The suitability of a poly(sodium methacrylate, methyl methacrylate) (NaPMM), a novel mucoadhesive material, to prepare fast-dissolving microparticles containing nifedipine (NIF) in the range of 25-75% w/w was verified. Microparticles made of a low-viscosity hydroxypropylmethylcellulose (HPMC), were also prepared to compare the NIF release profile and bioadhesive properties. The release test was carried out in oversaturation conditions. The physical state of microparticles was also investigated. The formulation stability was evaluated over a 3-month period in long-term and accelerated conditions. The presence of amorphous NIF within freshly prepared microparticles was attributed to interactions between the drug and both polymers. NaPMM conferred to microparticles suitable mucoadhesive properties and significantly increased NIF dissolution rate in comparison to HPMC. Nevertheless, NIF apparent solubilities obtained by NaPMM microparticles were lower than those obtained by the HPMC set. After 3-month storage in the case of HPMC microparticles, NIF dissolution rate and supersaturation degree significantly decreased due to drug crystallization. As far as NaPMM microparticles are concerned, neither NIF dissolution rate nor apparent solubility significantly changed.
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http://dx.doi.org/10.1016/j.ejpb.2007.06.012 | DOI Listing |
Mol Pharm
November 2024
Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota 55455, United States.
Using the time-temperature-transformation diagrams, we demonstrated a correlation between molecular mobility and crystallization in amorphous solid dispersions of nifedipine (NIF) with each polyvinylpyrrolidone vinyl acetate (PVPVA64) and polyvinyl caprolactam polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus). The behavior was compared with the NIF dispersions prepared with each polyvinylpyrrolidone (PVP) and hydroxypropyl methylcellulose acetate succinate (HPMCAS) [Lalge et al., 2023, (3), 1806-1817].
View Article and Find Full Text PDFAAPS PharmSciTech
June 2024
Chongqing Key Laboratory of Digitalization of Pharmaceutical Processes and Equipment, College of Chemistry and Chemical Engineering, Chongqing University of Science and Technology, No. 20, University City East Road, Chongqing, 401331, China.
Nifedipine (NIF) is a dihydropyridine calcium channel blocker primarily used to treat conditions such as hypertension and angina. However, its low solubility and low bioavailability limit its effectiveness in clinical practice. Here, we developed a cocrystal prediction model based on Graph Neural Networks (CocrystalGNN) for the screening of cocrystals with NIF.
View Article and Find Full Text PDFRSC Adv
May 2024
Shanghai Institute of Applied Physics, Chinese Academy of Sciences Shanghai 201800 China.
Pa, the precursor nuclide of U in the thorium-uranium conversion is prone to reductive deposition in 2LiF-BeF (66 : 34 mol%, FLiBe) molten salt. We explored the adjustment and control of the redox potential of the FLiBe melt to avoid the Pa reduction deposition. The experimental data indicated that the deposited Pa can be completely dissolved and reentered into the molten salt with the addition of oxidant NiF, and the distribution and behaviour of uranium, thorium, neptunium, and most fission products did not have any significant change in the NiF-oxidised FLiBe molten salt, showing the feasibility of this manner to make Pa exist stably in the melt.
View Article and Find Full Text PDFMol Pharm
February 2024
Department of Biochemical and Chemical Engineering, Laboratory of Thermodynamics, TU Dortmund University, Emil-Figge-Str. 70, D-44227 Dortmund, Germany.
One way to increase the slow dissolution rate and the associated low bioavailability of newly developed active pharmaceutical ingredients (APIs) is to dissolve the API in a polymer, leading to a so-called amorphous solid dispersion (ASD). However, APIs are often supersaturated in ASDs and thus tend to crystallize during storage. The kinetics of the crystallization process is determined by the amount of water the ASD absorbs during storage at relative humidity (RH), storage temperature, polymer type, and the drug load of the ASD.
View Article and Find Full Text PDFMol Pharm
March 2023
Development Sciences, Research and Development, AbbVie, Inc., North Chicago, Illinois 60064, United States.
Amorphous drugs are used to improve bioavailability of poorly water-soluble drugs. Crystallization must be managed to take full advantage of this formulation strategy. Crystallization of amorphous drugs proceeds in a sequence of crystal nucleation and growth, with different kinetics.
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