To develop an ophthalmic preparation of Shedan, an in situ forming gel was prepared with the formulation containing 18% of poloxamer 407 and 5% of poloxamer 188 by response surface designs plus central composite designs. The rheology results showed that LVE range gamma should limited within 0.5%, Shedan high-frequency region, and the thixotropy recovery time is less than 5 seconds. The phase transition temperature was 33.25 °C according to curve of storage modulus and loss modulus determined by temperature scanning. Surface tension and osmometer of it determined by surface tension meter and dew point osmometer were 36.43 mN · m(-1), and 320.6 mOsm · kg(-1), respectively. Fluorescein sodium was selected as the marker to monitor the corneal residence time, and the results showed that Shedan gel could prolong drug residence for 180 min. In line with zero-order kinetics, releases of muscone and salvianolic acid B in vitro depends on gels erosion. The results of rabbit ocular irritation experiments suggested that Shedan in situ forming gel was biocompatible and nonirritant. In conclusion, a novel Shedan in situ forming gel was developed and characterized for potential drug treatment of retinal vein occlusion.
Animals ; Benzofurans ; chemistry ; Cycloparaffins ; chemistry ; Female ; Gels ; chemistry ; Male ; Ophthalmic Solutions ; Poloxamer ; chemistry ; Rabbits ; Retinal Vein Occlusion ; drug therapy ; Viscosity

GJ-4 is crocin enrichments extracted from Gardenia jasminoides J. Ellis, and our previous studies have shown that GJ-4 significantly improved learning and memory impairment induced by Aβ in mice. Herein, a memory deficit model was developed by injecting okadaic acid (OA) into the lateral ventricle of mice, and the neuroprotection and underlying mechanism of GJ-4 on neuronal injury caused by Tau hyperphosphorylation were investigated. The Animal Care & Welfare Committee, Institute of Materia Medica, CAMS & PUMC has approved all procedures (No.00000318). GJ-4 at different doses was intragastric administration to mice for 16 days. Step-down test and Morris water maze test showed that GJ-4 could significantly improve OA-induced memory impairment in mice, and reduced the loss of Nissl bodies in the hippocampus of mice. GJ-4 could also decrease the phosphorylation level of Tau protein at Ser396, Thr231 and Ser404 via increasing protein phosphatase 2A (PP2A) activity and inhibiting glycogen synthase kinase-3β (GSK-3β) activity. Besides, further researches indicated that GJ-4 could inhibit the level of oxidative stress in the brain of OA mice, reduce neuronal apoptosis and inhibit the neuroinflammation mediated by activation of astrocytes in the hippocampus of mice, and eventually achieve its effects in improving learning and memory impairment in mice. According to these findings, we anticipated that GJ-4 might be a potential therapeutic drug for Alzheimer's disease.

OBJECTIVETo find the best condition of the preparation technology of Flos Magnoliae essential oil-beta-cyclodextrin inclusion complex.

METHODL9(3(4)) table was used to examine the effects of 4 factors, and the inclusion rate of each test was determined of orthogonal test.

RESULTThe best condition was:oil:beta-cyclodextrin:water = 1:8:60 (mL:g:mL), stirring for 1 hour at 80 degrees C.

CONCLUSIONThe complex prepared on the condition aforementioned is stable and stirring has a highest inclusion rate.

Cyclodextrins ; Drug Carriers ; Drug Stability ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; Flowers ; chemistry ; Magnolia ; chemistry ; Oils, Volatile ; administration & dosage ; isolation & purification ; Plants, Medicinal ; chemistry ; Technology, Pharmaceutical ; methods ; beta-Cyclodextrins

Compared with traditional drying methods for Chinese materia medica, microwave drying technology is not only with the features of easy and convenient to operate, rapidity, good effects, well remained appearance of medicine and low energy consumption, but also with the feature of extraordinary sterilization effects at the same time with drying. This article introduced the features and effects of microwave drying and sterilization technology, reviewed its application in the TCM field, and proposed existing problems and prospects in the recent research by targeting security problems (microwave radiation and microwave residue).

AIMTo observe the antagonistic effect of hydroxysafflor yellow A (HSYA) on the platelet activating factor (PAF).

METHODSWashed rabbit platelet (WRP) aggregation and rabbit polymorphonuclear leukocytes (PMNs) aggregation induced by PAF were observed by turbidimetric assay in vitro. The PAF receptor antagonistic effect of HSYA was investigated by radio ligand binding assay (RLBA).

RESULTSIn RLBA the specific binding inhibition effect of HSYA was found to be concentration-dependent in three different [3H]PAF concentrations. In the experiments, WRP aggregation and rabbit PMNs aggregation induced by PAF (9.55 x 10(-10), 9.55 x 10(-6) mol.L-1) were both inhibited by HSYA in a concentration-dependent manner in vitro. The IC50 of HSYA to inhibit WRP and rabbit PMNs aggregation was 0.99 and 0.70 mmol.L-1, respectively.

CONCLUSIONThe PAF receptor binding can be antagonized by HSYA.

Animals ; Carthamus ; chemistry ; Cell Aggregation ; drug effects ; Chalcone ; analogs & derivatives ; isolation & purification ; pharmacology ; In Vitro Techniques ; Male ; Neutrophils ; drug effects ; Plants, Medicinal ; chemistry ; Platelet Aggregation ; drug effects ; Platelet Membrane Glycoproteins ; antagonists & inhibitors ; Quinones ; isolation & purification ; pharmacology ; Rabbits ; Receptors, G-Protein-Coupled ; antagonists & inhibitors

OBJECTIVETo prepare tuizhang gel to cure cataract, the characteristics of Tuizhang gel on the drug-releasing in vitro were evaluated by compared with Tuizhang oculentum.

