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Drug mechanochemical activation
Journal of pharmaceutical sciences, 2009-11, Vol.98 (11), p.3961-3986
Colombo, I.
Grassi, G.
Grassi, M.
2009
Volltextzugriff (PDF)
Details
Autor(en) / Beteiligte
Colombo, I.
Grassi, G.
Grassi, M.
Titel
Drug mechanochemical activation
Ist Teil von
Journal of pharmaceutical sciences, 2009-11, Vol.98 (11), p.3961-3986
Ort / Verlag
Hoboken: Elsevier Inc
Erscheinungsjahr
2009
Quelle
Wiley Blackwell Single Titles
Beschreibungen/Notizen
The aim of this review is to describe the theoretical background lying behind the solid drug mechanochemical activation by cogrinding pointing out its advantages and drawbacks. A brief historical introduction precedes the discussion about the mechanisms leading to solid drug activation. This allows to clarify the concept of solid activation whose main effect is to improve drug solubility and, thus, drug bioavailability. Then, the attention is focused on the experimental tools used to evaluate drug activation before the in vivo use. This, of course, permits to properly modulate the milling conditions (milling time, mill revolution speed, drug/carrier ratio and so on) in the light of the optimisation of milling process and activated system properties. Thereafter, the discussion shifts on the different kinds of mills that can be used and on mills classification based on the energy transferred to the materials. Fundamental tool to perform this task is the mathematical modelling of mill dynamics that is here shown for different mills kinds. Finally, some examples of activated systems performance both in vitro and in vivo are presented and discussed. In conclusion, mechanochemical activation improves drug bioavailability. Interestingly, this activation does not require the use of solvents whose elimination from the activated product can be difficult and expensive but a relatively simple mechanical treatment. On the other hand, this approach, usually, works only for poorly water soluble drugs (solubility <100 µg/mL) that do not exhibit permeability problems. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:3961–3986, 2009
Sprache
Englisch
Identifikatoren
ISSN: 0022-3549
eISSN: 1520-6017
DOI: 10.1002/jps.21733
Titel-ID: cdi_proquest_miscellaneous_734067498
Format
–
Schlagworte
Biological and medical sciences
,
Biological Availability
,
Chemistry, Pharmaceutical
,
cogrinding bioavailability
,
Dosage Forms
,
Drug Carriers
,
General pharmacology
,
mechanical activation
,
Medical sciences
,
Models, Theoretical
,
Pharmaceutical Preparations - administration & dosage
,
Pharmaceutical Preparations - chemistry
,
Pharmaceutical Preparations - classification
,
Pharmaceutical technology. Pharmaceutical industry
,
Pharmacology. Drug treatments
,
Solubility
,
Technology, Pharmaceutical
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