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

Javadzadeh, Yousef; Siahi, M R; Asnaashari, Solmaz; Nokhodchi, Ali

doi:10.2478/v10007-007-0008-6

Cited by 49 publications

(29 citation statements)

References 18 publications

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“…8 During the past few years, there has been a great pace in using solubility enhancement techniques for the improvement of the dissolution rate and subsequently the bioavailability of poorly water soluble drugs. Several techniques like nanomaterialization, 9 salt formation, 10 hydrotropy, 11 liposome formation, 12 liquisolid compaction, 13 solid dispersion, 14 SMEDDS, 15 and many other significant techniques have been reported for improving bioavailability of poorly water soluble drugs of class BCS-II and BCS-IV. Solid dispersion (SD) is one of the most promising strategies to improve the dissolution properties and bioavailability of poorly water-soluble drugs where drug materials are dispersed in an inert carrier.…”

Section: Introductionmentioning

confidence: 99%

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

Dangre¹,

Godbole²,

Ingale³

et al. 2016

IJPER

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Background: Eprosartan mesylate (EM) is a poorly aqueous soluble drug belonging to BCS-class II suffers from low bioavailability (13%). The present study involves an effort for improving dissolution and thus the bioavailability of EM using solid dispersion approach. Methods: Solid dispersion (SD) was prepared by melting, solvent evaporation and kneading method using different ratios of drug and polymers (PEG-4000, Eudragit E-100, PVP K-30, Poloxamer-407, and Eudragit L-100). Phase solubility study revealed highest solubility in PVP K-30 at 1:2 ratios. The solid state characterizations of selected solid dispersion formulation (SD-15) were performed by infrared spectroscopy, differential scanning calorimeter, X-ray diffraction study and scanning electron microscopy. In vitro dissolution was carried out in phosphate buffer (pH 7.4) at 50 rpm in 900 ml of volume. The in vivo pharmacokinetic study of selected formulation (SD-15) was carried out in male Wistar rats using non-compartment analysis by linear trapezoidal method after a single oral dose of 10 mg/kg of EM. Results: The solid state characterization revealed no such drug-polymer interactions and rapid transformation of crystalline drug in an amorphous state, which amplifies the aqueous solubility and hence the dissolution rate. The in vitro dissolution study of the dispersions prepared by PVP K-30 (1:2) was found to be 95.5% after 1 hr. In vivo pharmacokinetic study in Wistar rats showed significant improvement in oral bioavailability of EM in SD-15 with the 2.4 fold increments than the pure drug. Conclusion: The solid dispersion prepared using PVP K-30 by kneading method showed improved dissolution and bioavailability. Therefore, solid dispersion formulation can be sorted as a promising approach for improving the dissolution and bioavailability of Eprosartan mesylate.

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Section: Introductionmentioning

confidence: 99%

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

Dangre¹,

Godbole²,

Ingale³

et al. 2016

IJPER

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“…The rate of absorption is controlled by how fast the drug dissolves in the fluid at the site of absorption. Therefore, it can be said that the dissolution rate is the rate-limiting step in drug absorption [5].…”

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confidence: 99%

“…The major obstacle that concerns the industry is the solubility of the active ingredient(s) [4]. This big challenge is important for the pharmaceutical scientists because active ingredients in tablets must undergo dissolution before they are available for absorption from the GI tract [5]. About 40% of today's newly developed drugs are known to be hydrophobic and thus do not dissolve in water [6].…”

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confidence: 99%

Wet Granulation to Overcome Liquisolid Technique Issues of Poor Flowability and Compactibility: A Study to Enhance Glibenclamide Dissolution

