Antiemetic Agent

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Mansoor Ahmad - One of the best experts on this subject based on the ideXlab platform.

  • Lipids bearing extruded-spheronized pellets for extended release of poorly soluble Antiemetic Agent—Meclizine HCl
    Lipids in Health and Disease, 2017
    Co-Authors: Faaiza Qazi, Muhammad Harris Shoaib, Rabia Ismail Yousuf, Muhammad Iqbal Nasiri, Kamran Ahmed, Mansoor Ahmad
    Abstract:

    Background Antiemetic Agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated. Methods Thirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol^®), Glyceryl palmitostearate (Precirol^®), Glyceryl behenate (Compritol^®) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5–1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found. Results Sphericity indicated by shape factor (e_R) varied with type and concentration of lipids: Geleol^® (e_R = 0.891–0.997), Precirol^® (e_R = 0.611–0.743), Compritol^® (e_R = 0.665–0.729) and Carnauba wax (e_R = 0.499-0.551). Highly spherical pellets were obtained with Geleol^® (Aspect ratio = 1.005–1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153–1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol^® and Compritol^®, (ii) Geleol^® and Carnauba wax and (iii) Geleol^®, Compritol^® and Carnauba wax. Scanning electron microscopy of Compritol^® pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol^® and Compritol^® pellets, explained by Korsmeyer-Peppas (R^2 = 0.978–0.993) indicated non-Fickian diffusion ( n  = 0.519-0.597). Combinations of (ii) Geleol^® and Carnauba wax and (iii) Geleol^®, Compritol^® and Carnauba wax pellets followed Zero-order (R^2 = 0.991–0.995). Similarity test was performed using combination of Geleol^® and Compritol^® (i) as a reference. Conclusions Matrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol^®, Compritol^® and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.

  • Lipids bearing extruded-spheronized pellets for extended release of poorly soluble Antiemetic Agent-Meclizine HCl.
    Lipids in Health and Disease, 2017
    Co-Authors: Faaiza Qazi, Muhammad Harris Shoaib, Rabia Ismail Yousuf, Muhammad Iqbal Nasiri, Kamran Ahmed, Mansoor Ahmad
    Abstract:

    Antiemetic Agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated. Thirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol®), Glyceryl palmitostearate (Precirol®), Glyceryl behenate (Compritol®) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5–1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found. Sphericity indicated by shape factor (eR) varied with type and concentration of lipids: Geleol® (eR = 0.891–0.997), Precirol® (eR = 0.611–0.743), Compritol® (eR = 0.665–0.729) and Carnauba wax (eR = 0.499-0.551). Highly spherical pellets were obtained with Geleol® (Aspect ratio = 1.005–1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153–1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol® and Compritol®, (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax. Scanning electron microscopy of Compritol® pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol® and Compritol® pellets, explained by Korsmeyer-Peppas (R2 = 0.978–0.993) indicated non-Fickian diffusion (n = 0.519-0.597). Combinations of (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax pellets followed Zero-order (R2 = 0.991–0.995). Similarity test was performed using combination of Geleol® and Compritol® (i) as a reference. Matrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol®, Compritol® and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.

Faaiza Qazi - One of the best experts on this subject based on the ideXlab platform.

  • Lipids bearing extruded-spheronized pellets for extended release of poorly soluble Antiemetic Agent—Meclizine HCl
    Lipids in Health and Disease, 2017
    Co-Authors: Faaiza Qazi, Muhammad Harris Shoaib, Rabia Ismail Yousuf, Muhammad Iqbal Nasiri, Kamran Ahmed, Mansoor Ahmad
    Abstract:

    Background Antiemetic Agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated. Methods Thirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol^®), Glyceryl palmitostearate (Precirol^®), Glyceryl behenate (Compritol^®) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5–1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found. Results Sphericity indicated by shape factor (e_R) varied with type and concentration of lipids: Geleol^® (e_R = 0.891–0.997), Precirol^® (e_R = 0.611–0.743), Compritol^® (e_R = 0.665–0.729) and Carnauba wax (e_R = 0.499-0.551). Highly spherical pellets were obtained with Geleol^® (Aspect ratio = 1.005–1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153–1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol^® and Compritol^®, (ii) Geleol^® and Carnauba wax and (iii) Geleol^®, Compritol^® and Carnauba wax. Scanning electron microscopy of Compritol^® pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol^® and Compritol^® pellets, explained by Korsmeyer-Peppas (R^2 = 0.978–0.993) indicated non-Fickian diffusion ( n  = 0.519-0.597). Combinations of (ii) Geleol^® and Carnauba wax and (iii) Geleol^®, Compritol^® and Carnauba wax pellets followed Zero-order (R^2 = 0.991–0.995). Similarity test was performed using combination of Geleol^® and Compritol^® (i) as a reference. Conclusions Matrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol^®, Compritol^® and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.

