Study on sustained release preparations of Epimedium component / 中国中药杂志

The formulation for sustained release tablet of Epinedium component was selected and the evaluation equation of in vitro release was established. The liquidity of component was improved with the help of colloidal silica aided by spray drying, which would be the main drug in the sustained release tablets. Dissolution was selected as an evaluation index to investigate skeletal material type, fillers, impact porogen, lubricants and other materials on the quality of sustained release tablet. The sustained release tablets were prepared by dry compression. Formulation of sustained release preparations was main drug 35%, HPMC K(4M) 20% and HPMC K(15M) 10% as skeleton material, MCC 31% as filler, PEG6000 2% as porogen and magnesium stearate 2% as lubricant. The sustained release tablets released up to 80% in 8 h. The zero order equation, primary equation and Higuchi equation could simulate the release characteristics of sustained release tablets in vitro, the correlation coefficients r were larger than 0.96. The primary equation was most similar in vitro release characteristics and its correlation coefficient r was 0.9950. The preparation method is simple and the results of formulation selection are reliable. It can be used to guide the production of Epimedium component sustained release preparations.

Micromeritic properties of tanshinone IIA spray drying powder / 中草药

Objective: To explore a method to improving the in vitro dissolution of tanshinone IIA spray drying powder and to study its pharmceutical properties. Methods: Tanshinone IIA was processed with spray drying method and analyzed by determination of the specific surface area (BET), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD). And in vitro dissolution and drug stability were also investigated. Results: The BET results showed that tanshinone IIA powder after spray drying had narrow particle size distribution range and large specific surface area; XRD and DSC analyses showed that most drug was transformed into amorphous form. The in vitro dissolution achieved 85.2% within 8 h. Accelerating experiment showed that the in vitro dissolution of tanshinone IIA decreased by approximately 21% stored for 6 months. Conclusion: The drug dissolution is improved by spray-drying method. It provides a reference for the research and development of poorly soluble pharmaceutical preparations for oral administration.

Effect of spray drying process on physical properties and dissolution of tanshinone / 中国中药杂志

In order to improve the dissolution in vitro of components by processing tanshinone with the pray drying method, the physical properties of tanshinone power was analyzed by BET, differential scanning calorimetry, scanning electron microscopy and X-ray powder diffraction, and its dissolution in vitro was also investigated. The results of characterization showed decreased power size and increased specific surface area of tanshinone powder, and its existence in an amorphous state. Within 4 h, the accumulated dissolutions of tanshinone I and tanshinone II(A) in components of tanshinone reached 78.3%, 81.9%, respectively. Therefore, the spray-drying method was conducive to enhance the dissolution of components of tanshinone.

Preparation of baicalin colon-specific solid dispersion and evaluation on its in vitro release / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare pH-dependent baicalin colon-specific solid dispersion, with the aim of colon-specific delivery and rapid drug release.</p><p><b>METHOD</b>Baicalin-eudragit S100 solid dispersion was prepared by using the solvent method. The microscopic structure and physicochemical properties were analyzed by using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD) and infrared spectroscopy (IR). And its in vitro release was also investigated.</p><p><b>RESULT</b>The results of DSC and XRD analysis suggested that baicalin may be dispersed in solid dispersion in the amorphous state. IR results indicated a non-covalent bond effect may exist between baicalin and eudragit S100. The results of in vitro release determination showed that very few baicalins in pH 1.2 diluted hydrochloric acid solution for 2 h at the baicalin-eudragit S100 ratio of 1 : 6. The accumulated dissolution rate was less than 15% in pH 6.8 phosphate buffer solution for 4 h, but exceeding 90% in pH 7.6 phosphate buffer solution for 1 h.</p><p><b>CONCLUSION</b>The prepared baicalin-eudragit S100 solid dispersion could achieve the objective of colon-specific delivery and rapid drug release, and helps increase the concentration of baicalin in colons.</p>

Preparation of baicalin-chitooligosaccharide compound and its characterization / 中国中药杂志

