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Petre Makreski - One of the best experts on this subject based on the ideXlab platform.

  • on the hydrates of Codeine Phosphate the remarkable influence of hydrogen bonding on the crystal size
    Chemical Communications, 2014
    Co-Authors: Tomce Runcevski, Gjorgji Petrusevski, Sonja Ugarkovic, Petre Makreski, Robert E Dinnebier
    Abstract:

    Codeine Phosphate forms three hydrates and two anhydrates. The sesquihydrate and hemihydrate, which differ by one water molecule, are stable at room temperature. The influence of this molecule on the internal crystal structure and how it translates into the external crystal shape are reported.

  • solvatomorphism of Codeine Phosphate sesquihydrate vibrational spectroscopy and thermoanalytical characterization
    Vibrational Spectroscopy, 2012
    Co-Authors: Gjorgji Petrusevski, Marina Kajdžanoska, Sonja Ugarkovic, Igor Micovski, Gordana Bogoevagaceva, Gligor Jovanovski, Petre Makreski
    Abstract:

    Abstract The detailed solvatomorphism study of Codeine Phosphate sesquihydrate – an important narcotic analgesic and antitusic active pharmaceutical ingredient (API) is reported. The extensive crystallization from a series of medium to high polarity solvents clearly exhibited the low affinity toward solvates building of this compound. The materials obtained after crystallization were investigated by vibrational spectroscopy (infrared and Raman) and thermoanalytical methods (DSC and TG/DTG). It was observed that after absolute ethanol, ethyl acetate, acetone and acetonitrile crystallization, direct solvent mediated phase transition of Codeine Phosphate sesquihydrate to anhydrous Codeine Phosphate was achieved. When N , N -dimethylformamide was used as crystallization medium, transformation to the hemihydrate form of Codeine Phosphate was induced. Only in the case of methanol solution, formation of mixed hydrate-methanolate solvate was observed. Compared to the commercial forms of Codeine Phosphate hydrates, according to the obtained spectroscopic and thermoanalytical data, the newly obtained compound has different molecular arrangement. Based on the data obtained from thermal analysis and water content study, tentative stoichiometry was established and the compound was labeled as Codeine Phosphate sesquihydrate methanolate. The X-ray powder diffraction (XRPD) measurements confirmed the spectroscopic and thermoanalytical findings about the existence of different crystal structures between the various obtained Codeine Phosphate solid forms.

  • solid state transformation of the pseudopolymorphic forms of Codeine Phosphate hemihydrate and Codeine Phosphate sesquihydrate monitored by vibrational spectroscopy and thermal analysis
    Journal of Molecular Structure, 2011
    Co-Authors: Gjorgji Petrusevski, Sonja Ugarkovic, Petre Makreski
    Abstract:

    Abstract The results from the first study on the pseudopolymorphism and solid-state transformations of Codeine Phosphate hemihydrate and Codeine Phosphate sesquihydrate are presented. The vibrational (infrared and Raman) spectra for both studied forms have revealed differences indicating that vibrational spectroscopy could discriminate between pseudopolymorphic forms of these compounds. Coupling the obtained spectroscopic data and the results from the thermoanalytical techniques (TGA/DSC) afforded interpretation of the undergoing solid-state transformations that occur when the compounds are being exposed at increased humidity and/or temperature. It was observed that, at room temperature, the hemihydrate and the sesquihydrate forms are the only sufficiently stable pseudopolymorphs of Codeine Phosphate explaining their intense pharmaceutical application.

Gjorgji Petrusevski - One of the best experts on this subject based on the ideXlab platform.

  • on the hydrates of Codeine Phosphate the remarkable influence of hydrogen bonding on the crystal size
    Chemical Communications, 2014
    Co-Authors: Tomce Runcevski, Gjorgji Petrusevski, Sonja Ugarkovic, Petre Makreski, Robert E Dinnebier
    Abstract:

    Codeine Phosphate forms three hydrates and two anhydrates. The sesquihydrate and hemihydrate, which differ by one water molecule, are stable at room temperature. The influence of this molecule on the internal crystal structure and how it translates into the external crystal shape are reported.

