Pellets

颗粒
  • 文章类型: Journal Article
    作为颗粒的前体,挤出物对粒料的成型质量有直接影响。因此,探索了挤出物的表面粗糙度与纯微晶纤维素(MCC)配方和含中药(TCM)配方的颗粒的成型质量之间的相关性。MCC用作造粒剂,用混合器转矩流变仪(MTR)来指导润湿剂的最佳用量,选择中药提取物(载药量为20%至40%)作为模型药物,在相同的挤出滚圆工艺条件下制备挤出物和微丸。通过显微镜和纹理分析仪分析了挤出物的表面粗糙度和纹理参数,分别,并对颗粒的质量进行了评价。纯MCC配方的挤出物粗糙度随着水添加量的增加而降低,然后增加。而含有中药提取物的处方的挤出物粗糙度呈先升高后降低的趋势。水的加入影响了挤出物的性能,中药提取物分子填补了MCC结构中的空白,导致粗糙的表面。在最佳水添加水平下,中药处方的挤出物粗糙度明显大于纯MCC处方的挤出物粗糙度,产生理想的颗粒。
    As the precursor of pellets, the extrudate has a direct impact on the molding quality of the pellets. Therefore, the correlation between the surface roughness of the extrudates and the molding quality of pellets with pure microcrystalline cellulose (MCC) formulations and those containing traditional Chinese medicine (TCM) formulations was explored. MCC was used as a pelleting agent, mixer torque rheometry (MTR) was used to guide the optimal dosage of the wetting agent, and TCM extracts (drug loadings of 20% to 40%) were selected as model drugs to prepare the extrudates and pellets under the same extrusion spheronization process conditions. The surface roughness and texture parameters of extrudates were analyzed via a microscope and texture analyzer, respectively, and the quality of pellets was evaluated. The extrudate roughness of the pure MCC prescription decreased and then increased with increasing water addition, while the extrudate roughness of the prescription containing TCM extracts tended to increase and then decrease. The addition of water affected the extrudate properties, with TCM extract molecules filling gaps in the MCC structure, leading to rough surfaces. The extrudate roughness of the TCM prescriptions was significantly greater than that of the pure MCC prescriptions at optimal water addition levels, resulting in ideal pellets.
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  • 文章类型: Journal Article
    丹酚酸B(SAB)是一种广泛使用的心脏保护剂,但其临床应用受到肠道吸收差和口服生物利用度低的限制。在这项研究中,首先制备SAB磷脂(SP)复合物以提高SAB的亲脂性,然后与d-葡萄糖结合以进一步增强肠道吸收。与免费SAB相比,SP或SAB和D-葡萄糖的混合物,SP和d-葡萄糖的组合显示出较高的肠吸收,这通过原位单程肠灌注(SPIP)测定中有效渗透系数(Peff)增加证明。随后,SP和d-葡萄糖的质量比为1:6,SAB的Peff最高,选择用于制备复合微丸以提高SAB的口服吸收效率。不出所料,在药代动力学研究中,获得的微丸显着提高了SAB的口服生物利用度,其特征是SAB的Cmax和AUC0-t比游离SAB增加了14.88倍和5.02倍,分别。总之,D-葡萄糖联合SP微丸可有效提高SAB的肠道吸收和口服生物利用度。
    Salvianolic acid B (SAB) is a widely used cardioprotective agent, while its clinical application was limited by poor intestinal absorption and low oral bioavailability. In this study, SAB phospholipid (SP) complex was first prepared to improve the lipophilicity of SAB and then combined with d-glucose to further enhance intestinal absorption. Compared with free SAB, SP or the mixture of SAB and d-glucose, combination of SP and d-glucose showed higher intestinal absorption evidenced by increased effective permeation coefficient (Peff) in the in situ single-pass intestinal perfusion (SPIP) assay. Subsequently, SP and d-glucose at mass ratio of 1:6, with the highest Peff of SAB, were chosen for the preparation of complexed pellets to improve oral absorption efficiency of SAB. As expected, the obtained pellets significantly enhanced oral bioavailability of SAB in the pharmacokinetic study characterized by increasing Cmax and AUC0-t of SAB by 14.88-fold and 5.02-fold than free SAB, respectively. In conclusion, combination of d-glucose in SP pellets can effectively improve the intestinal absorption and oral bioavailability of SAB.
