Application of factor analysis to evaluate deformation behaviors of frequently-used tablet excipients / 药学学报

The present work is to investigate the correlation between physical properties and deformation behaviors of tablet excipients, and rank them according to their plastic performances during compaction. The excipients selected were compacted using Korsch XP1 after measuring their physical properties where the compression parameters for evaluating deformation behaviors were Heckle equation, compression work and elastic stretch in die. The correlations between compaction descriptors and physical parameters were analyzed by canonical correlation analysis, and factor analysis was simultaneously employed to synthetically assess deformation behaviors for all our samples. The canonical variables show that true density (Pa) correlated negatively with plastic coefficient (PL) and positively with yield pressure (YP); compression degree (Cp) correlated negatively with fast elastic stretch (FES) as well as YP and positively with PL. When factor scores were used in combination with original data, the plasticity of our samples was sorted and ranked as high (-0.56 < F' < 0.21), intermediate (-0.16 < F' < 0.36), or low (0.38 < F' < 0.84), which are in accord with plasticity rankings previously reported in literature. This study indicates factor analysis can be an approach to evaluate deformation behaviors of pharmaceutical powders.

Discrimination of traditional Chinese medicinal materials with different tastes based on electronic tongue / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the use of the electronic tongue in the evaluation of traditional Chinese medicinal materials with sour, bitter, sweet or salty tastes, and assess the possible application of the sensor in the evaluation of different tastes of traditional Chinese medicinal materials.</p><p><b>METHOD</b>Aqueous extracts of 22 traditional Chinese medicinal materials were measured by the electronic tongue. The data collected with the tongue was evaluated for discrimination of the samples with multivariate statistical methods: principal component analysis (PCA) and discriminant factor analysis (DFA).</p><p><b>RESULT</b>The electronic tongue was capable of discriminating between samples with different taste modalities and could also distinguish different samples eliciting the same basic taste. Twenty-two traditional Chinese medicinal materials could be classified into five clusters based on PCA. These differences seem to derive from the different tastes. DFA was applied to construct a model to discriminate traditional Chinese medicinal materials with different tastes. And the samples yielded about 88.2% accuracy for cross-validation.</p><p><b>CONCLUSION</b>We confirmed that the electronic tongue may provide an analytical procedure for classification of the samples with respect to tastes of the traditional Chinese medicinal materials.</p>

Characterization of flowability of pharmaceutical powders based on multivariate analysis method / 药学学报

The main methods of characterizing the flowability of pharmaceutical powders include repose angle method, HR method, Carr's index method, Jenike flow function method, fractal dimension method, and mass flow rate method, etc. Regarding powders with different flowabilities as the research subject, comprehensive features of pharmaceutical materials were investigated and characterized. The multivariate analysis method was employed to evaluate and analyze flowability values of the tested pharmaceutical materials. Comparing with the method of the mass flow rate, it was feasible to use multivariate analysis method to evaluate the flowability of powders. Simultaneously, the flowability of pharmaceutical materials could be ranked and definitely quantified, and critical values be determined according to the actual production, which has promoted the previous methods dependent only on the single parameter, i.e. repose angle and compression degree methods. A relatively objective standard method of evaluating flowability of powders is formed.

Multivariate analysis of relationships between material properties and hygroscopicity of Chinese medicine raw materials / 药学学报

Material properties and hygroscopicity were determined. Principal component analysis and partial least squares regression were applied to evaluate relationships between material properties and hygroscopicity of Chinese medicine raw materials. The results showed that hygroscopicity was correlated with water content, particle size distribution, water soluble characteristic and cohesion. Balanced moisture content was positively correlated with water content, particle size distribution, water soluble characteristic and cohesion. Moisture absorption velocity was negatively correlated with particle size distribution, protruding degree and positively correlated with water soluble characteristic and cohesion. Moisture absorption acceleration was positively correlated with water content, particle size distribution and negatively correlated with water soluble characteristic and cohesion. Hygroscopicity of Chinese medicine raw materials is interpreted in terms of physics.

