Effect of Ultrafine Powder of Gastrodiae Rhizoma in Improving Learning and Memory Ability of Vascular Dementia Rats by Regulating Cholinergic System / 中国实验方剂学杂志

Objective:To investigate whether ultrafine powder of Gastrodiae Rhizoma （UPG） can alleviate the learning and memory impairment of vascular dementia rats and delay the process of VD， and whether this effect is related to the release of acetylcholine （Ach） through the regulation with acetylcholinesterase （AChE） and choline acetyltransferase （ChAT） and control of cholinergic system. Method:SD rats were randomly divided into sham operation group， UPG low dose group （0.45 g·kg-1）， UPG high dose group （1.8 g·kg-1） and Huperzine A group （80 μg·kg-1）， with 12 rats in each group. The drug administration groups were given orally drugs once a day for 8 weeks， and sham group and model group were given orally the same amount of distilled water. The learning and memory ability of the rats with VD were evaluated by the Morris water maze. Htoxylin eosin（HE） staining was used for pathomorphological observation of hippocampus CA1 area of the rats. The content of Ach was determined by enzyme-linked immunosorbent assay（ELISA）， AChE and ChAT protein expressions were detected by Western blot， and expression of ChAT in hippocampus CA1 area was observed by immunohistochemistry. Result:Compared with the sham operation group， the escape latency of the model group was significantly increased （P<0.01）， and the frequency of crossings platform and the time of staying in the target quadrant were reduced significantly （P<0.01）. HE staining of hippocampal tissues from VD rat showed neuron disorders， loss and degeneration and necrosis， pyknosis of the nucleus and light coloration of the cytoplasm. The level of acetylcholine in the hippocampus was significantly decreased by ELISA （P<0.05）， the expression level of AChE protein was significantly up-regulated， and the expression level of ChAT protein was significantly down-regulated （P<0.01）. Compared with model group， each administration group could significantly reduce the escape latency of the model rats， and significantly increase the frequency of crossing platform and the time of staying in the target quadrant （P<0.01）， the content of Ach was significantly increased （P<0.05）， the expression of AChE protein was significantly down-regulated （P<0.01）， while the expression of ChAT protein was significantly up-regulated （P<0.01）. Conclusion:UPG improves the learning and memory ability of vascular dementia rats， and its mechanism may be related to the increase of Ach， ChAT level and the decrease of AChE level.

Electrostatic dry powder coated moisture barrier films for Compound Danshen Tablets / 中草药

Objective: Using ultrafine hydroxypropyl cellulose (HPC) powders as coating material to prepare moisture barrier coating film for Compound Danshen Tablets by an innovative electrostatic powder coating technology. The effects of coating prescription and process parameters on coating efficiency and coating film properties were investigated, so as to provide new ideas for moistureproof coating of moisture sensitive traditional Chinese medicine such as Compound Danshen Tablets. Methods: Free films were prepared by applying an electrostatic deposition process, and the effects of liquid plasticizer on the mechanical properties and the water vapor permeability were investigated. And the Compound Danshen Tablets were dry coated with ultrafine powders by the electrostatic coating technology. The effects of coating formulations and processing conditions on the moisture sorption behavior of the barrier film coated tablets were studied. Results: The coating efficiency could be manipulated by adjusting the charging voltage of the electrostatic spray gun and the amount of the liquid plasticizer. Compared with static curing process, dynamic curing process was capable to produce a satisfactory film with an enhanced moisture barrier function for the herbal medicines. The best coating process parameters were plasticizer spraying time 3 min and titanium dioxide addition ratio 1%. The minimum hygroscopicity was achieved when the coating level was increased to 6.7%. Conclusion: The moisture-protective effect by using a novel electrostatic coating technology with ultrafine powders was efficiently achieved, suggesting that it was a promising alternative for the protection for the moisture sensitive drugs.

