OBJECTIVETo study and compare the conventional extraction procedure with microwave assisted extraction (MAE) for some Ayurvedic Rasayana drugs and to evaluate their antioxidant potential and carry out the characterization of extracts by thin layer chromatography.

METHODSThree Ayurvedic rasayana plants Allium sativum Linn., Bombax ceiba Linn. and Inula racemosa Hook. were evaluated for an improved MAE methodology by determining the effects of grinding degree, extraction solvent, effect of dielectric constant and duration of time on the extractive value. Antioxidant potential of all three drugs was evaluated with 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity and reducing power was determined by using Gallic acid as standard. Further thin layer chromatographic (TLC) analysis was performed on pre-activated Silica Gel G plates and Rf value were compared with those reported for the important biomarkers.

RESULTSThe total extractive value for Allium sativum Linn. was 36.95% (w/w) and 49.95% (w/w) for ethanol extraction respectively. In case of Bombax ceiba Linn. the yield of aqueous extract by MAE was 50% (w/w) compared to 42% (w/w) in ethanol (50% v/v). Percent yield of Inula racemosa Hook. in aqueous extract was found to be 27.55% (w/w) which was better than ethanol extract (50%) where the yield was 25.95% (w/w). Upon antioxidant activity evaluation. sativum extract showed an absorbance of 0.980±0.92 at concentration of 500 μg with maximum reducing capacity. This was followed by. ceiba Linn. 0.825±0.98 and. racemosa Hook. with 0.799±2.01 at a concentration of 500 μg. TLC based standardization of. sativum Linn. extract shows single spot with Rf value of 0.38, B. ceiba Linn. extract shows Rf values were 0.23, 0.58, 0.77, 0.92 and I. racemosa Hook. extract spot had a Rf value of 0.72.

CONCLUSIONSA significant improvement in extractive values was observed as a factor of time and other advantages by using MAE technology. All three drugs have high antioxidant potential and a TLC profiling similar to reported ones. The presence of fructan type polysaccharide can be further utilized for bioactivity directed fractionation and evaluation of immunomodulatory activity.

Antioxidants ; pharmacology ; Biphenyl Compounds ; chemistry ; Chromatography, Thin Layer ; methods ; Ethanol ; chemistry ; Free Radical Scavengers ; pharmacology ; Inhibitory Concentration 50 ; Medicine, Ayurvedic ; Microwaves ; Oxidation-Reduction ; drug effects ; Pharmaceutical Preparations ; isolation & purification ; Picrates ; chemistry ; Plants, Medicinal ; chemistry ; Solvents ; Time Factors

SCHWABE Company in German is the first and largest manufacturer of Ginkgo biloba preparation. The company not only has leading technology in this field, but also protects its own market effectively through the high quality of patent drafting and exactly patent layout. Based on multi-angle analysis for patent portfolio of G. biloba preparation at application time, legal status, globally layout, Chinese layout, the article provides technical reference of research and development of G. biloba, also provides valuable experience of traditonal Chinese medicine patent portfolio layout for Chinese enterprises.
Drug Industry ; economics ; legislation & jurisprudence ; trends ; Ginkgo biloba ; chemistry ; Humans ; Patents as Topic ; legislation & jurisprudence ; Phytotherapy ; economics ; trends ; Plant Preparations ; isolation & purification ; Technology, Pharmaceutical ; economics ; trends

OBJECTIVETo investigate the mechanism of drug resistance of carbapenems-resistant Acinetobacter baumannii (CRAB) in burn patients and the antimicrobial activity of a combination of drugs against this bacteria in vitro.

