Solid-state of pharmaceutical compounds

This article summarizes the different steps needed for a proper design and monitoring of the solid-state in pharmaceutical industry in order to fulfill the requirements of the guideline dealing with polymorphism of the International Conference of Harmonization.

[1]  Ulrich J. Griesser,et al.  Qualitative and quantitative study of polymorphic forms in drug formulations by near infrared FT-Raman spectroscopy , 2003 .

[2]  G A Stephenson,et al.  Characterization of the solid state: quantitative issues. , 2001, Advanced drug delivery reviews.

[3]  D. Bugay.  Characterization of the solid-state: spectroscopic techniques. , 2001, Advanced drug delivery reviews.

[4]  W Press,et al.  Crystalline solids. , 1980, Science.

[5]  H. Brittain,et al.  Spectral methods for the characterization of polymorphs and solvates. , 1997, Journal of pharmaceutical sciences.

[6]  M. E. Brown,et al.  Introduction to Thermal Analysis: Techniques and applications , 1988 .

[7]  M. Blanco,et al.  Development and validation of a method for the polymorphic analysis of pharmaceutical preparations using near infrared spectroscopy. , 2003, Journal of pharmaceutical sciences.

[8]  M. Mutz,et al.  Solid State Characterizations of Pharmaceutical Hydrates , 2002 .

[9]  S. Yamamura,et al.  Characterization of monoclinic crystals in tablets by pattern-fitting procedure using X-ray powder diffraction data. , 2003, International journal of pharmaceutics.

[10]  J. Ulrich,et al.  Solvent-Induced Phase Transformations of Hydrates , 1999 .

[11]  R. Suryanarayanan,et al.  A method for the rapid evaluation of the physical stability of pharmaceutical hydrates , 1999 .

[12]  Bruno C. Hancock,et al.  Modeling of transmitted X-ray intensity variation with sample thickness and solid fraction in glycine compacts. , 2003, Journal of pharmaceutical sciences.

[13]  Michael J. Pikal,et al.  Dynamics of pharmaceutical amorphous solids: the study of enthalpy relaxation by isothermal microcalorimetry. , 2002, Journal of pharmaceutical sciences.

[14]  S. Gupte,et al.  Applications of pressure differential scanning calorimetry in the study of pharmaceutical hydrates. II. Ampicillin trihydrate , 1998 .

[15]  D. Giron,et al.  Thermal Analysis, Microcalorimetry and Combined Techniques for the Study of the Polymorphic Behaviour of a Purine Derivative , 1999 .

[16]  L Yu,et al.  Amorphous pharmaceutical solids: preparation, characterization and stabilization. , 2001, Advanced drug delivery reviews.

[17]  Peter York,et al.  The improved compaction properties of mannitol after a moisture-induced polymorphic transition. , 2003, International journal of pharmaceutics.

[18]  D. Apperley,et al.  Quantitative nuclear magnetic resonance analysis of solid formoterol fumarate and its dihydrate. , 2003, Journal of pharmaceutical sciences.

[19]  Approach to the determination of hydrate form conversions of drug compounds and solid dosage forms by near-infrared spectroscopy. , 2003, Journal of pharmaceutical sciences.

[20]  D. Giron,et al.  X-Ray Quantitative Determination of Polymorphism in Pharmaceuticals , 1990 .

[21]  S. Toscani.  An up-to-date approach to drug polymorphism , 1998 .

[22]  N. Rasenack,et al.  Properties of Ibuprofen Crystallized Under Various Conditions: A Comparative Study , 2002, Drug development and industrial pharmacy.

[23]  G. Buckton,et al.  The use of isothermal microcalorimetry in the study of small degrees of amorphous content of a hydrophobic powder , 1996 .

[24]  Michael J Cima,et al.  High-throughput crystallization: polymorphs, salts, co-crystals and solvates of pharmaceutical solids. , 2004, Advanced drug delivery reviews.

[25]  R. G. Hollenbeck.  Determination of differential heat of solution in real solutions from variation in solubility with temperature. , 1980, Journal of pharmaceutical sciences.

[26]  M. Kitamura,et al.  Controlling factor of polymorphism in crystallization process , 2002 .

[27]  Structure determination from conventional powder diffraction data: application to hydrates, hydrochloride salts, and metastable polymorphs. , 2000, Journal of pharmaceutical sciences.

