Change search
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • harvard1
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf
Adsorption of pharmaceutical excipients onto microcrystals of siramesine hydrochloride: Effects on physicochemical properties
YKI – Ytkemiska institutet.
Show others and affiliations
2009 (English)In: European journal of pharmaceutics and biopharmaceutics, ISSN 0939-6411, E-ISSN 1873-3441, Vol. 71, no 1, 109-116 p.Article in journal (Refereed)
Abstract [en]

A common challenge in the development of new drug substances is poor dissolution characteristics caused by low aqueous solubility. In this study, microcrystals with optimized physicochemical properties were prepared by precipitation in the presence of excipients, which adsorbed to the particle surface and altered particle size, morphology, and dissolution rate. The poorly water-soluble drug siramesine hydrochloride was precipitated by the antisolvent method in the presence of each of various polymeric and surface active excipients. Powder dissolution studies of six of the resulting particle systems showed a significant increase in percent dissolved after 15 min compared to the starting material. A quantitative determination of the amount of excipient adsorbed to the surface of the drug particles proved that only a very small amount of excipient was needed to exert a marked effect on particle properties. The adsorbed amount of excipient constituted less than 1.4% (w/w) of the total particle weight, and thus powders of very high drug loads were obtained. Sodium lauryl sulphate (SLS), hydroxypropyl methylcellulose (HPMC), and hydroxypropyl cellulose (HPC), which exhibited the greatest degree of adsorption, also had the greatest effect on the physicochemical properties of the particles. X-ray Photoelectron Spectroscopy (XPS) analysis of the surface composition and scanning electron microscopy studies on particle morphology suggested that the excipients adsorbed to specific faces of the crystals.

Place, publisher, year, edition, pages
2009. Vol. 71, no 1, 109-116 p.
Keyword [en]
Antisolvent precipitation, Crystal habit, Dissolution rate, Excipient adsorption, Microcrystals, Particle size, Polymers, Poorly soluble drugs, Surfactants, XPS
National Category
Natural Sciences
Identifiers
URN: urn:nbn:se:ri:diva-26535DOI: 10.1016/j.ejpb.2008.06.014OAI: oai:DiVA.org:ri-26535DiVA: diva2:1053538
Note
A1954Available from: 2016-12-08 Created: 2016-12-08Bibliographically approved

Open Access in DiVA

No full text

Other links

Publisher's full text
By organisation
YKI – Ytkemiska institutet
In the same journal
European journal of pharmaceutics and biopharmaceutics
Natural Sciences

Search outside of DiVA

GoogleGoogle Scholar

Altmetric score

Total: 6 hits
CiteExportLink to record
Permanent link

Direct link
Cite
Citation style
  • apa
  • harvard1
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Other style
More styles
Language
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Other locale
More languages
Output format
  • html
  • text
  • asciidoc
  • rtf
v. 2.27.0