Intestinal absorption properties of Gastrodiae Rhizoma powder with different particle size by circulation pass perfusion model in rats / 中国中药杂志

This study is to study the absorption properties of different particle size of Gastrodiae Rhizoma powder in rats. In vivo circulation pass perfusion model combined with ultra high performance liquid chromatography-mass spectrometry(UPLC-MS/MS) method was used to determine the cumulative absorption of each component in different particle size of Gastrodiae Rhizoma powder, and the effect of different particle size, different concentrations, different intestine segments and bile on the intestine absorption of gastrodin and other compositions in Gastrodiae Rhizoma powder was investigated to illuminate the absorption properties and compare the absorption difference of gastrodin and other compositions in Gastrodiae Rhizoma powder in different particle size. The results showed that the absorption of gastrodin in each intestinal segment has no significant difference, pointing out that gastrodin may be passive absorption and the absorption of barrison glycosides may be active absorption; the absorption of gastrodin in ultrafine powder was better than that of common powder and superfine powder of Gastrodiae Rhizoma; the absorption of these barrison glycosides was good in ultrafine powder of Gastrodiae Rhizoma under the high concentration. However, an appropriate degree of superfine grinding can promote the absorption of active ingredients of Gastrodiae Rhizoma. This test can provide information for the deep development of Gastrodiae Rhizoma.

Comparison of Effect of Fine Powder and Ultrafine Powder of Dendrobium nobile Stem on Intestinal Transporters of Rats / 中国实验方剂学杂志

Objective:To compare the contents of alkaloids from fine and ultrafine powder of Dendrobium nobile stem in rat plasma,and investigate the effect of D. nobile stem with different particle sizes on gene expression of intestinal transporters. Method:Rats were randomly divided into the blank group,fine powder group of D. nobile stem(0.25 g·kg-1) and ultrafine powder group of D. nobile stem(0.25 g·kg-1).The rats were gavaged every 6 h for 5 days.The samples of rat plasma and small intestine were collected.The plasma samples were detected with UPLC-MS.The chromatography separation was performed on a Hypersil Gold C18 column(2.1 mm×150 mm,1.9 μm) with acetonitrile-0.1%formic acid solution as mobile phase for gradient elution.Electrospray ionization (ESI) was applied and operated in positive ion mode.The mRNA expression of multidrug resistance protein 1(MDR1),oligopeptide transporter protein 1(PEPT1),organic cation transporter protein 2(OCT2),breast cancer resistance protein 1(BCRP1),monocarboxylate transport protein 1(MCT1) and multidrug resistance related protein 2(MRP2) in small intestine were quantified by real time fluorescence quantitative polymerase chain reaction. Result:After intragastric administration of fine and ultrafine powder of D. nobile stem,dendrobine,mubironine B and dendramine could be detected in rat plasma.The contents of dendrobine and dendramine in the ultrafine powder group were significantly higher than that in the fine powder group(PD. nobile stem(PPD. nobile stem(PConclusion:Compared with the fine powder group of D. nobile stem,the plasma concentrations of dendrobine and dendramine in the ultrafine powder group are significantly increased,it may be related to the intestinal transporters of MDR1 and BCRP1.These results can provide experimental basis for selecting particle size of D. nobile stem.

Comparison of in Vitro Dissolution of Active Ingredients in Gastrodiae Rhizoma Powder with Different Particle Size / 中国实验方剂学杂志

Objective: To compare in vitro dissolution behaviors of active ingredients (gastrodin,parishin A,p-hydroxybenzyl alcohol,parishin B and parishin C) in Gastrodiae Rhizoma powder with different particle size.Method: In vitro dissolution of Gastrodiae Rhizoma powder in different dissolution media (water,artificial gastric juice and artificial intestinal juice) were detected by stirring paddle method.Dissolution of these five components in Gastrodiae Rhizoma powder with different particle size was determined by HPLC,mobile phase was acetonitrile-0.1% phosphoric acid solution for gradient elution,column temperature was set at 40℃ and detection wavelength was 220 nm.Result: In water and artificial intestinal juice,the dissolution rates of five active components in three kinds of Gastrodiae Rhizoma ultrafine powders were higher than that of the fine powder and the finest powder;in artificial gastric juice,the dissolution rates of gastrodin and p-hydroxybenzyl alcohol in Gastrodiae Rhizoma ultrafine powders were higher than that of the other powders,and the dissolution rate of parishin A in Gastrodiae Rhizoma ultrafine powders was lower than that of the other powders.Conclusion: An appropriate degree of superfine grinding can promote the dissolution of active ingredients in Gastrodiae Rhizoma,but not as fine as possible.The dissolution medium has an obvious influence on the dissolution behaviors of active components,which provides a reference for screening optical particle size of Gastrodiae Rhizoma powder in clinical application.

