Improving the solubility and bioavailability of dihydroartemisinin by solid dispersions and inclusion complexes.
Summary of "Improving the solubility and bioavailability of dihydroartemisinin by solid dispersions and inclusion complexes."
Dihydroartemisinin (DHA) is a poorly water-soluble drug that displays low bioavailability after oral administration. Attempts have been made to improve the solubility of DHA. Yet, no information is available concerning improved bioavailability. This study aimed to improve the water solubility of DHA by two systems: solid dispersions with polyvinylpyrrolidone (PVPK30, PVPK25, PVPK15) and inclusion complexes with hydroxypropyl-β-cyclodextrin (HPβCD), as well as improving the bioavailability of both systems. The phase transition of DHA with hydrophilic polymers was evaluated by X-ray diffraction (XRD) and differential scanning calorimetery (DSC). DHA became amorphous in DHA-HPβCD complexes and showed more amorphous behavior in XRD analyses with rise in molecular weight of PVP. Melting onset temperature of DHA decreased, while DSC thermograms revealed the peak area and enhanced enthalpy change (DH) in solid dispersions as well as inclusion complexes. DHA solubility was enhanced 84-fold in DHA-HPβCD complexes and 50-times in DHA-PVPK30. The improved solubility using the four polymers was in the following order: HPβCD > PVPK30 > PVPK25 > PVPK15. Values of area under curve (AUC) and half life (t(1/2)) of DHA-PVPK30 were highest followed by DHA-HPβCD, DHA-PVPK15 and DHA-PVPK25. V(d)/f of DHA-PVPK30 was 7-fold. DHA-HPβCD, DHA-PVPK15 and DHA-PVPK25 showed significantly different pharmacokinetic parameters compared with DHA solutions. The 95% confidence interval was meaningful in AUC and t(1/2). Pharmacokinetic parameters revealed that all four-test preparations were significantly more bioavailable than DHA alone.
Department of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan, Ansari.Muhammad@gmail.com.
This article was published in the following journal.
Name: Archives of pharmacal research
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/21656361
- DOI: http://dx.doi.org/10.1007/s12272-011-0509-1
The solubility of drugs in polymer matrices has been recognized as the one of the key factors governing the physical stability of solid dispersions. This study has explored the implications of drug so...
Objective: Norfloxacin has a low aqueous solubility which leads to poor dissolution. Keeping this fact in mind the purpose of this study is to formulate and evaluate norfloxacin solid dispersion. Meth...
The oral route of administration is the most common and preferred route of drug delivery due to its ease of administration, cost-effectiveness and flexibility in design. However, limited aqueous solub...
The most bioactive soy isoflavones (SI), daidzein (DAI) and genistein (GEN) have poor water solubility, which reduces their bioavailability and health benefits and limits their use in industry. The go...
The incorporation of poorly-soluble active pharmaceutical ingredients (APIs) into excipients (e.g. polymers) to formulate an amorphous solid dispersion is a promising strategy to improve the oral bioa...
This is an observational safety and efficacy study on dihydroartemisinin-piperaquine in Timika, Indonesia with a 42 day follow up period.
Dihydroartemisinin- Piperaquine is not inferior to artemether-lumefantrine
This will be an open-label trial in Burkina Faso assessing the pharmacokinetics of the antimalarial combination of dihydroartemisinin/piperaquine (DP, Duocotexcin) in children. Dihydroarte...
This study will evaluate the relative bioavailability of 2 oral formulations of TKI258, and the effect of food on the bioavailability of TKI258, in adult patients with advanced solid tumor...
This study will evaluate the relative bioavailability of 2 oral formulations of TKI258, and the effect of food on the bioavailability of TKI258, in adult patients with advanced solid tumor
Medical and Biotech [MESH] Definitions
Planning that has the goals of improving health, improving accessibility to health services, and promoting efficiency in the provision of services and resources on a comprehensive basis for a whole community. (From Facts on File Dictionary of Health Care Management, 1988, p299)
Complexes containing CHLOROPHYLL and other photosensitive molecules. They serve to capture energy in the form of PHOTONS are generally found as components of the PHOTOSYSTEM I PROTEIN COMPLEX or the PHOTOSYSTEM II PROTEIN COMPLEX.
Fractionation of a vaporized sample as a consequence of partition between a mobile gaseous phase and a stationary phase held in a column. Two types are gas-solid chromatography, where the fixed phase is a solid, and gas-liquid, in which the stationary phase is a nonvolatile liquid supported on an inert solid matrix.
A genus of DNA viruses in the family PAPILLOMAVIRIDAE, which cause cutaneous lesions in humans. They are histologically distinguishable by intracytoplasmic INCLUSION BODIES which are species specific.
Circumscribed masses of foreign or metabolically inactive materials, within the CELL NUCLEUS. Some are VIRAL INCLUSION BODIES.