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Physicochemical characterisation, drug polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000.
J Pharm Sci. 2011 Oct; 100(10):4281-94.JP

Abstract

Poor water solubility leads to low dissolution rate and consequently, it can limit bioavailability. Solid dispersions, where the drug is dispersed into an inert, hydrophilic polymer matrix can enhance drug dissolution. Solid dispersions were prepared using phenacetin and phenylbutazone as model drugs with polyethylene glycol (PEG) 8000 (carrier), by melt fusion method. Phenacetin and phenylbutazone displayed an increase in the dissolution rate when formulated as solid dispersions as compared with their physical mixture and drug alone counterparts. Characterisation of the solid dispersions was performed using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). DSC studies revealed that drugs were present in the amorphous form within the solid dispersions. FTIR spectra for the solid dispersions of drugs suggested that there was a lack of interaction between PEG 8000 and the drug. However, the physical mixture of phenacetin with PEG 8000 indicated the formation of hydrogen bond between phenacetin and the carrier. Permeability of phenacetin and phenylbutazone was higher for solid dispersions as compared with that of drug alone across Caco-2 cell monolayers. Permeability studies have shown that both phenacetin and phenylbutazone, and their solid dispersions can be categorised as well-absorbed compounds.

Authors+Show Affiliations

Aston Pharmacy School, Aston University, Birmingham B4 7ET, UK.No affiliation info availableNo 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

21560130

Citation

Khan, Sheraz, et al. "Physicochemical Characterisation, Drug Polymer Dissolution and in Vitro Evaluation of Phenacetin and Phenylbutazone Solid Dispersions With Polyethylene Glycol 8000." Journal of Pharmaceutical Sciences, vol. 100, no. 10, 2011, pp. 4281-94.
Khan S, Batchelor H, Hanson P, et al. Physicochemical characterisation, drug polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000. J Pharm Sci. 2011;100(10):4281-94.
Khan, S., Batchelor, H., Hanson, P., Perrie, Y., & Mohammed, A. R. (2011). Physicochemical characterisation, drug polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000. Journal of Pharmaceutical Sciences, 100(10), 4281-94. https://doi.org/10.1002/jps.22613
Khan S, et al. Physicochemical Characterisation, Drug Polymer Dissolution and in Vitro Evaluation of Phenacetin and Phenylbutazone Solid Dispersions With Polyethylene Glycol 8000. J Pharm Sci. 2011;100(10):4281-94. PubMed PMID: 21560130.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Physicochemical characterisation, drug polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000. AU - Khan,Sheraz, AU - Batchelor,Hannah, AU - Hanson,Peter, AU - Perrie,Yvonne, AU - Mohammed,Afzal R, Y1 - 2011/05/10/ PY - 2011/03/11/received PY - 2011/04/12/revised PY - 2011/04/20/accepted PY - 2011/5/12/entrez PY - 2011/5/12/pubmed PY - 2015/10/9/medline KW - DSC KW - Dissolution studies KW - FTIR KW - PEG 8000 KW - Permeability KW - Phenacetin KW - Phenylbutazone KW - amorphous form KW - solid dispersions SP - 4281 EP - 94 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 100 IS - 10 N2 - Poor water solubility leads to low dissolution rate and consequently, it can limit bioavailability. Solid dispersions, where the drug is dispersed into an inert, hydrophilic polymer matrix can enhance drug dissolution. Solid dispersions were prepared using phenacetin and phenylbutazone as model drugs with polyethylene glycol (PEG) 8000 (carrier), by melt fusion method. Phenacetin and phenylbutazone displayed an increase in the dissolution rate when formulated as solid dispersions as compared with their physical mixture and drug alone counterparts. Characterisation of the solid dispersions was performed using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). DSC studies revealed that drugs were present in the amorphous form within the solid dispersions. FTIR spectra for the solid dispersions of drugs suggested that there was a lack of interaction between PEG 8000 and the drug. However, the physical mixture of phenacetin with PEG 8000 indicated the formation of hydrogen bond between phenacetin and the carrier. Permeability of phenacetin and phenylbutazone was higher for solid dispersions as compared with that of drug alone across Caco-2 cell monolayers. Permeability studies have shown that both phenacetin and phenylbutazone, and their solid dispersions can be categorised as well-absorbed compounds. SN - 1520-6017 UR - https://www.unboundmedicine.com/medline/citation/21560130/Physicochemical_characterisation_drug_polymer_dissolution_and_in_vitro_evaluation_of_phenacetin_and_phenylbutazone_solid_dispersions_with_polyethylene_glycol_8000_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)31906-7 DB - PRIME DP - Unbound Medicine ER -