised (XRPD, DSC, SEM). Dissolution and triboelectric charging was also conducted. The results showed that the spray dried PXM alone, without GLU produced some PXM form II (DSC results) with no enhancement in solubility relative to that of the parent PXM.XRPD results also showed the spray drying process to decrease the crystallinity of GLU and solid dispersions produced. The presence of GLU improved the dissolution rate of PXM. Spray dried PXM: GLU at a ratio of 2:1 had the most improved dissolution. The spray drying process generally yielded PXM-GLU spherical particles of around 2.5 µm which may have contributed to the improved dissolution. PXM showed a higher tendency for charging in comparison to the carrier GLU (-3.8 versus 0.5 nC/g for untreated material and -7.5 versus 3.1 nC/g for spray dried materials). Spray dried PXM and spray dried GLU demonstrated higher charge densities than untreated PXM and untreated GLU, respectively. Regardless of PXM:GLU ratio, all spray dried PXM:GLU solid dispersions showed a negligible charge density (net-CMR: 0.1 -0.3 3 nC/g). Spray drying of PXM:GLU solid dispersions can be used to produce formulation powders with practically no charge and thereby improving handling as well as dissolution behaviour of PXM.

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Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine)

Cited by 175 publications

References 17 publications

Use of biorelevant media for assessment of a poorly soluble weakly basic drug in the form of liquisolid compacts: in vitro and in vivo study

Use of biorelevant media for assessment of a poorly soluble weakly basic drug in the form of liquisolid compacts: in vitro and in vivo study

Liquisolid systems and aspects influencing their research and development

Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

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