The Experts below are selected from a list of 1587 Experts worldwide ranked by ideXlab platform
Larry L. Augsburger - One of the best experts on this subject based on the ideXlab platform.
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The solution and solid state stability and Excipient Compatibility of parthenolide in feverfew.
Aaps Pharmscitech, 2007Co-Authors: Ping Jin, Shadi Madieh, Larry L. AugsburgerAbstract:The objectives of this research were to evaluate the stability of parthenolide in feverfew solution state and powdered feverfew (solid state), and explore the Compatibility between commonly used Excipients and parthenolide in feverfew. Feverfew extract solution was diluted with different pH buffers to study the solution stability of parthenolide in feverfew. Powdered feverfew extract was stored under 40°C/0%∼75% relative humidities (RH) or 31% RH/5∼50°C to study the influence of temperature and relative humidity on the stability of parthenolide in feverfew solid state. Binary mixtures of feverfew powered extract and different Excipients were stored at 50°C/ 75% RH for Excipient Compatibility evaluation. The degradation of parthenolide in feverfew solution appears to fit a typical first-order reaction. Parthenolide is comparatively stable when the environmental pH is in the range of 5 to 7, becoming unstable when pH is less than 3 or more than 7. Parthenolide degradation in feverfew in the solid state does not fit any obvious reaction model. Moisture content and temperature both play important roles affecting the degradation rate. A fter 6 months of storage, parthenolide in feverfew remains constant at 5°C/31% RH. However, ∼40% parthenolide in feverfew can be degraded if stored at 50°C/31% RH. When the moisture changed from 0% to 75% RH, the degradation of parthenolide in feverfew increased from 18% to 32% after 6-month storage under 40°C. Parthenolide in feverfew exhibits good Compatibility with commonly used Excipients under stressed conditions in a 3-week screening study.
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Excipient Compatibility study of hypericum perforatum extract st john s wort using similarity metrics to track phytochemical profile changes
International Journal of Pharmaceutics, 2002Co-Authors: Susan Kopelman, Larry L. AugsburgerAbstract:Abstract The formulation of botanical dietary supplements is challenging due to their complex activity–composition relationship, as well as physical and chemical stability issues. As Excipient Compatibility testing is a major component of sound formulation development, the objectives of this work were: (1) explore Excipient Compatibility storage paradigms; (2) determine interactions between phytochemicals of interest in Saint John's Wort (SJW) with several Excipients; and (3) explore the application of similarity metrics to the data. Modifications to conventional isothermal stress testing paradigms included additional storage conditions of heat and moisture (5, 50 °C, 5 and 0% added water), as well as more rigorous controls. Binary blends of SJW and ten commonly used Excipients were prepared and neat SJW was used as control. After 3 weeks, the percentage remaining of each phytochemical was determined by HPLC. Several similarity metrics were applied to the data. Common storage paradigms were suitable for Excipient Compatibility testing when controls of neat material are stored under similar conditions and the percentage of phytochemicals remaining in Excipient:SJW blends and neat SJW are compared. Excipient incompatibilities were determined for SJW phytochemicals of interest. Similarity metrics applied to the phytochemical profiles conveniently summarized the data. This work allows logical decisions to be made regarding the formulation of SJW.
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Excipient Compatibility study of Hypericum perforatum extract (St. John's wort) using similarity metrics to track phytochemical profile changes.
International journal of pharmaceutics, 2002Co-Authors: Susan Kopelman, Larry L. AugsburgerAbstract:The formulation of botanical dietary supplements is challenging due to their complex activity-composition relationship, as well as physical and chemical stability issues. As Excipient Compatibility testing is a major component of sound formulation development, the objectives of this work were: (1) explore Excipient Compatibility storage paradigms; (2) determine interactions between phytochemicals of interest in Saint John's Wort (SJW) with several Excipients; and (3) explore the application of similarity metrics to the data. Modifications to conventional isothermal stress testing paradigms included additional storage conditions of heat and moisture (5, 50 degrees C, 5 and 0% added water), as well as more rigorous controls. Binary blends of SJW and ten commonly used Excipients were prepared and neat SJW was used as control. After 3 weeks, the percentage remaining of each phytochemical was determined by HPLC. Several similarity metrics were applied to the data. Common storage paradigms were suitable for Excipient Compatibility testing when controls of neat material are stored under similar conditions and the percentage of phytochemicals remaining in Excipient:SJW blends and neat SJW are compared. Excipient incompatibilities were determined for SJW phytochemicals of interest. Similarity metrics applied to the phytochemical profiles conveniently summarized the data. This work allows logical decisions to be made regarding the formulation of SJW.