  • solvatomorphism of Codeine Phosphate sesquihydrate vibrational spectroscopy and thermoanalytical characterization
    Vibrational Spectroscopy, 2012
    Co-Authors: Gjorgji Petrusevski, Marina Kajdžanoska, Sonja Ugarkovic, Igor Micovski, Gordana Bogoevagaceva, Gligor Jovanovski, Petre Makreski
    Abstract:

    Abstract The detailed solvatomorphism study of Codeine Phosphate sesquihydrate – an important narcotic analgesic and antitusic active pharmaceutical ingredient (API) is reported. The extensive crystallization from a series of medium to high polarity solvents clearly exhibited the low affinity toward solvates building of this compound. The materials obtained after crystallization were investigated by vibrational spectroscopy (infrared and Raman) and thermoanalytical methods (DSC and TG/DTG). It was observed that after absolute ethanol, ethyl acetate, acetone and acetonitrile crystallization, direct solvent mediated phase transition of Codeine Phosphate sesquihydrate to anhydrous Codeine Phosphate was achieved. When N , N -dimethylformamide was used as crystallization medium, transformation to the hemihydrate form of Codeine Phosphate was induced. Only in the case of methanol solution, formation of mixed hydrate-methanolate solvate was observed. Compared to the commercial forms of Codeine Phosphate hydrates, according to the obtained spectroscopic and thermoanalytical data, the newly obtained compound has different molecular arrangement. Based on the data obtained from thermal analysis and water content study, tentative stoichiometry was established and the compound was labeled as Codeine Phosphate sesquihydrate methanolate. The X-ray powder diffraction (XRPD) measurements confirmed the spectroscopic and thermoanalytical findings about the existence of different crystal structures between the various obtained Codeine Phosphate solid forms.

  • solid state transformation of the pseudopolymorphic forms of Codeine Phosphate hemihydrate and Codeine Phosphate sesquihydrate monitored by vibrational spectroscopy and thermal analysis
    Journal of Molecular Structure, 2011
    Co-Authors: Gjorgji Petrusevski, Sonja Ugarkovic, Petre Makreski
    Abstract:

    Abstract The results from the first study on the pseudopolymorphism and solid-state transformations of Codeine Phosphate hemihydrate and Codeine Phosphate sesquihydrate are presented. The vibrational (infrared and Raman) spectra for both studied forms have revealed differences indicating that vibrational spectroscopy could discriminate between pseudopolymorphic forms of these compounds. Coupling the obtained spectroscopic data and the results from the thermoanalytical techniques (TGA/DSC) afforded interpretation of the undergoing solid-state transformations that occur when the compounds are being exposed at increased humidity and/or temperature. It was observed that, at room temperature, the hemihydrate and the sesquihydrate forms are the only sufficiently stable pseudopolymorphs of Codeine Phosphate explaining their intense pharmaceutical application.

Sonja Ugarkovic - One of the best experts on this subject based on the ideXlab platform.

  • on the hydrates of Codeine Phosphate the remarkable influence of hydrogen bonding on the crystal size
    Chemical Communications, 2014
    Co-Authors: Tomce Runcevski, Gjorgji Petrusevski, Sonja Ugarkovic, Petre Makreski, Robert E Dinnebier
    Abstract:

    Codeine Phosphate forms three hydrates and two anhydrates. The sesquihydrate and hemihydrate, which differ by one water molecule, are stable at room temperature. The influence of this molecule on the internal crystal structure and how it translates into the external crystal shape are reported.

