Sugar end-capped poly-D,L-lactides as excipients in oral sustained release tablets

Sirpa Vuorinen, Jyrki Heinämäki, Osmo Antikainen, Mohammed Lahcini, Timo Repo, Jouko Yliruusi

    Research output: Contribution to journalArticleScientificpeer-review

    Abstract

    Sugar end-capped poly-D,L-lactide (SPDLA) polymers were investigated as a potential release controlling excipient in oral sustained release matrix tablets. The SPDLA polymers were obtained by a catalytic ring-opening polymerization technique using methyl alpha-D-gluco-pyranoside as a multifunctional initiator in the polymerization. Polymers of different molecular weights were synthesized by varying molar ratios of monomer/catalyst. The matrix tablets were prepared by direct compression technique from the binary mixtures of SPDLA and microcrystalline cellulose, and theophylline was used as a model drug. The tablet matrices showed in vitro reproducible drug release profiles with a zero-order or diffusion-based kinetic depending on the SPDLA polymer grade used. Further release from the tablet matrices was dependent on the molecular weight of the SPDLA polymer applied. The drug release was the fastest with the lowest molecular weight SPDLA grade, and the drug release followed zero-order rate. With the higher molecular weight SPDLAs, more prolonged dissolution profiles for the matrix tablets (up to 8-10 h) were obtained. Furthermore, the prolonged drug release was independent of the pH of the dissolution media. In conclusion, SPDLAs are a novel type of drug carrier polymers applicable in oral controlled drug delivery systems.
    Original languageEnglish
    JournalAAPS PharmSciTech
    Volume10
    Issue number2
    Pages (from-to)566-573
    Number of pages8
    ISSN1530-9932
    DOIs
    Publication statusPublished - 2009
    MoE publication typeA1 Journal article-refereed

    Fields of Science

    • direct compression
    • matrix tablets
    • poly-D,L-lactide
    • release kinetics
    • sustained release
    • theophylline
    • POLY(DL-LACTIC ACID)
    • DIRECT COMPRESSION
    • MOLECULAR-WEIGHT
    • MATRIX TABLETS
    • DRUG-RELEASE
    • BIODEGRADABLE POLYMERS
    • GLASS-TRANSITION
    • POLYLACTIC ACID
    • LACTIC-ACID
    • COMPACTION
    • 116 Chemical sciences

    Cite this