The Experts below are selected from a list of 321 Experts worldwide ranked by ideXlab platform

Amnon Hoffman - One of the best experts on this subject based on the ideXlab platform.

  • A novel mechanism for Oral Controlled Release of drugs by continuous degradation of a phospholipid prodrug along the intestine: In-vivo and in-vitro evaluation of an indomethacin-lecithin conjugate
    Journal of Controlled Release, 2007
    Co-Authors: Arik Dahan, Anat Elmann, Revital Duvdevani, Eran Dvir, Amnon Hoffman
    Abstract:

    Purpose: To investigate a novel mechanism for Oral Controlled Release of drugs involving a continuous degradation of a phospholipid prodrug along the intestine. An indomethacin-lecithin conjugate with the drug attached to the sn-2 position of the phospholipid through a 5-carbon linker (DP-155) was used as a model molecule. Methods: The pharmacokinetics of DP-155 and free indomethacin liberated from the prodrug following intravenous, Oral or intra-colon administration was investigated in rats, and evaluated in comparison to free indomethacin administration. Degradation by phospholipase A2 (PLA2) enzymes was assessed in-vitro. The impact of the linker length was evaluated in comparison to an indomethacin-phospholipid conjugate with a shorter linker (2-carbons). Results: Following Oral or intra-colon DP-155 administration, free indomethacin was liberated along the intestine and absorbed into the systemic circulation, resulting in a Controlled Release profile of indomethacin in the plasma. The shorter linker caused a 20-fold decrease in the subsequent indomethacin absorption. DP-155 in-vitro degradation by PLA2 was over 60%, while shorter linkers were profoundly less degradable. Conclusions: DP-155 caused a continuous input of free indomethacin into the plasma following degradation by PLA2 in the gut lumen. Since the rate of drug Release is not formulation dependent, the prodrug can be compounded even in a liquid dosage form. The phospholipid-drug conjugate is thus a potential novel mechanism for Oral Controlled Release of drugs. ?? 2007 Elsevier B.V. All rights reserved.

Kofi Asareaddo - One of the best experts on this subject based on the ideXlab platform.

  • the role of Oral Controlled Release matrix tablets in drug delivery systems
    BioImpacts : BI, 2012
    Co-Authors: Ali Nokhodchi, Shaista Raja, Pryia Patel, Kofi Asareaddo
    Abstract:

    Formulations that are able to control the Release of drug have become an integral part of the pharmaceutical industry. In particular Oral drug delivery has been the focus of pharmaceutical research for many years. This type of drug delivery has been at the centre of research due to its many benefits over conventional dosage. The focus of this review is on matrix tablets due to their widely use and simplicity of the formulation. This includes the discussion of various types of matrix tablets and factors affecting the drug Release from these formulations. The mechanism of drug Release from HPMC matrices is also discussed.

Bhaskar Mazumder - One of the best experts on this subject based on the ideXlab platform.

  • albizia procera gum as an excipient for Oral Controlled Release matrix tablet
    Carbohydrate Polymers, 2012
    Co-Authors: Lalduhsanga Pachuau, Bhaskar Mazumder
    Abstract:

    Abstract The purpose of this research was to develop and evaluate Controlled Release matrix tablets of paracetamol based on natural gum exudates of Albizia procera. Procera gum was characterized of its properties like compressibility index, angle of repose, viscosity and moisture content. The interaction between the gum and paracetamol was also studied through differential scanning calorimetry (DSC) and FTIR spectroscopy. Matrix tablets were then prepared by wet granulation method with different concentrations of procera gum and hydroxypropyl methylcellulose (HPMC) and evaluated for their physical properties like weight variation, hardness, friability and content uniformity. Dissolution study was conducted to characterize Release mechanism from the matrix system and data were fitted to various kinetic models. The mechanism of drug Release from both types of matrix tablets was found to be anomalous type. Results from various evaluations suggested that A. procera gum could be used as drug Release retardant in Controlled Release matrix systems.

Paul Goldenheim - One of the best experts on this subject based on the ideXlab platform.

  • A Multi-Investigator Clinical Evaluation of Oral Controlled-Release Morphine (MS Contin® Tablets) Administered to Cancer Patients
    Hospice Journal The, 2017
    Co-Authors: Harry Lazarus, Ronald D. Fitzmartin, Paul Goldenheim
    Abstract:

    The analgesic efficacy of Oral Controlled-Release morphine (MS Contin Tablets; MSC) and its influence on quality of life, including parameters of nighttime sleep and daytime functioning, were evaluated in this open-label, sequential study in cancer patients. Seventy patients completed this multi-investigator study; each patient was assigned to one of two dosing protocols, as determined by their previous analgesic regimen. Evaluations were made at baseline (when patients were receiving their previous analgesic regimen) and again on the second visit, after a dosage level of MSC sufficient to control pain was reached for a minimum of two weeks. There were no significant (p greater than 0.17) differences in incidence of nausea, vomiting, or drowsiness experienced by patients during treatment with MSC and during previous analgesic regimens. A senna and docusate sodium preparation (Senokot-S Tablets; SKS) was used to alleviate opioid-induced constipation; consequently there was a significantly lower (p = 0.02) incidence of constipation during treatment with MSC. A moderate relationship between opioid dose and laxative consumption was observed. Pain intensity was significantly (p = 0.0001) decreased, and quality of nighttime sleep and daytime functioning were significantly (p = 0.0001) increased compared with baseline values. Patients' overall quality of life improved significantly (p = 0.0001) during treatment with MSC when compared to their previous analgesic regimens. In conclusion, the therapeutic merits afforded by MSC coupled with proper dose titration were perceived by the patients to be superior to those provided by their previous medications. The benefits of less frequent dosing combined with potent analgesic effect plus the aggressive use of laxatives resulted in a global improvement in quality of life for the patients involved in this study.