  • Lipids bearing extruded-spheronized pellets for extended release of poorly soluble Antiemetic Agent-Meclizine HCl.
    Lipids in Health and Disease, 2017
    Co-Authors: Faaiza Qazi, Muhammad Harris Shoaib, Rabia Ismail Yousuf, Muhammad Iqbal Nasiri, Kamran Ahmed, Mansoor Ahmad
    Abstract:

    Antiemetic Agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated. Thirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol®), Glyceryl palmitostearate (Precirol®), Glyceryl behenate (Compritol®) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5–1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found. Sphericity indicated by shape factor (eR) varied with type and concentration of lipids: Geleol® (eR = 0.891–0.997), Precirol® (eR = 0.611–0.743), Compritol® (eR = 0.665–0.729) and Carnauba wax (eR = 0.499-0.551). Highly spherical pellets were obtained with Geleol® (Aspect ratio = 1.005–1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153–1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol® and Compritol®, (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax. Scanning electron microscopy of Compritol® pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol® and Compritol® pellets, explained by Korsmeyer-Peppas (R2 = 0.978–0.993) indicated non-Fickian diffusion (n = 0.519-0.597). Combinations of (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax pellets followed Zero-order (R2 = 0.991–0.995). Similarity test was performed using combination of Geleol® and Compritol® (i) as a reference. Matrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol®, Compritol® and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.

Hosam A Saad - One of the best experts on this subject based on the ideXlab platform.

  • chemical and physical properties of the charge transfer complexes of domperidone Antiemetic Agent with π acceptors
    Journal of Molecular Liquids, 2019
    Co-Authors: Foziah A Alsaif, Abeer A Elhabeeb, Moamen S Refat, Hala H Eldaroti, Abdel Majid A Adam, Hammad Fetooh, Hosam A Saad
    Abstract:

    Abstract Domperidone (Dom) possesses a potent Antiemetic property, it increases the movements or contractions of the stomach and bowel. The current research aimed to synthesize and study the charge transfer (CT) complexes that originated from the interaction between Dom and different types of organic π-acceptors (PA, DNP, TCNQ, DDQ, DBQ, and DCQ). The targeted CT products were synthesized in methanol media, isolated, and thoroughly characterized by elemental analyses and spectroscopies (UV–Visible, IR, Raman, and 1H NMR). The thermal decomposition data of these products (from simultaneous TG analysis) were presented and discussed as well. Furthermore, the products' structural morphology was visualized by XRD and SEM-EDX. The results showed that the products have organized and homogeneously dispersed, uniform microstructures in the nanometer range.

Cameron Crandall - One of the best experts on this subject based on the ideXlab platform.

  • ondansetron versus promethazine to treat acute undifferentiated nausea in the emergency department a randomized double blind noninferiority trial
    Academic Emergency Medicine, 2008
    Co-Authors: Darren Braude, Cameron Crandall
    Abstract:

