PubMed · 14140149
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M SUZUKI. 1964. [CIRCULAR DICHROISM].. https://doi.org/10.1248/yakushi1947.84.2_95
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Covalent conjugates of polyvinylpyrrolidone (PVP) with para-nitroaniline (PNA) were synthesized as a model PVP-drug conjugate, and PNA release was evaluated in vitro. Pyrrolidone ring opening with subsequent t-BOC protection of the pyrrolidone nitrogen and reaction with PNA in methylene chloride (CH2Cl2) produced a PVP-PNA conjugate with 3% of the pyrrolidone groups modified. Rates of PNA release from N-deprotected conjugates were twofold greater than those that were N-protected, indicating participation of the pyrrolidone N in release. Additional studies with monomeric analogs supported intramolecular base catalysis rather than lactam formation as the mechanism of this involvement. The approach serves as a prototype for the conjugation of other drugs with primary and secondary amine functional groups with PVP, including peptides and proteins.
A portable system using light-induced fluorescence technology (LIF) was development as an analytical tool for on-line monitoring of various manufacturing process applications. The LIF system was verified in several laboratory scale process applications specifically in noninvasive real-time observations of blend kinetics in tumbler blenders. This technology, through careful selection of filters for specific formulations, can provide clean and unadulterated raw data that shows the actual blend characteristic behavior of powder mixtures such as homogeneity end point and blend stability. Consistent blend homogeneity end point was demonstrated for all runs with LIF where data were verified by thief sampling and UV spectrophotometric assays. A correlation between LIF signal and drug powder concentration was established with limits of detection below 0.02% w/w for the API, Triamterene.
A one-step sonochemical process starting with the native BSA and tetracycline was employed to encapsulate the antibiotic drug in microspheres of BSA. The tetracycline loading studies showed that the maximum tetracycline loading capacity was found to be 65%. The antimicrobial activity of the tetracycline loaded in BSA microspheres was demonstrated on two bacterial strains that are sensitive to tetracycline.