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  • 文章类型: Journal Article
    This study aimed to evaluate growth performance and meat quality of Ujimqin lambs fed native grass hay without or with concentrate (HC) or pellets. Ninety non-castrated 6-month-old male lambs of good health and similar body weight (26.83 ± 0.26 kg) were randomly divided into three groups (five lambs per cage). The average daily gain and intake of the pellets and HC groups were significantly greater (p < .05) than those in the hay group. The carcass weight, net meat mass, loin eye area, and backfat thickness were significantly greater (p < .05) in the HC groups. The intramuscular fat was significantly greater (p < .05) in the pellets and HC groups, while the shear force was significantly decreased (p < .05) in pellets and HC groups. The C16:0, C18:0, C18:1n9c, and C18:2n6 contents were significantly greater (p < .05) in the HC and pellet groups, while the C18:3n3 content was significantly greater (p < .05) in the hay group. Collectively, the present study suggested that feeding native grass hay with concentrate or pellets improved the growth in lambs.
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  • 文章类型: Journal Article
    Articular cartilage focal lesion remains an intractable challenge in sports medicine, and autologous chondrocytes\' implantation (ACI) is one of the most commonly utilized treatment modality for this ailment. However, the current ACI technique requires two surgical steps which increases patients\' morbidity and incurs additional medical costs. In the present study, we developed a one-step cryopreserved off-the-shelf ACI tissue-engineered (TE) cartilage by seeding pellets of spheroidal cartilage stem/progenitor cells (CSPCs) on a silk scaffold. The pellets were developed through a hanging-drop method, and the incubation time of 1 day could efficiently produce spheroidal pellets without any adverse influence on the cell activity. The pellet size was also optimized. Under chondrogenic induction, pellets consisting of 40 000 CSPCs were found to exhibit the most abundant cartilage matrix deposition and the highest mRNA expression levels of SOX9, aggrecan, and COL2A1, as compared with pellets consisting of 10 000, 100 000, or 200 000 CSPCs. Scaffolds seeded with CSPCs pellets containing 40 000 cells could be preserved in liquid nitrogen with the viability, migration, and chondrogenic ability remaining unaffected for as long as 3 months. When implanted in a rat trochlear cartilage defect model for 3 months, the ready-to-use, cryopreserved TE cartilage yielded fully cartilage reconstruction, which was comparable with the uncryopreserved control. Hence, our study provided preliminary data that our off-the-shell TE cartilage with optimally sized CSPCs pellets seeded within silk scaffolds exhibited strong cartilage repair capacity, which provided a convenient and promising one-step surgical approach to ACI.
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  • 文章类型: Journal Article
    Solidification of self-microemulsifying drug delivery systems (SMEDDS) is one of the major trends to promote the transformation of self-microemulsion technology into industrialization. Here, a preliminary curcumin SMEDDS formulation was constructed to improve the druggability of curcumin, through the determination of equilibrium solubility determination, self-emulsifying grading assessment, and pseudo-ternary phase diagrams drafting. Furthermore, the optimal curcumin SMEDDS formulation consisted of 10% Ethyl oleate, 57.82% Cremophor RH 40, and 32.18% Transcutol P was obtained by the simplex lattice design. Besides, curcumin solid self-microemulsifying drug delivery system (S-SMEDDS) was developed by the extrusion and spheronization process to achieve the solidification of SMEDDS. The formulation of curcumin S-SMEDDS pellets was screened by the single factor experiment and the process parameters were investigated using the orthogonal optimization method. Subsequently, curcumin S-SMEDDS pellets were evaluated by apparent morphology characterization, redispersibility study, drug release behavior, and pharmacokinetic evaluation. Results from the pharmacokinetic study in rabbits showed that the AUC0-τ of the curcumin S-SMEDDS pellets and curcumin suspension were 5.91 ± 0.28 µg/mL·h and 2.05 ± 0.04 µg/mL·h, while the relative bioavailability was 289.30%. These studies demonstrated that S-SMEDDS pellets can be a promising strategy for curcumin industrialized outputs.