    Objectives: The authors sought to compare ondansetron and promethazine among emergency department (ED) patients with undifferentiated nausea. The hypothesis was that ondansetron was not inferior to promethazine and that rates of adverse effects were similar. Methods: This was a randomized double-blind noninferiority clinical trial conducted in an urban academic ED. A convenience sample of nonpregnant adults with at least 40 mm of self-reported nausea measured on a 100-mm visual analog scale (VAS) were enrolled. Patients who had already received more than 1 L of intravenous fluid or an Antiemetic Agent were excluded. Subjects were block-randomized in groups of 10 to either 4 mg of ondansetron or 25 mg of promethazine delivered intravenously. The primary outcome was change in nausea over 30 minutes. The authors used a 15-mm margin of noninferiority. Secondary endpoints included changes in anxiety, sedation, and other adverse effects. Analyses included t-tests, tests for proportions, and 95% confidence intervals (CIs). Results: A total of 120 subjects completed the study, 60 in each arm. Baseline nausea, anxiety, and sedation scores were similar. Ondansetron and promethazine reduced nausea similarly (ondansetron )34 mm, promethazine )36 mm; difference )2 mm; 95% CI = )13 to 8 mm). The reduction in anxiety was similar (ondansetron )13 mm, promethazine )14 mm; difference )1 mm; 95% CI = )10 to 10 mm). Promethazine was associated with significantly more sedation than ondansetron (ondansetron 5 mm, promethazine 19 mm; difference 14 mm; 95% CI = 5 to 24 mm). There were no cases of akathisia in the ondansetron group and 2 cases in the promethazine group. Conclusions: Promethazine and ondansetron have similar efficacy in reducing nausea among ED patients. Change in anxiety was similar, but promethazine was associated with greater sedation. ACADEMIC EMERGENCY MEDICINE 2008; 15:209‐215 a 2008 by the Society for Academic Emergency Medicine

Muhammad Harris Shoaib - One of the best experts on this subject based on the ideXlab platform.

  • Lipids bearing extruded-spheronized pellets for extended release of poorly soluble Antiemetic Agent—Meclizine HCl
    Lipids in Health and Disease, 2017
    Co-Authors: Faaiza Qazi, Muhammad Harris Shoaib, Rabia Ismail Yousuf, Muhammad Iqbal Nasiri, Kamran Ahmed, Mansoor Ahmad
    Abstract:

    Background Antiemetic Agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated. Methods Thirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol^®), Glyceryl palmitostearate (Precirol^®), Glyceryl behenate (Compritol^®) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5–1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found. Results Sphericity indicated by shape factor (e_R) varied with type and concentration of lipids: Geleol^® (e_R = 0.891–0.997), Precirol^® (e_R = 0.611–0.743), Compritol^® (e_R = 0.665–0.729) and Carnauba wax (e_R = 0.499-0.551). Highly spherical pellets were obtained with Geleol^® (Aspect ratio = 1.005–1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153–1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol^® and Compritol^®, (ii) Geleol^® and Carnauba wax and (iii) Geleol^®, Compritol^® and Carnauba wax. Scanning electron microscopy of Compritol^® pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol^® and Compritol^® pellets, explained by Korsmeyer-Peppas (R^2 = 0.978–0.993) indicated non-Fickian diffusion ( n  = 0.519-0.597). Combinations of (ii) Geleol^® and Carnauba wax and (iii) Geleol^®, Compritol^® and Carnauba wax pellets followed Zero-order (R^2 = 0.991–0.995). Similarity test was performed using combination of Geleol^® and Compritol^® (i) as a reference. Conclusions Matrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol^®, Compritol^® and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.

  • Lipids bearing extruded-spheronized pellets for extended release of poorly soluble Antiemetic Agent-Meclizine HCl.
    Lipids in Health and Disease, 2017
    Co-Authors: Faaiza Qazi, Muhammad Harris Shoaib, Rabia Ismail Yousuf, Muhammad Iqbal Nasiri, Kamran Ahmed, Mansoor Ahmad
    Abstract:

    Antiemetic Agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated. Thirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol®), Glyceryl palmitostearate (Precirol®), Glyceryl behenate (Compritol®) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5–1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found. Sphericity indicated by shape factor (eR) varied with type and concentration of lipids: Geleol® (eR = 0.891–0.997), Precirol® (eR = 0.611–0.743), Compritol® (eR = 0.665–0.729) and Carnauba wax (eR = 0.499-0.551). Highly spherical pellets were obtained with Geleol® (Aspect ratio = 1.005–1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153–1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol® and Compritol®, (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax. Scanning electron microscopy of Compritol® pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol® and Compritol® pellets, explained by Korsmeyer-Peppas (R2 = 0.978–0.993) indicated non-Fickian diffusion (n = 0.519-0.597). Combinations of (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax pellets followed Zero-order (R2 = 0.991–0.995). Similarity test was performed using combination of Geleol® and Compritol® (i) as a reference. Matrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol®, Compritol® and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.