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Controlled poorly soluble drug release from solid self-microemulsifying formulations with high viscosity hydroxypropylmethylcellulose.
Eur J Pharm Sci. 2008 Aug 07; 34(4-5):274-80.EJ

Abstract

The objective of this work was the development of a controlled release system based on self-microemulsifying mixture aimed for oral delivery of poorly water-soluble drugs. HPMC-based particle formulations were prepared by spray drying containing a model drug (nimodipine) of low water solubility and hydroxypropylmethylcellulose (HPMC) of high viscosity. One type of formulations contained nimodipine mixed with HPMC and the other type of formulations contained HPMC and nimodipine dissolved in a self-microemulsifying system (SMES) consisting of ethyl oleate, Cremophor RH 40 and Labrasol. Based on investigation by transmission electron microscopy (TEM), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray powder diffraction, differences were found in the particle structure between both types of formulations. In vitro release was performed and characterized by the power law. Nimodipine release from both types of formulations showed a controlled release profile and the two power law parameters, n and K, correlated to the viscosity of HPMC. The parameters were also influenced by the presence of SMES. For the controlled release solid SMES, oil droplets containing dissolved nimodipine diffused out of HPMC matrices following exposure to aqueous media. Thus, it is possible to control the in vitro release of poorly soluble drugs from solid oral dosage forms containing SMES.

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Authors+Show Affiliations

Yi T
College of Life Science and Technology, Huazhong University of Science and Technology, 1037 Luoyu Road, Wuhan 430074, China.
Wan J
No affiliation info available
Xu H
No affiliation info available
Yang X
No affiliation info available

MeSH

Administration, OralCalcium Channel BlockersCalorimetry, Differential ScanningChemistry, PharmaceuticalCrystallography, X-RayDelayed-Action PreparationsDiffusionDrug CarriersDrug CompoundingEmulsionsGlyceridesHypromellose DerivativesKineticsLipidsMethylcelluloseMicroscopy, Electron, ScanningMicroscopy, Electron, TransmissionNimodipineOleic AcidsOrganic ChemicalsParticle SizePolyethylene GlycolsPowder DiffractionSolubilitySurface PropertiesTechnology, PharmaceuticalViscosity

Pub Type(s)

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

Language

eng

PubMed ID

18541418

Citation

Yi, Tao, et al. "Controlled Poorly Soluble Drug Release From Solid Self-microemulsifying Formulations With High Viscosity Hydroxypropylmethylcellulose." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 34, no. 4-5, 2008, pp. 274-80.
Yi T, Wan J, Xu H, et al. Controlled poorly soluble drug release from solid self-microemulsifying formulations with high viscosity hydroxypropylmethylcellulose. Eur J Pharm Sci. 2008;34(4-5):274-80.
Yi, T., Wan, J., Xu, H., & Yang, X. (2008). Controlled poorly soluble drug release from solid self-microemulsifying formulations with high viscosity hydroxypropylmethylcellulose. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 34(4-5), 274-80. https://doi.org/10.1016/j.ejps.2008.04.010
Yi T, et al. Controlled Poorly Soluble Drug Release From Solid Self-microemulsifying Formulations With High Viscosity Hydroxypropylmethylcellulose. Eur J Pharm Sci. 2008 Aug 7;34(4-5):274-80. PubMed PMID: 18541418.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Controlled poorly soluble drug release from solid self-microemulsifying formulations with high viscosity hydroxypropylmethylcellulose. AU - Yi,Tao, AU - Wan,Jiangling, AU - Xu,Huibi, AU - Yang,Xiangliang, Y1 - 2008/05/04/ PY - 2008/03/04/received PY - 2008/04/18/revised PY - 2008/04/30/accepted PY - 2008/6/11/pubmed PY - 2008/10/4/medline PY - 2008/6/11/entrez SP - 274 EP - 80 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 34 IS - 4-5 N2 - The objective of this work was the development of a controlled release system based on self-microemulsifying mixture aimed for oral delivery of poorly water-soluble drugs. HPMC-based particle formulations were prepared by spray drying containing a model drug (nimodipine) of low water solubility and hydroxypropylmethylcellulose (HPMC) of high viscosity. One type of formulations contained nimodipine mixed with HPMC and the other type of formulations contained HPMC and nimodipine dissolved in a self-microemulsifying system (SMES) consisting of ethyl oleate, Cremophor RH 40 and Labrasol. Based on investigation by transmission electron microscopy (TEM), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray powder diffraction, differences were found in the particle structure between both types of formulations. In vitro release was performed and characterized by the power law. Nimodipine release from both types of formulations showed a controlled release profile and the two power law parameters, n and K, correlated to the viscosity of HPMC. The parameters were also influenced by the presence of SMES. For the controlled release solid SMES, oil droplets containing dissolved nimodipine diffused out of HPMC matrices following exposure to aqueous media. Thus, it is possible to control the in vitro release of poorly soluble drugs from solid oral dosage forms containing SMES. SN - 0928-0987 UR - https://www.unboundmedicine.com/medline/citation/18541418/Controlled_poorly_soluble_drug_release_from_solid_self_microemulsifying_formulations_with_high_viscosity_hydroxypropylmethylcellulose_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(08)00254-6 DB - PRIME DP - Unbound Medicine ER -