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  • 文章类型: Journal Article
    Arsenic trioxide (ATO) is first-line drug for acute promyelocytic leukemia. Clinically, the continuously slow intravenous infusion is adopted to maintain effective blood concentration and reduce toxic effects, but it causes poor patient\' compliance for a considerable infusion period. To overcome these disadvantages, we developed an oral ATO sustained-release preparation which was constructed via the ATO core pellets prepared by extrusion spheronization and followed by a coating membrane by fluid-bed technology. The prepared coated pellets displayed a round surface and uniform particle size. All in vitro release profiles of ATO pellets in different pH media and rotation speeds had no statistical difference. Importantly, the coated pellets can release completely in 12 h without obvious burst release. There was no distinct change in appearance and release behaviors in stability experiments. In vivo pharmacokinetics was studied by one-time intragastric administration of rats. Compared with free drug, the AUC0-∞ of the ATO coated pellets was 2.3-fold higher, indicating the oral bioavailability was significantly increased. Cmax decreased by about a half and Tmax extended about 15 h. In particularly, the ATO level at 96 h only decreased about 20% of Cmax , suggesting that the ATO sustained-release preparation could not only decrease the peak concentration, but also maintain a relatively constant blood concentration for a long period. Further, the in vivo absorption could be well predicted by in vitro release experiments. Therefore, the ATO sustained-release preparation formulated by the mature preparation technology, possessing satisfactory stability and improving bioavailability, had great application potentials for industrialization.
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  • 文章类型: Journal Article
    Torrefaction integrated with pelletization has gained increasingly interest as it enhances the characteristics of fuel pellets (e.g. hydrophobicity and energy density). In current study, torrefaction of furfural residue pellets (FRPs) and sawdust pellets (SPs) was performed by employing tubular reactor furnace, and quality of pellets was compared. The characteristics of both types of pellets were significantly improved with increasing torrefaction temperature from 200 °C to 300 °C and residence time from 15 min to 30 min. The highest lower heating value of 23.78 MJ/kg and energy density ratio (1.27) for torrefied furfural residue pellets (TFRPs) and 26.76 MJ/kg and 1.46 for torrefied sawdust pellets (TSPs) were achieved at 300 °C and 120 min. Increasing torrefaction temperature and residence time, the volumetric energy densities of TFRPs increased from 25.69 (at 200 °C and 15 min) to 27.59 kJ/m3 (at 300 °C and 120 min), while those of TSPs correspondingly decreased from 20.81 to 16.69 kJ/m3. The highest true densities (i.e. 2.40 and 1.85 g/cm3) and porosities (i.e. 52 and 65 v %) of TFRPs and TSPs were achieved at 300 °C and 120 min, much higher than those of un-torrefied pellets. Moisture uptake of TFRPs and TSPs at 300 °C were only 1.4 wt% and 2.0-2.8 wt%, respectively, showing strong water-resistant ability. The crystallinity of cellulose in FRPs was found higher than that of SPs, while the crystallinity of cellulose in TFRPs was found lower than that of TSPs at same process conditions. FTIR showed that O-H bond was destroyed after torrefaction for both FRP and SP.