Sanjay Garg - One of the best experts on this subject based on the ideXlab platform.
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Development of Novel Sustained Release Bioadhesive Vaginal Tablets of Povidone Iodine
Drug Development and Industrial Pharmacy, 2008Co-Authors: Sanjay Garg, Lavit Jambu, Kavita VermaniAbstract:Iodine has long been used as an antiseptic for the prevention and treatment of vaginal infections. The present study was aimed at the development of rapidly disintegrating, bioadhesive and sustained release vaginal tablets of an iodophore, polyvinylpyrrolidone (povidone iodine), their evaluation and comparison with the marketed formulations. The formulation development included drug-Excipient Compatibility studies, optimization of performance parameters like disintegration time, bioadhesion and drug release profile and comparison of physical properties and performance parameters with the marketed formulation. The developed formulation provided a sustained release of polymer complexed iodine (up to 8 hrs), rapid disintegration (< 1 min.), desired bioadhesive properties and retention for a prolonged time.
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selection of Excipients for extended release formulations of glipizide through drug Excipient Compatibility testing
Journal of Pharmaceutical and Biomedical Analysis, 2005Co-Authors: Rajan K Verma, Sanjay GargAbstract:Abstract For the development of extended release formulations of glipizide, techniques of thermal and isothermal stress testing (IST) were used to assess the Compatibility of glipizide with selected Excipients. Initially, differential scanning calorimeter (DSC) was used to evaluate the Compatibility. IR spectrum of drug–Excipient mixture was also compared with that of pure drug and Excipient. Compatibility of Excipients defined in the prototype formula was tested using IST. Based on the DSC results alone, magnesium stearate, meglumine, TRIS buffer, and lactose, were found to exhibit interaction with glipizide. Stressed binary mixtures (stored at 50 °C for 3 weeks) of glipizide and meglumine showed yellow coloration indicating potential inCompatibility. Based on the results of DSC, IR, and/or HPLC, Excipients defined in the prototype formula were found to be compatible with glipizide. The optimized formulation developed using the compatible Excipients were found to be stable after 3 months of accelerated stability studies (40 °C and 75% RH). Overall, Compatibility of Excipients with glipizide was successfully evaluated using the combination of thermal and IST methods and the formulations developed using the compatible Excipients was found to be stable.
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Selection of Excipients for extended release formulations of glipizide through drug–Excipient Compatibility testing
Journal of Pharmaceutical and Biomedical Analysis, 2005Co-Authors: Rajan K Verma, Sanjay GargAbstract:Abstract For the development of extended release formulations of glipizide, techniques of thermal and isothermal stress testing (IST) were used to assess the Compatibility of glipizide with selected Excipients. Initially, differential scanning calorimeter (DSC) was used to evaluate the Compatibility. IR spectrum of drug–Excipient mixture was also compared with that of pure drug and Excipient. Compatibility of Excipients defined in the prototype formula was tested using IST. Based on the DSC results alone, magnesium stearate, meglumine, TRIS buffer, and lactose, were found to exhibit interaction with glipizide. Stressed binary mixtures (stored at 50 °C for 3 weeks) of glipizide and meglumine showed yellow coloration indicating potential inCompatibility. Based on the results of DSC, IR, and/or HPLC, Excipients defined in the prototype formula were found to be compatible with glipizide. The optimized formulation developed using the compatible Excipients were found to be stable after 3 months of accelerated stability studies (40 °C and 75% RH). Overall, Compatibility of Excipients with glipizide was successfully evaluated using the combination of thermal and IST methods and the formulations developed using the compatible Excipients was found to be stable.
