Dissolution rate improvement of poorly water-soluble drugs obtained by adsorbing solutions of drugs in hydrophilic solvents onto high surface area carriers

Friedrich, H; Fussnegger, Bernd; Kolter, Karl; Bodmeier, Roland

doi:10.1016/j.ejpb.2005.08.013

Cited by 81 publications

(40 citation statements)

References 12 publications

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“…10 Although nanoparticle formulations of silica, such as Aerosil First reported by Mobil scientists, 11,12 mesoporous silica has attracted considerable attention as a molecular sieve due to its inherent properties, such as a large pore volume and surface area, and a tunable narrow pore size distribution. 13,14 These properties suggest that mesoporous silica may have a higher liquid adsorption capacity when used in liquisolid formulations as compared with conventional silica.…”

Section: Introductionmentioning

confidence: 99%

In vitro and in vivo evaluation of ordered mesoporous silica as a novel adsorbent in liquisolid formulation

Bao¹,

Wang²,

Quan³

et al. 2012

IJN

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Background: A liquisolid technique has been reported to be a new approach to improve the release of poorly water-soluble drugs for oral administration. However, an apparent limitation of this technique is the formulation of a high dose because a large amount of liquid vehicle is needed, which finally results in a low-dose liquisolid formulation. Silica as an absorbent has been used extensively in liquisolid formulations. Although nanoparticle silica can be prepared and used to improve liquid adsorption capacity, loading a high dose of drug into a liquisolid is still a challenge. With the aim of improving adsorption capacity and accordingly achieving high drug loading, ordered mesoporous silica with a high surface area and narrow pore size distribution was synthesized and used in a liquisolid formulation. Methods: Ordered mesoporous silica was synthesized and its particle size and morphology were tailored by controlling the concentration of cetyltrimethyl ammonium bromide. The ordered mesoporous silica synthesized was characterized by transmission electron microscopy, scanning electron microscopy, Fourier transform infrared spectroscopy, small-angle x-ray diffraction, wide angle x-ray diffraction, and nitrogen adsorption-desorption measurements. The liquid adsorption capacity of ordered mesoporous silica was subsequently compared with that of conventional silica materials using PEG400 as the model liquid. Carbamazepine was chosen as a model drug to prepare the liquisolid formulation, with ordered mesoporous silica as the adsorbent material. The preparation was evaluated and compared with commercially available fast-release carbamazepine tablets in vitro and in vivo. Results: Characterization of the ordered mesoporous silica synthesized in this study indicated a huge Brunauer-Emmett-Teller surface area (1030 m 2 /g), an ordered mesoporous structure with a pore size of 2.8 nm, and high adsorption capacity for liquid compared with conventional silica. Compared with fast-release commercial carbamazepine tablets, drug release from the liquisolid capsules was greatly improved, and the bioavailability of the liquisolid preparation was enhanced by 182.7%. Conclusion: Ordered mesoporous silica is a potentially attractive adsorbent which may lead to a new approach for development of liquisolid products.

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Section: Introductionmentioning

confidence: 99%

In vitro and in vivo evaluation of ordered mesoporous silica as a novel adsorbent in liquisolid formulation

Bao¹,

Wang²,

Quan³

et al. 2012

IJN

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show abstract

“…Various ratios of carrier to coating materials are selected. Desired quantities of drug and non-volatile solvents were accurately weighed in a beaker and then stirred continuously until a homogenous drug solution/suspension was obtained [18]. Selected amounts of the resultant liquid medication were incorporated into calculated quantities of carrier contained in a mortar.…”

Section: Calculation Of Load Factormentioning

confidence: 99%

Formulation and Evaluation of Lumefantrine Capsule Prepared by Using Liquisolid Technique

Khan

Agrawal

2018

Int J Curr Pharm Sci

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Objective: The objective of present research work was to formulate and evaluate of Lumefantrine capsule by using novel liquisolid technique to give increased dissolution rate of poorly water-soluble drug Lumefantrine.Methods: Formulation of lumefantrine capsule using drug solution and suspension method was used. Different liquisolid formulations were prepared using a mathematical model for calculating required quantities of powder and liquid ingredients to produce an acceptably flowable and compressible admixture. Liquisolid capsule formulation F-1 to F-9 were prepared by using different type and different concentration of non-volatile solvent like PEG-400, Tween 80, propylene glycol and avicels, aerosil as carrier and coating material respectively. Results:The liquisolid formulation were within the acceptable limits and drug release rates of all prepared liquisolid were distinctly higher as compared to pure drug. Lumefantrine shows maximum solubility in tween 80 as a non-volatile solvent. All the preformulation parameters were evaluated such as organoleptic characterization of the drug sample, melting point, pH, identification of drug samples by using UV spectroscopy and FTIR analytical method, preparation of calibration curves, solubility studies of drug sample like qualitative, quantitative and pH-dependent solubility of the drug in a buffer solution of different pH. They were further processed for solid-state characterization such as, DSC and SEM and the results confirmed the transformation of native crystalline nature of drug to an amorphous state. FTIR analysis also confirmed no drug-excipient interaction. Liquisolid formulations showed improved in vitro dissolution behaviour of lumefantrine over that of pure drug. Conclusion:From this study, it was concluded that liquisolid method is a promising alternative for improvement of dissolution property of waterinsoluble drugs.

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“…Among these methods, adsorption onto porous substrates with a high surface area is a well-known and widely used technique to enhance dissolution of poorly soluble drugs. [10][11][12][13][14] Porous silicate is a porous material that has been commonly used as a pharmaceutical excipient. Several grades of porous silicate having different characteristics such as particle size, pore size, and specific surface area are commercially available and have been widely employed to encapsulate poorly soluble drugs, such as Aerosil [15][16][17][18] Since the discovery of mesoporous (2 nm ,pore size ,50 nm) silica materials in the 1990s, the synthesis and application of mesoporous silica have received substantial attention due to their high surface area, well defined and tunable pore size, uniform porous structure, and easily modified surface.…”

Section: Wang Et Almentioning

confidence: 99%

Ordered nanoporous silica as carriers for improved delivery of water insoluble drugs: a comparative study between three dimensional and two dimensional macroporous silica

Wang¹,

Zhao²,

Hu³

et al. 2013

IJN

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Dissolution rate improvement of poorly water-soluble drugs obtained by adsorbing solutions of drugs in hydrophilic solvents onto high surface area carriers

Cited by 81 publications

References 12 publications

In vitro and in vivo evaluation of ordered mesoporous silica as a novel adsorbent in liquisolid formulation

In vitro and in vivo evaluation of ordered mesoporous silica as a novel adsorbent in liquisolid formulation

Formulation and Evaluation of Lumefantrine Capsule Prepared by Using Liquisolid Technique

Ordered nanoporous silica as carriers for improved delivery of water insoluble drugs: a comparative study between three dimensional and two dimensional macroporous silica

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