To apply chitooligosaccharide in the preparation of baicalin compound, in order to increase the drug dissolution in vitro, and investigate the basic property of the compound. Baicalin-chitooligosaccharide compound was prepared by using the solvent method. The structure and physicochemical properties of compound were analyzed by using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD) and infrared vibrational spectrum (IR), and its dissolution behavior was also investigated. The results showed that the compound prepared at baicalin-chitooligosaccharide molar ratio of 1 : 1 could significantly improve the dissolution of baicalin. The results of DSC and XRD analysis suggested that baicalin may exist in an amorphous state. IR results indicated the interaction between baicalin and chitooligosaccharide. The baicalin-chitooligosaccharide compound could significantly improve dissolution in vitro of drug.

Effects of micronization on micromeritics properties of baicalin / 中国中药杂志

Baicalin extremely fine powder was made by using ball-mill and the effect of micronization on the micromeritics properties of baicalin was studied and analyzed. The microstructures of baicalin ordinary and extremely fine powder were compared by scanning electron microscope, differential scanning calorimeter and X-ray diffraction and the powder characteristic of them was investigated. The hygroscopicity was studied. The effect of micronization on the dissolution of baicalin was investigated. The results showed that the chemical constituents of baicalin were not changed after micronization with better compressibility. It was confirmed that micronization technology had a certain application value in promoting the insoluble component of baicalin absorption with higher dissolution.

Compared with colloidal silica and porous silica as baicalin solid dispersion carrier / 中国中药杂志

<p><b>OBJECTIVE</b>To compare the dissolution characteristics of colloidal silica and porous silica as the solid dispersion carrier, with baicalin as the model drug.</p><p><b>METHOD</b>The baicalin solid dispersion was prepared by the solvent method, with colloidal silica and porous silica as the carriers. In the in vitro dissolution experiment, the solid dispersion was identified by scanning electron microscopy, differential scanning and X-ray diffraction.</p><p><b>RESULT</b>The solid dispersion carriers prepared with both colloidal silica and porous silica could achieve the purpose of rapid release. Along with the increase in the proportion of the carriers, the dissolution rate is accelerated to more than 80% within 60 min. Baicalin existed in the solid dispersion carriers in the non-crystalline form.</p><p><b>CONCLUSION</b>The release behaviors of the baicalin solid dispersion prepared with two types of carrier were different. Among the two solid dispersion carriers, porous silica dissolved slowly than colloidal silica within 60 min, and they showed similar dissolutions after 60 min.</p>

Advance in studies on phospholipid compound of traditional Chinese medicines / 中国中药杂志

According to Chinese and foreign literatures and reports in recent years, this article introduced the latest advance in studies on phospholipid compound of traditional Chinese medicines in terms of its preparation mechanism, preparation process, characterization and transmembrane absorption. Under appropriate conditions, traditional Chinese medicines could generate phospholipid compound, whose physico-chemical property differs from the original drug, with a better absorption and improved bioavailability. Therefore, there is huge room for further study and development of phospholipid compound with traditional Chinese medicines.

Study on porous maize starch preparation and powdering coix seed oil / 中国中药杂志

To optimize the preparation conditions of porous starch The porous starch was used to powder coix seed oil. Porous starch was made of maize starch by using compound enzymes of glucoamylase and alpha-amylase. The preparation process was optimized through orthogonal test design with oil absorption rate to salad oil as indexes. The effect of different dosages of porous starch on yield of triglyceride by powdering coix seed oil was studied. The triglyceride release behaviors and fluidity of powdered coix seed oil were also studied. The results showed that the optimum conditions for preparation of porous maize starch were as follows, the mass radio of glucoamylase to a-amylase was 3:1, the temperatures was 55 degrees C, pH was 5.0, and hydrolysis time was 12 h. Under these conditions, the oil absorption rate to salad oil was 98.5% for porous maize starch. Porous starch was used to power coix seed oil. When porous starch to coix seed oil was 4:1, the triglyceride yield of powering coix seed oil was up to 97.02%. The fluidity of powdered coix seed oil was favorable and control released. The preparation of powdered liquid oil with porous starch had many advantages such as simple production technology, convenient operation, low cost and was worth generalizing.

