• Journal of Pharmaceutical Investigation
• /
• v.29 no.3
• /
• pp.227-234
• /
• 1999

Solid dispersions were prepared to increase the dissolution rate of biphenyl dimethyl dicarboxylate (DDB) using water-soluble carriers such as povidone, copolyvidone, $2-hydroxypropyl-{\beta}-cyclodextrin (HPCD)$, sodium salicylate or sodium benzoate by solvent evaporation method. Solid dispersions were characterized by infrared spectrometry, differential scanning calorimetry (DSC) and powder X-ray diffractometry, dissolution and permeation studies. DDB tablets (7.5 mg) were prepared by compressing the powder mixtures composed of solid dispersions, lactose, com starch, crospovidone and magnesium stearate using a single-punch press. DDB capsules (7.5 mg) were also prepared by filling the mixtures in empty hard gelatin capsules (size No.1). From the DSC and powder x-ray diffractometric studies, it was found that DDB was amorphous in the HPCD or copolyvidone solid dispersions. Dissolution rates after 10 min of DDB alone and solid dispersions (1 : 10) in sodium benzoate, sodium salicylate and copolyvidone were 11.8, 23.5, 22.8 and 82.5%, respectively. Dissolution rates of DDB after 30 min from 1 : 10 and 1 : 20 copolyvidone solid dispersions were 80.5 and 95.0%, respectively. For the DDB tablets prepared using solid dispersions (1 : 20), the initial dissolution rate was dependent on carrier material, and was ranked in order, $Kollidon\;30\;{\ll}$ copolyvidone < HPCD. For the HPCD solid dispersion tablets, dissolution rate reached 97.4% after 15 min, but thereafter slowly decreased to 80.7% after 2 hr due to the precipitation of DDB. However, in the case of copolyvidone solid dispersion tablets, dissolution increased linearly and reached 93.4% after 2 hr. Reducing the volume of test medium from 900 to 300 ml markedly decreased the dissolution rate of the tablets containing 1 : 20 HPCD solid dispersions and 1 : 10 copolyvidone solid dispersion. For 1 : 20 copolyvidone solid dispersion tablets, there was no significant change in dissolution rate up to 1 hr with different volumes of test medium. Preparation of the copolyvidone solid dispersion (1 : 20) in capsules markedly delayed the dissolution (31.2 % after 2hr) due to the limited diffusion within capsules. The permeation rate $(13.4\;g/cm^2\;after\;8\;hr)$ of DDB through rabbit duodenal mucosa from copolyvidone solid dispersion (1 : 10) was markedly enhanced, when compared with drug alone or physical mixtures. From overall findings, DDB formulations containing copolyvidone solid dispersions (1 : 20) could be used to remarkably improve the dissolution rate in dosage form of powders and tablets.

• Herbal Formula Science
• /
• v.31 no.4
• /
• pp.215-230
• /
• 2023

Objectives : Schisandra chinensis (Turcz.) Baill contains many nutrients and exhibits high physiological functions. It has been shown that Schisandra seed and pamace contains more nutrients than fruits and thus have higher antioxidant efficacy. In this study, seed and pamace of Schisandra chinensis (Turcz.) Baill (SPSC) were treated with hot-melt extrudate (HME) extrusion to produce water-soluble nanoparticles. Methods : SPSC was treated with HME to prepare nanoparticles. In this process, excipients (hydroxypropyl methylcellulose, pullulan, 2-hydroxylpropyl-beta-cyclodextrin, lecithin) were added to prepare a hydrophilic polymer matrix. To compare and analyze the antioxidant effect and schizandrin content, total flavonoid content, total phenol content and ABTS assay were measured. To confirm the effect of increasing the water solubility of the particles, particle size and water solubility index measurements were performed. The molecular of the material was analyzed using Fourier transform infrared spectroscopy (FT-IR). Results : The particle size of HME extrudates decreased, while total phenols, flavonoids, schizandrin, antioxidant effect, and solubility increased. Through FT-IR, it was confirmed that the SPSC and the extrudate exhibit the same chemical properties. In addition, it was confirmed that when extracted with water, it exhibited a higher antioxidant effect than the ethanol extract. Conclusions : HME technology increased the solubility of SPSC, which are processing by-products, and improved their antioxidant effect to a higher degree. It was confirmed that SPSC could be used as an eco-friendly, high value-added material.

• Korean Journal of Microbiology
• /
• v.49 no.1
• /
• pp.24-29
• /
• 2013

In the present study, the effects of prebiotics and prebiotics+probiotics on intestinal microflora and fermentation products were evaluated in a pig in vitro fermentation model. The substrates used in this study were iso-malto oligosaccharide (IMO), partially digested chicory-inulin (CI), raffinose (RA), and cyclodextrin (CD) as prebiotics and Lactobacillus reiteri as probiotics. For a pig in vitro fermentation, the experimental diet for growing pigs was predigested using digestive enzymes secreted by small intestine and this hydrolyzed diet was mixed with a buffer solution containing 5% fresh swine feces. The mixture was then incubated with either prebiotics or prebiotics+probiotics for 24 h. Samples were taken at 24 h, and viable counts of microflora, gas, pH, volatile organic compounds (VOCs) and short-chain fatty acid (SCFA) were analyzed. The viable count of Enterobacteriaceae was significantly decreased (p<0.001) in all treatments containing prebiotics and prebiotics+probiotics when compared to the control. However, the number of lactic acid bacteria increased in the prebiotics and prebiotics+probiotics treatment. The pH values in the fermentation fluid decreased in all treatments when compared to the control, and their effects were greater in the prebiotics+probiotics group than prebiotics group. Fermentation with prebiotics resulted in a reduction in malodorous compounds such as ammonia, hydrogen sulfide and skatole when compared to the prebiotics+probiotics group. Short-chain fatty acid production was also higher for treatment with prebiotics+probiotics than treatment with prebiotics. In conclusion, the results of this study demonstrated that fermentation with prebiotics was effective in reducing the formation of malodorous compounds and prebiotics+probiotics was effective in increasing lactic acid bacteria and SCFA and reducing the pH. Moreover, further studies will be needed to determine whether the results observed in the in vitro model would occur in pigs that ingest these prebiotics or probiotics.