Dissolution Rates of Corticosteroids Utilizing Sugar Glass Dispersions

Allen, Loyd V; Yanchick, Victor A.; Maness, Dale D.

doi:10.1002/jps.2600660409

Cited by 56 publications

(25 citation statements)

References 23 publications

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“…These systems consist of amorphous carriers and the drug can be either molecularly dispersed or form an amorphous precipitate into its carrier, which can possibly crystallize upon time. Examples of carriers that favour the formation of glass solutions are sugars, such as dextrose, fructose, galactose, trehalose, sucrose, and different types of inulin, [53][54][55] or amorphous polymers such as PVP, Polyvinylpyrrolidone-co-vinylacetate (PVPVA) and HPMC. The earliest examples of such glassy dispersions were prepared with PVP [56] and currently this class represents the most intensively studied and applied solid dispersion system.…”

Section: Glass Solutionsmentioning

confidence: 99%

Review: physical chemistry of solid dispersions

2009

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Objectives With poorly soluble drug candidates emerging in the drug discovery pipeline, the importance of the solid dispersion formulation approach is increasing. This strategy includes complete removal of drug crystallinity, and molecular dispersion of the poorly soluble compound in a hydrophilic polymeric carrier. The potential of this technique to increase oral absorption and hence bioavailability is enormous. Nevertheless, some issues have to be considered regarding thermodynamic instability, as well in supersaturated solutions that are formed upon dissolution as in the solid state. Key findings After a brief discussion on the historical background of solid dispersions and their current role in formulation, an overview will be given on the physical chemistry and stability of glass solutions as they form supersaturated solutions, and during their shelf life. Conclusions Thorough understanding of these aspects will elicit conscious evaluation of carrier properties and eventually facilitate rational excipient selection. Thus, full exploitation of the solid dispersion strategy may provide an appropriate answer to drug attrition due to low aqueous solubility in later stages of development.

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Section: Glass Solutionsmentioning

confidence: 99%

Review: physical chemistry of solid dispersions

2009

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“…The time to solidification of the liquid mixture can be a critical factor in the saturation of the dispersed system (Chiou, Riegelman, 1971;Allen et al, 1977;Lin, Cham, 1996). Dittgen et al (1995) evaluated this parameter in the SDs of riboflavin, testosterone and progesterone and stated that the solubility of SD increased with reduced cooling time.…”

Section: Dissolution Studiesmentioning

confidence: 99%

Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel

Chaud

Tamascia

Lima

et al. 2010

Braz. J. Pharm. Sci.

