Ketoconazole ion-exchange fiber complex: a novel method to reduce the individual difference of bioavailability in oral administration caused by gastric anacidity.
Summary of "Ketoconazole ion-exchange fiber complex: a novel method to reduce the individual difference of bioavailability in oral administration caused by gastric anacidity."
Water insoluble faintly alkaline drugs often have potential absorption problem in gastrointestinal tract in oral administration for patients with gastric anacidity. The purpose of the present study is to develop a novel method to improve the absorption of the water insoluble faintly alkaline drug in peroral administration. This method is based on ion exchange of ion-exchange fibers. Water-insoluble faintly alkaline drug ketoconazole was used as a model drug. Ketoconazole and the active groups of the ion-exchange fibers combined into ion pairs based on the acid-base reaction. This drug carrier did not release drugs in deionized water, but in water solution containing other ions it would release the drugs into the solution by ion exchange. Confirmed by the X-ray diffraction and the differential scanning calorimetry (DSC), the ketoconazole combined onto the ion-exchange fibers was in a highly molecular level dispersed state. The improved dissolution of ketoconazole ion-exchange fiber complexes is likely to originate from this ketoconazole's highly dispersed state. Furthermore, due to this ketoconazole's highly dispersed state, ketoconazole ion-exchange fiber complexes significantly decreased the individual difference of absorption in oral administration of ketoconazole caused by the fluctuation of the acid degree in the gastric fluid.
Affiliation
School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China.
Journal Details
This article was published in the following journal.
Name: Pharmaceutical development and technology
ISSN: 1097-9867
Pages:
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/22670853
- DOI: http://dx.doi.org/10.3109/10837450.2012.696266
Medical and Biotech [MESH] Definitions
Directly Observed Therapy
A treatment method in which patients are under direct observation when they take their medication or receive their treatment. This method is designed to reduce the risk of treatment interruption and to ensure patient compliance.
Cotton Fiber
A TEXTILE fiber obtained from the pappus (outside the SEEDS) of cotton plant (GOSSYPIUM). Inhalation of cotton fiber dust over a prolonged period can result in BYSSINOSIS.
Colestipol
Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels.
Ion Exchange Resins
High molecular weight, insoluble polymers which contain functional groups that are capable of undergoing exchange reactions (ION EXCHANGE) with either cations or anions.
Solid Phase Microextraction
A solventless sample preparation method, invented in 1989, that uses a fused silica fiber which is coated with a stationary phase. It is used for sample cleanup before using other analytical methods.
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