• Journal of Pharmaceutical Investigation
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• 제29권3호
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• pp.227-234
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• 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.

• 대한한의학방제학회지
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• 제31권4호
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• pp.215-230
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• 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.

• 미생물학회지
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• 제49권1호
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• pp.24-29
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• 2013

본 연구는 prebiotics와 probiotics가 in vitro 배양조건에서 돼지 장내 미생물 및 발효산물에 미치는 영향에 대하여 검토 하였다. prebiotics로써 이소말토-올리고당(IMO), 부분분해 치커리이눌린(CI), 라피노스(RA), 사이클로덱스트린(CD)을 사용하였으며 probiotics로는 Lactobacillus reuteri를 사용하였다. In vitro 발효시험은 육성돈 사료를 소화효소로 가수분해 시킨 사료와 5%의 돈분 그리고 prebiotics와 probiotics를 첨가 또는 무첨가하여 24시간 동안 배양시켰다. 배양 후 발효액 내의 미생물, 가스, pH, 암모니아, 황화수소, 단쇄지방산을 분석하였다. 엔테로박테리아는 prebiotics와 probiotics 첨가구가 대조구와 비교하여 유의적으로 감소하였으며, 락토바실러스 수는 유의적으로 증가하였다. 발효액의 pH는 대조구에 비하여 첨가구에서 낮았으며 prebiotics보다 prebiotics+probiotics 첨가구에서 더욱 낮았다. 암모니아, 황화수소 및 스카톨의 농도는 prebiotics+probiotics 구보다 prebiotics 첨가시 유의적으로 감소하였다. 단쇄지방산은 prebiotics 보다 prebiotics+probiotics 구에서 유의적으로 많이 생성되었다. 본 시험의 결과 prebiotics 첨가는 암모니아, 황화수소 및 스카톨의 농도를 감소시키는데 효과가 있었으며, prebiotics+probiotics는 유산균과 단쇄지방산의 농도를 증가시키는 효과가 있었다. In vitro에서 얻어진 실험 결과가 실제로 돼지에 급여 시 같은 결과가 얻어질런지에 대한 추가적인 연구가 필요하다.