Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

Patel, Vaibhav I.; Dave, Rutesh H.

doi:10.1208/s12249-013-9947-z

Cited by 17 publications

(17 citation statements)

References 30 publications

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“…The temperatures ranged from 2°C to 60°C and the relative humidity varied between 0% and 100%. The duration also varied significantly, with stability studies lasting from 24 h to two years ( 73 , 74 , 81 , 82 , 84 , 86 , 88 , 92 , 93 , 104 , 105 , 109 , 110 , 113 , 115 , 116 , 118 , 120 , 123 , 124 , 126 , 127 , 129 , 130 , 132 , 134 , 135 , 139 , 143 , 146 , 149 , 153 , 158 , 166 , 169 , 172 , 175 , 176 ). While most of the studies did not mention the container used for the physical stability test, a few specified, for example, whether a closed or open container was used ( 88 , 92 , 113 , 123 , 132 , 146 ).…”

Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago. In this review we try to answer the following questions: What model compounds and excipients have been used in amorphous-based research? How were these two components selected and prepared? What methods have been used to assess the performance of amorphous formulation? What methodology have evolved and/or been standardized since amorphous-based formulation was first introduced and to what extent have we embraced on new methods? Is the extent of research mirrored in the number of marketed amorphous drug products? We have summarized the history and evolution of amorphous formulation and discuss the current status of amorphous formulation-related research practice. We also explore the potential uses of old experimental methods and how they can be used in tandem with computational tools in designing amorphous formulation more efficiently than the traditional trial-and-error approach.

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Section: Current Status Of Research On Amorphous Formulationsmentioning

confidence: 99%

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

2017

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“…The surface adsorbent, Sylysia 350 was used not only to impart good flow and compressibility to dispersion granules but also to improve the dissolution rate by increasing the effective surface area [81]. Another study was conducted using poorly soluble drug sulfathiazole and polyvinyl pyrrolidone as a carrier and Syloid 244FP as an adsorbent [82]. This method combined the advantages of conventional solid dispersion and surface solid dispersion by utilizing the adsorptive nature of porous silica particle and modifying the model drug into optimal molecular form [82].…”

Section: Use Of Non-ordered Mesoporous Silica In Convention Solid Dismentioning

confidence: 99%

“…Another study was conducted using poorly soluble drug sulfathiazole and polyvinyl pyrrolidone as a carrier and Syloid 244FP as an adsorbent [82]. This method combined the advantages of conventional solid dispersion and surface solid dispersion by utilizing the adsorptive nature of porous silica particle and modifying the model drug into optimal molecular form [82]. This technology helps to prevent the recrystallization of the drug on storage by forming strong hydrogen bonds between the drug and polymer complex, which is adsorbed on the porous carrier with further stabilization effects of silanol group present on the pore surfaces.…”

Section: Use Of Non-ordered Mesoporous Silica In Convention Solid Dismentioning

confidence: 99%

Mesoporous Silica as a Carrier for Amorphous Solid Dispersion

Chaudhari¹,

Gupte²

2017

BJPR

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In the past decade, the discovery of active pharmaceutical substances with high therapeutic value but poor aqueous solubility has increased, thus making it challenging to formulate these compounds as oral dosage forms. The bioavailability of these drugs can be increased by formulating these drugs as an amorphous drug delivery system. Use of porous media like mesoporous silica has been investigated as a potential means to increase the solubility of poorly soluble drugs and to stabilize the amorphous drug delivery system. These materials have nanosized capillaries and the large surface area which enable the materials to accommodate high drug loading and promote the controlled and fast release. Therefore, mesoporous silica has been used as a carrier in the solid dispersion to form an amorphous solid dispersion (ASD). Mesoporous silica is also being used as an adsorbent in a conventional solid dispersion, which has many useful aspects. This review focuses on the use of mesoporous silica in ASD as potential means to increase the dissolution rate and to provide or increase the stability of the ASD. First, an overview of mesoporous silica and the classification is discussed. Subsequently, methods of drug incorporation, the stability of dispersion and, much more are discussed.

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“…The addition of stabilizers in the solid dispersion can lead to a reduction in the energy and increase the stability of the SD 12,13 . Many excipients have been used in literature as a stabilizer.…”

Section: Introductionmentioning

confidence: 99%

Evaluating the effect of the porous and non-porous colloidal silicon dioxide as a stabilizer on amorphous solid dispersion

Chaudhari¹,

Bhadiyadra

Dave

2020

J. Drug Delivery Ther.

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Advancement in the discovery of drugs has led to many highly lipophilic compounds with very low water solubility. Amorphous solid dispersion is one of the emerging technologies to increase the solubility of these drugs. The stability of these systems is critical since the high energy system tends to recrystallize, which negates the benefits of these systems. In this paper, we are evaluating the use of colloidal silicon dioxide as a potential stabilizer to stabilize the amorphous solid dispersions. Two types of colloidal silicon dioxide are used: porous colloidal silicon dioxide -Syloid 244 Fp and nonporous fumed silica – Aerosil 200. These silicon dioxides have a high surface area. Two methods of incorporation are used to incorporate silicon dioxide into the solid dispersion. The spray drying method is used to make amorphous solid dispersion. It was found that porous silicon dioxide is better to increase stability as well as increasing dissolution rate and % release of the drug. The addition of silicon dioxide internally to the dispersion increases the dissolution rate, and the addition of silicon dioxide externally increases the stability of the solid dispersion. Keywords: colloidal silicon dioxide, stabilizer, amorphous solid dispersion, low water solubility

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Evaluation of Colloidal Solid Dispersions: Physiochemical Considerations and In Vitro Release Profile

Cited by 17 publications

References 30 publications

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

The Need for Restructuring the Disordered Science of Amorphous Drug Formulations

Mesoporous Silica as a Carrier for Amorphous Solid Dispersion

Evaluating the effect of the porous and non-porous colloidal silicon dioxide as a stabilizer on amorphous solid dispersion

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