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- Alskär, Linda C.Uppsala universitet,Institutionen för farmaci (author)
Impact of Drug Physicochemical Properties on Lipolysis-Triggered Drug Supersaturation and Precipitation from Lipid-Based Formulations
- Article/chapterEnglish2018
Publisher, publication year, extent ...
- 2018-08-24
- American Chemical Society (ACS),2018
- electronicrdacarrier
Numbers
- LIBRIS-ID:oai:DiVA.org:uu-366563
- https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-366563URI
- https://doi.org/10.1021/acs.molpharmaceut.8b00699DOI
Supplementary language notes
- Language:English
- Summary in:English
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Notes
- In this study we investigated lipolysis-triggered supersaturation and precipitation of a set of model compounds formulated in lipid-based formulations (LBFs). The purpose was to explore the relationship between precipitated solid form and inherent physicochemical properties of the drug. Eight drugs were studied after formulation in three LBFs, representing lipid-rich (extensively digestible) to surfactant-rich (less digestible) formulations. In vitro lipolysis of drug-loaded LBFs were conducted, and the amount of dissolved and precipitated drug was quantified. Solid form of the precipitated drug was characterized with polarized light microscopy (PLM) and Raman spectroscopy. A significant solubility increase for the weak bases in the presence of digestion products was observed, in contrast to the neutral and acidic compounds for which the solubility decreased. The fold-increase in solubility was linked to the degree of ionization of the weak bases and thus their attraction to free fatty acids. A high level of supersaturation was needed to cause precipitation. For the weak bases, the dose number indicated that precipitation would not occur during lipolysis; hence, these compounds were not included in further studies. The solid state analysis proved that danazol and griseofulvin precipitated in a crystalline form, while niclosamide precipitated as a hydrate. Felodipine and indomethacin crystals were visible in the PLM, whereas the Raman spectra showed presence of amorphous drug, indicating amorphous precipitation that quickly crystallized. The solid state analysis was combined with literature data to allow analysis of the relationship between solid form and the physicochemical properties of the drug. It was found that low molecular weight and high melting temperature increases the probability of crystalline precipitation, whereas precipitation in an amorphous form was favored by high molecular weight, low melting temperature, and positive charge.
Subject headings and genre
- MEDICIN OCH HÄLSOVETENSKAP Medicinska och farmaceutiska grundvetenskaper Farmaceutiska vetenskaper hsv//swe
- MEDICAL AND HEALTH SCIENCES Basic Medicine Pharmaceutical Sciences hsv//eng
- Poorly water-soluble drugs
- lipid digestion
- physicochemical properties
- precipitation
- solid state
- supersaturation
Added entries (persons, corporate bodies, meetings, titles ...)
- Keemink, JannekeUppsala universitet,Institutionen för farmaci(Swepub:uu)janke374 (author)
- Johannesson, JennyUppsala universitet,Institutionen för farmaci (author)
- Porter, Christopher J HDrug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia (author)
- Bergström, Christel A. S.,1973-Uppsala universitet,Institutionen för farmaci,Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia(Swepub:uu)cjo29958 (author)
- Uppsala universitetInstitutionen för farmaci (creator_code:org_t)
Related titles
- In:Molecular Pharmaceutics: American Chemical Society (ACS)15:10, s. 4733-47441543-83841543-8392
Internet link
- https://doi.org/10.1021/acs.molpharmaceut.8b00699Fulltext
- https://uu.diva-portal.org/smash/get/diva2:1264926/FULLTEXT01.pdffulltext:print
- https://pubs.acs.org/doi/pdf/10.1021/acs.molpharmaceut.8b00699
- https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-366563
- https://doi.org/10.1021/acs.molpharmaceut.8b00699
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