Dissolution properties of polyethylene glycols and polyethylene glycol-drug systems

Corrigan, Owen I.; Murphy, Conor; Timoney, R.P.

doi:10.1016/0378-5173(79)90099-1

Cited by 47 publications

(41 citation statements)

References 13 publications

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“…15 Therefore, the slightly higher dissolution rate from PEG 20000 was considered to be due to the slightly higher molecular dispersion of OFX in this system.…”

Section: Org)mentioning

confidence: 99%

Dissolution improvement of high drug-loaded solid dispersion

Okonogi¹,

Puttipipatkhachorn

2006

AAPS PharmSciTech

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This study focused on an investigation of a high drugloaded solid dispersion system consisting of drug, carrier, and surfactant. Solid dispersions of a water-insoluble ofloxacin (OFX) with polyethylene glycol (PEG) of different molecular weights, namely binary solid dispersion systems, were prepared at drug to carrier not less than 5:5. Polysorbate 80, a nonionic surfactant, was incorporated into the binary solid dispersion systems as the third component to obtain the ternary solid dispersion systems. The powder x-ray diffraction and differential scanning calorimetric studies indicated that crystalline OFX existed in the solid dispersions with high drug loading. However, a decreased crystallinity of the solid dispersions obtained revealed that a portion of OFX was in an amorphous state. The results indicated a remarkably improved dissolution of drug from the ternary solid dispersion systems when compared with the binary solid dispersion systems. This was because of polysorbate 80, which improved wettability and solubilized the non-molecularly dispersed or crystalline fraction of OFX.

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“…15 Therefore, the slightly higher dissolution rate from PEG 20000 was considered to be due to the slightly higher molecular dispersion of OFX in this system.…”

Section: Org)mentioning

confidence: 99%

Dissolution improvement of high drug-loaded solid dispersion

Okonogi¹,

Puttipipatkhachorn

2006

AAPS PharmSciTech

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“…The term Solid Dispersion (SD) is used to describe a solid system in which the drug is dispersed in a biologically innocuous hydrophilic carrier. These systems are generally centered on the conversion of a candidate pharmaceutical/carrier mix from liquid to solid state (Chiou, Riegelman, 1971;Corrigan, et al, 1979;Saito et al, 2002;Shim, Kim, 2003;Juppo et al, 2003;Liu et al, 2006;Ahuja et al, 2007). The aim of SD in pharmaceutical manufacture is to alter the solid state properties of the candidate pharmaceutical, thereby increasing dispersion rate, improving the solubility coefficient as well as raising stability.…”

Section: Introductionmentioning

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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“…In a number of studies focusing on PEG-based solid dispersions, Corrigan et al measured the dissolution rate of not only the drug but also the carrier [13,82,83]. The authors observed that the dissolution rate of PEG from solid dispersions with hydroflumethiazide and bendrofluazide was lower than that of the pure carrier and the rate was decreasing as the drug loading increased.…”

Section: Dissolution Rate Of Carriermentioning

confidence: 96%

The role of the carrier in the formulation of pharmaceutical solid dispersions. Part I: crystalline and semi-crystalline carriers

Duong

Mooter

2016

Expert Opinion on Drug Delivery

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As a consequence of the target and drug candidate identification process, drugs with higher hydrophobicity and/or lipophilicity are being selected for further development, leading to solubility and dissolution rate limited oral bioavailability, and hence potential failure of the intended therapeutic goal. Solid dispersions were introduced as a formulation strategy in the early 1960s to tackle this issue and are still an area of intensive research activity. Areas covered: There has been a shift in the type of carriers that were used in the formulation of solid dispersions as nowadays, amorphous carriers are most often used, whereas in early stages of solid dispersions development, crystalline and semi-crystalline carriers were most commonly applied. In this review, we will discuss several aspects related to the use of crystalline and semi-crystalline carriers such as their molecular and related physical structure, and their physical chemical properties related to formulation of poorly soluble drugs. Expert opinion: The inherent crystallinity of this type of carrier hinders the formation of high-load solid solutions as mainly the amorphous domains of a carrier are able to accommodate drug molecules. Hence these carriers are not currently first choice excipients to formulate solid dispersions.

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Dissolution properties of polyethylene glycols and polyethylene glycol-drug systems

Cited by 47 publications

References 13 publications

Dissolution improvement of high drug-loaded solid dispersion

Dissolution improvement of high drug-loaded solid dispersion

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

The role of the carrier in the formulation of pharmaceutical solid dispersions. Part I: crystalline and semi-crystalline carriers

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