Izvorni znanstveni članak
From Supersaturated Drug Delivery Systems to the Rising Era of Pediatric Formulations
G. Charkoftaki
; Laboratory of Biopharmaceutics and Pharmacokinetics, School of Pharmacy, University of Athens, Athens 15771, Greece
G. Valsami
; Laboratory of Biopharmaceutics and Pharmacokinetics, School of Pharmacy, University of Athens, Athens 15771, Greece
P. Macheras
; Laboratory of Biopharmaceutics and Pharmacokinetics, School of Pharmacy, University of Athens, Athens 15771, Greece
Sažetak
The number of options available to drug discovery scientists to enhance the solubility of poorly soluble compounds by conventional formulation approaches is limited. In most cases, drug formulation is oriented toward the creation of a supersaturated solution
upon contact with aqueous environment, often combined with solubilizing agents and precipitation inhibitors. The most popular formulations for achieving this target are the lipid-based formulations called self-emulsifying and self-microemulsifying drug delivery
systems, SEDDS and SMEDDS, respectively. They offer enhanced absorption and hence enhanced oral bioavailability of lipophilic drugs, presenting the drug in solubilized form in vivo, avoiding dissolution, which can be the rate limiting step in drug absorption for
sparingly soluble drugs. The production of high energy or rapid dissolving solid state formulations using drug particle engineering to enhance drug solubility and bioavailability is also applied. These formulations include solid dispersions, nanoparticles, co-ground mixtures etc. Furthermore, the development of prodrugs is also a useful strategy to improve the physicochemical, biopharmaceutical or pharmacokinetic properties of pharmacologically potent compounds, and thereby increase the developability and usefulness
of a potential drug. Up to now, most medications were made for adults and children’s requirements were not taken into account. Since the recent adoption of Paediatric Regulations in the U.S. and E.U., there is a greater demand for age-appropriate medicines
for children. The challenges in paediatric formulation development are mostly associated with the difficulty in defining design requirements for the intended dosage form that is most appropriate for the target patient population, due to the diversity of the paediatric
population (range of ages, physical size and capabilities) that varies significantly from birth to age 12 yrs old along with the dosage flexibility. The last years there has been an effort to develop solid paediatric formulations that deliver the appropriate dose
in a “user friendly” way and to find alternative drug delivery vehicles, such as mini-tablets, dairy products, and new taste masking techniques in order to improve drug acceptability.
In addition, alternative routes of administration have been proposed such as inhalation and nasal administration.
Ključne riječi
Supersaturation; solubility; dissolution; drug delivery systems; pediatric formulations
Hrčak ID:
94205
URI
Datum izdavanja:
19.12.2012.
Posjeta: 1.513 *