Preventive effect and mechanism of ultrafine powder of Dendrobium candidum on photoaging model mice / 中国中药杂志

Chinese herbal medicine ultrafine powder has become a research hotspot for the addition of cosmetic raw materials. Dendrobium candidum is a traditional Chinese herbal medicine. Its extract and stem extract are already cosmetic raw materials and its water extract has the effect of preventing photoaging,but D. candidum ultrafine powder has not been accepted as a raw material for cosmetics,and no relevant research on photoaging prevention has been reported. In this experiment,the ultra-fine powder and fine powder of D. candidum to prevent photoaging were observed and compared,and its mechanism of action was discussed to provide a basis for the prevention of skin photoaging products. Seventy-two female ICR mice were randomly divided into normal group,model group,solvent group,titanium dioxide(Ti O2) group,isooctyl salicylate(2-ES) group,D. candidum ultrafine powder 1(DP1),ultrafine powder 2(DP2) and fine powder(DP3) groups. The photoaging model was established by ultraviolet irradiation for 8 weeks,and the model was intervened while modeling. The skin wrinkle grade,elastic parameters,skin microcirculation blood flow,skin structure and pathological changes(skin thickness,skin collagen fiber,elastic fiber) were observed,the skin transforming growth factor-β1(TGF-β1),Smad3 levels were determined,and the type Ⅰ and type Ⅲ collagen,matrix metalloproteinase-1(MMP-1),activated protein-1(AP-1),VEGF expression were detected. The results showed that ultrafine powder(DP1,DP2) significantly reduced the wrinkle level and skin blood flow of the model mice(P<0. 05,P<0. 01); DP1,DP2 and DP3 could significantly reduce the thickness of the epidermis(P<0. 001),improve collagen fiber,elastic fiber hyperplasia,and distortion and decrease VEGF expression,and DP1 is better than DP2 and DP3; each group could up-regulate type Ⅰ collagen,down-regulate type Ⅲ collagen,AP-1,MMP-1 protein expression,and DP1 improvement optimal. However,it has no obvious effect on TGF-β1 and Smad3. The ultrafine powder and fine powder of D. candidum have certain preventive effect on photoaging,and the effect of ultrafine powder is better than that of fine powder. Ultrafine powder may down-regulate the expression of type Ⅲ collagen,AP-1 and MMP-1 by up-regulating type Ⅰ collagen. Inhibition of collagen degradation plays a role in preventing photoaging.

Optimization of Ultrafine Pulverization Technology in Chaige Tuire Powder / 中国药房

OBJECTIVE:To optimize the ultrafine pulverization technology in Chaige tuire powder;to compare the content and microcharacteristics between ultrafine powder and ordinary powder. METHODS:Using contents of 3 active ingredients(puera-rin,glycyrrhizin and baicalin)and powder d(0.5)as main indexes,bulk density,angle of repose and microcharacteristic as refer-ence indexes,orthogonal test was designed to optimize the initial particle size,moisture and pulverized frequency in ultrafine pul-verization technology. Contents of 3 active ingredients of ultrafine powder and ordinary powder(over 65/80 mesh sieve)and obser-vation results of calcium oxalate crystal under microscope were compared. RESULTS:The optimized technology was as follow as over 65 mesh sieve,moisture of 2.5%preliminary powder in 60 Hz of frequency for pulverization. In verification test,d(0.5)aver-age value of 3 ultrafine powder samples was 31.5 μm(RSD=0.45%,n=3);contents of puerarin,glycyrrhizin and baicalin were 0.232 mg/g(RSD=1.31%,n=3),0.212 mg/g(RSD=1.62%,n=3),8.962 mg/g(RSD=0.89%,n=3),respectively,which were increased about 30%-40% than in ordinary powder(0.158,0.15669,6.140 mg/g). There were no or little bundles of calci-um oxalate crystal that is common in ordinary powder. CONCLUSIONS:Optimized ultrafine pulverization technology is stable and feasible;contents of 3 active ingredients in Chaige tuire ultrafine powder are higher and calcium oxalate crystal are litter than ordi-nary powder,which possibly reduces the adverse reactions in clinical application.

