Review of Limited Systemic Absorption of Orlistat, a Lipase Inhibitor, in Healthy Human Volunteers

@article{Zhi1995ReviewOL,
  title={Review of Limited Systemic Absorption of Orlistat, a Lipase Inhibitor, in Healthy Human Volunteers},
  author={Jianguo Zhi and Angela T. Melia and Herwig Eggers and Regine Joly and Indravadan H. Patel},
  journal={The Journal of Clinical Pharmacology},
  year={1995},
  volume={35}
}
  • J. Zhi, A. Melia, +2 authors I. Patel
  • Published 1 November 1995
  • Chemistry, Medicine
  • The Journal of Clinical Pharmacology
Orlistat, a lipase inhibitor, acts locally in the gastrointestinal tract. Systemic absorption is not required for its efficacy, but knowledge of the extent of its systemic absorption is important for its safe use in obese patients, the intended target population. Pharmacokinetic screening was carried out by monitoring plasma concentrations of unchanged orlistat in 25 phase 1 studies (including two mass balance studies) in normal and obese healthy volunteers. The results of these studies… Expand
Long‐Term Systemic Exposure of Orlistat, a Lipase Inhibitor, and Its Metabolites in Obese Patients
TLDR
Results of these studies involving the monitoring of plasma samples indicate that detection of intact orlistat in plasma was sporadic, and measurable concentrations were low (<10 ng/mL or 0.02 μM), which is consistent with minimal absorption. Expand
The pharmacodynamic equivalence of Orlistat 60 mg capsule. An open label, balanced, randomized, multiple-dose, cross-over pharmacodynamic end-point bioequivalence study in healthy, adult, human Asian Indian subjects under fed conditions
TLDR
Results from this study suggest that the test formulation of Orlistat capsule is bioequivalent to the reference marketed Alli™ when administered to healthy volunteers as a multiple dose under fed conditions. Expand
Lack of Effect of Orlistat on the Bioavailability of a Single Dose of Nifedipine Extended‐Release Tablets (Procardia XL) in Healthy Volunteers
TLDR
The 90% confidence intervals for the ratio of geometric least‐square means for maximum concentration (Cmax) and area under the concentration‐time curve (AUCo‐t) indicate that the bioavailability of nifedipine was not altered by treatment with orlistat. Expand
Orlistat, a New Lipase Inhibitor for the Management of Obesity
TLDR
The potential for severe gastrointestinal discomfort and the modest degree of weight loss may limit the agent's clinical utility, while its long‐term safety and effectiveness for weight maintenance, cost‐effectiveness of treatment, and overall reduction in obesity‐related morbidity and mortality remain to be determined. Expand
Inhibition of gastrointestinal lipolysis by Orlistat during digestion of test meals in healthy volunteers.
TLDR
The inhibition of digestive lipases by the antiobesity drug Orlistat along with lipolysis levels and fecal fat excretion were measured in healthy humans and found to be a powerful gastric lipase inhibitor, greatly reducing gastriclipolysis of solid and liquid meals. Expand
Intestinal delivery in a long-chain fatty acid formulation enables lymphatic transport and systemic exposure of orlistat.
TLDR
Administration of orlistat in a long-chain fatty acid formulation promotes lymph and systemic uptake which may enable treatment of diseases associated with elevated systemic PL activity. Expand
Metabolic Profiles of Minimally Absorbed Orlistat in Obese/Overweight Volunteers
TLDR
The disposition of orlistat appears to be similar between normal and obese/overweight subjects. Expand
The Effect of Orlistat, an Inhibitor of Dietary Fat Absorption, on the Pharmacokinetics of β‐Carotene in Healthy Volunteers
TLDR
It was concluded that two thirds of a supplemental dose ofβ‐carotene will be absorbed during orlistat treatment; this may be sufficient to achieve physiologic levels of β‐ carotene with an appropriate dose of β-carotenes, should supplementation be needed in obese patients who have developed β‐Carotene deficiency during therapy with or listat. Expand
Orlistat: a review of its use in the management of obesity.
TLDR
Orlistat in conjunction with a hypocaloric diet has been shown to induce clinically significant weight loss in keeping with current guidelines for the management of obesity and its acceptable tolerability profile and lack of systemic adverse events make it an attractive option in the treatment of obesity. Expand
Orlistat — A Novel Weight Loss Therapy
TLDR
Preliminary data from clinical trials suggest that orlistat may be beneficial in patients with comorbid conditions related to obesity, such as diabetes and hyperlipidemia, however, further studies during postmarketing surveillance are needed to fully establish orlistsat's long-term benefits and safety. Expand
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