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Evaluating side‐by‐side diffusion models for studying drug supersaturation in an absorptive environment: a case example of fenofibrate and felodipine Evaluating side‐by‐side diffusion models for studying drug supersaturation in an absorptive environment: a case example of fenofibrate and felodipine

To test whether a side‐by‐side diffusion model is suitable for studying drug supersaturation in an absorptive environment.

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Diclofenac Prodrugs for Intra-articular Depot Injectables: In Vitro Hydrolysis and Species Variation Diclofenac Prodrugs for Intra-articular Depot Injectables: In Vitro Hydrolysis and Species Variation

Intra-articular depot injectables based on in situ suspension formation of ester prodrugs of nonsteroidal anti-inflammatory drugs are promising for management of joint pain. As candidates for this delivery approach, 5 diclofenac ester prodrugs comprising different imidazole-containing promoieties were synthesized and their physicochemical properties characterized. In vitro hydrolysis rates were investigated in buffer solutions, in 40% (v/v) human, equine, canine, and rat plasma, and in 80% (v/v) human and equine synovial fluid. Bioconversion of the prodrugs to diclofenac was found to be enzyme-mediated and follow pseudo-first-order kinetics. Large variations in hydrolysis rates were observed between species and between prodrugs, with prodrug half-lives in plasma from canine, rat, horse, and human of 3.44-141 min, 2.51-14 min, 0.58-1.31 min, and 0.23-1.70 min, respectively. Half-lives in human and equine synovial fluid were 1.6- to 28-fold larger than in plasma. The results highlight the significance of species and tissue variation in prodrug design and suggest that the horse may constitute a suitable model for testing the intra-articular depot approach. Two prodrug candidates appeared promising for future in vivo studies based on their rapid in vitro enzyme-mediated bioconversion to diclofenac and physiochemical characteristics.

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Release notes - DissoPro 3.5 Release notes - DissoPro 3.5

DissoPro 3.5 is now available with improved functionality to make administrative duties simpler, security setup more straight forward and data analysis more capable and flexible. Please see the release note for more detailed information.

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A video introduction into microDISS Profiler™ instrument and its applications A video introduction into microDISS Profiler™ instrument and its applications

An overview of Pions flagship product, the microDiss Profiler incorporating the Rainbow fiber optic system. 

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Probing the mechanism of bupivacaine drug release from multivesicular liposomes Probing the mechanism of bupivacaine drug release from multivesicular liposomes

Researchers from FDA use Pion’s MicroDISS Profiler to probe mechanism of the release kinetics of a drug from multivesicular liposomes

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Degree and Extent of Supersaturation of Amorphous Pharmaceuticals and Their Flux through Lipophilic Membrane Degree and Extent of Supersaturation of Amorphous Pharmaceuticals and Their Flux through Lipophilic Membrane

The goal of this study was to apply in situ concentration monitoring for quick assessment of degree and extent of supersaturation that can be achieved by amorphization of the drug. In addition the comparison of the flux through artificial lipophilic membrane from drug loaded below and above their amorphous solubility threshold was investigated.

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In Situ Fiber Optic Dissolution Monitoring of Combination Drug Product Containing Three Actives In Situ Fiber Optic Dissolution Monitoring of Combination Drug Product Containing Three Actives

This study introduces a developed computational method for real time concentration measurements of multiple APIs using in situ fiber optic UV-Vis monitoring.

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Using Biorelevant Flux Measurements for Prediction of Fraction Absorbed for the Drug Products of Poorly Soluble Compounds Using Biorelevant Flux Measurements for Prediction of Fraction Absorbed for the Drug Products of Poorly Soluble Compounds

This study demonstrated a feasibility of using flux measurements through gastro-intestinal tract (GIT) mimicking artificial membrane to predict MAD and Fa values in biopharmaceutics modelling for BCS Class 2 drugs.

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Simultaneous in situ monitoring of free drug concentration and nanoparticles during dissolution testing of nanocrystalline and amorphous formulations Simultaneous in situ monitoring of free drug concentration and nanoparticles during dissolution testing of nanocrystalline and amorphous formulations

The goal of this study was to develop a method of de-convoluting the UV-Vis spectra measured in situ to not only obtain the concentration of free drug in the presence of light absorbing nanoparticles but also to quantify the
concentration of nanoparticles present in suspensions.interplay between dissolution, solubility and permeability

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From Traditional Dissolution to  In Vivo Predictive Flux Measurements From Traditional Dissolution to In Vivo Predictive Flux Measurements

The webinar introduces the use of in situ fiber optic technique for traditional dissolution monitoring as well as for in vivo predictive flux measurements that uncover the interplay between dissolution, solubility and permeability

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