METHODSA total of 135 strains of Acinetobacter baumannii (AB) from wound excretion, sputum, and venous catheter wall of patients hospitalized in our department from January 2011 to July 2013 were collected individually. Drug resistance of 135 strains of AB to 12 antibiotics commonly-used in clinic was detected using K-B paper diffusion method. Among the CRAB strains, double-disk synergy test was used to screen metallo-β-lactamase (MBL)-producing strains, and the drug resistance rates between MBL-producing strains and non-MBL-producing strains were compared. Minimal inhibitory concentration (MIC), 50% MIC (MIC50), and 90% MIC (MIC90) of cefoperazone/sulbactam, imipenem, cefepime, ampicillin/sulbactam, and amikacin used alone against MBL-producing CRAB were determined by broth microdilution method. MIC, MIC50, and MIC90 of amikacin respectively combined with imipenem, cefoperazone/sulbactam, cefepime, or ampicillin/sulbactam against MBL-producing CRAB were determined by checkerboard method with diluted agar. Fractional inhibitory concentration (FIC) index was calculated to determine the antibacterial effect of each combination of two antibiotics. Synergy with FIC lower than or equal to 0.5, or additivity with FIC higher than 0.5 and lower than or equal to 1.0 was regarded as effective, and indifference with FIC higher than 1.0 and lower than or equal to 2.0 or antagonism with FIC higher than 2.0 was regarded as ineffective. The effective rate was calculated. Data were processed with Chi-square test.

RESULTSThe resistant rates of the 135 strains of AB to imipenem, meropenem, and ceftazidime were high, and those of piperacillin/tazobactam and ampicillin/sulbactam were low. A total of 120 strains of CRAB was screened, accounting for 88.89%, among which the MBL-producing strains accounted for 78.33% (94/120). The resistant rates of MBL-producing strains to piperacillin/tazobactam, imipenem, meropenem, piperacillin, and cefepime were respectively 59.5%, 87.2%, 93.5%, 87.0%, 86.0%, and they were significantly higher than those of non-MBL-producing strains (respectively 43.0%, 81.3%, 87.5%, 78.4%, 64.0%, with χ(2) values from 4.571 to 8.260, P < 0.05 or P < 0.01). Among the inhibition concentrations of each of the 5 antibiotics used alone against MBL-producing strains, MIC, MIC50, and MIC90 of ampicillin/sulbactam were the lowest, respectively 4.00, 16, 64 µg/mL, while those of cefepime were high, respectively 32.00, 128, 512 µg/mL. MIC, MIC50, and MIC90 of amikacin combined with each of the other 4 antibiotics were decreased from 50.00% to 98.44% as compared with that of single administration of each antibiotic. Among the 94 strains of MBL-producing CRAB, the synergic, additive, indifferent, and antagonistic effects were respectively observed in 40, 33, 6, and 15 strains applied with combination of amikacin and ampicillin/sulbactam; 42, 30, 5, 17 strains applied with combination of amikacin and cefoperazone/sulbactam; 38, 15, 19, 22 strains applied with combination of amikacin and cefepime; 34, 2, 37, 21 strains applied with combination of amikacin and imipenem, among which the antibacterial effective rates decreased successively, respectively 77.7%, 76.6%, 56.4%, and 38.3%. The former two rates were respectively significantly higher than the latter two rates (with χ(2) values from 8.618 to 29.889, P values below 0.01).

CONCLUSIONSProduction of MBL is the main mechanism of resistance of the CRAB isolated from burn patients hospitalized in our department against carbapenems in about 3 years. The antibacterial effects of amikacin combined with each of the former-mentioned 4 agents are better than those of each of the five antibiotics used singly, and the effects are particularly obvious when combining amikacin with compound agent containing enzyme inhibitors.

Acinetobacter Infections ; drug therapy ; microbiology ; Acinetobacter baumannii ; drug effects ; isolation & purification ; Ampicillin ; pharmacology ; Anti-Bacterial Agents ; pharmacology ; Carbapenems ; pharmacology ; Cephalosporins ; pharmacology ; Drug Resistance ; Humans ; In Vitro Techniques ; Microbial Sensitivity Tests ; Penicillanic Acid ; analogs & derivatives ; pharmacology ; Pharmaceutical Preparations ; Piperacillin ; pharmacology ; Sulbactam ; pharmacology ; Thienamycins ; pharmacology ; beta-Lactamase Inhibitors ; pharmacology

