Friend D R
Controlled Release and Biomedical Polymers Department, SRI International, Menlo Park, CA 94025.
J Microencapsul. 1992 Oct-Dec;9(4):469-80. doi: 10.3109/02652049209040486.
Various microencapsulated dosage forms were prepared to limit the release of an antibiotic in solution for up to 3 days and in the oral cavity following per oral administration. An experimental antibiotic, clarithromycin (TE-031), was used in these studies. The drug was first encapsulated in gelatin followed in some cases by crosslinking with glutaraldehyde. The gelatin microcapsules were then coated with acrylic resins (Eudragit), whose solubility properties vary according to pH. A non-solvent coacervation technique was used to apply the Eudragit resins. It was found that crosslinking the gelatin retarded release of TE-031 somewhat relative to that from uncrosslinked gelatin microcapsules in a 72h release experiment conducted at room temperature. Coating the gelatin microcapsules with Eudragit resins L100, S100, or E100 slowed the release of TE-031 further still; less TE-031 was released over 72 h from the Eudragit-coated formulations prepared with crosslinked gelatin compared with formulations prepared with uncrosslinked gelatin. The Eudragit E100-coated crosslinked gelatin microcapsule formulation was most effective in preventing release of the TE-031 under simulated conditions of storage in an aqueous solution.
制备了各种微囊剂型，以限制抗生素在溶液中的释放长达3天，并在口服给药后在口腔中释放。在这些研究中使用了一种实验性抗生素，克拉霉素（TE-031）。该药物首先被包裹在明胶中，在某些情况下随后与戊二醛交联。然后用丙烯酸树脂（尤特奇）包被明胶微囊，其溶解特性随pH值而变化。采用非溶剂凝聚技术应用尤特奇树脂。发现在室温下进行的72小时释放实验中，相对于未交联的明胶微囊，明胶交联会使TE-031的释放有所延迟。用尤特奇树脂L100、S100或E100包被明胶微囊进一步减缓了TE-031的释放；与用未交联明胶制备的制剂相比，用交联明胶制备的尤特奇包被制剂在72小时内释放的TE-031更少。在模拟水溶液储存条件下，尤特奇E100包被的交联明胶微囊制剂在防止TE-031释放方面最有效。