Pharmacokinetics of a long-circulating PEGylated Radix Ophiopogonis polysaccharide / 药学学报

The pharmacokinetics of a long-circulating PEGylated Radix Ophiopogonis polysaccharide (ROP) was investigated in rats following i.v. or s.c. administration at three dose levels (9, 20, 50 mg x kg(-1)). A moderate coupling reaction between the hydroxyl-activated ROP and the amino-terminated mPEG was chosen to produce PEGylate ROP. The grafting degree of the prepared conjugate was 1.03, and the molecular mass of mPEG used was 20 kDa. High-performance gel permeation chromatorgraphy with fluorescein isothiocyanate prelabeling was established to determine levels of the conjugate in plasma. The results showed that the elimination half-life of the conjugate following s.c. administration was basically identical to that after iv administration. An accurate linear correlation was observed between administration doses and areas under the curve of plasma conjugate level vs. time profile, regardless of the administration route. The absolute bioavailability of the conjugate following sc administration was approximately 56%, and the mean in vivo residence time was 52.1 h, increased 2.4 times compared to those of iv administration. In general, linear pharmacokinetics was observed for the conjugate within the dose range studied, and sc should be a promising administration route for the conjugate.

Pharmacokinetics study on characteristic ingredients of different-dose herbs of shaoyao-gancao decoction / 药学学报

The paper is to report the observation of pharmacokinetic changes of the characteristic ingredients in the combinations of different-dose herbs of Shaoyao-Gancao decoction. After the establishment of HPLC analytical method of plasma effective constituents, rats were orally administered with different-dose herbs of Shaoyao-Gancao decoction. Blood samples at different times after administering these decoctions were collected, and then were analyzed by HPLC fingerprints technology. Pharmacokinetic parameters of characteristic peaks were analyzed by SPSS 15.0 software and DAS 2.0. At last, we looked for the correlation of those pharmacokinetic parameters and the dosage of Gancao. The best dose of Shaoyao-Gancao decoction was at the ratio of 4 to 4, which was consistent with the dose commonly used in ancient times. The absorption of characteristic peaks from Shaoyao-Gancao decoction was related with the dosage of Gancao, and there existed interaction between each characteristic ingredients. There existed the right dose-ratio of Shaoyao and Gancao to get the best effect. The absorptions of effective constitutents were mutual waxing and waning in order to increase biological effects together. It's demonstrated the compatibility connotation at a right dose-ratio of Shaoyao-Gancao decoction through the angle of pharmacokinetics.

Magnetic resonance imaging in assessment of treatment response of gamma knife for brain tumors / 中华医学杂志(英文版)

<p><b>OBJECTIVE</b>To review the applications of magnetic resonance imaging (MRI) techniques in assessing treatment response to gamma knife radiosurgery for brain tumors.</p><p><b>DATA SOURCES</b>Published articles about assessing treatment response to gamma knife radiosurgery for brain tumors were selected using PubMed. The search terms were "MRI", "gamma knife" and "brain tumors".</p><p><b>STUDY SELECTION</b>Articles regarding the MRI techniques using for early assessment of treatment response of gamma knife were selected.</p><p><b>RESULTS</b>MRI techniques, especially diffusion weighted imaging, perfusion weighted imaging, magnetic resonance spectroscopy, are useful for early assessment of treatment response of gamma knife by detecting the hemodynamic, metabolic, and cellular alterations. Moreover, they can also provide important information on prognosis.</p><p><b>CONCLUSIONS</b>Diffusion weighted imaging, perfusion weighted imaging and magnetic resonance spectroscopy can provide early assessment of treatment response of gamma knife for brain tumors, and also information of tumor progression or recurrence earlier than conventional MRI. But there are still many questions to be answered which should be based on the development and advancement of MRI and related disciplines.</p>

