scholarly journals Liquisolid technique as a tool for enhancement of poorly water-soluble drugs and evaluation of their physicochemical properties

2007 ◽  
Vol 57 (1) ◽  
pp. 99-109 ◽  
Author(s):  
Yousef Javadzadeh ◽  
Mohammad Siahi ◽  
Solmaz Asnaashari ◽  
Ali Nokhodchi
Keyword(s):  
Physicochemical Properties ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Scanning Calorimetry ◽  
Dissolution Rates ◽  
Compression Technique ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Liquisolid Compacts

Liquisolid technique as a tool for enhancement of poorly water-soluble drugs and evaluation of their physicochemical properties The potential of liquisolid systems to improve the dissolution properties of a water-insoluble agent (indomethacin) was investigated. In this study, different formulations of liquisolid tablets using different co-solvents (non-volatile solvents) were prepared and the effect of aging on the dissolution behaviour of indomethacin liquisolid compacts was investigated. To evaluate any interaction between indomethacin and the other components in liquisolid formulations, X-ray powder diffraction (XPD) and differential scanning calorimetry (DSC) were used. Dissolution test was carried out at two different pH, 1.2 and 7.2, to simulate the stomach or intestine fluid, respectively. The results showed that liquisolid formulations exhibited significantly higher drug dissolution rates at pH 1.2 and 7.2 compared to compacts prepared by the direct compression technique. The enhanced rate of indomethacin dissolution from liquisolid tablets was probably due to an increase in wetting properties and surface area of drug particles available for dissolution. In order to investigate the effect of aging on the hardness and dissolution rate of liquisolid compacts, the formulations were stored at 25 °C/75% relative humidity for a period of 12 months. The results showed that aging had no significant effect on dissolution profiles of liquisolid tablets. Liquisolid compacts containing propylene glycol as vehicle produced higher dissolution rates in comparison with liquisolid compacts containing PEG 400 or Tween 80 of the same concentration. The DSC and XPD results showed no changes in crystallinity of the drug and interaction between indomethacin and excipients (Avicel and silica) during the process.

Liquisolid Compacts Technique of Poor Water Soluble Drugs: An Overview

2021 ◽  
pp. 5569-5572
Author(s):  
E. Bhavya ◽  
M.D. Dhere
Keyword(s):  
Mathematical Models ◽  
Dissolution Rate ◽  
Coating Material ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Coating Materials ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Liquisolid Compacts

Liquisolid technique is new and promising method that can use to enhance the dissolution rate of poorly water soluble drugs. Liquisolid compact technique is based upon the dissolving the drug in a suitable non-volatile solvent by using carrier and coating material for the conversion of acceptable flowing and compressible powders. By applying the mathematical models the carrier and coating materials optimized. In this case the drug is almost solubilised in the solvent or molecularly dispersed state which contributes the enhanced drug dissolution.

It is Possible to Achieve Tablets with Good Tabletability from Solid Dispersions – the Case of the High Dose Drug Gemfibrozil

2020 ◽  
Vol 17 ◽  
Author(s):  
Eduarda Rocha Bigogno ◽  
Luciano Soares ◽  
Matheus Henrique Ruela Mews ◽  
Melissa Zétola ◽  
Giovana Carolina Bazzo ◽  
...  
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Croscarmellose Sodium ◽  
Poorly Water Soluble

Background: Solid dispersions (SDs) have been extensively used to increase dissolution of poorly water-soluble drugs. However, there are few studies exploring SDs properties that must be considered during tablet development, like tabletability. Poorly water-soluble drugs with poor compression properties and high therapeutic doses, like gemfibrozil, are an additional challenge in the production of SDs-based tablets. Objective: This study evaluates the applicability of SDs to improve both tabletability and dissolution rate of gemfibrozil. A SD-based tablet formulation was also proposed. Method: SDs were prepared by ball milling, using hydroxypropyl methylcellulose (HPMC) as carrier, according to a 23 factorial design. The formulation variables were: gemfibrozil:HPMC ratio, milling speed, and milling time. The response in the factorial analysis was the tensile strength of the compacted SDs. Dissolution rate and solid-state characterization of SDs were also performed. Results: SDs showed simultaneous drug dissolution enhancement and improved tabletability when compared to corresponding physical mixtures and gemfibrozil. The main variable influencing drug dissolution and tabletability was the gemfibrozil:HPMC ratio. Tablets containing gemfibrozil-HPMC-SD (1:0.250 w/w) and croscarmellose sodium showed fast and complete drug release while those containing the same SD and sodium starch glycolate exhibited poor drug release due to their prolonged disintegration time. Conclusion: SDs proved to be effective for simultaneously improving tabletability and dissolution profile of gemfibrozil. Tablets containing gemfibrozil-HPMC-SD and croscarmellose sodium as disintegrating agent showed improved drug release and good mechanical strength, demonstrating the potential of HPMC-based SDs to simultaneously overcome the poor dissolution and tabletability properties of this drug.

