Quantitative Evaluation of Drug Distribution in Tablets of Various Structures via Raman Mapping

Balogh

Period. Polytech. Chem. Eng.

et al. 2018

Self Cite

Novel medicated straws were developed based on drug-loaded electrospun fibers prepared by direct current electrospinning (DCES) and high-speed electrospinning (HSES) of scaled-up productivity. Good quality micro- and nanofibers were electrospun using both techniques despite the multiple times higher throughput rate of HSES based on the scanning electron microscopic imaging (SEM). Solid state analyses revealed that the poorly soluble model drug carvedilol (CAR) was dispersed in an amorphous form in the electrospun polyvinylpyrrolidone (PVPK30) fibers. In vitro dissolution studies revealed ultrafast drug release from the prepared fibrous formulations inserted into plastic straws. Based on the results the developed drug delivery system is suitable for storing the formulation in a solid dosage form and in situ turning it into liquid form when administered.

Section: Solid State Analyses With Dsc Xrpd and Raman Spectroscopymentioning

confidence: 99%

Medicated Straws Based on Electrospun Solid Dispersions

Balogh

Period. Polytech. Chem. Eng.

et al. 2018

Self Cite

Period. Polytech. Chem. Eng.

“…Nano-fibrous form of amorphous solid drug dispersions, prepared by various electrospinning (ES) techniques of increased productivity, using melt (MES) high speed (HSES), alternating current (ACES) circumstances, facilitate the bioavailability of drugs having poor water solubility [48][49][50][51]. Completely homogeneous distribution of drugs in polymer matrix was achieved this way according to Raman chemical mapping [52]. Ultrafast drug release of cardiovascular drug (carvedilol) was achieved from the prepared fibrous formulations (inserted into straws) suggesting that such a drug delivery system is suitable for storing the formulation in a stable solid dosage form and turning it rapidly into liquid form before administration [53].…”

Section: Technologies Of Innovative Pharmaceuticalsmentioning

confidence: 99%

Pharmaceutical and Macromolecular Technologies in the Spirit of Industry 4.0

Marosi

Hirsch

Bocz

et al. 2018

Self Cite

Well designed (multilayer, adaptive, reactive) interphases, being a key element of multicomponent structures, could be tailored to different requirements through controlled technologies. This is the link connecting various green, safe, healthy materials and innovative pharmaceuticals. Upgraded recycling could be performed by interfacial consolidation of self-reinforced composites, the flame retardancy of which is feasible with surprisingly low amount of flame retardant. Examples are shown how the reinforced and foamed forms of thermosetting and thermoplastic biopolymers can play a significant role (after flame retardant modification) in the development of airplanes and electric cars. Biopolymer nanofibres, such as polycaprolactone and polyhydroxybutyrate, could be formed with increased productivity for various medical uses. Raman-based control of the units of integrated continuous technologies has been elaborated including controlled formation of crystals with polymer interlayer for direct tableting.

“…To this end, the non-destructive, label-free and reagent (solvent)-free inherent features of infrared spectroscopy and Raman scattering enables identifying ingredient distribution, providing for the optimization of the final product quality. Several methods were developed to analyze the chemical images, such as the distributional homogeneity index (DHI, an index based in macropixels and continuous-level moving block) 10 , Poole-index (where the algorithm binarized the maps and works with non-overlapping macropixels) 11 and variographic analysis (where the variance values are estimated by comparing pairs of observations at different lags) 12 , which have brought progress in describing sample homogeneity. 13,14 For instance, Ma et al 15 have successfully used near infrared (NIR) images and DHI to evaluate the homogeneity of commercial chlorpheniramine maleate tablets.…”

Section: Introductionmentioning

confidence: 99%

Neither too little nor too much: finding the ideal proportion of excipients

Mitsutake

Silva

Breitkreitz

et al. 2022

Preprint

Excipient’s homogeneity is of paramount importance during the development of pharmaceutical formulations due to its relation to stability, safety and efficacy. A direct and unique approach to evaluate such property is 3D Raman imaging. This technique characterizes the surface and inner part of preformulation samples, allowing to determine phase separation in the early stages of pharmaceutical development. Aiming to promote controlled release of the local anesthetic butamben (BTB), confocal 3D Raman microscopy was used to obtain its optimal proportion in Apifil®, Capryol® 90 and Transcutol®. Even if the microscopic images of some samples displayed very homogeneous surfaces, analysis of 3D maps showed that chemical distribution throughout the material was different. To investigate how concentration affects the homogeneity, mixture experimental design (DoE) was employed. From this analysis, it was revealed that correct amount of Capryol® 90 enhances both miscibility and solubility. Furthermore, suitable miscibility was observed in two ratio proportions of excipients: Solution 1: Apifil® 30.00%, Capryol 20.00% and Transcutol 10.00% (w/w), with a desirability of 0.783; and Solution 2: Apifil® 25.00%, Capryol 25.00% and Transcutol 10.00% (w/w), with 0.742 desirability. These results unequivocally demonstrated that confocal Raman microscopy combined to DoE can bring pharmaceutical development to a higher level.