Physicochemical properties and in vitro dissolution behavior of active ingredients in ultrafine powder of Eucommia ulmoides / 中草药

Objective: Comparing the differences about physicochemical properties and in vitro dissolution behavior of active ingredients between ultrafine powder and common powder of Eucommia ulmoides to provide the experimental evidence for the ultrafine powder application and the control of particle size. Methods: Ultrafine powders were produced by using ultra mill. Particle size, cell wall breaking rate, morphology, and dissolution were used to evaluate the effect of particle size on microcharacteristic and dissolution behavior of powders of E. ulmoides. Results: There were significant differences between ultrafine and common powders of microcharacteristic. The extraction rates and dissolution rates of the active ingredients of ultrafine powders were higher than those of common powders. Conclusion: An appropriate degree of superfine grinding can increase the wall-breaking rate and promote the dissolution of active ingredients of E. ulmoides, and the dissolution medium has an obvious influence on the dissolution rates. The application of ultrafine grinding technology to E. ulmoides is feasible.

Comparison on in vitro dissolution behavior of notoginsenoside R1, ginsenosides Rb1 and Rg1 between ordinary fine and ultrafine powder of Panax notoginseng / 中草药

Objective: To compare the dissolution behavior of notoginsenoside R1, ginsenoside Rb1 and Rg1 between the ordinary fine and ultrafine powder of Panax notoginseng and to investigate the effect of micronization on the dissolution of saponin ingredients in P. notoginseng. Methods: The oar method was adopted. The in vitro dissolution of the three kinds of saponins including notoginsenoside R1, ginsenoside Rg1 and Rb1 in different particle sizes was determined by HPLC. The dissolving rates of the powder in various particle sizes were compared. Results: The dissolving rates of the three kinds of saponins were greatly increased after ultramicro-pulverization. Conclusion: The ultramicro-pulverization is helpful to the dissolution of saponins in P. notoginseng pieces, and the particle size of the powder exerts the great influence on the dissolution of the three kinds of saponins.

Comparison of Dissolution of Corydalis yanhusuo Fine Powder and Its Ultrafine Powder / 中国药房

OBJECTIVE:To investigate the dissolution of Corydalis yanhusuo fine powder and its ultrafine powder in order to provide theory basis for improving the bioavailability of preparation.METHODS:The paddle method was applied to prepare test sample solution and HPLC was used to determine the content of tetrahydropalmatine.The dissolution of C.yanhusuo fine powder and its ultrafine powder were calculated.RESULTS:The dissolution and dissolution rate of C.yanhusuo ultrafine powder were all higher than its fine powder.CONCLUSION:Micronization contributes to the dissolution of effective components.

Extraction Rates of Flavonoids from Ultrafine Powder vs.Fine Powder of Gleditsia sinensis / 中国药房

OBJECTIVE:To compare the extraction yield of total flavonoids from fine powder vs.ultrafine powder of Gleditsia sinersis.METHODS:The absorbance was detected under a wavelength of 510 nm by ultraviolet spectrophotometry. The extraction rates of flavonoids from fine powder vs.ultrafine powder of Gleditsia sinersis were computed.RESULTS:The extraction rate of flavonoids from ultrafine powder was 29.1%higher than that from the fine powder of Gleditsia sinersis. CONCLUSION:The extraction rate of flavonoids was increased by superfine comminution.

Preparation of nanometer crystalline powder of dental ZrO_2 ceramics by heterog eneous azeotropic distillation / 实用口腔医学杂志

Objective: To explore the preparation methods of nanomete r powder of ZrO 2 for dental application. Methods:Zirconia gel wa s dehydrated by heterogeneous azeotropic distillation process and n-butanol was used as azeotropic solvent. The properties of ultrafine powder obtained via dec ompression (process b), atmosphere pressure (process c) and direct ethanol-wash ing (process a) were studied. Results: After drying and calcini ng the gel, the ultrafine powder obtained from process a,b and c was about 25 n m,22 nm and 17 nm respectively. 3Y-TZP ceramic prepared with the three kinds of nanometer powder had bending strength of 660 MPa,710 MPa and 640 MPa; fracture toughness of 4.34 MPa?m 1/2 ,4.77 MPa?m 1/2 and 4.24 MPa?m 1/2 , respectively. Conclusion: By the heterogeneous azeotropic dis tillation process, zirconia ultrafine powder without hard agglomeration (d BE T=17 nm) can be obtained.