Preparation of cinnamomi cortex oil microspheres based on porous silicon dioxide and its property characterizations / 中国中药杂志

To determine the optimum process for preparing Cinnamomi Cortex oil microspheres based on porous silicon dioxide. After porous silica dioxide adsorbed Cinnamomi Cortex oil, Cinnamomi Cortex oil microspheres were prepared by the dropping method, with sodium alginate as the skeleton materials. The preparation process was optimized through the L(9) (3(4)) orthogonal test design, with microspheres diameter, distribution, drug loading capacity and entrapment efficiency as the indexes. The cinnamon volatile oil microspheres were characterized by scanning election microscope (SEM), thermogravimetric analysis (TGA), and infrared (IR) spectroscopy. An in vitro drug release experiment was conducted. The results showed that the microspheres prepared with the optimal process parameters were in good shape, even in size and good in dispersibility, with an average diameter of 1.61 mm, an average drug loading capacity of 32.85%, an entrapment efficiency of 94.79%. The maximum drug release capacity reached 72.6%, 95.0%, 97.4%, respectively, under pH 4.0, 6.8, 7.4 in 6 hours. Meanwhile, microsphere generation was tested by IR, TGA and other methods. The established optimum process for preparing Cinnamomi Cortex oil microspheres was proved to be stable and practical.

Study on Xinyueshu spray drying assisted with copovidone and its effect on powder property / 中国中药杂志

To study the application characteristics of copovidone (PVP-S630) in Xinyueshu extracts during the spray drying process, and its effect on such pharmaceutical properties as micromeritics and drug release behavior. PVP-S630 was added into Xinyueshu extracts to study on the spray drying, the effect of different dosages of PVP-S630 against the wall sticking effect of the spray drying, as well as the power property of Xinyueshu spray drying power and the dissolution in vitro behavior of the effective component of hyperoside. The results showed that PVP-S630 revealed a significant anti-wall sticking effect, with no notable change in the grain size of the spray drying power, increase in the fluidity, improvement in the moisture absorption and remarkable rise in the dissolution in vitro behavior of hyperoside. It was worth further studying the application of PVP-S630 in spray drying power of traditional Chinese medicine.

Advance in studies on biotransformation of flavonoids by intestinal bacteria / 中国中药杂志

Flavonoids are widely distributed in the nature, and have various biological activities. Flavonoids can be degraded by intestinal bacteria, so as to impact their bioavailability in vivo. Studies on metabolism of flavonoids by intestinal bacteria could provide basis for screening out biotransformation of flavonoids and interpreting their in vivo metabolic process. Being taken as the lead compounds, flavonoids can be modified by intestinal bacteria to achieve new compounds with high efficiency, bioavailability and solubility, which lays a foundation for the research and development of new drugs, selection of drug dosage forms and drug production. This article summarizes the main reaction types and impacting factors of intestinal bacteria on biotransformation of flavonoids, for reference of studies on biotransformation.

Comparison of different preparation methods of tanshinoneporous silica solid dispersion / 中国中药杂志

Porous silica was used as a carrier to prepare tanshinone solid dispersions (SDs). sThe effect of the spray drying method or the solvent method on the drug dissolution of SD was studied. The structure characteristics of SDs was analyzed by SEM, DSC,XPRD and FTIR. And in vitro dissolution was also investigated. The results showed that drugs were highly dispersed into SDs prepared by spray drying method and the solvent method in amorphous form. In addition, the results of the dissolution tested in vitro exhibited that the tanshinone I and tanshinone II A, accumulated dissolutions of SDs prepared using solvent achieved 80. 9% ,84. 6% and 86. 2% ,88. 7% within 45,60 min, respectively. And SDs prepared using spray-drying method were 92.7% ,95. 3% and 95. 8%, 97. 1% within 45,60 min, respectively. The tanshinone SDs were prepared successfully by spray drying method and solvent method. The SDs prepared by spray drying method was more conducive to improving the dissolution.