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A validated high performance liquid chromatographic method for analysis of nicotine in pure form and from formulations
Journal of Pharmaceutical and Biomedical Analysis, 2003Co-Authors: Kaustubh Tambwekar, Ritesh B Kakariya, Sanjay GargAbstract:Abstract A reverse phase HPLC method using C 18 column has been developed for the quantitative estimation of nicotine in the bulk material and formulations (extended release and immediate release dosage forms). The method is specific to nicotine (RT ∼4.64 min, asymmetry ∼1.75), and can resolve analyte peak from Excipient interferences. It is linear (coefficient of variation∼0.9993), accurate (average recovery ∼100%), and passed all the system suitability requirements. Applicability of the method was evaluated in analysis of drug-Excipient Compatibility samples, commercial dosage form (such as nicotine gum) and two novel in-house formulations.
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A validated high performance liquid chromatographic method for analysis of isosorbide mononitrate in bulk material and extended release formulations.
Journal of Pharmaceutical and Biomedical Analysis, 2002Co-Authors: Rajan K Verma, Sanjay GargAbstract:Abstract A reversed phase HPLC method using C 18 column was developed for the quantitative determination of isosorbide mononitrate (IMN) in the bulk material and extended release dosage forms. The method was specific to IMN and able to resolve the drug peak from the pharmacopoeial impurities and formulation Excipients. The method was accurate, precise, and linear within the desired range. In addition to analysis of assay and dissolution samples, the method was successfully used for analysis of drug–Excipient Compatibility samples of IMN used for development of extended release formulations in our laboratory and their subsequent stability studies. The method was also used for analysis of IMN in commercially available raw material.
Susan Kopelman - One of the best experts on this subject based on the ideXlab platform.
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Excipient Compatibility study of hypericum perforatum extract st john s wort using similarity metrics to track phytochemical profile changes
International Journal of Pharmaceutics, 2002Co-Authors: Susan Kopelman, Larry L. AugsburgerAbstract:Abstract The formulation of botanical dietary supplements is challenging due to their complex activity–composition relationship, as well as physical and chemical stability issues. As Excipient Compatibility testing is a major component of sound formulation development, the objectives of this work were: (1) explore Excipient Compatibility storage paradigms; (2) determine interactions between phytochemicals of interest in Saint John's Wort (SJW) with several Excipients; and (3) explore the application of similarity metrics to the data. Modifications to conventional isothermal stress testing paradigms included additional storage conditions of heat and moisture (5, 50 °C, 5 and 0% added water), as well as more rigorous controls. Binary blends of SJW and ten commonly used Excipients were prepared and neat SJW was used as control. After 3 weeks, the percentage remaining of each phytochemical was determined by HPLC. Several similarity metrics were applied to the data. Common storage paradigms were suitable for Excipient Compatibility testing when controls of neat material are stored under similar conditions and the percentage of phytochemicals remaining in Excipient:SJW blends and neat SJW are compared. Excipient incompatibilities were determined for SJW phytochemicals of interest. Similarity metrics applied to the phytochemical profiles conveniently summarized the data. This work allows logical decisions to be made regarding the formulation of SJW.
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Excipient Compatibility study of Hypericum perforatum extract (St. John's wort) using similarity metrics to track phytochemical profile changes.
International journal of pharmaceutics, 2002Co-Authors: Susan Kopelman, Larry L. AugsburgerAbstract:The formulation of botanical dietary supplements is challenging due to their complex activity-composition relationship, as well as physical and chemical stability issues. As Excipient Compatibility testing is a major component of sound formulation development, the objectives of this work were: (1) explore Excipient Compatibility storage paradigms; (2) determine interactions between phytochemicals of interest in Saint John's Wort (SJW) with several Excipients; and (3) explore the application of similarity metrics to the data. Modifications to conventional isothermal stress testing paradigms included additional storage conditions of heat and moisture (5, 50 degrees C, 5 and 0% added water), as well as more rigorous controls. Binary blends of SJW and ten commonly used Excipients were prepared and neat SJW was used as control. After 3 weeks, the percentage remaining of each phytochemical was determined by HPLC. Several similarity metrics were applied to the data. Common storage paradigms were suitable for Excipient Compatibility testing when controls of neat material are stored under similar conditions and the percentage of phytochemicals remaining in Excipient:SJW blends and neat SJW are compared. Excipient incompatibilities were determined for SJW phytochemicals of interest. Similarity metrics applied to the phytochemical profiles conveniently summarized the data. This work allows logical decisions to be made regarding the formulation of SJW.
