Dissolution behaviour of drugs from binary and ternary systems

Veiga, María-Dolores; Escobar, Camila Ferreira; Bernad, María Josefa Bernad

doi:10.1016/0378-5173(93)90180-n

Cited by 20 publications

(6 citation statements)

References 10 publications

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“…71 The crystalline structure of solid PEG was minimally affected by polysorbate 80 because the two compounds have low miscibility in each other. Other investigators also reported enhanced dissolution 72 and bioavailability 65 of drugs from PEG-polysorbate carriers. Law et al 73 reported a >2-fold increase in the dissolution rate of nifedipine from a PEG-based solid dispersion after incorporation of 5% (w/w) phosphatidylcholine.…”

Section: Breakthroughs In Solid Dispersion Technologymentioning

confidence: 88%

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

Serajuddin

1999

Journal of Pharmaceutical Sciences

1,431

780

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Although there was a great interest in solid dispersion systems during the past four decades to increase dissolution rate and bioavailability of poorly water-soluble drugs, their commercial use has been very limited, primarily because of manufacturing difficulties and stability problems. Solid dispersions of drugs were generally produced by melt or solvent evaporation methods. The materials, which were usually semisolid and waxy in nature, were hardened by cooling to very low temperatures. They were then pulverized, sieved, mixed with relatively large amounts of excipients, and encapsulated into hard gelatin capsules or compressed into tablets. These operations were difficult to scale up for the manufacture of dosage forms. The situation has, however, been changing in recent years because of the availability of surface-active and self-emulsifying carriers and the development of technologies to encapsulate solid dispersions directly into hard gelatin capsules as melts. Solid plugs are formed inside the capsules when the melts are cooled to room temperature. Because of surface activity of carriers used, complete dissolution of drug from such solid dispersions can be obtained without the need for pulverization, sieving, mixing with excipients, etc. Equipment is available for large-scale manufacturing of such capsules. Some practical limitations of dosage form development might be the inadequate solubility of drugs in carriers and the instability of drugs and carriers at elevated temperatures necessary to manufacture capsules.

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Section: Breakthroughs In Solid Dispersion Technologymentioning

confidence: 88%

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

Serajuddin

1999

Journal of Pharmaceutical Sciences

1,431

780

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“…We hypothesized that an increased release of oleic acid from the cubic nanoparticles would cause a greater permeation enhancing effect of oleic acid. To increase the amount of oleic acid released from the cubic nanoparticles, we co-administered PEG 200 with oleic acid since PEGs have the ability to solubilize lipophilic compounds (Veiga et al, 1993). Thus, in this study, the impact of PEG 200 (1%) on increasing the permeability enhancing ability of a lipophilic permeation enhancer, oleic acid (1%), incorporated into the cubic nanoparticles was investigated.…”

Section: Effect Of Oleic Acid and Peg 200 For Permeation Enhancementmentioning

confidence: 99%

Identification and assessment of permeability enhancing vehicles for transdermal delivery of glucosamine hydrochloride

et al. 2010

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As an initial step to develop the transdermal delivery system of glucosamine hydrochloride (GL-HCl), the permeation study across the rat skin in vitro was performed to identify the most efficient vehicle with regard to the ability to deliver GL-HCl transdermally. The GL-HCl formulations such as o/w cream, liposome suspension, liposomal gel, and liquid crystalline vehicles were prepared and compared for transdermal flux of GL-HCl. The liquid crystalline vehicles were more effective in increasing the skin permeation of GL-HCl than o/w cream and liposomal vehicles. Of the liquid crystalline vehicles tested, the permeation enhancing ability of the cubic phase was greater than that of the hexagonal phase when the nanoparticle dispersion was used. The skin permeation enhancing ability of the cubic nanoparticles for GL-HCl was further increased by employing both oleic acid and polyethylene glycol 200. Therefore, the cubic liquid crystalline nanodispersion containing oleic acid and PEG 200 can provide a possibility of clinical application of transdermal GL-HCl.

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“…The slow dissolution rate is the dominating factor in producing irregular and incomplete absorption of this drug. To date, solid dispersions [5][6][7][8] and freeze-drying 9 have been used successfully to improve the dissolution of griseofulvin. However, use of cyclodextrins to enhance the solubility and dissolution of griseofulvin was not promising because of its low binding constant with respect to other drugs studied.…”

mentioning

confidence: 99%

Interactions of Griseofulvin with Cyclodextrins in Solid Binary Systems

Veiga¹,

Díaz²,

Ahsan³

1998

Journal of Pharmaceutical Sciences

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Griseofulvin/cyclodextrin interactions were investigated in aqueous environment and in solid state. Two cyclodextrin derivatives (beta-cyclodextrin and 2-hydroxypropyl beta-cyclodextrin) were used to prepare different physical mixtures and kneaded systems, and the drug/cyclodextrin ratios were 1:1 and 1:2 mol/mol. Scanning electron microscopy (SEM), hot-stage microscopy (HSM), differential scanning calorimetry (DSC), thermogravimetry (TG), and X-ray powder diffractometry were employed to characterize pure substances and their kneaded counterparts and all of the binary systems. The solubility of griseofulvin was increased in accord with the quantity of cyclodextrin added. HSM examination revealed that 2-hydroxypropyl-beta-cyclodextrin was dissolved in the droplets of melted griseofulvin, but did not show any interactions between melted griseofulvin and beta-cyclodextrin particles. The presence of griseofulvin endothermic peak in the DSC curves of all binary systems suggests the absence of any griseofulvin/cylcodextrin inclusion compound in the solid state. In TG, data of weight loss owing to the dehydration of cyclodextrins was similar for both kneaded systems and physical mixtures. X-ray diffraction patterns exhibited the amorphous nature of 2-hydroxypropyl-beta-cyclodextrin and the crystalline nature of griseofulvin and binary systems. Griseofulvin dissolution profiles from all binary systems showed an improvement in drug dissolution, which indicates that an "in situ" drug/cyclodextrin inclusion compound was formed in the aqueous dissolution medium.

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Dissolution behaviour of drugs from binary and ternary systems

Cited by 20 publications

References 10 publications

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

Identification and assessment of permeability enhancing vehicles for transdermal delivery of glucosamine hydrochloride

Interactions of Griseofulvin with Cyclodextrins in Solid Binary Systems

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