Solubilization of Biphenyl Dimethyl Dicarboxylate by Cosolvency

Biphenyl dimethyl dicarboxylate (BDD) is a synthetic analogue of schizandrin C, one of the components isolated from Fructus schizandrae, and has been widely prescribed for improvement of liver functions and symptoms of patients with liver disease. However, its oral preparations have been known to ha...

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Bibliographic Details
Published in:Drug development and industrial pharmacy 1999-01, Vol.25 (11), p.1193-1197
Main Authors: Han, Suk Kyu, Kim, Gap Yul, Park, Yong Hun
Format: Article
Language:English
Subjects:
Biological and medical sciences
Cyclooctanes
Dioxoles - chemistry
Drugs, Chinese Herbal - chemistry
General pharmacology
Infusions, Intravenous
Lignans
Medical sciences
Pharmaceutical Solutions
Pharmaceutical technology. Pharmaceutical industry
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Polycyclic Compounds - chemistry
Solubility
Solvents
Temperature
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Summary:Biphenyl dimethyl dicarboxylate (BDD) is a synthetic analogue of schizandrin C, one of the components isolated from Fructus schizandrae, and has been widely prescribed for improvement of liver functions and symptoms of patients with liver disease. However, its oral preparations have been known to have limited bioavailability due to its extremely low solubility in water, and its solubility problem also limits preparation of its parenteral dosage forms. In this research, we searched for solvent systems to solubilize BDD to overcome these problems. The ternary solvent systems of N,N′- dimethylacetamide (DMA) alcohol water and Cremophor EL DMA alcohol were studied intensively for this purpose. BDD was solubilized effectively in these cosolvents, and the results showed that the cosolvent systems were effective for solubilizing BDD up to the concentration that might be employed for preparation of parenteral dosage forms. Formulation of a BDD concentrate for intravenous infusion was proposed employing the cosolvent system of Cremophor EL DMA alcohol.
ISSN:0363-9045
1520-5762
DOI:10.1081/DDC-100102287