Preparation and properties of sustained-release pellets of glycyrrhizin effective components / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare the glycyrrhizin pellets by extrusion-spheronization, and optimize the formulation of sustained release pellets of glycyrrhizin effective components coated with mixed Eudragit RS 100 and Eudragit RL 100.</p><p><b>METHOD</b>The sustained-release pellets of glycyrrhizin were prepared by Glatt fluid bed technique. The ratio of Eudragit RS 100 to Eudragit RL 100 in the formulation was optimized. The factors that influence the drug release behaviors and their properties were evaluated.</p><p><b>RESULT</b>The optimal coat for drug sustained-release was shown at the ratio of Eudragit RS 100 to Eudragit RL 100 of 4:1, the loading weight of copolymers of 5% and the plasticizer concentration of 15%. The curves of cumulative drug release were fit for Peppas and Higuchi equation.</p><p><b>CONCLUSION</b>The optimal sustained release of the glycyrrhizin effective component pellets is featured by adjusting the ratio of Eudragit RS 100 to Eudragit RL 100 and the loading weight of copolymers.</p>

Enriching of total flavonoids from Herba Leonuri with polyamide and macroporous resin / 中国中药杂志

<p><b>OBJECTIVE</b>To study the enriching method of total flavonoid from Herba Leonuri with polyamide and macroporous resin.</p><p><b>METHOD</b>Seven enriching and purifying methods were compared with the yield and purity as indexes. The method of enriching with polyamide and macroporous resin was confirmed and the process of purifying was determined by orthogonal design.</p><p><b>RESULT</b>D101 resin is packed by wet method, the ratio of diameter to height is 1:7. After mixed with the extract liquids, the weight of wet resin increased to 3 times of the dry resin. Evaporated the wet resin to dryness, mixed well with a little of 95% ethanol and dry polyamide powder, evaporated them to dryness again. Elute with deionized water until the effluent being colourless, then loaded it on the macroporous adsorptive resin, elute with 50% ethanol, the volume of effluents was collected to 7 times of the column volume. The purity of total flavonoids reached to 23%, while the diversion rate from raw Herba Leonuri was to 69%.</p><p><b>CONCLUSION</b>The process is simple and convenient, and the regeneration of resin is easy, which has a good application foreground.</p>

Advances in research on in vivo-in vitro correlation of sustained-release oral dosage forms in traditional Chinese medicine / 中国中药杂志

In this review, methods for testing in vitro release rate of sustained release preparations of traditional Chinese medicine (TCM) and in vivo-in vitro correlation were introduced. Studies indicated that a good correlation between in vivo and in vitro release can be obtained by establishing methods of in vitro release and it is important for the development of sustained release drug delivery system in TCM.

Study on fingerprints correlated with pharmacodynamic of Paeonia lacliflora and Glycyrrhiza uralensis effective compounds / 中国中药杂志

<p><b>OBJECTIVE</b>To study the spasmolysisy activity constituents of the Radix Paeoniae alba and Radix et Rhizoma compound.</p><p><b>METHOD</b>The three effective compounds of Radix Paeoniae and Radix et Rhizoma were arrayed to eight groups by orthogonal design rat, serum samples were collected after administered in these groups, and these serum samples were used to carry out the experiments of serum pharmacology of spasmolysis. The inhibition ratios were assigned as pharmacodynamic variable X, the areas of characteristic peaks on HPLC fingerprints were assigned as variable Y, and the correlation of X and Y was studied in order to research the activity spasmolysisy compounds of effective constituents. Serum samples were analyzed by HPLC-ESI-MS/MS.</p><p><b>RESULT</b>The correlation of fingerprints and pharmacology showed that four compounds were the main spasmolysisy activity compounds. The correlation parameter was greater than >0.4, whose value were 0.774, 0.678, 0.566 and 0.472 respectively, and their retention times were 8.03, 51.7, 54.59 and 72.43 min respectively. They were metabolites of effective compounds.</p><p><b>CONCLUSION</b>This study makes a valid approach for understanding the material foundation of TCM by establishing the correlation of fingerprints and pharmacology of activity compounds in vivo.</p>