The purpose of this study is to investigate the applicability of a natural swelling matrix derived from boat-fruited sterculia seed (SMS) as the propellant of osmotic pump tablets. The sugar components, static swelling, water uptake and viscosity of SMS were determined and compared with that of polythylene oxide (WSR-N10 and WSR-303). Both ribavirin and glipizide were used as water-soluble and water-insoluble model drugs. Then, the monolayer osmotic pump tablets of ribavirin and the bilayer osmotic pump tablets of glipizide were prepared using SMS as the osmotically active substance and propellant. SMS was mainly composed of rhamnose, arabinose, xylose and galactose and exhibited relatively high swelling ability. The area of the disintegrated matrix tablet was 20.1 times as that at initial after swelling for 600 s. SMS swelled rapidly and was fully swelled (0.5%) in aqueous solution with relative low viscosity (3.66 +/- 0.03) mPa x s at 25 degrees C. The monolayer osmotic pump tablets of ribavirin and the bilayer osmotic pump tablets of glipizide using SMS as propellant exhibited typical drug release features of osmotic pumps. In conclusion, the swelling matrix derived from boat-fruited sterculia seed, with low viscosity and high swelling, is a potential propellant in the application of osmotic pump tablets.
Arabinose ; chemistry ; isolation & purification ; Chemistry, Pharmaceutical ; Delayed-Action Preparations ; Drug Carriers ; Galactose ; chemistry ; isolation & purification ; Glipizide ; administration & dosage ; chemistry ; Osmosis ; Plants, Medicinal ; chemistry ; Rhamnose ; chemistry ; isolation & purification ; Ribavirin ; administration & dosage ; chemistry ; Seeds ; chemistry ; Solubility ; Sterculiaceae ; chemistry ; Tablets ; Technology, Pharmaceutical ; methods ; Viscosity ; Water ; Xylose ; chemistry ; isolation & purification

OBJECTIVETaking alkaloids and iridoid as the study, relationships of quantitative molecular structure and transmission rate on UF membrane were developed initially at exploring the mechanism of UF in Chinese herb decoction and to lay a foundation for the optimal design of membrane technology in the production of Chinese drugs preparation.

METHODThe transmission rate of eight alkaloids and iridoid compounds in three UF membranes was determined, and quantitative structure-property relationships between quantitative molecular structure and transmission rate were developed by the data mining method of PLS or SVM.

RESULTQuantitative structure-property relationship models of three membranes were developed by the data mining method of PLS or SVM, correlation coefficients were all greater than 0.9. The parameters in the models included LUMO, AlogP, CMR, K&H2, K&H3.

CONCLUSIONThe relationship of UF transmission rate of these eight compounds and their molecular weight are not simply linearly dependent, the main factors which affect the UF transmission rate are capacity of gain or loss electron, hydrophilicity or hydrophobic and compound spatial structure.

Alkaloids ; chemistry ; isolation & purification ; pharmacology ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Iridoids ; chemistry ; isolation & purification ; pharmacology ; Molecular Weight ; Permeability ; Pharmaceutical Preparations ; chemistry ; isolation & purification ; Quantitative Structure-Activity Relationship ; Ultrafiltration ; methods

In recent years, more and more researchers focus on the selectivity of RP-HPLC columns. Among these columns, C18 column is the most commonly used the column. Yet even the same filler can not give us the same separation effect with the columns of different brands and different types, therefore, it is important to choose the suitable HPLC column for carrying out an experiment. After study in recent years, some column classification, selection methods (e.g.: column parameter method, F value method) have been achieved and contributed to the finding of suitable columns and reducing the blindness of column selection. This paper summarizes the advantages of these methods and their limitations in the application process, and gives some advice and expectations to pharmaceutical analysis works based on the works of other researchers.
Chromatography, High Pressure Liquid ; methods ; Chromatography, Reverse-Phase ; instrumentation ; methods ; Drug Contamination ; Pharmaceutical Preparations ; isolation & purification

