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Controlled drug release from pellets containing water-insoluble drugs dissolved in a self-emulsifying system.
Eur J Pharm Biopharm. 2007 Jan; 65(1):94-8.EJ

Abstract

The aim of the study was to provide a controlled release system, which could be used for the oral administration of highly water-insoluble drugs. Pellets have been prepared by extrusion/spheronization containing two model drugs (methyl and propyl parabens) of low water solubility. One type of pellets contained the drugs mixed with lactose and microcrystalline cellulose (MCC) and the other types of pellets contained the model drugs dissolved in a self-emulsifying system (4.8%) consisting of equal parts of mono-diglycerides and polysorbate 80 and MCC. Pellets of all types in the same size fraction (1.4-2.0 mm) were coated to different levels of weight gain, with ethylcellulose, talc and glycerol. A sample of pellets containing methyl parabens in the self-emulsifying system was pre-coated with a film of hydroxypropylmethyl cellulose from an aqueous solution and then coated as above. Dissolution experiments established that the presence of the self-emulsifying system enhanced the drug release of both model drugs and that the film coating considerably reduced the drug release from pellets made with just water, lactose and MCC. The coating reduced the drug release from the pellets containing the self-emulsifying system to a lesser extent but in relation to the quantity of coat applied to the pellets. The application of a sub-coating of hydroxypropylmethyl cellulose was able to reduce the release rate of methyl parabens self-emulsifying system ethyl cellulose coated pellets. Thus, the formulation approach offers the possibility of formulating and controlling the in vitro release of water-insoluble drugs from solid oral dosage forms.

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Authors+Show Affiliations

Serratoni M
The School of Pharmacy, University of London, London, UK.
Newton M
No affiliation info available
Booth S
No affiliation info available
Clarke A
No affiliation info available

MeSH

CapsulesCelluloseChemistry, PharmaceuticalDelayed-Action PreparationsDiglyceridesEmulsionsExcipientsHypromellose DerivativesLactoseMethylcelluloseMonoglyceridesParabensParticle SizePharmaceutical PreparationsPolysorbatesSolubilityTechnology, PharmaceuticalTime FactorsWater

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17056237

Citation

Serratoni, Mauro, et al. "Controlled Drug Release From Pellets Containing Water-insoluble Drugs Dissolved in a Self-emulsifying System." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 65, no. 1, 2007, pp. 94-8.
Serratoni M, Newton M, Booth S, et al. Controlled drug release from pellets containing water-insoluble drugs dissolved in a self-emulsifying system. Eur J Pharm Biopharm. 2007;65(1):94-8.
Serratoni, M., Newton, M., Booth, S., & Clarke, A. (2007). Controlled drug release from pellets containing water-insoluble drugs dissolved in a self-emulsifying system. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 65(1), 94-8.
Serratoni M, et al. Controlled Drug Release From Pellets Containing Water-insoluble Drugs Dissolved in a Self-emulsifying System. Eur J Pharm Biopharm. 2007;65(1):94-8. PubMed PMID: 17056237.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Controlled drug release from pellets containing water-insoluble drugs dissolved in a self-emulsifying system. AU - Serratoni,Mauro, AU - Newton,Michael, AU - Booth,Steven, AU - Clarke,Ashley, Y1 - 2006/07/22/ PY - 2006/06/08/received PY - 2006/07/18/accepted PY - 2006/10/24/pubmed PY - 2007/2/3/medline PY - 2006/10/24/entrez SP - 94 EP - 8 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 65 IS - 1 N2 - The aim of the study was to provide a controlled release system, which could be used for the oral administration of highly water-insoluble drugs. Pellets have been prepared by extrusion/spheronization containing two model drugs (methyl and propyl parabens) of low water solubility. One type of pellets contained the drugs mixed with lactose and microcrystalline cellulose (MCC) and the other types of pellets contained the model drugs dissolved in a self-emulsifying system (4.8%) consisting of equal parts of mono-diglycerides and polysorbate 80 and MCC. Pellets of all types in the same size fraction (1.4-2.0 mm) were coated to different levels of weight gain, with ethylcellulose, talc and glycerol. A sample of pellets containing methyl parabens in the self-emulsifying system was pre-coated with a film of hydroxypropylmethyl cellulose from an aqueous solution and then coated as above. Dissolution experiments established that the presence of the self-emulsifying system enhanced the drug release of both model drugs and that the film coating considerably reduced the drug release from pellets made with just water, lactose and MCC. The coating reduced the drug release from the pellets containing the self-emulsifying system to a lesser extent but in relation to the quantity of coat applied to the pellets. The application of a sub-coating of hydroxypropylmethyl cellulose was able to reduce the release rate of methyl parabens self-emulsifying system ethyl cellulose coated pellets. Thus, the formulation approach offers the possibility of formulating and controlling the in vitro release of water-insoluble drugs from solid oral dosage forms. SN - 0939-6411 UR - https://www.unboundmedicine.com/medline/citation/17056237/Controlled_drug_release_from_pellets_containing_water_insoluble_drugs_dissolved_in_a_self_emulsifying_system_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(06)00195-0 DB - PRIME DP - Unbound Medicine ER -