  • solvatomorphism of Codeine Phosphate sesquihydrate vibrational spectroscopy and thermoanalytical characterization
    Vibrational Spectroscopy, 2012
    Co-Authors: Gjorgji Petrusevski, Marina Kajdžanoska, Sonja Ugarkovic, Igor Micovski, Gordana Bogoevagaceva, Gligor Jovanovski, Petre Makreski
    Abstract:

    Abstract The detailed solvatomorphism study of Codeine Phosphate sesquihydrate – an important narcotic analgesic and antitusic active pharmaceutical ingredient (API) is reported. The extensive crystallization from a series of medium to high polarity solvents clearly exhibited the low affinity toward solvates building of this compound. The materials obtained after crystallization were investigated by vibrational spectroscopy (infrared and Raman) and thermoanalytical methods (DSC and TG/DTG). It was observed that after absolute ethanol, ethyl acetate, acetone and acetonitrile crystallization, direct solvent mediated phase transition of Codeine Phosphate sesquihydrate to anhydrous Codeine Phosphate was achieved. When N , N -dimethylformamide was used as crystallization medium, transformation to the hemihydrate form of Codeine Phosphate was induced. Only in the case of methanol solution, formation of mixed hydrate-methanolate solvate was observed. Compared to the commercial forms of Codeine Phosphate hydrates, according to the obtained spectroscopic and thermoanalytical data, the newly obtained compound has different molecular arrangement. Based on the data obtained from thermal analysis and water content study, tentative stoichiometry was established and the compound was labeled as Codeine Phosphate sesquihydrate methanolate. The X-ray powder diffraction (XRPD) measurements confirmed the spectroscopic and thermoanalytical findings about the existence of different crystal structures between the various obtained Codeine Phosphate solid forms.

  • solid state transformation of the pseudopolymorphic forms of Codeine Phosphate hemihydrate and Codeine Phosphate sesquihydrate monitored by vibrational spectroscopy and thermal analysis
    Journal of Molecular Structure, 2011
    Co-Authors: Gjorgji Petrusevski, Sonja Ugarkovic, Petre Makreski
    Abstract:

    Abstract The results from the first study on the pseudopolymorphism and solid-state transformations of Codeine Phosphate hemihydrate and Codeine Phosphate sesquihydrate are presented. The vibrational (infrared and Raman) spectra for both studied forms have revealed differences indicating that vibrational spectroscopy could discriminate between pseudopolymorphic forms of these compounds. Coupling the obtained spectroscopic data and the results from the thermoanalytical techniques (TGA/DSC) afforded interpretation of the undergoing solid-state transformations that occur when the compounds are being exposed at increased humidity and/or temperature. It was observed that, at room temperature, the hemihydrate and the sesquihydrate forms are the only sufficiently stable pseudopolymorphs of Codeine Phosphate explaining their intense pharmaceutical application.

James E Polli - One of the best experts on this subject based on the ideXlab platform.

  • biowaiver monographs for immediate release solid oral dosage forms Codeine Phosphate
    Journal of Pharmaceutical Sciences, 2014
    Co-Authors: Arik Dahan, Omri Wolk, Moran Zur, Gordon L Amidon, Bertil Abrahamsson, Rodrigo Cristofoletti, D W Groot, Sabine Kopp, Peter Langguth, James E Polli
    Abstract:

    The present monograph reviews data relevant to applying the biowaiver procedure for the approval of immediate-release multisource solid dosage forms containing Codeine Phosphate. Both biopharmaceutical and clinical data of Codeine were assessed. Solubility studies revealed that Codeine meets the "highly soluble" criteria according to World Health Organization (WHO), the European Medicines Agency (EMA), and the United States Food and Drug Administration (US FDA). Codeine's fraction of dose absorbed in humans was reported to be high (>90%) based on cumulative urinary excretion of drug and drug-related material following oral administration. The permeability of Codeine was also assessed to be high in both Caco-2 monolayers and rat intestinal perfusion studies. The main risks associated with Codeine, that is, toxicity (attributed to CYP2D6 polymorphism) and its abuse potential, are present irrespective of the dosage form, and do not need to be taken into account for bioequivalence (BE) considerations. Taken together, Codeine is a class 1 drug with manageable risk and is a good candidate for waiver of in vivo BE studies.