Advances in research on drug release mechanisms and modes of thermosensitive gel / 中国中药杂志

Thermosensitive gel with the property of LCST (Lower Critical Solution Temperature) was studied as a hot spot these years for it can be used as one supportor of drug controlled release system which can release drug at right point, right time and right quantity. With further reseaches and applications of thermosensitive gel, the modes and mechanisms of it were discovered and poited out, drug release models were also established step by step. Resesrches on drug release mechanisms and modes of thermosensitive gel will make it applied better in fields of medicine and biology.

Studies on taste-masking technology of traditional Chinese medicine compounds / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the preparation of Shuanghuanglian taste-masking microspheres by spray-drying.</p><p><b>METHOD</b>Traced the compounds bitterness source, marked its curve and optimized the microspheres preparation by taking taste evaluation, microspheres yield and inclusion rate as the indexes.</p><p><b>RESULT</b>The bitter taste of compounds comes from Forsythia suspensa. The best taste-masking material is Eudragit E100. The optimal spray-drying parameters: solvent concentration 2.0%, inlet air temperature 75 degrees C, aspirator 35.0 m3 x h(-1), spray flow 0.35 m3 x h(-1), pump speed 8.0 mL x min(-1).</p><p><b>CONCLUSION</b>The spray-drying as a method of masking the traditional Chinese medicine compound taste have advantages of simple process and efficient masking.</p>

Influencing factors on dampproof effect of microcapsules and study on mechanism / 中国中药杂志

<p><b>OBJECTIVE</b>The influence of spray drying technology on the damp proof effect of microcapsules and the mechanism were studied.</p><p><b>METHOD</b>The microcapsules prepared with different spray drying parameters have been put in certain surroundings for 12 hours, then the hygroscopic curves were gotten; the mechanism was studied from the following aspects: solvent residue, film's shrink and particle size.</p><p><b>RESULT</b>The damp proof effect enhanced with the increase of inlet air temperature and the decrease of flow rate and air pressure. The properties of the wall, the solvent residue and particle size can influence the damp proof effect of the microcapsules.</p><p><b>CONCLUSION</b>The physical properties of microcapsules are different because of the different spray drying parameters, which lead to different damp proof effect of microcapsules.</p>

Establishment of bitterness appraisal method of Chinese drugs and preparation / 中国中药杂志

<p><b>OBJECTIVE</b>Bitterness appraisal method of Chinese drugs and preparation is established.</p><p><b>METHOD</b>The investigation table was designed by analogical epidemiology investigation. Then the statistical analysis was made for the data, and berberine bitter taste threshold was calculated. Verification experiment was made by two kinds of complex prescription.</p><p><b>RESULT</b>Berberine is determined as the standard bitter material. Statistics results about verification experiment are significant.</p><p><b>CONCLUSION</b>The system could be bitterness appraisal method of Chinese drugs and preparation.</p>

Studies on extraction and purification of active parts of ferulic acid from Ligusticun chuanxiong / 中国中药杂志

<p><b>OBJECTIVE</b>To study on the process of extraction and purification of active parts from Ligusticun chuanxiong.</p><p><b>METHOD</b>The processes of extraction and purification of active parts of ferulic acid were optimized by direct comparison and orthogonal design.</p><p><b>RESULT</b>Extract rate of active parts of ferulic acid was 1.67% and the content of ferulic acid was 5.82%.</p><p><b>CONCLUSION</b>Active parts of ferulic acid from L. chuanxiong were extracted and purified effectively.</p>

Study on adscription of plasma effective constituents of rat after administrated with Paeonia lacliflora and Glycyrrhiza uralensis compound / 中国中药杂志