Javaheri¹,

Carter²,

Elkordy³

2014

Journal of Pharmaceutics and Drug Development

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The aim of this study is to apply wet granulation on liquisolid powders to overcome issues of poor powder flowability and compressibility especially with using high viscosity liquid vehicles. Different liquisolid formulations were made using three excipients where the effect of each excipient used in the dissolution of the model hydrophobic drug (Glibenclamide) was evaluated. The Glibenclamide tablets were formulated using PEG 400, Synperonic PE/L44 and Cremophor ELP, at a 10 %w/w in liquid vehicle drug concentration. The carrier (Avicel®PH102) was used followed by colloidal silicon dioxide (coating material) that converted the wet mixture into dry powder. Potato starch, 5%w/w, as a disintegrant was mixed with the mixture manually for 10 minutes and was finalized by adding 0.75% of magnesium stearate as a lubricant. The final powder (depending on its flowability and compactability) was then compacted automatically using a single-punch tableting machine to give tablets with 4mg unit drug dose. Prepared liquisolid compacts were characterised via B.P. quality control tests. In this study, a novel discovery was achieved to overcome the major problems with liquisolid preparations (flowability and compactability). This new technique is the wet granulation process to be applied with liquisolid powders just before the compaction stage of the powders into tablets. Consequently, it was found that by application of wet granulation to liquisolid powder admixture, the large-scale production of liquisolid compacts is feasible and can be easily applied by pharmaceutical industry. As with some liquisolid vehicles especially high viscosity although very good to enhance dissolution usually formulations are studied in powder forms [1,2].Keywords: Liquisolid compacts; Granulation; Glibenclamide; Flowability and compactibility; Dissolution rate; Wettability Abstract Oral drug delivery is the main and most common route of administration. There are various types of dosage forms that can be formulated, and tablets are known to be the most common type. Tablets can be manufactured by several stages where the final stage is the compression of the powder held within a confined space. In addition, the use of tablets as dosage form became of interest to the pharmaceutical industry, thus the formulation of tablet with variety of forms were formulated [3]. Tablets are solid preparations each containing a single dose of one or more active ingredients and produced via compression of uniform volumes of particles. The secret behind the difference between each tablet is in the type of excipients used. Pharmaceutical industry use different excipients, diluents, disintegrants and lubricants to ensure that tablets of specified quality are prepared. However, one excipient can affect the properties of the tablets. Thus, it can be said that each excipient added has a specific role in the formulation of the oral tablets. ISSN: 2348-9782In addition, the In-vitro dissolution study found that granulated liquisolid tablets enhanced not only the flowability an...

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“…Micronization drugs also have a tendency to form agglomerates due to hydrophobic properties and will reduce its surface area. 2 Currently, the liquisolid technique is one of the most promising methods to improve the dissolution rates of the drugs with low solubility in water. This technique is easy due to the relatively low cost and can be used in an industrial scale.…”

Section: Introductionmentioning

confidence: 99%

Liquisolid Technique for Ibuprofen Tablet

Hadisoewignyo¹,

Purnama²,

Fenny³

et al. 2013

Int. Res. J. Pharm.

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Ibuprofen is a drug with poor solubility in water but good permeability in the gastrointestinal tract. Liquisolid tablet is one method of increasing solubility and dissolution rate s of ibuprofen. The aim of this study is to determine the effects of glycerine, PEG 400, and propylene glycol as a non-volatile solvent and HPMC K4M as a hydrophilic polymer in order to understand the dissolution rates of ibuprofen liquisolid tablets. In this research, 10 formulas of ibuprofen liquisolid tablets were made. The ratio of ibuprofen in glycerinee is 3:1; in PEG 400 and in propylene glycol is 5:1 with various concentration of HPMC K4M (2.5, 5 and 10 %). Formula non liquisolid was made as a control, so there was no addition of non-volatile solvent and hydrophilic polymer. Based on the results, ibuprofen liquisolid tablets that use glycerine, PEG400 or propylene glycol as the non-volatile solvent and HPMC K4M as the hydrophilic polymer can increase the dissolution rate constant of ibuprofen compared with non liquisolid ibuprofen tablets. The addition of HPMC K4M can increase the dissolution rate constant of ibuprofen liquisolid tablets until concentration of less than 2.5 % in glycerine; in PEG 400 can increase the dissolution rate constant of ibuprofen liquisolid tablets until concentration up to 5 % and in propylene glycol can increase the dissolution rate constant of ibuprofen until concentration up to 10 % because the polymer will swell and form a viscous layer that inhibits the disintegration; therefore, the percent release is decreasing.

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

Cited by 49 publications

References 18 publications

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

Wet Granulation to Overcome Liquisolid Technique Issues of Poor Flowability and Compactibility: A Study to Enhance Glibenclamide Dissolution

Liquisolid Technique for Ibuprofen Tablet

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