The aim of this study is to prepare self-microemulsifying drug delivery system (SMEDDS) of the mixture of paeonol (Pae) and borneol (Bor). Solubility test, ternary phase diagrams and simplex lattice method were employed to screen and optimize the formulation of the mixture of Pae and Bor-loaded SMEDDS. After formed into microemulsions, the particle diameter (PD) was determined and a TEM was employed to observe the microemulsions' morphology. The contents of Pae and Bor were determined by gas chromatography. As a result, while ethyl oleate (EO) as the oil phase, cremophor EL35 (EL35) as surfactant and Transcutol HP (HP) as cosurfactant, the range of the microemulsion on the ternary phase diagram was larger than other combinations. And at a ratio of 20:45:35, the microemulsions' PD was about 34 nm and the polydispersity index (PI) was about 0.2. There were 16% of Pae, 2% of Bor, 16% of EO, 37% of EL35 and 29% of HP in the prepared SMEDDS. The preparation process of the Pae and Bor-loaded SMEDDS based on Xingbi Fang is simple and feasible. This study provides a reference for the researches on the related traditional Chinese medicine and the related components.

Objective To study the nasal mucosa absorption of paeonol ofXingbi microemulsion-based thermo-sensitive gel in rats; To evaluate the nasal mucosa absorption of medicine and the rationality of preparation form.Methods According to the nasal administration method, the blood medicine concentration of paeonol was determined at different time points.Results The nasal administration bioavailability of paeonol in Xingbi microemulsion-based thermo-sensitive gel was 78.68%, the plasma concentration reached the maximum (0.3404 μg/mL) after 3 min of administration, and the average residence time was 9.23 h. After reaching Cmax, The plasma concentration changed similar to intravenous administration of paeonol. The concentration data of paeonol in plasma was consistent with a two-compartment model, with a weight of 1.Conclusion Xingbi microemulsion-based thermo- sensitive gel has a higher bioavailability, and the preparation form was reasonable.

Objective To compare and study species homology of two kinds of Antrodia Cinnamomea; To conduct the study on quality control. Methods HPLC fingerprint of two kinds of Antrodia Cinnamomea was applied. The HPLC fingerprints were determined on an Diamonsil C18 (2) column (250 mm × 4.6 mm, 5 μm) eluted with the mobile phase consisting of 1% formic acid solution and acetonitrile in gradient mode at a flow rate of 0.8 mL/min; the detection wavelength was set at 254 nm; the column temperature was 30 ℃. Results There were 9 common peaks in the HPLC fingerprints of Antrodia Cinnamomea. The similarities varied from 0.906 to 0.995 and from 0.956 to 0.998 in 11 batches and 10 batches of two kinds of Antrodia Cinnamomea, respectively. Conclusion The method is simple and with good reproducibility, which shows that the HPLC fingerprint and infrared spectrum share similarity for two kindsof Antrodia Cinnamomea.

Objective To establish the quality standards of Gualou Guizhi Dropping Pills; To investigate the vitro dissolution. Methods HPLC was used to determine the contents of paeoniflorin, albiflorin, cinnamic acid, 6-gingerol, liquiritin, glycyrrhizic acid and liquiritigenin in the dropping pills. The vitro dissolution rate of dropping pills was determined by rotating basket method. Results The calibration curves of paeoniflorin and albiflorin were in a good linearity in the range of 0.690–6.900 μg, 0.300–2.996 μg, respectively, and the average recoveries were 101.12% and 98.52%, respectively, with RSD of 2.24%, 1.37%, respectively. Cinnamic acid was linear in the range of 0.023–0.348 μg and the average recovery was 98.21% with RSD of 2.00%. 6-Gingerol was linear in the range of 0.025–0.382 μg, and the average recovery was 99.19% with RSD of 2.18%. The calibration curves of liquiritin, glycyrrhizic acid and liquiritigenin were in a good linearity in the ranges of 0.120–2.498 μg, 0.150–2.253 μg, and 0.010–0.147 μg, respectively, and the average recoveries were 99.80%, 100.38%, and 100.62%, respectively with RSD of 2.10%, 1.91%, 1.66%, respectively. The accumulated dissolution rates of seven kinds of elements in the dropping pills all reached more than 98% in 15 min. Conclusion The method is simple and accurate, with repeatability, which can be applied to the quality control of Gualou Guizhi Dropping Pills. The vitro dissolution rates meet relevant standards.

