Interdependence of Physiological Surfactant and Drug Particle Size on the Dissolution Behavior of Water-Insoluble Drugs

Lin, Song-Ling; Menig, Johanne; Lachman, Leon

doi:10.1002/jps.2600571225

Cited by 64 publications

(12 citation statements)

References 31 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The most common method is to increase surface area of the drug by micronization. But, in practice the effect of micronization is often disappointing, especially when the drugs are encapsulated or tableted (Aguiar et al, 1979;Finholt and Solvang, 1968;Lin et al, 1968). Micronised drugs also have the tendency to agglomerate as a result of their hydrophobicity, thus reducing their available surface area (Finholt and Solvang, 1968).…”

Section: Introductionmentioning

confidence: 99%

Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine)

Javadzadeh

Jafari-Navimipour

Nokhodchi

2007

International Journal of Pharmaceutics

178

135

View full text Add to dashboard Cite

Different liquisolid formulations of carbamazepine were accomplished by dissolving the drug in the non-toxic hydrophilic liquids, and adsorbing the solution onto the surface of silica. In order to reduce the amounts of carrier and aerosil in liquisolid formulations, some additives namely polyvinylpyrrolidone (PVP), hydroxypropyle methylcellulose (HPMC) and polyethylene glycol (PEG 35000) were added to liquid medication to increase loading factor. The effects of various ratios of carrier to coating material, PVP concentration, effect of aging and type of the carrier on dissolution rate of liquisolid compacts were studied. X-ray crystallography and differential scanning calorimetery (DSC) were used for evaluation of physicochemical properties of carbamazepine in liquisolid formulations. The results showed that the drug loading factor was increased significantly in the presence of additives. Liquisolid formulations containing PVP as additive, exhibited significantly higher drug dissolution rates compared to the compacts prepared by the direct compression technique. It was shown that microcrystalline cellulose had more liquid retention potential in comparison with lactose, and the formulations containing microcrystalline cellulose as carrier, showed higher dissolution rate. By decreasing the ratio of microcrystalline cellulose to silica from 20 to 10, an improvement in dissolution rate was observed. Further decrease in the ratio of microcrystalline cellulose:silica from 10 to 5 resulted in a significant reduction in dissolution rate. Increasing of PVP concentration in liquid medication caused a dramatic increase in dissolution rate at first 30 min. The results showed that the dissolution rate of liquisolid tablets was not significantly affected by storing the tablets at 25• C/75% relative humidity for a period of 6 months. The results of DSC and X-ray crystallography did not show any changes in crystallinity of the drug and interaction between carbamazepine and exipients during the process.

show abstract

Section: Introductionmentioning

confidence: 99%

Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine)

Javadzadeh

Jafari-Navimipour

Nokhodchi

2007

International Journal of Pharmaceutics

178

135

View full text Add to dashboard Cite

show abstract

“…Griseofulvin used as an antifungal agent is a practically insoluble compound. However, fine particles may not necessarily produce the expected dissolution rate and bioavailability due to their aggregation and agglomeration (4,9). A good correlation between the bioavailability and dissolution rate was found for griseofulvin tablets (7,8).…”

mentioning

confidence: 99%

Bioavailability of Griseofulvin from Tablets in Humans and the Correlation with its Dissolution Rate

Aoyagi

Ogata

Kaniwa

et al. 1982

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

“…These factors may be concerned with the total system, the solute particle, or the dissolution medium. In recent years, the effect of surfactants in the dissolution medium on dissolution kinetics has been the subject of considerable research in terms of wetting (2)(3)(4)(5) and solubilization (6)(7)(8). The effect on dissolution rate of unreactive additives (9) and reactive additives (10, 11) has been studied.…”

mentioning

confidence: 99%

Influence of Viscosity and Solubilization on Dissolution Rate

Braun

Parrott

1972

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Interdependence of Physiological Surfactant and Drug Particle Size on the Dissolution Behavior of Water-Insoluble Drugs

Cited by 64 publications

References 31 publications

Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine)

Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine)

Bioavailability of Griseofulvin from Tablets in Humans and the Correlation with its Dissolution Rate

Influence of Viscosity and Solubilization on Dissolution Rate

Contact Info

Product

Resources

About