12.05.2010 | M. H. D. Kamal Al-Hallak, Shirzad Azarmi, Zhenghe Xu, Yadollah Maham, Raimar Löbenberg, The AAPS Journal, 2010

This study was designed to assess the value of isothermal microcalorimetry (ITMC) as a quality by design (QbD) tool to optimize blending conditions during tablet preparation. Powder mixtures that contain microcrystalline cellulose (MCC), dibasic calcium phosphate dihydrate (DCPD), and ...

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12.05.2010 | Melanie A. Felmlee, Qi Wang, Dapeng Cui, Samuel A. Roiko, Marilyn E. Morris, The AAPS Journal, 2010

γ-Hydroxybutyric acid (GHB), a drug of abuse, exhibits saturable renal clearance and capacity-limited metabolism. The objectives of this study were to construct a mechanistic toxicokinetic (TK) model describing saturable renal reabsorption and capacity-limited metabolism of GHB and to predict ...

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11.05.2010 | Sandra Klein, The AAPS Journal, 2010

Simulation of gastrointestinal conditions is essential to adequately predict the in vivo behavior of drug formulations. To reduce the size and number of human studies required to identify a drug product with appropriate performance in both the fed and fasted states, it is advantageous to be ...

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07.05.2010 | Diana Højmark Omkvist, Simon Birksø Larsen, Carsten Uhd Nielsen, Bente Steffansen, Lars Olsen, Flemming Steen Jørgen ..., The AAPS Journal, 2010

The human intestinal proton-coupled peptide transporter, hPEPT1 (SLC15A1), has been identified as an absorptive transporter for both drug substances and prodrugs. An understanding of the prerequisites for transport has so far been obtained from models based on competition experiments. These ...

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06.05.2010 | Akihiko Ozawa, Iris Lindberg, Bryan Roth, Wesley K. Kroeze, The AAPS Journal, 2010

Peptide hormones and neuropeptides play important roles in endocrine and neural signaling, often using G protein-coupled receptor (GPCR)-mediated signaling pathways. However, the rate of novel peptide discovery has slowed dramatically in recent years. Genomic sequencing efforts have yielded a ...

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04.05.2010 | Mei-Ling Chen, Vinod P. Shah, Derek Ganes, Kamal K. Midha, James Caro, Prabu Nambiar, Mario L. Rocci, Avinash G. Tho ..., The AAPS Journal, 2010

Modified release products are complex dosage forms designed to release drug in a controlled manner to achieve desired efficacy and safety. Inappropriate control of drug release from such products may result in reduced efficacy or increased toxicity. This workshop provided an opportunity for ...

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04.05.2010 | Louis S. Premkumar, The AAPS Journal, 2010

In spite of intense research efforts and after the dedicated Decade of Pain Control and Research, there are not many alternatives to opioid-based narcotic analgesics in the therapeutic armamentarium to treat chronic pain conditions. Chronic opioid treatment is associated with sedation, ...

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01.05.2010 | Ripal Gaudana, Hari Krishna Ananthula, Ashwin Parenky, Ashim K. Mitra, The AAPS Journal, 2010

Ocular drug delivery has been a major challenge to pharmacologists and drug delivery scientists due to its unique anatomy and physiology. Static barriers (different layers of cornea, sclera, and retina including blood aqueous and blood–retinal barriers), dynamic barriers (choroidal and ...

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27.04.2010 | Kate J. Reilley, Marc Giulianotti, Colette T. Dooley, Adel Nefzi, Jay P. McLaughlin, Richard A. Houghten, The AAPS Journal, 2010

Synthetic combinatorial methods now make it practical to readily produce hundreds of thousands of individual compounds, but it is clearly impractical to screen each separately in vivo. We theorized that the direct in vivo testing of mixture-based combinatorial libraries during the discovery ...

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27.04.2010 | Dongmei Lu, Lucila Garcia-Contreras, Pavan Muttil, Danielle Padilla, Ding Xu, Jian Liu, Miriam Braunstein, David N. ..., The AAPS Journal, 2010

This study aims to evaluate immunization with polymeric microparticles containing recombinant antigen 85B (rAg85B) delivered directly to the lungs to protect against tuberculosis. rAg85B was expressed in Escherichia coli and encapsulated in poly(lactic-co-glycolic acid) microparticles ...

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