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Dissolution rate improvement of poorly water-soluble drugs obtained by adsorbing solutions of drugs in hydrophilic solvents onto high surface area carriers.
Eur J Pharm Biopharm. 2006 Feb; 62(2):171-7.EJ

Abstract

The dissolution rate of the model drugs carbamazepine and nifedipine was improved by adsorbing solutions of the drugs in hydrophilic non-volatile or volatile solvents onto carriers with a large surface area. This was accomplished by dissolving the drug in methanol or the non-toxic hydrophilic liquids PEG 400 or 2-pyrrolidone, and adsorbing these solutions onto the surface of silica (Aerosil) or crosslinked polyvinylpyrrolidone (Kollidon CL-M). The solvent binding capacities decreased in the order of methanol, PEG 400, 2-pyrrolidone for Aerosil 200, 300, 380 and for Kollidon CL-M. Kollidon bound less liquid than Aerosil because of the smaller surface area. Differential scanning calorimetry measurements showed higher interactions between drugs and Kollidon compared to Aerosil, suggesting a low aggregation of precipitated drug particles. The drug release from the adsorbent systems was enhanced when compared to micronized drug and independent of the drug loading in the investigated range. The drugs were also dissolved in various liquid, paste-like or solid solubilisers (polyoxyl-40-hydrogenated castor oil (Cremophor RH 40), macrogol-15-hydroxystearate (Solutol HS), poloxamers (Lutrol F68, Pluronic F87NF and Pluronic L44NF) and adsorbed onto Kollidon. These adsorbent systems also exhibited an increased dissolution rate when compared to pure drug.

Authors+Show Affiliations

College of Pharmacy, Freie Universität Berlin, Berlin, Germany.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

16275049

Citation

Friedrich, Heike, et al. "Dissolution Rate Improvement of Poorly Water-soluble Drugs Obtained By Adsorbing Solutions of Drugs in Hydrophilic Solvents Onto High Surface Area Carriers." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 62, no. 2, 2006, pp. 171-7.
Friedrich H, Fussnegger B, Kolter K, et al. Dissolution rate improvement of poorly water-soluble drugs obtained by adsorbing solutions of drugs in hydrophilic solvents onto high surface area carriers. Eur J Pharm Biopharm. 2006;62(2):171-7.
Friedrich, H., Fussnegger, B., Kolter, K., & Bodmeier, R. (2006). Dissolution rate improvement of poorly water-soluble drugs obtained by adsorbing solutions of drugs in hydrophilic solvents onto high surface area carriers. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 62(2), 171-7.
Friedrich H, et al. Dissolution Rate Improvement of Poorly Water-soluble Drugs Obtained By Adsorbing Solutions of Drugs in Hydrophilic Solvents Onto High Surface Area Carriers. Eur J Pharm Biopharm. 2006;62(2):171-7. PubMed PMID: 16275049.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Dissolution rate improvement of poorly water-soluble drugs obtained by adsorbing solutions of drugs in hydrophilic solvents onto high surface area carriers. AU - Friedrich,Heike, AU - Fussnegger,Bernd, AU - Kolter,Karl, AU - Bodmeier,Roland, Y1 - 2005/11/04/ PY - 2005/03/02/received PY - 2005/04/29/revised PY - 2005/08/04/accepted PY - 2005/11/9/pubmed PY - 2007/2/21/medline PY - 2005/11/9/entrez SP - 171 EP - 7 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 62 IS - 2 N2 - The dissolution rate of the model drugs carbamazepine and nifedipine was improved by adsorbing solutions of the drugs in hydrophilic non-volatile or volatile solvents onto carriers with a large surface area. This was accomplished by dissolving the drug in methanol or the non-toxic hydrophilic liquids PEG 400 or 2-pyrrolidone, and adsorbing these solutions onto the surface of silica (Aerosil) or crosslinked polyvinylpyrrolidone (Kollidon CL-M). The solvent binding capacities decreased in the order of methanol, PEG 400, 2-pyrrolidone for Aerosil 200, 300, 380 and for Kollidon CL-M. Kollidon bound less liquid than Aerosil because of the smaller surface area. Differential scanning calorimetry measurements showed higher interactions between drugs and Kollidon compared to Aerosil, suggesting a low aggregation of precipitated drug particles. The drug release from the adsorbent systems was enhanced when compared to micronized drug and independent of the drug loading in the investigated range. The drugs were also dissolved in various liquid, paste-like or solid solubilisers (polyoxyl-40-hydrogenated castor oil (Cremophor RH 40), macrogol-15-hydroxystearate (Solutol HS), poloxamers (Lutrol F68, Pluronic F87NF and Pluronic L44NF) and adsorbed onto Kollidon. These adsorbent systems also exhibited an increased dissolution rate when compared to pure drug. SN - 0939-6411 UR - https://www.unboundmedicine.com/medline/citation/16275049/Dissolution_rate_improvement_of_poorly_water_soluble_drugs_obtained_by_adsorbing_solutions_of_drugs_in_hydrophilic_solvents_onto_high_surface_area_carriers_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(05)00249-3 DB - PRIME DP - Unbound Medicine ER -