Steven W. Baertschi - One of the best experts on this subject based on the ideXlab platform.
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Pharmaceutical Stress Testing: Predicting Drug Degradation - Pharmaceutical Stress Testing : Predicting Drug Degradation
2005Co-Authors: Steven W. BaertschiAbstract:Stress Testing: A Predictive Tool. Stress Testing: Relation to the Development Timeline. Stress Testing: Frequently Asked Questions. Stress Testing: Analytical Considerations. Oxidative Susceptibility Testing. Photostability Stress Testing. Comparative Stress Stability Studies for Rapid Evaluation of Manufacturing Changes of Materials from Multiple Sources. The Chemistry of Drug Degradation. The Role of "Mass Balance" in Pharmaceutical Stress Testing. Physical and Chemical Stability Considerations in the Development and Stress Testing of Freeze-Dried Pharmaceuticals. Excipient Compatibility Studies
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pharmaceutical stress testing predicting drug degradation
2005Co-Authors: Steven W. BaertschiAbstract:Stress Testing: A Predictive Tool. Stress Testing: Relation to the Development Timeline. Stress Testing: Frequently Asked Questions. Stress Testing: Analytical Considerations. Oxidative Susceptibility Testing. Photostability Stress Testing. Comparative Stress Stability Studies for Rapid Evaluation of Manufacturing Changes of Materials from Multiple Sources. The Chemistry of Drug Degradation. The Role of "Mass Balance" in Pharmaceutical Stress Testing. Physical and Chemical Stability Considerations in the Development and Stress Testing of Freeze-Dried Pharmaceuticals. Excipient Compatibility Studies
Nalini R. Shastri - One of the best experts on this subject based on the ideXlab platform.
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Brexpiprazole–catechol cocrystal: structure elucidation, Excipient Compatibility and stability
CrystEngComm, 2019Co-Authors: Mohsin R. Arabiani, Bal Raju K, Surojit Bhunia, Pyla Kranthi Teja, Anurag Lodagekar, Rahul B. Chavan, Nalini R. Shastri, C. Malla Reddy, Pragna K. Shelat, Divyang J. DaveAbstract:Brexpiprazole (BREX) is a well known drug used in the treatment of atypical psychotic disorder. BREX is known to exhibit photo-instability on granulation with the most commonly used binder, polyvinylpyrrolidone (PVP), in wet granulation. The present study reports a cocrystal of BREX with catechol (CAT), its structure elucidation using single crystal X-ray diffraction and its processability. The brexpiprazole–catechol (BRC) cocrystal crystallizes in the P21/c space group. Structural analysis of BRC shows R22(8) between BREX and CAT through weak C–H⋯O and strong O–H⋯O hydrogen bond interactions. BREX is marketed in tablet dosage form. The Compatibility of the generated cocrystal in the presence of several Excipients was evaluated using differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). The cocrystal remained stable, with no signs of inCompatibility during the Excipient Compatibility study. Additionally, the cocrystal and plain BREX granulated with PVP as a binder and the chemical stability of the granules were investigated. Plain BREX showed oxidative degradation and formation of N-oxide degradation products under stability conditions within 7 days. More importantly, the BRC cocrystal displayed superior stability against stability conditions because the reactive site in the piperazine ring of the BREX moiety was blocked in the BRC cocrystal due to the hydrogen bond between the drug and co-former.
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brexpiprazole catechol cocrystal structure elucidation Excipient Compatibility and stability
CrystEngComm, 2019Co-Authors: Mohsin R. Arabiani, Bal Raju K, Surojit Bhunia, Pyla Kranthi Teja, Anurag Lodagekar, Rahul B. Chavan, Nalini R. Shastri, Pragna K. Shelat, Malla C Reddy, Divyang J. DaveAbstract:Brexpiprazole (BREX) is a well known drug used in the treatment of atypical psychotic disorder. BREX is known to exhibit photo-instability on granulation with the most commonly used binder, polyvinylpyrrolidone (PVP), in wet granulation. The present study reports a cocrystal of BREX with catechol (CAT), its structure elucidation using single crystal X-ray diffraction and its processability. The brexpiprazole–catechol (BRC) cocrystal crystallizes in the P21/c space group. Structural analysis of BRC shows R22(8) between BREX and CAT through weak C–H⋯O and strong O–H⋯O hydrogen bond interactions. BREX is marketed in tablet dosage form. The Compatibility of the generated cocrystal in the presence of several Excipients was evaluated using differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). The cocrystal remained stable, with no signs of inCompatibility during the Excipient Compatibility study. Additionally, the cocrystal and plain BREX granulated with PVP as a binder and the chemical stability of the granules were investigated. Plain BREX showed oxidative degradation and formation of N-oxide degradation products under stability conditions within 7 days. More importantly, the BRC cocrystal displayed superior stability against stability conditions because the reactive site in the piperazine ring of the BREX moiety was blocked in the BRC cocrystal due to the hydrogen bond between the drug and co-former.
