Physicochemical aspects of drug release. XIV. The effects of some ionic and non-ionic surfactants on properties of a sparingly soluble drug in solid dispersions

Sjökvist, Eva; Nyström, Christer; Aldén, Maggie; Caram-Lelham, Ninus

doi:10.1016/0378-5173(92)90103-9

Cited by 52 publications

(18 citation statements)

References 18 publications

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“…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. Increased dissolution rate of drug from solid dispersions in PEG containing varying amounts of ionic and nonionic surfactants, including sodium dodecyl sulfate and polysorbate 80, were also reported by Sjökvist et al 74 The authors, however, pulverized the waxy material instead of filling them into hard gelatin capsules as melts.…”

Section: Breakthroughs In Solid Dispersion Technologymentioning

confidence: 67%

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

Serajuddin

1999

Journal of Pharmaceutical Sciences

1,434

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: 67%

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

Serajuddin

1999

Journal of Pharmaceutical Sciences

1,434

780

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“…It is easy to understand that a bio-relevant medium will need a similar surface activity as bio-fluids. Studies on sodium lauryl sulfate (SLS) solutions (7) indicated that the surface tension of SLS solutions decreased dramatically above the critical the micelle concentration (0.023%) and it reached a minimum surface tension at 0.2% with no significant change at higher concentrations. This suggested that a bio-comparable surface activity can be achieved at low surfactant concentrations (0.2%).…”

Section: Introductionmentioning

confidence: 99%

Evaluation and Selection of Bio-relevant Dissolution Media for a Poorly Water-Soluble New Chemical Entity

Tang

Khan

Muhammad

2001

Pharmaceutical Development and Technology

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The purpose of this work is to develop a bio-relevant dissolution method for formulation screening in order to select an enhanced bioavailable formulation for a poorly water-soluble drug. The methods used included a modified rotating disk apparatus for measuring intrinsic dissolution rate of the new chemical entity (NCE) and the USP dissolution method II for evaluating dissolution profiles of the drug in three different dosage forms. The in vitro dissolution results were compared with the in vivo bioavailability for selecting a bio-relevant medium. The results showed that the solubility of the NCE was proportional to the concentration of sodium lauryl sulfate (SLS) in the media. The apparent intrinsic dissolution rate of the NCE was linear to the rotational speed of the disk, which indicated that the dissolution of the drug is a diffusion-controlled mechanism. The apparent intrinsic dissolution rate was also linear to the surfactant concentration in the media, which was interpreted using the Noyes and Whitney Empirical Theory. Three formulations were studied in three different SLS media using the bulk drug as a reference. The dissolution results were compared with the corresponding bioavailability results in dogs. In the 1% SLS--sink conditions--the drug release from all the formulations was complete and the dissolution results were discriminative for the difference in particle size of the drug in the formulations. However, the data showed poor IVIV correlation. In the 0.5% SLS medium--non-sink conditions--the dissolution results showed the same rank order among the tested formulations as the bioavailability. The best IVIV correlation was obtained from the dissolution in 0.25% SLS medium, an over-saturated condition. The conclusions are: a surfactant medium increases the apparent intrinsic dissolution rate of the NCE linearly due to an increase in solubility. A low concentration of surfactant in the medium (0.25%) is more bio-relevant than higher concentrations of surfactant in the media for the poorly water-soluble drug. Creating sink conditions (based on bulk drug solubilities) by using a high concentration of a surfactant in the dissolution medium may not be a proper approach in developing a bio-relevant dissolution method for a poorly water-soluble drug.

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“…Nonionic surfactants are also used in pharmaceuticals to increase their stability (11) and to enhance the dissolution rate of active ingredients from suppositories (12) and solid dispersions (13), for example. The pharmaceutical industry also uses nonionic surfactants to facilitate solubilization (14) and to increase the stability of drugcarrier emulsions (15).…”

mentioning

confidence: 99%

Alkyl Ethoxylated and Alkylphenol Ethoxylated Nonionic Surfactants: Interaction with Bioactive Compounds and Biological Effects

Cserháti¹

1995

Environ Health Perspect

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Physicochemical aspects of drug release. XIV. The effects of some ionic and non-ionic surfactants on properties of a sparingly soluble drug in solid dispersions

Cited by 52 publications

References 18 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

Evaluation and Selection of Bio-relevant Dissolution Media for a Poorly Water-Soluble New Chemical Entity

Alkyl Ethoxylated and Alkylphenol Ethoxylated Nonionic Surfactants: Interaction with Bioactive Compounds and Biological Effects

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