Evaluation of heat-conduction microcalorimetry in pharmaceutical stability studies. V. A new approach for continuous measurements in abundant water vapour

Angberg, M.; Nyström, Christer; Castensson, Staffan

doi:10.1016/0378-5173(92)90007-o

Cited by 69 publications

(16 citation statements)

References 14 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Other samples were equilibrated with "microhygrostats" containing small quantities of saturated salt solutions that were sealed within the ampules. 9 This arrangement provided for nearly constant RH as the crystal conversion proceeded.…”

Section: Experimental Methodsmentioning

confidence: 98%

Characterization and Interconversion of Polymorphs of Premafloxacin, a New Quinolone Antibiotic

Schinzer

Bergren

Aldrich

et al. 1997

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

The quinolone antibiotic premafloxacin crystallizes in at least five solid modifications, including three anhydrous phases (Forms I-III), a hydrate, and a methanolate. The anhydrous phases were studied by optical microscopy, X-ray powder diffraction, HPLC, hot-stage microscopy, dynamic moisture sorption gravimetry, differential scanning calorimetry, thermal gravimetry, and solution and isothermal calorimetry. Dry samples of Form I converted to Form II and ultimately to Form III through a sequence of melts and recrystallizations. Form III was stable to its melting temperature near 200 degrees C. Humidified samples of Form I converted directly to Form III via a moisture-mediated solid-state phase transformation at temperatures as low as 40 degrees C. The calorimetric and solubility data confirmed that Form III was lower in free energy and enthalpy than Form I at room temperature. Our investigation revealed that Form I was not crystallized directly from solution. Rather, Form I was the product of facile solid-state desolvation of the methanol solvate.

show abstract

Section: Experimental Methodsmentioning

confidence: 98%

Characterization and Interconversion of Polymorphs of Premafloxacin, a New Quinolone Antibiotic

Schinzer

Bergren

Aldrich

et al. 1997

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

show abstract

“…Nuclear magnetic resonance (NMR) and FT Raman spectroscopy Nuclear magnetic resonance spectra Mobility of water molecules in a system Khan and Pilpel 1987;Martinez et al 1990;Suryanarayanan and Wiedmann 1990;Yoshioka et al 1992Yoshioka et al , 1995Aso et al 1994Aso et al , 1997Taylor et al 2001;McCrystal et al 2002;Suzuki and Kawasaki 2005 Strength of the hydrogen bonds with water Determination of plasticizing effect of water on polymer mobility, differentiation between samples in rubbery and glassy state Pikal et al 1977;Hollenbeck et al 1978;Angberg et al 1988Angberg et al , 1990Angberg et al , 1991Angberg et al , 1992aAngberg et al , 1992bFielden et al 1988;Buckton andBeezer, 1988, 1991;Pikal and Dellerman 1989;Blair et al 1990;Angberg 1995;Pudipeddi et al 1996;Buckton 2000 …”

Section: Analytical Techniques Used To Characterize Water In Solidsmentioning

confidence: 99%

“…the rate of heat production, with a sensitivity of about 10 4 greater than it is possible with a conventional DSC (Pikal and Dellerman 1989). In a series of publications (Angberg et al 1988(Angberg et al , 1990(Angberg et al , 1991(Angberg et al , 1992aAngberg 1995), the use of heat-conduction microcalorimetry in pharmaceutical stability studies was evaluated. The authors showed that, with the help of microcalorimetry, it was possible to detect the hydration process of anhydrous lactose after only one day of storage at 58 % RH.…”

Section: Analytical Techniques Used To Characterize Water In Solidsmentioning

confidence: 99%

Excipient Selection in Oral Solid Dosage Formulations Containing Moisture Sensitive Drugs

Rajabi‐Siahboomi

Levina²,

Upadhye

et al. 2015

Excipient Applications in Formulation Design and Drug Delivery

View full text Add to dashboard Cite

Moisture sensitivity of active pharmaceutical ingredients (APIs) presents a formidable challenge in the formulation of oral dosage forms. The interaction of moisture with APIs is crucial to an understanding of water-based processes, e.g. manufacturing or prediction of solid dosage form stability and shelf-life. Unwarranted moisture sorption by either APIs or excipients can result in unstable oral solid formulations. The appropriate selection of excipients for the core formulation and appropriate moisture barrier film coating helps to remedy the moisture-related issues with APIs and thus can improve the storage stability of the final formulations. In this chapter, we review the nature and extent of the moisture sensitivity and possible approaches taken to overcome it. Use of excipients that bind tightly with water reduce its potential interaction with the API. In addition, application of a barrier coating to reduce rate and extent of moisture ingress into the core of the solid dosage form during the storage (in original packaging or while in-use), are some of the many simple options that have been considered and described.Keywords Calorimetry · Degradation · Differential scanning calorimetry · Dynamic vapor sorption · Equilibrium relative humidity · Excipients · Isothermal microcalorimetry · Moisture · Moisture-barrier coating · Near-infra red Spectroscopy · Opadry · Optical waveguide spectroscopy · Packaging · Stability · Water · Water vapor transmission rate Abbreviations AluAluminum API Active pharmaceutical ingredient

show abstract

“…Both modes were applied and the results compared for the purine derivative. Different levels of controlled humidity were obtained by using a small glass vial containing pure water or saturated solutions [4] according to the technique of Angerg et al [5]. Different amounts of sample (5 to 130 mg) were investigated.…”

Section: Experimental and Instrumentationmentioning

confidence: 99%

Quantitation of amorphicity by microcalorimetry

Giron¹,

Remy²,

Thomas³

et al. 1997

Journal of Thermal Analysis

View full text Add to dashboard Cite

The amorphous state of solids is characterized by a higher chemical and physical reactivity and a hygroscopic behaviour. Furthermore processing of amorphous powders is often difficult, because of the instability. Fast crystallizations, precipitations and milling favour the formation of the amorphous state. Galenical processes like granulation, drying, lyophilization, mixing, may also induce amorphous regions in the drug products.X-ray diffraction techniques can be used for the determination of the amorphicity of drug raw materials or drug products. Unfortunately, 10% is the detection limit, which in normal cases can be attained. Amorphous substances undergo an exothermic crystallization at temperatures above the glass transition point. Water which is a plasticizer decreases the temperature of the glass transition point, allowing the crystallization to occur at lower temperatures. The crystallization energy is measure of by microcalorimetry.Examples show the influence of the choice of the experimental conditions, especially the influence of the amorphicity on the kinetic of the reaction. Critical steps are discussed for three different drug substances. Limits of detection in the magnitude of 1% are possible using microcalorimetry.

show abstract

Evaluation of heat-conduction microcalorimetry in pharmaceutical stability studies. V. A new approach for continuous measurements in abundant water vapour

Cited by 69 publications

References 14 publications

Characterization and Interconversion of Polymorphs of Premafloxacin, a New Quinolone Antibiotic

Characterization and Interconversion of Polymorphs of Premafloxacin, a New Quinolone Antibiotic

Excipient Selection in Oral Solid Dosage Formulations Containing Moisture Sensitive Drugs

Quantitation of amorphicity by microcalorimetry

Contact Info

Product

Resources

About