Objective To investigate the effects of Gualou Guizhi Granules on excitatory toxic damage of PC12 induced by glutamate; To primarily explore the involved protective mechanism of Gualou Guizhi Granules. Methods Excitatory toxic damage of PC12 induced by glutamate was used to establish models. Cells were divided into normal group, glutamate group, and Gualou Guizhi Granules low- (200 μg/mL), medium- (400 μg/mL) and high-dose (800 μg/mL) groups. MTT and LDH assay methods were used to detect PC12 activity; Caspase-3 activity detection method and Annexine V/PI double staining method were used to detect cell apoptosis; Western blot and RT-PCR were used to detect Bcl-2, Bax protein and mRNA expression. Results Compared with glutamate group, MTT showed that all Gualou Guizhi Granules groups could improve PC12 activity, and LDH showed that cell activity in all Gualou Guizhi Granules groups decreased; Annexine V/PI double staining method showed that all Gualou Guizhi Granules groups could decrease the PC12 apoptosis; Caspase-3 activity detection method showed that all Gualou Guizhi Granules groups could decrease the activity of Caspase-3; Western blot and RT-PCR showed that all Gualou Guizhi Granules groups could reduce Bax expression and increase Bcl-2 expression. Conclusion Gualou Guizhi Granules have certain protective effects on excitatory toxic damage of PC12 induced by glutamate, which may be related to its anti-apoptotic activity.

OBJECTIVETo develop an HPLC method for gradient elution determination of danshensu and protocatechuic aldehyde in Shengkangling granula.

METHODThe analysis was carried on a column of Hypersil ODS2-C18 with a mobile phase consisted of methanol-1% glacial acetic acid 0-8 min (5:95), 8-11 min (6:94-5:95), 11-20 min (5:95) gradient elution at the flow rate of 1 mL x min(-1). The detection wavelength was 280 nm.

RESULTThe linearity was obtained in the range of 0.0504-0.504 microg (r = 0.9998) for tanshinol and 0.1090-1.090 microg (r = 0.9999) for protocatechuic aldehyde, respectively. The average recoveries of tanshinol and protocatechuic aldehyde in Shenkangling granula were 98.40% and 98.85%, and the RSDs were all less than 2.0%.

CONCLUSIONThe method is simple, accurate and rapid. It may be suitable for the usual quality control of tanshinol and protocatechuic aldehyde in Shengkangling granula.

Benzaldehydes ; analysis ; Catechols ; analysis ; Chromatography, High Pressure Liquid ; methods ; Dosage Forms ; Drugs, Chinese Herbal ; analysis

OBJECTIVEThe optimum conditions of SFE-CO2 extraction of Plantaginis Semen oil (SPO), the composition of SPO and its antioxidant activities of SPO were all investigated in this paper.

METHODResponse surface method (RSM) was used to establish the mathematical model of SFE-CO2 extraction of SPO to obtain the optimum conditions based on Single factor experiments. Fatty acid compositions and contents of SPO were tested by GC-MS, and antioxidant activities of SPO were studied by DPPH and ABTS free radical elimination method.

RESULTThe optimum conditions obtained through RSM analysis were as follows: extraction tempreture 70 degrees C, extraction pressure 30 MPa, extraction time 120 min and flow rate 30 L x h(-1). Under the optimal condition, predicted value was 35.91%, while the experimental value was 35.07%. The experimental values agree with the predicted from the regression model with a relative error less than 5%. The main components of SPO were 9,12,15-octadecatrienoic acid, 8,11-octadecadienoic acid, octadecanoic acid and hexadecanoic acid. Most of the fatty acids were polyunsaturated fatty ones, whose quantities were obtained more than 88%. The IC50DPPH and IC50ABTS were 1.13, 3.57 g x L(-1) respectively in DPPH and ABTS assay.

CONCLUSIONOptimization of the extraction process by RSM of SPO is convenient and feasible. SPO has good antioxidant activity and is worth to develop for application.

Antioxidants ; chemistry ; isolation & purification ; Carbon Dioxide ; chemistry ; Chromatography, Supercritical Fluid ; methods ; Cupressaceae ; chemistry ; Gas Chromatography-Mass Spectrometry ; Plant Oils ; chemistry ; isolation & purification

OBJECTIVETo prepare the nasal thermosensible gels of Chinese medicine Xingbi and study the release mechanism.

METHODThe gels were prepared by using P407 as the gel matrix and P188 and PEG 6000 were used to adjust the gelatination temperature. The formulations were screened by the method of orthogonal test. Mathematic models were used to imitate the drug release.

RESULT20% poloxmar 407, 2% poloxmar 188 and 2% PEG 6000 were suitable to Chinese medicine Xingbi thermosensitive gel in situ. Nasal thermosensible gels of Chinese medicine Xingbi was gelated at the temperature between 32-34 degrees C and the dissolution curves in vitro showed that the drug release could be best described by the Higuchi equation.

CONCLUSIONThe formulation of the nasal thermosensible gels of Chinese medicine Xingbi is reasonable and it is worth doing further research.

Chemistry, Pharmaceutical ; methods ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Gels ; chemistry ; Humans ; Nose Diseases ; drug therapy ; Temperature