  • A bioequivalence study of Oral Controlled-Release morphine using naltrexone blockade.
    The Journal of Clinical Pharmacology, 1995
    Co-Authors: Robert F. Kaiko, R. Grandy, Robert F. Reder, Paul Goldenheim, Richard Sackler
    Abstract:

    Twenty-three normal volunteers who received morphine sulphate (MS Contin) with naltrexone completed this randomized, analytically blinded, two-way crossover comparison of the bioavailability of one 200-mg Oral Controlled-Release morphine sulfate tablet with two 100-mg MSC tablets. Morphine effects were blocked by three 100-mg doses of naltrexone. The first dose of naltrexone was given 24 hours before MSC dosing, followed by a second dose at the time of MSC dosing and a third dose 24 hours after MSC administration. Compared with two 100-mg MSC tablets, the 200-mg tablet was 96% bioavailable (90% confidence interval, 88.14-105.74%). The 90% confidence intervals for mean Cmax and AUC0-24 for one 200-mg MSC tablet were within +/- 20% of the Cmax and AUC0-24 of two 100-mg tablets, indicating the two dosage forms are bioequivalent. Single 200-mg doses of MSC given with the naltrexone blockade were generally well tolerated, and adverse effects were similar to those reported for naltrexone alone and for lower doses of morphine without naltrexone. Naltrexone proved safe and effective in blocking the effects of Controlled-Release morphine, permitting bioequivalence studies of a high dose of morphine in normal volunteers.

  • Analgesic efficacy and potency of two Oral Controlled-Release morphine preparations.
    Clinical Pharmacology & Therapeutics, 1993
    Co-Authors: Saul S Bloomfield, Robert F. Kaiko, R. Grandy, Gail B Cissell, Jeanette Mitchell, Tom P Barden, Ronald D. Fitzmartin, James Komorowski, Paul Goldenheim
    Abstract:

    MS Contin tablets and Oramorph SR tablets are two forms of Oral Controlled-Release morphine sulfate available for the alleviation of pain. Our objective was to compare their analgesic effects in a relative potency assay. In this study, 151 patients undergoing caesarean section or abdominal hysterectomy and reporting moderate or severe postoperative pain received a 30 or 90 mg dose of either drug in a balanced, randomized, double-blind, parallel-group, single-dose experimental design. Patients provided self-ratings of analgesia. Relative potency for pain relief were calculated from log dose-effect curves. For total pain relief (rated by visual analog scales) over 12 hours, the log dose relative potency estimate for MS Contin tablets/Oramorph SR tablets was 1.9 (95% confidence limits, 0.89 to 11.1); for peak pain relief (visual analog scales) the relative potency estimate was 1.7 (95% confidence limits, 0.65 to 48.3). Overall, the 90 mg dose of MS Contin was more effective than 30 or 90 mg doses of Oramorph SR and the 30 mg dose of MS Contin at hours 6 to 12. Adverse experiences (mainly drowsiness) were mostly mild to moderate, with no significant differences in their overall incidence or severity between equivalent doses. MS Contin tablets provided greater peak, total, and duration of analgesia, without higher incidence of adverse experiences. Clinical Pharmacology and Therapeutics (1993) 53, 469–478; doi:10.1038/clpt.1993.53

Sanjay Garg - One of the best experts on this subject based on the ideXlab platform.

  • Minimizing bioavailability variations with Oral Controlled Release formulations
    American Journal of Drug Delivery, 2003
    Co-Authors: Aditya Mohan Kaushal, Sanjay Garg
    Abstract:

    Despite various routes of drug delivery being explored, the Oral route has continued to be the most popular route of drug administration. However, the complexities associated with the gastrointestinal tract lead to variations in the rate and extent of bioavailability of drugs administered as Oral dosage forms. This variation in the bioavailability of drugs is responsible for the majority of adverse effects, lack of efficacy, and development of tolerance, etc. This review explores the possibilities of minimizing these bioavailability variations with the use of Oral Controlled Release (CR) dosage forms. The use of CR preparations, in lieu of the immediate preparations in itself, leads to better control over plasma levels. Furthermore, the additional benefits offered by CR products, such as the reduction in first-pass metabolism, enhanced and reproducible bioavailability with gastro retentive preparations, overcoming circadian rhythm variations, and the lesser effect of fed condition on bioavailability, can be effectively utilized for bioavailability variation minimization. However, CR products cannot be use indiscriminately. The use of CR products to serve the purpose of bioavailability variation minimization should be based on due consideration to the role of metabolizing enzymes, the permeability variations, and the area available for absorption.

  • Minimizing bioavailability variations with Oral Controlled Release formulations
    American Journal of Drug Delivery, 2003
    Co-Authors: Aditya Mohan Kaushal, Sanjay Garg
    Abstract:

    Despite various routes of drug delivery being explored, the Oral route has continued to be the most popular route of drug administration. However, the complexities associated with the gastrointestinal tract lead to variations in the rate and extent of bioavailability of drugs administered as Oral dosage forms. This variation in the bioavailability of drugs is responsible for the majority of adverse effects, lack of efficacy, and development of tolerance, etc.