Evaluation of the impact of sodium lauryl sulfate source variability on solid oral dosage form development

Qiang, Dongmei; Gunn, Jocelyn A.; Schultz, Leon; Li, Z. Jane

doi:10.3109/03639045.2010.488647

Cited by 9 publications

(3 citation statements)

References 38 publications

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“…Improving the dissolution rate and hence the solubility of hydrophobic (class II) drugs is essential for increasing their oral bioavailability ( Qiang et al, 2010 , Rasenack and Muller, 2005 ). A widely adopted strategy to improve both the dissolution rate and the solubility of hydrophobic drugs is to incorporate the anionic surfactant sodium lauryl sulfate (SLS) into the formulation.…”

Section: Introductionmentioning

confidence: 99%

Preparation, characterization, dissolution, and permeation of flibanserin − 2-HP-β-cyclodextrin inclusion complexes

Alghaith

Mahrous

Zidan

et al. 2021

Saudi Pharmaceutical Journal

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Flibanserin (FLB), an antiserotonin drug, is used to treat women with hypoactive sexual appetite disorder. FLB shows low bioavailability (~33%) probably due to its low water solubility. The current study investigated the impact of hydroxypropyl-β-cyclodextrin (HP-β-CD) and sodium lauryl sulfate (SLS) on the dissolution and permeation of FLB. HP-β-CD–FLB inclusion complexes were prepared using physical mixing and kneading at 1:1 and 1:2 M ratios and characterized using differential scanning calorimetry, Fourier transform infrared spectroscopy, and powder X-ray diffractometry. The dissolution and permeation of the complexes through a cellophane membrane were performed in, 0.1, 0.3 and 0.5% SLS in phosphate buffer (pH 6.8). Derived from the slope of the linear phase solubility diagram, the apparent stability constant ( K 1:1 ) was 372.54 M −1 . Kneading changed the crystalline form of FLB to an amorphous appearance characterized by minimal crystalline peaks, indicating successful inclusion complex formation. In addition, the HP-β-CD–FLB inclusion complexes showed twofold increased dissolution efficiency at 6 h. The cumulative FLB amount permeated at 6 h increased from 14.1% to 21.88% and 34.56% in the presence of 0.1% and 0.3% of SLS, respectively. However, increasing SLS to 0.5% did not show an increase in FLB permeation. Therefore, the HP-β-CD–FLB inclusion complex has an improved dissolution rate compared to FLB alone. The presence of SLS in the dissolution medium increases the dissolution rate of pure FLB and its complex with HP-β-CD. kneaded 1:1 complex was formulated bioadhesive buccal tablets and showed enhanced drug release.

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Section: Introductionmentioning

confidence: 99%

Preparation, characterization, dissolution, and permeation of flibanserin − 2-HP-β-cyclodextrin inclusion complexes

Alghaith

Mahrous

Zidan

et al. 2021

Saudi Pharmaceutical Journal

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“…The proposed model was able to predict the dissolution and the solubility of ionizable water-insoluble drug as functions of pH and surfactant concentration (5). Moreover, the purity of the surfactant also must be investigated due to its significant influence in the size and loading capacity of micelles, which results in changes in solubility and dissolution rate (117).…”

Section: Surfactantsmentioning

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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“…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). Moreover, interactions among the ions and the type of surfactant used must also be considered carefully when dissolution media are selected.…”

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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Evaluation of the impact of sodium lauryl sulfate source variability on solid oral dosage form development

Cited by 9 publications

References 38 publications

Preparation, characterization, dissolution, and permeation of flibanserin − 2-HP-β-cyclodextrin inclusion complexes

Preparation, characterization, dissolution, and permeation of flibanserin − 2-HP-β-cyclodextrin inclusion complexes

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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