Artificial neural network (ANN) is a multi-objective optimization method that needs mathematic and statistic knowledge which restricts its application in the pharmaceutical research area. An artificial neural network parameters optimization software (ANNPOS) programmed by the Visual Basic language was developed to overcome this shortcoming. In the design of a sustained release formulation, the suitable parameters of ANN were estimated by the ANNPOS. And then the Matlab 5.0 Neural Network Toolbox was used to determine the optimal formulation. It showed that the ANNPOS reduced the complexity and difficulty in the ANN's application.
Chemistry, Pharmaceutical ; Delayed-Action Preparations ; Drug Design ; Ligusticum ; chemistry ; Neural Networks (Computer) ; Pyrazines ; administration & dosage ; isolation & purification ; Software ; Tablets

Yinqiaojiedu honeyed pills were equally divided into 1/4, 1/8, 1/12, and 1/16 parts. The materiomics release rates within 12 h of the intact Yinqiaojiedu honeyed pills and the divided granules were determined by the paddle method with a rotate speed at 100 r x min(-1), and the materiome was quantified by UV-scan and Kalman filter methods. The intact Yinqiaojiedu honeyed pills behaved typical sustained release profiles, while the well-divided portions also maintained a sustained release profile over 2-4 h. The release rates were well correlated with the extents for the divisions of the pills. The Weibull distribution parameters, Td and T50, were reduced in line with the particle size, indicating that the ways of administration of the pills may play a role in the in vivo pharmacokinetics of the pills. The visualization results showed obvious difference of materiomic release synchronicities between the intact pills and the equally divided particles, and the divisions enhanced the asynchronization. Therefore the novel theory of materiomic release/dissolution kinetics of traditional Chinese medicines (TCMs) quantitatively proved the traditional dosage form, namely, honeyed pills, as a prototype of the sustained-release dosage form with a visualization of the scientific connotation to the old saying in the classics of TCM, Pills, the moderate ones in action. In terms of materiome increase for each period of the release profiles, the materiomic release synchronicity was visually demonstrated. The novel theories provided methodological basis for the evaluation of traditional dosage forms and the design of the modern drug delivery systems for TCMs.
Delayed-Action Preparations ; Drug Combinations ; Drug Delivery Systems ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; isolation & purification ; pharmacokinetics ; Kinetics ; Medicine, Chinese Traditional ; Particle Size ; Plants, Medicinal ; chemistry ; Solubility ; Technology, Pharmaceutical ; methods

Pellets are multiple-unit drug delivery system, which have good fluidity, release stability and uniformity. With preparation techniques and excipient materials gradually established, pellets play an important part in the development of sustained/controlled release drug delivery system. The recent advances in pellets including the release mechanism, preparation methods, excipients and the characteristics in vivo for the sustained/controlled release pellets in traditional Chinese medicine (TCM) were reviewed in order to provide the strategies and rational methods for further investigations and applications.
Animals ; Capsules ; Delayed-Action Preparations ; chemistry ; Drug Delivery Systems ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; isolation & purification ; Humans ; Microspheres ; Plants, Medicinal ; chemistry ; Polyethylene Glycols ; chemistry ; Technology, Pharmaceutical ; methods

OBJECTIVETo prepare sustained-release microsphere containing extract of Sanguis Draconis and to measure its dissolution in vitro.

METHODSustained-release microsphere was prepared with polylactic acid (PLA) as carriers using the oil-in-water (O/W) emulsion solvent evaporation method. The powder particle's characteristics of sustainded-release microsphere were evaluated comprehensively, and its dissolution characteristics in vitro were studied.

RESULTThe microsphere was round and its surface was smooth, drug-loading rate was 21.97% and the entrapment rate was 55.76%, the accumulative release percentage was 76. 71% in 16 hours.

CONCLUSIONThe sustained release effect of Sanguis Draconis microspheres was formed with potentially wide applications.

Arecaceae ; chemistry ; Delayed-Action Preparations ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Lactic Acid ; chemistry ; Microspheres ; Particle Size ; Plants, Medicinal ; chemistry ; Polyesters ; Polymers ; chemistry ; Reproducibility of Results ; Resins, Plant ; chemistry ; Technology, Pharmaceutical ; methods