• Biomolecules & Therapeutics
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• v.4 no.4
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• pp.419-427
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• 1996

To solubilize practically insoluble biphenyl dimethyl dicarboxylate (DDB), which has been used for the treatment of chronic hepatitis as tablets or hard capsules, the solubilities of DDB in various hydrophilic, oily and hydrocarbon vehicles, and aqueous surfactant solutions were measured by high performance liquid chromatography. It was found that, among the vehicles studied, polyethylene glycol (PEG) 300 revealed the best solvency, and the solubility reached 17.6 mg/ml at 37$^{\circ}C$. The addition of glycyrrhizic acid ammonium salt (GAA) to DDB-PEG 300 solution (5-20 mg/g) inhibited the formation of precipitates, and at the concentration of 10 mg/g, any precipitaction was not observed even after 2 years at 4$^{\circ}C$. Furthermore, GAA markedly enhanced the permeation of DDB through the rabbit duodenal mucosa in a concentration dependent manner. The addition of copolyvidone (ca. 1.0%) to DDB-GAA-PEG 300 system (1 : 0.5 97.5 w/w) was most effective in preventing the considerable precipitation of DDB-PEG 300 solution (7.5 mg/750 mg) when mixed with water of 300-900 ml at 37$^{\circ}C$. GAA showed a synergistic effect in the prevention of precipitate formation. This finding suggests that this DDB formulation may form less precipitation when DDB soft capsules disintegrate and diffuse into the gastrointestinal fluid, resulting in improving the bioavailability Dissolution rate of DDB (7.5 mg) from sort elastic capsules of DDB-GAA-PEG 300 system was rapid. The supersaturation state was maintained for 2 hr at the concentration of 7.35$\pm$3.3 mg in 900 ml of water without precipitation. The total amount of DDB dissolved from this new formulation was 5.3 and 6.1 times higher, when compared to marketed DDB tablets (25 mg) and capsules (7.5 mg), respectively.

• The Journal of Korean Medicine
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• v.26 no.3 s.63
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• pp.249-262
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• 2005

Backgrounds : As obesity prevails as an epidemic. diet programs including low-calorie diets are developed continuously. It is generally believed that a low-calorie diet is commonly followed by resting metabolic rate decrease and ultimate weight regain. Ephedra and Evodia are known to have sympathomimetic and anti-obesity effect. Objectives : This study was a prospective, double-blinded, randomized md placebo-controlled clinical trial to evaluate the effects of Ephedra sinica and Evodia rutaecarpa on resting metabolic rate (RMR), weight, body composition, and short-term safety in obese women on low-calorie diet. Methods : 125 otherwise healthy obese women (body mass Index ${\geq}\;25kg/m^2$) were recruited and randomly assigned to three groups: Ephedra group (n=41), Evodia group (n =45), and placebo group (n=39). Subjects were administered Ephedra extract in capsules (pseudo-ephedrine 31.52mg) or Evodia extract in capsules (evodiamine 6.75mg, rutaecarpine 0.66mg) or placebo capsules as well as participating in a low-calorie diet for 8 weeks, Resting metabolic rate and body composition were measured at baseline,4 and 8 weeks. Basic serum exams were performed to evaluate the short-term safety of the herbs and changes of lipid variables. Results : All three groups showed significant BMI decreases probably due to low-calorie diet. Among them, the Ephedra group manifested most prominent BMI-reducing effect and towered total cholesterol and triglycerides significantly. The RMR was not changed during the 8-week diet in all groups. No significant difference among the groups was found in RMR, either. Stbject with higher RMR than the mean at the baseline showed a tendency to keep their RMR more stable during the diet program. Conclusions : Ephedra with a low-calorie diet was effective in reducing BMI. RMR change was not compensated by herbal medicines. RMR change seemed to be affected rather by constitution and body composition than medicine. Ephedra and Evodia were proven to be safe for sort-term use in herbal form. Especially, Ephedra was effective in lowering total cholesterol and triglycerides during the 8 weeks.