Solid-state β-cyclodextrin complexes containing indomethacin, ammonia and water. II. Solubility studies

Casella, R.; Williams, David A.; Jambhekar, Sunil S.

doi:10.1016/s0378-5173(98)00003-9

Cited by 24 publications

(5 citation statements)

References 7 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Dissolution performance was found to be dependent on the enthalpy and suggests that the energy needed to desolvate these complexes was similar to the energy needed to dissolve the complexes in water. Casella et al (14) showed that enthalpy measurements could be used to predict dissolution performance from indomethacin-β-cyclodextrin complexes.…”

Section: Dissolution Studiesmentioning

confidence: 99%

Direct Compression Tablets Containing a Series of Four β-Cyclodextrin Complexes Formed by Neutralizing an Acidic Drug

Moore

Bergamo²,

Casella³

2000

Drug Development and Industrial Pharmacy

View full text Add to dashboard Cite

A series of four beta-cyclodextrin complexes (called products) was formed by neutralizing an acidic drug to study the effect of drug solubility on complex formation and the dissolution performance from direct compression tablets. Four solid products were prepared by neutralizing the drug in 0.05, 0.10, 0.20, and 0.30 M tromethamine solutions with a constant 0.09 M beta-cyclodextrin concentration, filtering the solutions, and removing the water through evaporation with heat and vacuum. The four products contained drug and water in a distinct relationship, thus suggesting a complex formation that was dependent on the tromethamine concentration. Infrared, powder X-ray diffraction, differential scanning calorimetry (DSC), phase solubility, and scanning electron microscopy (SEM) techniques revealed distinct differences among the four products, suggesting three of the four products were complexes, and one product was either a weak complex or a physical mixture. Ultraviolet (UV) analysis showed no evidence of complex formation. Phase solubility results showed one product had a slight increase in drug solubility, and three products had no increase in drug solubility with increasing beta-cyclodextrin concentration. The lack of a solubility increase suggests insoluble complex formation. Drug dissolution in water was improved significantly in all tablets containing either a product or a physical mixture when compared to the pure drug. The products prepared with the two highest concentrations of tromethamine showed a dissolution performance that was superior to all other formulations. Enthalpy measurements by DSC were a good indicator of dissolution performance for tablets containing the four products. Drug dissolution through salt formation in the absence of beta-cyclodextrin showed the drug-salt dissolution varied from better to worse when compared to the dissolution profiles of the four products. The varying dissolution performance was attributed to the formation of distinct beta-cyclodextrin complexes with varing solubilities.

show abstract

Section: Dissolution Studiesmentioning

confidence: 99%

Direct Compression Tablets Containing a Series of Four β-Cyclodextrin Complexes Formed by Neutralizing an Acidic Drug

Moore

Bergamo²,

Casella³

2000

Drug Development and Industrial Pharmacy

View full text Add to dashboard Cite

show abstract

“…The reported water solubility values of IND vary considerably, from 2 to 50 mg/mL (Casella et al, 1998;Bergstroem et al, 2003;Nandi et al, 2003;Faller and Ertl, 2007). Therefore, the solubility of IND was determined and the effects of using sonication, propylene glycol and the presence of MWCNTs were also investigated ( Figure 6).…”

Section: Solubility Experimentsmentioning

confidence: 99%

Carbon nanotubes for transdermal drug delivery

Değim

Burgess

Papadimitrakopoulos

2010

Journal of Microencapsulation

View full text Add to dashboard Cite

In this study, drug carrier properties through skin and penetration enhancement effects of carbon nanotubes (CNTs) are presented. Multi-walled and double-walled carbon nanotubes were used. Penetration enhancement into the skin following passive diffusion and iontophoresis were determined. Possible solubility enhancement effects and drug adsorption properties of CNTs were investigated. CNTs were found to be a useful drug carrier system and they can provide a high loading and enhanced transdermal penetration for especially hydrophobic drugs. The electroconductive nature of CNTs allows easy application of iontophoresis and the additional advantage of CNTs appears to be using them as electrodes.

show abstract

“…On account of its structure and the relatively lipophilic surface of the internal cavity, which is in contrast with the hydrophilic feature of the external hydroxyl faces, β-CD molecules can easily form inclusion complexes with a wide variety of molecules and molecular ions [10–13]. In the pharmaceutical industry, β-CD has often been used to enhance the solubility of drugs, such as indomethacin, naringin, celecoxib, and citric acid [14–17]. This lets us speculate that preparing naringin inclusion complexes may increase the solubility and the enzymatic hydrolysis rate of naringin.…”

Section: Introductionmentioning

confidence: 99%

Effect of β-Cyclodextrin Complexation on Solubility and Enzymatic Conversion of Naringin

Cui

Zhang

Sun

et al. 2012

IJMS

View full text Add to dashboard Cite

In the present paper, the effect of β-cyclodextrin (β-CD) inclusion complexation on the solubility and enzymatic hydrolysis of naringin was investigated. The inclusion complex of naringin/β-CD at the molar ratio of 1:1 was obtained by the dropping method and was characterized by differential scanning calorimetry. The solubility of naringin complexes in water at 37 ± 0.1 °C was 15 times greater than that of free naringin. Snailase-involved hydrolysis conditions were tested for the bioconversion of naringin into naringenin using the univariate experimental design. Naringin can be transformed into naringenin by snailase-involved hydrolysis. The optimum conditions for enzymatic hydrolysis were determined as follows: pH 5.0, temperature 37 °C, ratio of snailase/substrate 0.8, substrate concentration 20 mg·mL−1, and reaction time 12 h. Under the optimum conditions, the transforming rate of naringenin from naringin for inclusion complexes and free naringin was 98.7% and 56.2% respectively, suggesting that β-CD complexation can improve the aqueous solubility and consequently the enzymatic hydrolysis rate of naringin.

show abstract

Solid-state β-cyclodextrin complexes containing indomethacin, ammonia and water. II. Solubility studies

Cited by 24 publications

References 7 publications

Direct Compression Tablets Containing a Series of Four β-Cyclodextrin Complexes Formed by Neutralizing an Acidic Drug

Direct Compression Tablets Containing a Series of Four β-Cyclodextrin Complexes Formed by Neutralizing an Acidic Drug

Carbon nanotubes for transdermal drug delivery

Effect of β-Cyclodextrin Complexation on Solubility and Enzymatic Conversion of Naringin

Contact Info

Product

Resources

About