Abstract:
:Sustained-release formulations such as hydroxypropyl methylcellulose (HPMC)-based hydrophilic matrix tablets of poorly water-soluble drugs often result in incomplete release because of the poor solubility and dissolution rate of the drug in the hydrophilic matrix. Sulfobutylether-beta-cyclodextrins ((SBE)(7M)-beta-CDs) have been known to improve the solubility of such drugs by forming inclusion complexes. The present paper deals with the modification of drug release from an HPMC-based matrix tablet of a sparingly water-soluble drug, prednisolone (PDL), using (SBE)(7M)-beta-CD as a solubilizing agent. Tablets were prepared by direct compression of a physically mixed PDL, (SBE)(7M)-beta-CD, and polymer. On exposure to water, an in situ PDL:(SBE)(7M)-beta-CD complex was formed in the gel layer, and enhanced drug release relative to a control formulation was observed (lactose used as the excipient instead of (SBE)(7M)-beta-CD ). Other possible changes due to the incorporation of (SBE)(7M)-beta-CD in the formulation were also probed. Incorporation of (SBE)(7M)-beta-CD lead to a higher water uptake relative to the control (lactose) formulation. For a fixed total tablet weight, polymer type, and loading, the drug release rate appeared to depend on the molar ratio of (SBE)(7M)-beta-CD to PDL and not the absolute amount of (SBE)(7M)-beta-CD present in the matrix tablet. This work shows that incorporation of (SBE)(7M)-beta-CD into the matrix tablets could be considered in designing a sustained-release tablet of poorly water-soluble drugs.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Rao VM,Haslam JL,Stella VJdoi
10.1002/jps.1034subject
Has Abstractpub_date
2001-07-01 00:00:00pages
807-16issue
7eissn
0022-3549issn
1520-6017pii
S0022-3549(16)30772-9journal_volume
90pub_type
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