<p><b>OBJECTIVE</b>To study the adscription of plasma effective constituents of rat after oral administration of Paeonia lacliflora and Glycyrrhiza uralensis compound.</p><p><b>METHOD</b>Based on the established HPLC analytical method of plasma effective constituents, analysis and comparison were carried out among HPLC profiles of plasma samples obtained after oral administration of different ingredient preparations such as P. lacliflora and G. uralensis compound, single ingredient and all the preparations. The adscription of plasma effective compounds were identified.</p><p><b>RESULT</b>Eighteen compounds were detected under this method, three of which are metabolites and thirteen are original forum of compounds contained in P. laclflora and G. uralensis compound.</p><p><b>CONCLUSION</b>This method is simple, accurate and stable, it could be used to analyze plasma effective constituents of P. lacliflora and G. uralensis compound. Affirmation of plasma effective compounds is the basis of to explore active compounds of P. lacliflora and G. uralensis compound.</p>

Advances of sustained/controlled release pellets in traditional Chinese medicine / 中国中药杂志

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.

Shengdi injection on rat model of lung inflammation induced by lipopolysaccharides / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the effect of Shengdi injection on rat model of lung inflammation.</p><p><b>METHOD</b>The rat model was established by intratrachea instillation of lipopolysaccharides (LPS). The total and different white blood cell counts in bronchoalvoelar lavage fluid (BALF) were performed and the level of tumor necrosis factor-alpha (TNF-alpha), superoxide anion radical (O2-) and myeloperoxidase (MPO) was measured, as well as pathologic change of pulmonary tissue was tested.</p><p><b>RESULT</b>Shengdi injection could depress the increasing of the amount of total white blood cells and neutrophils and inhibit the increasing of TNF-alpha, O2-, MPO caused by LPS, as well as relieve the pathologic change including Neutrophils infiltrating and mucous edema in tracheae after intravenous administration. While it did not show the effect on monocyte, and histological lesion of the lung tissue.</p><p><b>CONCLUSION</b>Shengdi injection shows some anti-inflammatory effect in rat lung induced by LPS and it can be concluded tentatively that anti-inflammatory, inhibiting the release of cytokine and inflammatory medium, and antioxidation are some of the mechanism of its effect on COPD.</p>

Protective effect of Ophiopogonis polysaccharide MDG-1 on experimental myocardial ischemic rats / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To investigate the protective effect of Ophiopogonis polysaccharide (MDG-1) on isolated myocardium ischemia/reperfusion injury (IRI) and subcutaneous injection of isoprenaline induced acute myocardial ischemia.</p><p><b>METHODS</b>In ex vivo heart experiment: Langendorff guinea pigs were randomly divided into the IRI group, the fructose sodium diphosphate (FDP) group, treated with FDP 10(-6) - 10(-4) g/mL for positive control and the MDG groups treated with MDG-1 10(-6) - 10(-4) g/mL. The amplitude and frequency of cardiac contraction, coronary blood flow at different time points after ischemia reperfusion were measured. In integral animal experiments: acute myocardium ischemia model rats established by subcutaneous injection of isoprenaline were used, they were administered with MDG-1 in dosage of 10, 20 and 40 mg/kg respectively, and controlled with propranolol. Besides, a normal control group and an untreated model group for control were set up. The ST segment shift in ECG and lactate dehydrogenase (LDH) activity in serum were observed.</p><p><b>RESULTS</b>Ex vivo heart experiment showed that different doses of MDG-1 can increase IRI caused abnormal coronary blood flow, quickly resume the heart contraction and restrain the quickened heart rate (all P < 0.01). The integral animal experiment showed that oral administration of 40 mg/kg can reduce the increased activity of LDH in serum (P < 0.05) induced by isoprenaline, but almost had no effect on ST-segment shift in ECG.</p><p><b>CONCLUSION</b>MDG-1 can alleviate IRI isolated myocardium of guinea pigs, and oral administration of MDG-1 showed a definite protection on isoprenaline caused rats' myocardial ischemia damage.</p>