scholarly journals Enhancement of the dissolution rates of poorly water-soluble drugs by water-soluble gelatin.

1989 ◽  
Vol 37 (8) ◽  
pp. 2251-2252 ◽  
Author(s):  
Teruko IMAI ◽  
Tetsuyuki NISHIYAMA ◽  
Masao UENO ◽  
Masaki OTAGIRI
Keyword(s):  
Water Soluble ◽  
Dissolution Rates ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

scholarly journals Nanoparticulation of Poorly Water Soluble Drugs Using a Wet-Mill Process and Physicochemical Properties of the Nanopowders

2009 ◽  
Vol 57 (10) ◽  
pp. 1050-1057 ◽  
Author(s):  
Yusuke Tanaka ◽  
Mitsugi Inkyo ◽  
Ryoko Yumoto ◽  
Junya Nagai ◽  
Mikihisa Takano ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Mill Process

Modulation of Drug Crystallization and Molecular Interactions by Additives in Solid Dispersions for Improving Drug Bioavailability

2019 ◽  
Vol 25 (18) ◽  
pp. 2099-2107 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Wei Duan ◽  
Beom-Jin Lee ◽  
Thao T.D. Tran
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Drug Bioavailability ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Potential Applications ◽  
Poorly Water Soluble ◽  
The Right

Background:: An increase in poorly water-soluble drugs makes the design of drug delivery systems challenging. Methods:: Currently, a number of prospective solid dispersions have been investigated with potential applications for delivering a variety of poorly water-soluble drugs. A number of traditional solid dispersions and modifiedsolid dispersions offer attractive advantages in the fabrication, design and development of those drugs for effective therapeutics. Results:: Although traditional solid dispersions can produce a higher release rate, resulting in higher bioavailability compared to conventional dosage forms, this method is not always a promising approach. Modified-solid dispersion has demonstrated both the ability of its polymers to transform drug crystals into amorphous forms and molecular interactivity, thereby improving drug dissolution rate and bioavailability, especially with tough drugs. However, the classification of modified-solid dispersion, which guides the selection of the right strategy in solid dispersion preparation, remains ill-defined. Conclusions:: This review focused on effective strategies in using additives in solid dispersion for improving drug bioavailability.

Fast-dissolving Solid Dispersions for the Controlled Release of Poorly Water-soluble Drugs

2020 ◽  
Vol 26 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Beom-Jin Lee ◽  
Thao T.D. Tran
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Oral Drug Delivery ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Oral Drug ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

: Solid dispersions offer many advantages for oral drug delivery of poorly water-soluble drugs over other systems, including an increase in drug solubility and drug dissolution. The improvement of drug absorption and higher bioavailability of active pharmaceutical ingredients in the gastrointestinal tract have been reported in various studies. In certain circumstances, a rapid pharmacological effect is required for patients. Fast-dissolving solid dispersions provide an ideal formulation in such cases. This report will provide an overview of current studies on fast-dissolving solid dispersions, including not only solid dispersion powders with fast dissolution rates but also specific does forms for the controlled release of poorly water-soluble drugs. Specifically, the applications of fast-dissolving solid dispersions will be described in every specific case. Moreover, pharmaceutical approaches and the utilization of polymers will be summarized. The classification and analysis of fast-dissolving solid dispersions could provide insight into strategies and potential applications in future drug delivery developments.

Encapsulation of poorly water-soluble drugs into organic nanotubes for improving drug dissolution

2014 ◽  
Vol 469 (1) ◽  
pp. 190-196 ◽  
Author(s):  
Kunikazu Moribe ◽  
Takashi Makishima ◽  
Kenjirou Higashi ◽  
Nan Liu ◽  
Waree Limwikrant ◽  
...  
Keyword(s):  
Water Soluble ◽  
Drug Dissolution ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Organic Nanotubes
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