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Polymorphic transformation as a result of atovaquone inCompatibility with selected Excipients
Journal of Thermal Analysis and Calorimetry, 2018Co-Authors: Rahul B. Chavan, Nalini R. ShastriAbstract:Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy, and hot-stage microscopy were employed to evaluate the drug–Excipient Compatibility of atovaquone with commonly used tablet Excipients. The DSC curves of pure drug and Excipients were compared with their physical mixtures. Microcrystalline cellulose, titanium dioxide, colloidal silica, ferric oxide, lactose monohydrate, and sodium starch glycolate were compatible, while magnesium stearate, polyethylene glycol (PEG) 8000, Poloxamer 188, and hydroxypropyl methyl cellulose (HPMC) E15 showed inCompatibility with the drug. Heat–cool–heat analysis of the physical and the ground mixture of later three Excipients showed polymorphic transformation of atovaquone form III to form I, which occurred via amorphization with HPMC E15 and through solubilization mechanism with remaining two Excipients. These outcomes were further supported by hot-stage microscopy. Results of milling experiments revealed a milling time-dependent polymorphic transformation and solubilization with HPMC E15 and PEG 8000, respectively. This study highlights the importance of Compatibility assessment for selection of Excipients in specific unit operations such as milling and grinding.
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Rufinamide: Crystal structure elucidation and solid state characterization.
Journal of Pharmaceutical and Biomedical Analysis, 2017Co-Authors: Nita Salunke, Anurag Lodagekar, Rahul B. Chavan, Rajesh Thipparaboina, Sudhir Mittapalli, Ashwini Nangia, Nalini R. ShastriAbstract:Abstract Rufinamide (R) is a triazole derivative approved for the management of partial seizures and seizures associated with Lennox-Gastaut Syndrome, in November 2007. Crystal structure, solid state characterization, drug-Excipient Compatibility and solubility play a pivotal role in formulation development. This work deals with the crystal structure elucidation of R by single crystal X-ray diffraction and solid state characterization by thermal, spectroscopic and crystallographic techniques. Drug- Excipient Compatibility was assessed by differential scanning calorimetry (DSC). New RP-HPLC method for quantification of R was developed with improved retention time. Solubility and dissolution of drug in different media was determined. Additionally, the flow behavior of the drug was evaluated by measuring Carr’s index and Hausner’s ratio, while the compressibility behavior was studied using Well’s protocol. R crystallized from dimethylformamide (R-DMF) was utilized for single crystal analysis. The drug crystallized in triclinic crystal system with P-1 space group. Asymmetric unit cell consists of two molecules of R held by intermolecular hydrogen bond (connected by N H⋯O, which forms the catemeric chain). Analytical outcomes from DSC, thermogravimetric analysis (TGA) and powder X-ray diffraction (PXRD) revealed that the drug was present in pure crystalline form and was devoid of any polymorphic or pseudopolymorphic impurities. Influence of pH on the solubility and dissolution of R-DMF was found to be insignificant. The drug exhibited poor aqueous solubility, which was improved nearly 4.6 fold with the addition of 2% sodium lauryl sulphate (SLS). The drug exhibits poor flow and elastic compression nature. Excipients such as poly ethylene glycol (PEG) 8000, SLS, lactose monohydrate, starch and Hydroxypropyl methylcellulose (HPMC) E15 were incompatible with R-DMF as identified by thermal analysis. It is envisaged that these information regarding solid state properties of R-DMF would aid in identifying a logical path for formulation development.