  • biowaiver monographs for immediate release solid oral dosage forms Codeine Phosphate
    Journal of Pharmaceutical Sciences, 2014
    Co-Authors: Arik Dahan, Omri Wolk, Gordon L Amidon, Bertil Abrahamsson, Rodrigo Cristofoletti, D W Groot, Sabine Kopp, Peter Langguth, James E Polli, Vinod P Shah
    Abstract:

    ABSTRACT The present monograph reviews data relevant to applying the biowaiver procedure for the approval of immediate-release multisource solid dosage forms containing Codeine Phosphate. Both biopharmaceutical and clinical data of Codeine were assessed. Solubility studies revealed that Codeine meets the "highly soluble" criteria according to World Health Organization (WHO), the European Medicines Agency (EMA), and the United States Food and Drug Administration (US FDA). Codeine's fraction of dose absorbed in humans was reported to be high (>90%) based on cumulative urinary excretion of drug and drug-related material following oral administration. The permeability of Codeine was also assessed to be high in both Caco-2 monolayers and rat intestinal perfusion studies. The main risks associated with Codeine, that is, toxicity (attributed to CYP2D6 polymorphism) and its abuse potential, are present irrespective of the dosage form, and do not need to be taken into account for bioequivalence (BE) considerations. Taken together, Codeine is a class 1 drug with manageable risk and is a good candidate for waiver of in vivo BE studies. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:1592–1600, 2014

Arik Dahan - One of the best experts on this subject based on the ideXlab platform.

  • biowaiver monographs for immediate release solid oral dosage forms Codeine Phosphate
    Journal of Pharmaceutical Sciences, 2014
    Co-Authors: Arik Dahan, Omri Wolk, Moran Zur, Gordon L Amidon, Bertil Abrahamsson, Rodrigo Cristofoletti, D W Groot, Sabine Kopp, Peter Langguth, James E Polli
    Abstract:

    The present monograph reviews data relevant to applying the biowaiver procedure for the approval of immediate-release multisource solid dosage forms containing Codeine Phosphate. Both biopharmaceutical and clinical data of Codeine were assessed. Solubility studies revealed that Codeine meets the "highly soluble" criteria according to World Health Organization (WHO), the European Medicines Agency (EMA), and the United States Food and Drug Administration (US FDA). Codeine's fraction of dose absorbed in humans was reported to be high (>90%) based on cumulative urinary excretion of drug and drug-related material following oral administration. The permeability of Codeine was also assessed to be high in both Caco-2 monolayers and rat intestinal perfusion studies. The main risks associated with Codeine, that is, toxicity (attributed to CYP2D6 polymorphism) and its abuse potential, are present irrespective of the dosage form, and do not need to be taken into account for bioequivalence (BE) considerations. Taken together, Codeine is a class 1 drug with manageable risk and is a good candidate for waiver of in vivo BE studies.

  • biowaiver monographs for immediate release solid oral dosage forms Codeine Phosphate
    Journal of Pharmaceutical Sciences, 2014
    Co-Authors: Arik Dahan, Omri Wolk, Gordon L Amidon, Bertil Abrahamsson, Rodrigo Cristofoletti, D W Groot, Sabine Kopp, Peter Langguth, James E Polli, Vinod P Shah
    Abstract:

    ABSTRACT The present monograph reviews data relevant to applying the biowaiver procedure for the approval of immediate-release multisource solid dosage forms containing Codeine Phosphate. Both biopharmaceutical and clinical data of Codeine were assessed. Solubility studies revealed that Codeine meets the "highly soluble" criteria according to World Health Organization (WHO), the European Medicines Agency (EMA), and the United States Food and Drug Administration (US FDA). Codeine's fraction of dose absorbed in humans was reported to be high (>90%) based on cumulative urinary excretion of drug and drug-related material following oral administration. The permeability of Codeine was also assessed to be high in both Caco-2 monolayers and rat intestinal perfusion studies. The main risks associated with Codeine, that is, toxicity (attributed to CYP2D6 polymorphism) and its abuse potential, are present irrespective of the dosage form, and do not need to be taken into account for bioequivalence (BE) considerations. Taken together, Codeine is a class 1 drug with manageable risk and is a good candidate for waiver of in vivo BE studies. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:1592–1600, 2014