Design and characterization of a surfactant-enriched tablet formulation for oral delivery of a poorly water-soluble immunosuppressive agent

Ruddy, Shaun; Matuszewska, Bozena; Grim, Yvetta A.; Ostovic, Drazen; Storey, David

doi:10.1016/s0378-5173(99)00056-3

Cited by 27 publications

(20 citation statements)

References 11 publications

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“…The enhanced release rate has been rationalized by the ability of the surfactant to (i) increase the hydrophilicity of the dosage form, [24] (ii) act as a wetting agent [25] and (iii) increase micellar solubilization [26] . It is well documented that the addition of surfactants to dissolution media can maintain sink conditions and assist with the dissolution of IR products [27–29] …”

Section: Methods For Maintaining Dissolution Sink Conditionsmentioning

confidence: 99%

Overcoming sink limitations in dissolution testing: a review of traditional methods and the potential utility of biphasic systems

Phillips

Pygall²,

Cooper³

et al. 2012

Journal of Pharmacy and Pharmacology

165

109

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Objectives The conventional dissolution test, particularly the USP apparatus I and II, remains an important tool in the armory of the pharmaceutical development scientist. For realistic dissolution characterization, sink conditions, where saturation solubility of a drug in the dissolution medium is at least three times more than the drug concentration, are critical. These conditions can be problematic to maintain with formulations containing poorly-soluble actives. This review summarizes the role of the dissolution test in the pharmaceutical industry, together with some traditional techniques/additives used to enhance solubility and facilitate the achievement of sink conditions. The biphasic dissolution system, an innovative model for the treatment of poorly-soluble species, will also be discussed. Key findings The biphasic dissolution model utilizes media comprising immiscible aqueous and organic layers whereby the drug, following initial aqueous dissolution, partitions into the organic layer. This step, which acts to remove all dissolved species from the aqueous layer, enables further aqueous dissolution to occur and hence the dissolution-partition cycle continues. Crucially, the aqueous layer does not saturate allowing sink conditions to be maintained and hence the experiment will, in theory, yield complete dissolution. Summary This review highlights important concepts regarding solubility/sink limitation and intends to provoke debate among analytical and formulation scientists as to the potential advantages, long-term development and widespread implementation of a biphasic dissolution system in drug development.

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Section: Methods For Maintaining Dissolution Sink Conditionsmentioning

confidence: 99%

Overcoming sink limitations in dissolution testing: a review of traditional methods and the potential utility of biphasic systems

Phillips

Pygall²,

Cooper³

et al. 2012

Journal of Pharmacy and Pharmacology

165

109

View full text Add to dashboard Cite

show abstract

“…Entrained air is incorporated by means of a suitable agent so that excess water readily can escape into adjacent air-filled voids. 15 Because of its amphibious nature, SDS is an anionic surfactant widely used in pharmaceutical preparations 16,17 and cardiovascular applications.…”

Section: Introductionmentioning

confidence: 99%

Influence of surfactant molecules as air‐entraining agent for bone cement macroporosity

Sarda

Nilsson

Balcells

et al. 2003

J Biomedical Materials Res

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Calcium phosphate bone cements (CPBCs) represent a potential synthetic alternative to bone-graft materials in bone surgery applications. CPBCs are biocompatible, bioresorbable, and slowly are replaced by new bone in vivo. However, CPBCs do not develop a macroporosity during setting that would allow fast bone ingrowth and good osteointegration of the implant. For this reason, recent research has approached the problem of inducing macroporosity inside the bone cement without influencing its normal setting. In this study, a new method for obtaining injectable macroporous CPBCs is proposed. It is based on the use of sodium dodecyl sulphate (SDS) as an air-entraining agent. The results have shown that the liquid-to-powder ratio and the SDS concentration, as well as the diameter and the interconnectivity of the macropores, can control the micro- and macroporosity. This new technology can be used to develop and optimize new commercial products for osteoporotic bone filling applications. Furthermore, the presented method also can be used at low temperatures before an operation to produce preformed implants to fit the particular needs of a patient.

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“…Phospholipid‐bile salt mixed micelles are a significant component of bile and function to solubilize food to promote nutrient absorption, and can dramatically enhance the absorption of poorly soluble drugs 1,2,4–6. Formulation design strategies of poorly soluble drugs parallel these food effects; pharmaceutical surfactants are included in formulations of poorly soluble drugs to enhance drug absorption by enhancing drug dissolution 7–10. Although food effects on dosage form performance and surfactant‐based strategies to enhance drug absorption are important areas in the development and use of poorly soluble drugs, a comprehensive and predictive understanding of surfactant‐mediated enhancement of drug dissolution has not been attained.…”

Section: Introductionmentioning

confidence: 99%

Surfactant-mediated dissolution: Contributions of solubility enhancement and relatively low micelle diffusivity

Balakrishnan

Rege

Amidon

et al. 2004

Journal of Pharmaceutical Sciences

127

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Design and characterization of a surfactant-enriched tablet formulation for oral delivery of a poorly water-soluble immunosuppressive agent

Cited by 27 publications

References 11 publications

Overcoming sink limitations in dissolution testing: a review of traditional methods and the potential utility of biphasic systems

Overcoming sink limitations in dissolution testing: a review of traditional methods and the potential utility of biphasic systems

Influence of surfactant molecules as air‐entraining agent for bone cement macroporosity

Surfactant-mediated dissolution: Contributions of solubility enhancement and relatively low micelle diffusivity

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