ArticlePharmaceutical research2008
Effect of stabilizer on the maximum degree and extent of supersaturation and oral absorption of tacrolimus made by ultra-rapid freezing.
Article in Pharmaceutical research, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 104 citations in OpenAlex.
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- Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles.Pharmaceutics · 2019Article
- Orally Disintegrating Tablets Containing Melt Extruded Amorphous Solid Dispersion of Tacrolimus for Dissolution Enhancement.Pharmaceutics · 2018Article
- Investigation of Polymer-Surfactant and Polymer-Drug-Surfactant Miscibility for Solid Dispersion.The AAPS journal · 2016Article
- Aminoclay-lipid hybrid composite as a novel drug carrier of fenofibrate for the enhancement of drug release and oral absorption.International journal of nanomedicine · 2016Article
- Preparation and in vivo evaluation of a dutasteride-loaded solid-supersaturatable self-microemulsifying drug delivery system.International journal of molecular sciences · 2015Article
- Evaluation of nanodispersion of iron oxides using various polymers.Indian journal of pharmaceutical sciences · 2014Article
- Respirable low-density microparticles formed in situ from aerosolized brittle matrices.Pharmaceutical research · 2013Article
- Influence of hydrophilic additives on the supersaturation and bioavailability of dutasteride-loaded hydroxypropyl-β-cyclodextrin nanostructures.International journal of nanomedicine · 2013Article
- The amorphous solid dispersion of the poorly soluble ABT-102 forms nano/microparticulate structures in aqueous medium: impact on solubility.International journal of nanomedicine · 2012Article
- A novel domperidone hydrogel: preparation, characterization, pharmacokinetic, and pharmacodynamic properties.Journal of drug delivery · 2011Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeSolid dispersions containing various stabilizers and tacrolimus (TAC) prepared by an Ultra-rapid Freezing (URF) process were investigated to determine the effect on their ability to form supersaturated solutions in aqueous media and on enhancing transport across biological membranes. MATERIALS AND
methodsThe stabilizers included poly(vinyl alcohol; PVA), poloxamer 407 (P407), and sodium dodecyl sulfate (SDS). In vivo absorption enhancement in rats was also investigated. Dissolution studies were conducted at supersaturated conditions in both acidic media for 24 h and at delayed release (enteric) conditions to simulate intestinal transit.
resultsThe rank order of C/Ceq(max) in the dissolution studies at acidic conditions was URF-P407 > URF-SDS > Prograf (PRO) > URF-PVA:P407. For C/Ceq(max) under enteric conditions, the order was URF-SDS > PRO > URF-PVA:P407 > URF-P407, and for the extent of supersaturation (AUC) in acidic and pH shift conditions it was URF-SDS>PRO>URF-PVA:P407>URF-P407. The pharmacokinetic data suggests URF-P407 had the greatest absorption having higher C (max) with a 1.5-fold increase in AUC compared to PRO. All URF compositions had a shorter T (max) compared to PRO.
conclusionsThe nanostructured powders containing various stabilizing polymers formed by the URF process offer enhanced supersaturation characteristics leading to increased oral absorption of TAC.
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