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The solubility behavior of drugs remains one of the most challenging aspects in formulation development. Solid Dispersion (SD) has tremendous potential for improving drug solubility. Although praziquantel (PZQ) is the first drug of choice in the treatment of schistosomiasis, its poor solubility has restricted its delivery oral route. In spite of its poor solubility, PZQ is well absorbed in the gastrointestinal tract, but large doses are required to achieve adequate concentration at the target sites. The aim of this study was to improve the solubility and dissolution rate of PZQ and to evaluate its intestinal absorption. SDs were formulated with PEG-60 castor oil hydrogenated (CR-60) using a fusion and evaporation method. Pure PZQ and physical mixtures (PM) and PZQ-CR-60 (2:1; 1:1; 1:2 ratios) were compared as regards their solubility, dissolution and intestinal absorption. The experimental results demonstrated the improvement in the solubility, dissolution rate and intestinal absorption. In addition, the solubility behavior showed pH dependency and that the solubility of PZQ was slower in acidic medium than in neutral and basic mediums. The increase in PZQ solubility of the SD with the CR-60 could be attributed to several factors such as improved wettability, local solubilization, drug particle size reduction and crystalline or, interstitial solid solution reduction.Uniterms: Solid dispersion. Praziquantel/dissolution rates. Praziquantel/solubility. Praziquantel/intestinal absorption.A solubilidade de fármacos ainda é um dos principais desafios no desenvolvimento de formulações farmacêuticas. As dispersões sólidas (DS) apresentam grande potencial para melhorar a solubilidade de fármacos. O praziquantel é o fármaco de primeira escolha no tratamento da esquistossomose, contudo a baixa solubilidade em água restringe seu uso à administração pela via oral. Apesar da baixa solubilidade, o PZQ é bem absorvido através do trato gastrintestinal, mas doses orais elevadas são requeridas para garantir concentrações suficientes de fármaco para o tecido alvo. O objetivo deste estudo foi melhorar a solubilidade, a dissolução e avaliar a absorção do PZQ. As DS foram formuladas com óleo de castor hidrogenado -PEG 60 (CR-60), pelo uso dos métodos de fusão e evaporação do solvente. PZQ puro, mistura física (MF) e DS de CR-60-PZQ (1:2; 1:1; 2:1) foram comparados quanto à solubilidade, dissolução e absorção intestinal. Os resultados experimentais mostraram aumento na solubilidade, na taxa de dissolução e na absorção intestinal do PZQ nas DS. A solubilidade do PZQ foi maior em meio ácido, mostrando uma dependência do pH. O aumento na solubilidade do PZQ nas DS com CR-60 foi atribuída a fatores como aumento da molhabilidade, solubilização local, redução granulométrica e redução da cristalinidade ou, ainda, a ocorrência de uma solução sólida intersticial.Unitermos: Dispersão sólida. Praziquantel/taxa de dissolução. Praziquantel/solubilidade. Praziquantel/ absorção intestinal.

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“…The use of sugar combinations overcame some difficulties previously reported with single-sugar systems. Lloyd et al (16) reported enhancement in the dissolution rates of hydrocortisone and prednisone utilizing ternary sugar solid dispersion systems in tablet form. The dispersion systems were prepared by the fusion method using 50:50 sucrose/mannitol and 50:50 sorbitol/mannitol.…”

mentioning

confidence: 99%

Dissolution Behavior and Thermodynamic Stability of Fused-Sugar Dispersions of a Poorly Water-Soluble Drug

Singh¹,

Chhabra²,

Pathak³

2011

Dissolution Technol.

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The current research was undertaken to develop and evaluate dissolution profiles of thermodynamically stabilized sugar dispersions of the poorly water-soluble, model drug etoricoxib (ETX). Fused-sugar dispersions were formulated using sorbitol, xylitol, and maltose separately, and the binary systems were stabilized by incorporation of the antiplasticizing agents poloxamer 407 and PVP K30 to obtain ternary and quaternary systems. The sugar dispersions (F1-F12) were subjected to in vitro dissolution studies, and based on model-independent dissolution parameters, ETX-sorbitol binary/ ternary/composite systems were selected for thermodynamic stability study. The aged ETX-sorbitol composite dispersion (SF8) displayed the highest percent dissolution efficiency (%DE 80min of 78.48), the minimum t 50% of 4.45 min, and the least tendency to recrystallize (D cryst of 0.68), confirming maximum amorphization and thermodynamic stability among all the composite dispersions. The SEM photomicrographs reveal complete miscibility of drug in the aged quaternary dispersion SF8, and its diffuse reflectance (DR) spectrum confirms the absence of any chemical change. Conclusively, sorbitol binary systems can be effectively stabilized by incorporation of PVP K30-poloxamer 407 and retain the dissolution characteristics of sugar dispersions upon aging.

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Dissolution Rates of Corticosteroids Utilizing Sugar Glass Dispersions

Cited by 56 publications

References 23 publications

Review: physical chemistry of solid dispersions

Review: physical chemistry of solid dispersions

Solid dispersions with hydrogenated castor oil increase solubility, dissolution rate and intestinal absorption of praziquantel

Dissolution Behavior and Thermodynamic Stability of Fused-Sugar Dispersions of a Poorly Water-Soluble Drug

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