[Study on solid dispersion of precipitated calcium carbonate-based oleanolic acid].

Oleanolic acid-precipitated calcium carbonate solid dispersion was prepared by using solvent evaporation method. The microscopic structure and physicochemical properties of solid dispersion were analyzed using differential scanning calorimetry and scanning electron microscopy (SEM). And its in vitro release also was investigated. The properties of the precipitated calcium carbonate was studied which was as a carrier of oleanolic acid solid dispersion. Differential scanning calorimetry analysis suggested that oleanolic acid may be present in solid dispersion as amorphous substance. The in vitro release determination results of oleanolic acid-precipitated calcium carbonate (1: 5) solid dispersion showed accumulated dissolution rate of.oleanolic acid was up to 90% at 45 min. Accelerating experiment showed that content and in vitro dissolution of oleanolic acid solid dispersion did not change after storing over 6 months. The results indicated that in vitro dissolution of oleanolic acid was improved greatly by the solid dispersion with precipitated calcium carbonate as a carrier. The solid dispersion is a stabilizing system which has actual applied value.

[Preparation of baicalin-chitooligosaccharide compound and its characterization].

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.

[Effect of spray drying process on physical properties and dissolution of tanshinone].

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].

OBJECTIVE: To prepare pH-dependent baicalin colon-specific solid dispersion, with the aim of colon-specific delivery and rapid drug release. METHOD: 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. RESULT: 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. CONCLUSION: 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.

[Study on porous maize starch preparation and powdering coix seed oil].

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.

[Advance in studies on phospholipid compound of traditional Chinese medicines].

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 solid dispersion of copovidone-based tanshinone II(A)].

OBJECTIVE: To apply PVP-S630 in the preparation of tanshinone II(A) (TS II(A)) solid dispersion, in order to improve its dissolution in vitro and reduce the moisture absorption of the solid dispersion. METHOD: Tanshinone II(A) solid dispersion was prepared by spray drying method. Such analytical methods as SEM, DSC, XRD were used to characterize their phases and detect their dissolution, moisture absorption and stability. RESULT: In the solid dispersion prepared with tanshinone II(A) and copovidone with proportion of 1:10, tanshinone II(A) was scattered on the surface of the carrier in the amorphous form, with a dissolution in vitro up to 100% at 0.5 h and a lower moisture absorption than PVP-K30 solid dispersion prepared with the same proportion. After a three-month accelerated stability test, it showed no significant change in drug dissolution and content. CONCLUSION: The solid dispersion prepared with copovidone as the carrier can significantly improve the dissolution of tanshinone II(A), with a relatively low moisture absorption and high stability, thereby having a good prospect of application.

[Study on solidifying volatile oil of cinnamon with colloidal silicon dioxide SYLOID244FP].

OBJECTIVE: To evaluate the properties of solidifying volatile oil of cinnamon with colloidal silicon dioxide SYLOID244FP. METHOD: Volatile oil of cinnamon was solidified by SYLOID244FP. The amount of SYLOID244FP was optimized with the cinnamaldehyde yield as criteria. Curing powder was characterized by scanning electron microscopy (SEM) and differential scanning calorimetry(DSC). The effects of SYLOID244FP on dissolution in vitro and thermal stability of cinnamaldehyde were studied. RESULT: The optimum solidification ratio of SYLOID244FP to volatile oil of cinnamon was 1: 1. Dissolution rate of cinnamaldehyde increasesd and its thermal stability improved after volatile oil of cinnamon was solidified. CONCLUSION: Solidifying herbal volatile oil with SYLOID244FP deserves studying further.

[Preparation of cinnamomi cortex oil microspheres based on porous silicon dioxide and its property characterizations].

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.

[Advances in studies on modification technology of traditional Chinese medicine powders].

Most of the traditional Chinese medicine (TCM) powders showed bad physical properties, such as poor flowability, high hygroscopicity, agglomeration and poor wettability, which will affect the production process and even the efficacy of Chinese materia medica preparations. The exact characterization of the physical properties of TCM powders and the reshaping technology become the key to improve the quality and efficacy of Chinese materia medica preparations and to promote the modernization process of TCM. This article summarizes the evaluation methods of the physical properties and the modification technology of TCM powders, in order to solve the problems existing in the research and production of Chinese materia medica preparations, and to achieve the quality control of drugs and modernization of dosage forms.

[Comparison of different preparation methods of tanshinoneporous silica solid dispersion].

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.

[Study on Xinyueshu spray drying assisted with copovidone and its effect on powder property].

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.

[Study on nano-CaCO3 applicated in Xin Yue Shu Capsules preliminarily].

OBJECTIVE: To investigate the characteristics of nano-CaCO3 applicated in Xin Yue Shu Capsules. METHODS: Studied the effect of different dosages of aerosil or nano-CaCO3 on fluidity, bulk density, moisture absorption of Xin Yue Shu capsules spray drying powder. In vitro dissolution and ferulic acid stability of Xin Yue Shu capsules was observed. RESULTS: It significantly improved powder fluidity and bulk density of Xin Yue Shu spray drying powder when aerosil or nano-CaCO3 was added. But there was no significant effect on powder moisture absorption, ferulic acid in vitro dissolution and ferulic acid stability. CONCLUSION: The effect of Nano-CaCO3 on improving powder fluidity and bulk density applicated in the spray drying powder of traditional Chinese medicine deserves studying further.

[Studies on sustained release solid dispersion of tripterine carried by HPMC-stearic acid].

OBJECTIVE: To prepare the sustained release solid dispersion of tripterine, using HPMC-stearic acid with the intention of improving drug dissolution and controlling drug releases moderate, so that the drug performances lower toxicity. METHOD: Tripterine sustained release solid dispersions was prepared by the solvent method with different weight ratios of HPMC-stearic acid and tripterine, which were dissolved in 95% ethanol. And in vitro dissolution experiment was conducted. Differential scanning calorimetry, scanning electron microscopy and X-ray powder diffraction can prove the formation of solid dispersions. RESULT: The ideal tripterine sustained release solid dispersions were prepared under the condition as follows, the weight ratio of tripterine and HPMC-stearic acid was 1: 10, and the release rate of drug can keep moderate and controllable. In vitro cumulative release of tripterine sustained release solid dispersion is up to more than 90% after 8 h, and the tripterine exist as amorphous in the solid dispersion. CONCLUSION: The sustained release solid dispersion of tripterine, carried by HPMC-stearic acid, can improve the release of tripterine effectively and controls the release rate keep moderate and controllable, and the preparation process is simple, which has potential applications.