[28]  T. Threlfall.  Analysis of organic polymorphs. A review , 1995 .

[29]  Stephen Byrn,et al.  Pharmaceutical Solids: A Strategic Approach to Regulatory Considerations , 1995, Pharmaceutical Research.

[30]  L. Addadi,et al.  Molecular Recognition at Crystal Interfaces , 1991, Science.

[31]  Danielle Giron,et al.  Applications of Thermal Analysis and Coupled Techniques in Pharmaceutical Industry , 2002 .

[32]  M. Angberg,et al.  Evaluation of heat-conduction microcalorimetry in pharmaceutical stability studies. V. A new approach for continuous measurements in abundant water vapour , 1992 .

[33]  Joel Bernstein,et al.  Polymorphism in Molecular Crystals , 2002 .

[34]  Z. Zhang,et al.  Crystal growth. , 1999, Proceedings of the National Academy of Sciences of the United States of America.

[35]  D. Giron.  Characterisation of salts of drug substances , 2003 .

[36]  Rolf Hilfiker,et al.  POLYMORPHISM , 1945 .

[37]  Solvent effects on kinetics of solution-mediated transition of stearic acid polymorphs , 1985 .

[38]  H. Hakusui,et al.  Thermal dehydration of nafagrel hydrochloride hydrate at controlled water vapor partial pressures , 1995 .

[39]  Lawrence X. Yu,et al.  Scientific Considerations of Pharmaceutical Solid Polymorphism in Abbreviated New Drug Applications , 2003, Pharmaceutical Research.

[40]  M. Otsuka,et al.  Determination of indomethacin polymorphic contents by chemometric near-infrared spectroscopy and conventional powder X-ray diffractometry. , 2001, The Analyst.

[41]  J. A. Wachter,et al.  An Investigation of Solvent-Mediated Polymorphic Transformation of Progesterone Using in Situ Raman Spectroscopy , 2000 .

[42]  D. Giron.  Thermal Analysis, Microcalorimetry and Combined Techniques for the Study of Pharmaceuticals , 1999 .

[43]  M. Mutz,et al.  Evaluation of Calorimetric and Gravimetric Methods to Quantify the Amorphous Content of Desferal , 1999 .

[44]  Low-level determination of polymorph composition in physical mixtures by near-infrared reflectance spectroscopy. , 2001, Journal of pharmaceutical sciences.

[45]  J. Guillory.  GENERATION OF POLYMORPHS, HYDRATES, SOLVATES, AND AMORPHOUS SOLIDS , 1999 .

[46]  George Zhou,et al.  Process Optimization of a Complex Pharmaceutical Polymorphic System via In Situ Raman Spectroscopy , 2002 .

[47]  R. Davey,et al.  Disappearing polymorphs and the role of reaction by-products: the case of sulphathiazole , 1998 .

[48]  Lian Yu,et al.  Inferring thermodynamic stability relationship of polymorphs from melting data. , 1995, Journal of pharmaceutical sciences.

[49]  David J.W. Grant,et al.  Solid-state pharmaceutical chemistry , 1994 .

[50]  Giuseppe Filippini,et al.  Computer Prediction of Organic Crystal Structures Using Partial X-ray Diffraction Data , 1996 .

[51]  A. Beezer,et al.  A kinetic and thermodynamic study of seratrodast polymorphic transition by isothermal microcalorimetry. , 2003, International journal of pharmaceutics.

[52]  G. Stephenson,et al.  Physical characterization of polymorphic drugs: an integrated characterization strategy , 1998 .

[53]  K. Morris.  STRUCTURAL ASPECTS OF HYDRATES AND SOLVATES , 1999 .

[54]  W. Mccrone,et al.  Pharmaceutical applications of polymorphism. , 1969, Journal of pharmaceutical sciences.

[55]  Lawrence X. Yu,et al.  Regulatory considerations of pharmaceutical solid polymorphism in Abbreviated New Drug Applications (ANDAs). , 2004, Advanced drug delivery reviews.

[56]  S. Byrn.  Solid state chemistry of drugs , 1982 .

[57]  D. Giron,et al.  Study of the polymorphic behaviour of some local anesthetic drugs , 1997 .

[58]  W. Curatolo,et al.  Drug polymorphism and dosage form design: a practical perspective. , 2004, Advanced drug delivery reviews.

