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Bioavailability

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Abu T M Serajuddin – One of the best experts on this subject based on the ideXlab platform.

  • development of clinical dosage forms for a poorly water soluble drug i application of polyethylene glycol polysorbate 80 solid dispersion carrier system
    Journal of Pharmaceutical Sciences, 2004
    Co-Authors: Rosemarie Dannenfelser, Handan He, Yatindra Joshi, Simon David Bateman, Abu T M Serajuddin

    Abstract:

    Different formulation approaches were evaluated to ensure that the formulation of a poorly water soluble compound chosen during early development achieves optimum Bioavailability. The insoluble compound has an aqueous solubility of 0.17 µg/mL at 25 ± 1°C, a relatively high permeability (Caco2 Papp = 6.1 × 10−4 cm/min), and poor Bioavailability in dogs (dry blend formulation). Based on the prediction by GastroPlus™, the oral absorption of this compound is sensitive to its apparent solubility and particle size. The oral Bioavailability of three different formulations was compared in a dog model: a cosolvent-surfactant solution, a solid dispersion in a mixture of polyethylene glycol 3350 and polysorbate 80, and a dry blend of micronized drug with microcrystalline cellulose. In absence of a parenteral injection, the Bioavailability of the solution was considered to be 100%, and the relative oral Bioavailability of the three formulations was 100, 99.1, 9.8, respectively. Comparable Bioavailability was obtained with the solid dispersion and the cosolvent-surfactant solution, both of which showed a 10-fold higher Bioavailability than the dry blend. Thus, a 20 mg dose strength capsule containing the solid dispersion formulation was selected for clinical development. The selected solid dispersion system was physically and chemically stable for at least 16 months at 25°C/60% RH. In conclusion, the Bioavailability of a poorly water soluble drug was greatly enhanced using the solid dispersion formulation containing a water soluble polymer with a surface active agent. © 2004 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 93:1165–1175, 2004

Rosemarie Dannenfelser – One of the best experts on this subject based on the ideXlab platform.

  • development of clinical dosage forms for a poorly water soluble drug i application of polyethylene glycol polysorbate 80 solid dispersion carrier system
    Journal of Pharmaceutical Sciences, 2004
    Co-Authors: Rosemarie Dannenfelser, Handan He, Yatindra Joshi, Simon David Bateman, Abu T M Serajuddin

    Abstract:

    Different formulation approaches were evaluated to ensure that the formulation of a poorly water soluble compound chosen during early development achieves optimum Bioavailability. The insoluble compound has an aqueous solubility of 0.17 µg/mL at 25 ± 1°C, a relatively high permeability (Caco2 Papp = 6.1 × 10−4 cm/min), and poor Bioavailability in dogs (dry blend formulation). Based on the prediction by GastroPlus™, the oral absorption of this compound is sensitive to its apparent solubility and particle size. The oral Bioavailability of three different formulations was compared in a dog model: a cosolvent-surfactant solution, a solid dispersion in a mixture of polyethylene glycol 3350 and polysorbate 80, and a dry blend of micronized drug with microcrystalline cellulose. In absence of a parenteral injection, the Bioavailability of the solution was considered to be 100%, and the relative oral Bioavailability of the three formulations was 100, 99.1, 9.8, respectively. Comparable Bioavailability was obtained with the solid dispersion and the cosolvent-surfactant solution, both of which showed a 10-fold higher Bioavailability than the dry blend. Thus, a 20 mg dose strength capsule containing the solid dispersion formulation was selected for clinical development. The selected solid dispersion system was physically and chemically stable for at least 16 months at 25°C/60% RH. In conclusion, the Bioavailability of a poorly water soluble drug was greatly enhanced using the solid dispersion formulation containing a water soluble polymer with a surface active agent. © 2004 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 93:1165–1175, 2004

Kamla Pathak – One of the best experts on this subject based on the ideXlab platform.

  • recent advances in delivery systems and therapeutics of cinnarizine a poorly water soluble drug with absorption window in stomach
    Journal of drug delivery, 2014
    Co-Authors: Smita Raghuvanshi, Kamla Pathak

    Abstract:

    Low solubility causing low dissolution in gastrointestinal tract is the major problem for drugs meant for systemic action after oral administration, like cinnarizine. Pharmaceutical products of cinnarizine are commercialized globally as immediate release preparations presenting low absorption with low and erratic Bioavailability. Approaches to enhance Bioavailability are widely cited in the literature. An attempt has been made to review the Bioavailability complications and clinical therapeutics of poorly water soluble drug: cinnarizine. The interest of writing this paper is to summarize the pharmacokinetic limitations of drug with special focus on strategies to improvise Bioavailability along with effectiveness of novel dosage forms to circumvent the obstacle. The paper provides insight to the approaches to overcome low and erratic Bioavailability of cinnarizine by cyclodextrin complexes and novel dosage forms: self-nanoemulsifying systems and buoyant microparticulates. Nanoformulations need to systematically explored in future, for their new clinical role in prophylaxis of migraine attacks in children. Clinical reports have affirmed the role of cinnarizine in migraine prophylaxis. Research needs to be dedicated to develop dosage forms for efficacious Bioavailability and drug directly to brain.