The effects of surfactants on the dissolution profiles of poorly water-soluble acidic drugs

Park, Sung Hyun; Choi, Hoo‐Kyun

doi:10.1016/j.ijpharm.2006.05.004

Cited by 111 publications

(70 citation statements)

References 16 publications

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“…MFA is a lipophilic molecule. Park and Choi, (2006) reported that the dissolution rate of MFA was substantially enhanced in phosphate buffer medium (pH 6.8) containing CTAB. Figure 5 shows that the drug release rate depends on the concentration of CA in the formulation.…”

Section: In Vitro Releasementioning

confidence: 99%

Development of nanostructured lipid carriers for controlled delivery of mefenamic acid

Khurana

Bedi

Jain

2012

IJBNN

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This study was aimed to develop nanostructured lipid carriers (NLC) for the possible delivery of mefenamic acid. This study describes the effect of liquid lipid concentration on the characteristics of NLC such as particle size, polydispersity index, zeta potential, drug entrapment efficiency, and occlusivity index. Transmission electron microscopy revealed nearly spherical shape NLC with negligible effect of liquid lipid content on the particle morphology. The differential scanning calorimetry demonstrated a depression in the melting point and crystallinity index of the NLC with an increase in the amount of liquid lipid. The in vitro drug release studies demonstrated that solid lipid nanoparticle (0% oil), and NLC possessed a biphasic release pattern characterised by a rapid initial release followed by a sustained release, in comparison to nanoemulsions (100% oil) of which a nearly constant release was observed. Compared to NE and SLN, the excellent physical stability of NLC against drug leakage was seen.

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Section: In Vitro Releasementioning

confidence: 99%

Development of nanostructured lipid carriers for controlled delivery of mefenamic acid

Khurana

Bedi

Jain

2012

IJBNN

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“…Differently, cetyltrimethylammonium bromide (CTAB) did not show the same effect. In general, CTAB, SLS, and polysorbate 80 are common choices for cationic, anionic, and non-ionic surfactants (Table VI) (115).…”

Section: Surfactantsmentioning

confidence: 99%

“…In contrast, the EMA guidance documents (128), WHO Technical Report (2015) (129), and Health Canada (126) require determining the solubility of the highest single dose administered, which in certain cases can be two or more units in 250 mL (115). This shifts many drugs into the Bpoorly soluble^classification category.…”

Section: Regulatory View Of Biopharmaceutics Drug Classification Systmentioning

confidence: 99%

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Bou‐Chacra

Melo

Morales

et al. 2017

AAPS J

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Abstract.The introduction of the biopharmaceutics drug classification system (Biopharmaceutics Classification System (BCS)), in 1995, provided a simple way to describe the biopharmaceutics behavior of a drug. Solubility and permeability are among the major parameters, which determine the fraction dose absorbed of a drug substance and consequently its chances to be bioavailable. The purpose of this review is to summarize the evolution of the media used for determining solubility and dissolution and how this can be used in modern drug development. Over the years, physiologically adapted media and buffers were introduced with the intention to better predict the in vivo solubility and dissolution of drug substances. Water, buffer solutions, compendial media, micellar solubilization media, and biorelevant media are reviewed. At this time point, there is no universal medium available which can be used to predict every drug substance's solubility or a drug product's in vivo dissolution behavior. However, there have been many improvements and additions made to media to optimize their in vivo predictability; for example, the current phosphate concentrations in buffers seem to be too high to correlate with the carbonate buffer concentrations in vivo. Biorelevant media were updated to correlate them better with the composition of human intestinal fluids. The BCS was introduced into regulatory sciences as a scientific risk management tool to waive bioequivalence studies under certain conditions. Today's different guidance documents define the dose-solubility ratio differently. As shown for amoxicillin, this can cause more confusion than certainty for globally operating companies. Harmonization of BCS guidelines is highly desirable.

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“…e-mail: vagray@rcn.com lar size increases upon addition of an electrolyte to the solution. The type of surfactant determines the effect of ionic strength; for example, the solubility of mefenamic acid is affected by a change in ionic strength when SLS is used but not when CTAB is used (9). In addition, the purity of the surfactant must be considered because it can extensively affect the size and loading capacity of a micelle, which results in changes in solubility and dissolution rate (10,11).…”

Section: Introductionmentioning

confidence: 99%

Rationale for Selection of Dissolution Media: Three Case Studies

Fotaki¹,

Brown

Kochling

et al. 2013

Dissolution Technol.

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The selection of media in dissolution method development can sometimes be an arbitrary decision. The case studies in this article give a practical rationale that should help in selecting media, especially surfactants.Three cases were studied: (1) the role of surfactants versus compound stability in the dissolution medium during dissolution method development, (2) the selection of a surfactant based on interactions between the dissolution medium and the drug substance, and (3) the selection of media based on formulation properties.In the first case study, the choice of surfactant in relation to solubility and physical stability of the drug substance is shown. The second revealed an unexpected synergy between polysorbate 20 (Tween) and acetic acid solution that caused an unusual increase in the dissolution rate compared with these media used separately. In the last case study, the medium was modified by addition of surfactant to reflect a change in the formulation.The selection of a dissolution medium should be based on drug substance and formulation characteristics as well as on interactions among components.

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The effects of surfactants on the dissolution profiles of poorly water-soluble acidic drugs

Cited by 111 publications

References 16 publications

Development of nanostructured lipid carriers for controlled delivery of mefenamic acid

Development of nanostructured lipid carriers for controlled delivery of mefenamic acid

Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System

Rationale for Selection of Dissolution Media: Three Case Studies

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