[59]  Rumi Faizer,et al.  Quantification of crystallinity in blends of lyophilized and crystalline MK-0591 using x-ray powder diffraction , 1995 .

[60]  P. Royall,et al.  The relevance of the amorphous state to pharmaceutical dosage forms: glassy drugs and freeze dried systems. , 1999, International journal of pharmaceutics.

[61]  Yadan W. Chen,et al.  Characterization and quantitation of aprepitant drug substance polymorphs by attenuated total reflectance fourier transform infrared spectroscopy. , 2003, Analytical chemistry.

[62]  Stephen R. Byrn,et al.  Anhydrates and Hydrates of Olanzapine: Crystallization, Solid-State Characterization, and Structural Relationships , 2003 .

[63]  T. Rades,et al.  Determination of polymorphic forms of ranitidine-HCl by DRIFTS and XRPD. , 2001, Journal of pharmaceutical and biomedical analysis.

[64]  N. Rodríguez-Hornedo,et al.  Significance of controlling crystallization mechanisms and kinetics in pharmaceutical systems. , 1999, Journal of pharmaceutical sciences.

[65]  D. Giron.  Investigations of Polymorphism and Pseudo-polymorphism in Pharmaceuticals by Combined Thermoanalytical Techniques , 2001 .

[66]  H. Brittain.  Polymorphism in Pharmaceutical Solids , 1999 .

[67]  B. Shekunov,et al.  Thermal Analysis of Trace Levels of Polymorphic Impurity in Salmeterol Xinafoate Samples , 2003, Pharmaceutical Research.

[68]  G. Verreck,et al.  Evaluation of different calorimetric methods to determine the glass transition temperature and molecular mobility below T(g) for amorphous drugs. , 2003, International journal of pharmaceutics.

[69]  K. Gordon,et al.  Quantitative analysis of polymorphic mixtures of ranitidine hydrochloride by Raman spectroscopy and principal components analysis. , 2002, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[70]  J. Williams,et al.  Handbook of Powder Technology , 1988 .

[71]  W. Addicks,et al.  Polymorphism in generic drug product development. , 2004, Advanced drug delivery reviews.

[72]  Bruno C. Hancock,et al.  What is the True Solubility Advantage for Amorphous Pharmaceuticals? , 2000, Pharmaceutical Research.

[73]  S. Byrn,et al.  Solid-state nuclear magnetic resonance spectroscopy--pharmaceutical applications. , 2003, Journal of pharmaceutical sciences.

[74]  Stacy Denton,et al.  Thermally-prepared polymorphic forms of cilostazol. , 2002, Journal of pharmaceutical sciences.

[75]  K. Kawakami,et al.  Assessment of amorphous content by microcalorimetry. , 2002, Journal of pharmaceutical sciences.

[76]  Bruno C. Hancock,et al.  Characteristics and Significance of the Amorphous State in Pharmaceutical Systems , 1997 .

[77]  D. Levorse,et al.  The effect of polymorphism and metastability on the characterization and isolation of two pharmaceutical compounds , 1993 .

[78]  D. Giron.  Impact of Solid State Reactions on Medicaments , 1988 .

[79]  D. Grant.  THEORY AND ORIGIN OF POLYMORPHISM , 1999 .

[80]  M. Angberg.  Lactose and thermal analysis with special emphasis on microcalorimetry , 1995 .

[81]  F. Puel,et al.  Applications of NIR spectroscopy to monitoring and analyzing the solid state during industrial crystallization processes. , 2004, International journal of pharmaceutics.

[82]  S. Price.  The computational prediction of pharmaceutical crystal structures and polymorphism. , 2004, Advanced drug delivery reviews.

[83]  D. Giron,et al.  Quantitation of amorphicity by microcalorimetry , 1997 .

[84]  M. Otsuka,et al.  Physicochemical Stability of Phenobarbital Polymorphs at Various Levels of Humidity and Temperature , 1993, Pharmaceutical Research.

[85]  Pablo G. Debenedetti,et al.  Engineering pharmaceutical stability with amorphous solids , 2002 .

[86]  Steven W Booth,et al.  Quantitative analysis of mannitol polymorphs. FT-Raman spectroscopy. , 2002, Journal of pharmaceutical and biomedical analysis.

[87]  Crystalline Solids , 2018, Statistical Thermodynamics.