METHODThe emodin and chrysophanol in the releasing mediator were determined by HPLC, and the drug releasing characteristics of Tuizhang gel and Tuizhang oculentum were studied by bag filter method.

RESULTThe emodin and chrysophanol in Tuizhang gel released (98.3, 1.1)%, (95.8, 1.8)% within 24 hours, respectively, while those in tuizhang oculentum released (10.62, 0.7)%, (10.46, 0.4)%, respectively. The emodin and chrysophanol in Tuizhang gel released more quickly and completely than in Tuizhang oculentum, so Tuizhang gel has enhanced the bioavailability.

CONCLUSIONThe Tuizhang gel is characterized by slow-release to some degree, and it shows a promising future on ophthalmic drug delivery.

Acrylic Resins ; chemistry ; Anthraquinones ; chemistry ; pharmacokinetics ; Delayed-Action Preparations ; chemistry ; pharmacokinetics ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Emodin ; chemistry ; pharmacokinetics ; Gels ; Ointments ; Plants, Medicinal ; chemistry ; Solubility ; Technology, Pharmaceutical ; methods

OBJECTIVETo optimize the process of extracting effective constituents from lotus leaf.

METHODIndependent variables were ethanol concentration reflux time and solvent fold, dependent variables were extraction rates of nuciferine and flavone in lotus leaf, central composite design and response surface methodology were used for optimization of extraction of lotus leaf.

RESULTThe optimum conditions of extraction process were 75% -80% ethanol, 2-3 hours for reflux, 20-25 fold solvent and 2 times for extraction. Bias between observed and predicted of rates of nuciferine and flavone values were 5.53%, -6.02%, respectively.

CONCLUSIONThe values observed and predicted were close to each other, which proved that the optimization of of extraction of lotus leaf by central composite design and response surface methodology was reasonable and successful.

Aporphines ; chemistry ; isolation & purification ; Flavones ; Flavonoids ; chemistry ; isolation & purification ; Loteae ; chemistry ; Plant Leaves ; chemistry ; Reproducibility of Results

OBJECTIVETo evaluate different methods by treating water-decocted liquid of 6 Chinese medical herbs and 4 co-prescription respectively with alcohol, ultrafilter, macroporousresin and clarifier.

METHODThe contents of target component in those extracts were determined with HPLC or titration, and quantitative and qualitative determination of the impurity components, such as polysaccharide and protein, was made.

RESULTEach method showed its advantages and disavantages.

CONCLUSIONDifferent method can be chosen according to the clinical and preparation demands or the characteristic of components.

Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; analysis ; isolation & purification ; Methods ; Plants, Medicinal ; chemistry ; Polysaccharides ; analysis

OBJECTIVETo observe the platelet activating factor (PAF) antagonistic effect of kaempferol.

METHODThe specific binding of [3H] PAF to rabbit platelet receptor was investigatedwith radio ligand binding assay (RLBA). Platelet adhesion induced by PAF was measured with spectrophotometry. The elevation of inner free calcium concentration in rabbit polymorphonuclear leukocytes (PMNs) induced by PAF was determined with Fura-2 fluorescent technique.

RESULTThe 1, 2 or 4 nmol x L(-1) [3H]PAF specific binding to rabbit platelet receptor was inhibited by Kae dosage dependently and the IC50 were 30.8, 74.6 and 92.0 micro mol x L(-1), respectively. The PAF induced reactions of rabbit platelet adhesion and PMNs inner free calcium concentration elevation were inhibited by Kae in a dose-dependent manner. The IC50 of Kae to inhibit platelet adhesion was 65 micromol x L(-1).

CONCLUSIONKae is effective in inhibiting the action of PAF and it is a new PAF receptor antagonist.

Animals ; Blood Platelets ; drug effects ; physiology ; Calcium ; metabolism ; Kaempferols ; pharmacology ; Male ; Neutrophils ; metabolism ; Platelet Activating Factor ; metabolism ; Platelet Adhesiveness ; drug effects ; Platelet Membrane Glycoproteins ; antagonists & inhibitors ; metabolism ; Rabbits ; Radioligand Assay ; Receptors, G-Protein-Coupled ; antagonists & inhibitors ; metabolism

AIMTo study the antagonistic effect of myricetin on platelet activing factor (PAF).

METHODSThe specific binding of [3H] PAF to rabbit platelet receptor was investigated using radio ligand binding assay (RLBA). Platelet adhesion induced by PAF was measured with spectrophotometry. The elevation of inner free calcium concentration in rabbit polymorphonuclear leukocytes (PMNs) induced by PAF was assayed by Fura-2 fluorescent technique.

RESULTSThe specific binding inhibition potency of Myr was found to be concentration-dependent. The IC50 of Myr in [3H] PAF 1, 2 and 4 nmol.L-1 were 34.8, 85.7 and 118.6 mumol.L-1, respectively. The PAF induced reactions of rabbit platelet adhesion and PMNs inner free calcium concentration increase were inhibited by Myr in a dose-dependent manner. The IC50 of Myr to inhibit platelet adhesion was 13.1 mumol.L-1.

CONCLUSIONThe specific receptor binding of PAF can be antagonized by myricetin.

Animals ; Calcium ; metabolism ; Flavonoids ; pharmacology ; Male ; Neutrophils ; metabolism ; Platelet Activating Factor ; antagonists & inhibitors ; metabolism ; Platelet Activation ; drug effects ; Platelet Adhesiveness ; drug effects ; Platelet Aggregation Inhibitors ; pharmacology ; Platelet Membrane Glycoproteins ; metabolism ; Rabbits ; Receptors, G-Protein-Coupled ; metabolism