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A novel drug delivery system combining oral fast dissolving film with sodium deoxycholate/phospholipid mixed micelles was prepared to increase the absorption of cucurbitacin B that is a poor aqueous solubility substance. Encapsulation efficiency, particle size, zeta potential, polydispersity coefficient, investigated the morphology, disintegration time of oral fast dissolving film and the pharmacodynamic properties of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles before and after solidified in mice were evaluated and compared. The oral fast dissolving film prepared in this study showed a homogeneous pale yellow and could completely disintegrated in the 30 s. It could meet the requirements of rapidly disintegrating fully. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles loaded in oral fast dissolving film were (43.36 +/- 2.12)%, (108.82 +/- 5.2) nm, (-34.18 +/- 1.07) mV, 0.088 +/- 0.012, respectively. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles in solution were (41.26 +/- 2.22)%, (181.82 +/- 4.48) nm, (-30.67 +/- 0.81) mV, 0.092 +/- 0.012, respectively. The difference of pharmacodynamics among film of cucurbitacin B-loaded micelles, cucurbitacin B-loaded micelles and free cucurbitacin B in vivo was compared. Solubility of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles has also been greatly improved. The tumor inhibition rate of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles was significantly improved and did not change significantly before and after solidified. These showed that the sodium deoxycholate/phospholipid-mixed micelles could enhance the antitumor activities of cucurbitacin B and the stability of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles was improved significantly after solidified by oral fast dissolving film technology without pharmacodynamic properties changed significantly.

Objective: To prepare puerarin deoxycholate/phospholipid mixed micelle to increase the solubility of puerarin., Method: Sodium deoxycholate and soybean phospholipids were used to prepare puerarin mixed micelle through orthogonal design experiments. With the solubility, shape and particle size as the response indexes, the preparing process of puerarin mixed micelle was optimized., Result: The optimized process for the puerarin deoxycholate/phospholipid mixed micelle was that the puerarin, soya phosphatidylcholine and sodium deoxycholate with the mole ratio of 3:2:4 should be dissolved in methanol-chloroform (1:1), and the solvents should be evaporated rotatively at 30 degrees C. The particle diameter of the mixed micelle was (64.8 +/- 13) nm (volume-weighted particle size distribution), and the solubility was 0.811 1 g x L(-1) in water at the room temperature, which was 22.3 times as that of the raw puerarin (0.036 4 g x L-1)., Conclusion: The puerarin deoxycholate/phospholipid mixed micelle can improve the solubility of puerarin significantly.

In the simulation experiments in vitro of the formation of gallstone, adenosine-triphosphate(ATP)-Co(2+)-deoxycholic acid(DC) gel system was chosen to study the periodic precipitation progress. The effect of ATP on the Co(2+)-DC gel system was also determined, and the structure of the periodic precipitation formed was characterized by FTIR. The results show that the patterns formed in the systems with ATP are different, ATP affected the rate and structure of precipitation through its variable participation in the metal coordination complexes as judged by the phosphate P=O bands and the deoxycholate COO- symmetric and asymmetric vibration bands as measured by FTIR Theses spectroscopic differences were correlated with color and pattern differences in the precipitates. ATP has a more remarkable function than AMP to the modes of patterns, meanwhile the system patterns transform from fractal to periodic precipitation. There is a complex interaction among ATP, sodium deoxycholic and Co2+ with a transparent crystal produced. The crystal is deoxycholic acid and the periodic precipitation is composed of ATP and DC covalent to Co2+. These results indicate that stone formation and remodeling is a dynamic, nonlinear progress. Much of the precipitate, as judged by local differences in composition, is not in equilibrium with the general gel environment. The authors conclude that the formation of gallstone features complex and nonlinear chemical character, in which nucleotides as living material play a very important role.

Objective: To study the preparation of alpha-Hydrocycholic-beta-Cyclodextrin inclusion compound., Methods: It was studied with orthogonal design to analysis three factors of inclusion rate such as the weight ratio between HDCA and beta-Cyclodextrin, the temperature and the reaction time. Fourier transform infrared spectroscopy, scanning electron microscopy, taste and solubility test were used to identify the inclusion compound., Results: Stable inclusion compound was made by HDCA and beta-Cyclodextrin. The weight ratio between HDCA and beta-Cyclodextrin was the most important factor. The alpha-Hydrocycholic-beta-Cyclodextrin inclusion compound taste and the solubility were improved., Conclusion: The optimum preparation condition is alpha-Hydrocycholic : beta-Cyclodextrin = 8.67 : 1, the inclusion temperature is 60 degrees C and the inclusion time is 30 minutes.

This is an in vitro model to mimic the conditions present during gallstone formation. Adenosine mono-phosphate (AMP), an important bio-molecule, was chosen. Its effect on the formation of periodic/chaotic patterns in the deoxycholate-CuCl2-gel and deoxycholate-CuCl2-glucose-gel systems were studied. FTIR spectroscopy was used to identify the structure of the precipitates. The results indicate that the patterns formed in the systems with AMP are different. And FTIR spectra show that AMP may also be involved in the coordination sphere of Cu2+ ion. The results are more complicated in the deoxycholate-CuCl2 system containing glucose, suggesting that the nonlinear scientific concept should be considered in understanding gallstone formation.

Aim: To investigate the transdermal delivery effects of cyclosporine A solubilized in mixed micelles composed of phospholipid and different surfactants., Methods: When applied onto the excised abdominal skin of the mice occlusively, the enhancing effects of various mixed micelles on the penetration of cyclosporin A were assessed by an in vitro permeation technique. In vivo study was carried out by topical application of sodium cholate-phospholipid mixed micelles onto the mice skin and drug blood concentration was detected., Results: In vitro, mixed micelles containing different surfactants displayed distinct permeability and corresponded to the following order: sodium cholate > sodium deoxycholate > Trition X-100 > Tween-20. In vivo, peak drug concentration was detected at 5 h and after that the concentration fell down slowly., Conclusion: Mixed micelles were shown to be efficient carrier for the transdermal delivery of the lipophilic polypeptide when kept in solution during the application process.

Eight coordinated complex samples of CoCl2-NaDC were obtained,using various concentration and initial molar ratio of CoCl2 and NaDC. They exhibited distinct appearances and characters. Their different structures and components were investigated by FTIR spectroscopy, X-ray diffraction analysis and ICP analysis. We can give the following conclusions: (1) when the concentration of NaDC is smaller than C.M.C, Co2+ ions react with mono-molecular NaDC and the component of the pink wadding-like resultant is Co(DC)2 x 3H2O. (2) When the concentration of NaDC is larger than C.M.C, and the concentration of CoCl2 is higher (0.5 mol/L), Co2+ ions destroy NaDC micelles, and the component of the pink wadding-like resultant is also Co(DC)2 x 3H2O. (3) When the concentration of NaDC is larger than C.M.C, and the concentration of CoCl2 is lower (0.1 mol/L or more lower), Co(DC)2 and NaDC may form mixed micelles, and some of NaDC micelles connect with each other through the Co2+ bridges to produce complicate Co(DC)2-NaDC complex with gel character and macromolecular network structure. In human body,the concentration of metal ions is usually lower and the concentration of NaDC is larger than C.M.C, So the third kind is suggested as an ideal model of the interaction between Co2+ ions and NaDC in vivo.