Controlled Release — Small Molecules
A prodrug is generally designed to improve the physical and chemical properties of a parent drug to enable formulation development, improve delivery, and/or achieve targeting. Similarly a prodrug approach can be used to enable development of a controlled release formulation, i.e., to provide a pharmacokinetic profile with sustained plasma levels. In the following discussion the term controlled release (CR) is used to include all prodrug approaches that result in sustained plasma levels over a dosing duration, thus reducing dosing frequency of the parent drug or the active moiety. CR technologies could include osmotic devices, polymeric matrix, implants, and microspheres and suspensions for parenteral depots that result in sustained plasma levels of the drug.
KeywordsEster Prodrug Haloperidol Decanoate Nandrolone Decanoate Fluphenazine Decanoate Prodrug Approach
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- Al-Hindawi M, James K, and Nicholls P. The Influence of the Solvent on the Availability of Testosterone Propionate from Oily Injections. J Pharm Pharmacol 1981; 81:65PGoogle Scholar
- Drug Facts and Comparisons 2004, Facts and Comparisons, 58th Edition, 2003Google Scholar
- Gennaro AR. In: Remington: The Science and Practice of Pharmacy, Easton, PA: Mack Publishing Co., 19th Edition, 1995Google Scholar
- Hirabayashi H, Takahashi T, Fujisaki J, Masunaga T, Sato S, Hiroi J, Tokunaga Y, Kimura S, and Hata, T. Bone Specific Delivery and Sustained Release of Diclofenac, A Non-Steroidal Anti-inflammatory Drug via Bisphosphonic Prodrug Based on the Osteotropic Drug Delivery System (ODDS). J Control Release 2001; 70:183–191PubMedCrossRefGoogle Scholar
- Murdan S, and Florence A. Non-aqueous Solutions and Suspensions as Sustained-Release Injectable Formulations. In: Senior J, and Radomsky M. Sustained Release Injectable Products Denver, Co: Interpharm Press; 2000:71–108Google Scholar
- Parfitt K, Martindale: The Complete Drug Reference, London, UK: Pharmaceutical Press, 32nd Edition, 1999Google Scholar
- Physicians’ Desk Reference®-2004. Thomson Healthcare, The Medical Economics Company. 58th Edition, 2004.Google Scholar
- Senior J. Insoluble Salt Forms and Drug Complexes. In: Senior J, and Radomsky M. Sustained Release Injectable Products. Denver, Co: Interpharm Press; 2000:41–70Google Scholar
- Tipton A, and Dunn R. In Situ Gelling Systems. In: Senior J, and Radomsky M. Sustained Release Injectable Products. Denver, Co: Interpharm Press; 2000:241–278Google Scholar