Drug solubilization capacity

It should be noted that this procedure needs to be carried out on a case-by-case basis—there is no indication that the relative solubilization capacity (ability of bile components or surfactants to enhance solubility/dissolution of a drug) is consistent from drug to drug. Therefore, use of a standard medium containing a synthetic surfactant to correspond to either FaSSIF or FeSSIF results is not possible. 

Once it is conLrmed that a simple LBDDS provides measurable improvement in bioavailability, the next step is development and optimization of the formulation. Currently there are no deLnitive tests that will translate vitro measures tan vivo performance. At the same time, this does not mean that development of such formulations should be conducted using a trial-and-error approach. Pouton s classiLcation system points out that the factors to be considered in interpreitingvtde behavior of the formulations are effects of lipolysis, dispersibility, and solubilization capacity on dilution. It is important to understand that the balance of each of these effects will depend on the drug being formulated, and that there is unlikely to be a universal formulation that works for all compounds. 

Microemulsion system applications span many areas including enhanced oil recovery, soil and aquifer decontamination and remediation, foods, pharmaceuticals (drug delivery systems), cosmetics, and pesticides [2,5,33,37,232,233]. Some of these are listed in Table 3.6. The widespread interest in microemulsions and use in these different industrial applications are based mainly on their high solubilization capac-... 

The solubilizing capacity of micelles and microemulsions prepared using the surfactant N,N-dimethyl-dodecylamine-N-oxide (C12AO), and containing either one of two semipolar ethyl ester oils (i.e., EH or EO) for the poorly water soluble, lipophilic steroidal drug, testosterone enanthate, has been determined recently (Barlow, D.J. Lawrence, M.J. Zuberi, T. Zuberi, S. Heenan, R.K. Personal communication, 2005). 

The solubilizing capacity for a given surfactant system is a complex function of the physicochemical properties of the two components which, in turn, influence the location or sites where the drug is bound to the micelle. The molar volume of the solubilizate together with its lipophilicity are important factors, the former reducing and the latter increasing solubilization. ... 

Clarysse S, Psachoulias D, Brouwers J, et al. Postprandial Changes in solubilizing capacity of human intestinal fluids for BCS Class II Drugs. Hiarm Res 2009, in press. 

The drug-loading capacities of liposomes depend on the properties of the drug, phospholipids, and other additives used. Typically, hydrophobic drugs are solubilized... 

Many drugs interact most favorably with P-CD. Unfortunately, P-CD has the lowest solubility (1.8% in water at 25 C) among the three non-derivatized CDs, thereby limiting its solubilization capacity. To enhance the solubility of the P-CD and to improve its safety, derivatives of P-CD have been developed. Among them, hydroxypropyl-j8-cyclodextrins (HP-/3-CDs) and sulfobutylether-jS-cyclodex-trins (SBE-/3-CDs, mainly as SBE7-J3-CD,... 

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