Evaluation of Drug–Polymer Solubility Curves Through Formal Statistical Analysis: Comparison of Preparation Techniques

Knopp, Matthias Manne; Olesen, Niels Erik; Holm, Per; Löbmann, Korbinian; Holm, René; Langguth, Peter; Rades, Thomas

doi:10.1002/jps.24207

Cited by 37 publications

(51 citation statements)

References 28 publications

(55 reference statements)

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“…A commonly used method for stabilizing amorphous drugs is their molecular incorporation into water soluble amorphous polymers, forming glass solutions. However, the physical stability of these systems may still be limited by several environmental factors such as humidity, heat and the limited solubility of drug molecules in commonly used pharmaceutical polymers (1). The stability of amorphous systems is not only critical with regards to re-crystallization during storage, but is often also a requirement in order to form a supersaturated solution by preventing recrystallization upon administration (2).…”

Section: Introductionmentioning

confidence: 99%

Influence of variation in molar ratio on co-amorphous drug-amino acid systems

Jensen

Larsen

Löbmann

2016

European Journal of Pharmaceutics and Biopharmaceutics

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Section: Introductionmentioning

confidence: 99%

Influence of variation in molar ratio on co-amorphous drug-amino acid systems

Jensen

Larsen

Löbmann

2016

European Journal of Pharmaceutics and Biopharmaceutics

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“…If the drug is molecularly dispersed in the polymer below the equilibrium solubility, it will remain physically stable during storage at least as long as significant water sorption into the glass solution can be avoided. Therefore, different methods to measure the solubility of drugs in polymers have been developed based on differential scanning calorimetry (DSC) and several studies have already determined the solubility of different drugs in PVP . Furthermore, according to Marsac et al, the solubility of a drug in PVP can be predicted from the solubility in a low‐molecular‐weight analogue of PVP by assuming that the analogue constitutes the lattice of the polymer.…”

Section: Introductionmentioning

confidence: 99%

“…Therefore, different methods to measure the solubility of drugs in polymers have been developed based on differential scanning calorimetry (DSC) and several studies have already determined the solubility of different drugs in PVP. [23][24][25][26][27][28] Furthermore, according to Marsac et al, 23 the solubility of a drug in PVP can be predicted from the solubility in a low-molecular-weight analogue of PVP by assuming that the analogue constitutes the lattice of the polymer.…”

Section: Introductionmentioning

confidence: 99%

Influence of Polymer Molecular Weight on Drug–polymer Solubility: A Comparison between Experimentally Determined Solubility in PVP and Prediction Derived from Solubility in Monomer

Knopp

Olesen

Holm

et al. 2015

Journal of Pharmaceutical Sciences

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In this study, the influence of polymer molecular weight on drug-polymer solubility was investigated using binary systems containing indomethacin (IMC) and polyvinylpyrrolidone (PVP) of different molecular weights. The experimental solubility in PVP, measured using a differential scanning calorimetry annealing method, was compared with the solubility calculated from the solubility of the drug in the liquid analogue N-vinylpyrrolidone (NVP). The experimental solubility of IMC in the low-molecular-weight PVP K12 was not significantly different from that in the higher molecular weight PVPs (K25, K30, and K90). The calculated solubilities derived from the solubility in NVP (0.31-0.32 g/g) were found to be lower than those experimentally determined in PVP (0.38-0.40 g/g). Nevertheless, the similarity between the values indicates that the analogue solubility can provide valuable indications on the solubility in the polymer. Hence, if a drug is soluble in an analogue of the polymer, it is most likely also soluble in the polymer. In conclusion, the solubility of a given drug-polymer system is determined by the strength of the drug-polymer interactions rather than the molecular weight of the polymer. Therefore, during the first screenings for drug solubility in polymers, only one representative molecular weight per polymer is needed.

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“…(53,72). Solid-state structures of spray-dried dispersions showed a single-glass transition of a homogeneous mixture of drug/polymer.…”

Section: (1) Formulation Aspectsmentioning

confidence: 99%

Bioavailability Improvement Strategies for Poorly Water-Soluble Drugs Based on the Supersaturation Mechanism: An Update

Yang¹,

Gong²,

Wang³

et al. 2016

J Pharm Pharm Sci

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-The formulation development for poorly soluble drugs still remains a challenge. Supersaturating drug delivery systems (SDDS) or drug delivery systems based on supersaturating provide a promising way to improve the oral bioavailability of poorly water-soluble drugs. In supersaturable formulations, drug concentration exceeds the equilibrium solubility when exposed to gastrointestinal fluids, and the supersaturation state is maintained long enough to be absorbed, resulting in compromised bioavailability. In this article, the mechanism of generating and maintaining supersaturation and the evaluation methods of supersaturation assays are discussed. Recent advances in different drug delivery systems based on supersaturating are the focus and are discussed in detail.

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Evaluation of Drug–Polymer Solubility Curves Through Formal Statistical Analysis: Comparison of Preparation Techniques

Cited by 37 publications

References 28 publications

Influence of variation in molar ratio on co-amorphous drug-amino acid systems

Influence of variation in molar ratio on co-amorphous drug-amino acid systems

Influence of Polymer Molecular Weight on Drug–polymer Solubility: A Comparison between Experimentally Determined Solubility in PVP and Prediction Derived from Solubility in Monomer

Bioavailability Improvement Strategies for Poorly Water-Soluble Drugs Based on the Supersaturation Mechanism: An Update

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