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  • 文章类型: Journal Article
    Berberine chloride (BBR) is a pharmacokinetic profile of drug with poor bioavailability but good therapeutic efficacy, which is closely related to the discovery of BBR intestinal target. The major aim of this paper is to develop BBR intestinal retention type sustained-release pellets and evaluate their in vivo and in vitro behaviors base on the aspect of local action on intestinal tract. Here, wet milling technology is used to improve dissolution and dissolution rate of BBR by decreasing the particle size and increasing the wettability. The pellets are prepared by liquid layer deposition technology, and then the core pellets are coated with Eudragit® L30D-55 and Eudragit® NE30D aqueous dispersion. The prepared pellets show high drug loading capacity, and the drug loading up to 93%. Meanwhile, it possesses significant sustained drug release effect in purified water which is expected to improve the pharmacokinetic behavior of BBR. The pharmacokinetics results demonstrate that the half-life of BBR was increased significantly from 24 h to 36 h and the inter- and intra-subject variability are decreased compared to commercial BBR tablets. The retention test results indicate that the pellet size and Eudragit® NE30D plays an important role in retention time of the pellet, and it is found that the pellets with small particle size and high Eudragit® NE30D coating content can stay longer in the intestine than the pellets with large particle size. All in all, BBR intestinal retention type pellets are prepared successfully in this study, and the pellets show satisfactory in vivo and in vitro behaviors.
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  • 文章类型: Journal Article
    Extrusion-spheronisation method was used to prepare Rhus chinensis total phenolic acid pellets. The formula and preparation of R. chinensis total phenolic acid pellets were optimized. The formulas( drug loading capacity,diluent,wetting agent and anti-sticking agent) were determined by the single factor test with yield,appearance and performance as the indexes. The preparation was optimized by Box-Behnken design and response surface method,with the rate of extrusion,rate of spheronization and time of spheronization as the independent variables and the overall desirability value of yield,friability and roundness as the dependent variables. The optimal formula of pellets was as follows: drug loading capacity 28. 7%,MCC-lactose 9 ∶1,silicon dioxide as anti-sticking agent,and 60% ethanol as wetting agent. The optimal preparation was determined as follows: the rate of extrusion was 43 r·min-1,the rate of spheronization was 1 800 r·min-1,and the time of spheronization was 4 min. The absolute deviation between predicted value and estimated value under the conditions was less than 5. 0%,with a high degree of model fit. The preparation parameters obtained were accurate,reliable and reproducible. Under scanning electron microscopy( SEM),R. chinensis total phenolic acid pellets were uniform in diameter,round and smooth. The optimal formulation and process are stable and feasible for preparing R. chinensis total phenolic acid pellets.
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  • 文章类型: Journal Article
    Calcium looping has been proposed as one of the most promising technologies for CO2 capture to mitigate the growing problem of global warming. However, the loss in capacity and attrition are two issues lying on the way to practical application for calcium looping process. To improve CO2 capture performance and mechanical strength of CaO sorbents, a biomass templated extrusion-spheronization palletization technique was employed to manufacture porous calcium aluminate-supported CaO-based pellets. For the first time, this work investigated the granulation of calcium aluminate-supported CaO-based sorbents and also the effectiveness of three novel biomass-based pore-creating materials of straw, willow, and wheat. The results indicated that the incorporation of calcium aluminate-based supports could effectively enhance cyclic performance and stability. Besides, the 5 wt.% addition of pore-creating materials could further promote the cyclic CO2 capture capacity of calcium aluminate-supported CaO-based pellets. The pellets added with 25 wt.% calcium aluminate-based supports and 5 wt.% straw still held a good carbonation conversion of 46.45% after 50 cycles even tested under CO2-rich calcination atmospheres. In addition, the anti-attrition ability tests by friability tester (FT) demonstrated that all the prepared pellets owned an excellent degree of attrition (less than 1%). The good CO2 capture performance and mechanical strength endowed biomass-templated calcium aluminate-supported CaO-based pellets with promising prospects for practical CO2 removal.
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