The release kinetics research of sustained-release formulations of traditional Chinese medicines (TCM) is an inalienable part of the chain of TCM modernization, which plays an important role in the development of modern compound TCM preparation. However, the research method or pattern in line with the specific characteristics of TCM, i.e., multi-component and multi-target, is still lacking. On the basis of material rough set theory, this paper reviewed the advantages and disadvantages of the existing evaluation patterns and methods, a tentative idea about the "total amount" release characteristics evaluation on TCM compound sustained-release preparation has suggested so as to evaluate the release kinetics and to promote the development of evaluation methodology on TCM sustained-release preparations.

AIM: To establish the drug release method of Compound Salvia Multi-component released Doublelayer Tablet and investigate its in vitro drug release behavior and the influencing factors of the drug release rate.METHODS: The method of evaluating in vitro release rate of double-layer tablet was established with salvianolic acid B and gindenoside Rg_1 as index,The influencing factors of the release of rapid release layer and sustained release layer of double-layer tablet and their in vitro drug release behavior were studied.RESULTS: The rapid release layer showed the quick releasing effect; The drug release curve of sustained release layer accorded with Ritger-Peppas equation; artificial gastric juice had significant effect on the release curve of gindenoside Rg_1 which in double-layer tablets,but had no significant effect on the release curve of salvianolic acid B.CONCLUSION: The evaluation of in vitro release rate of Compound Salvia Multi-component released Double-layer Tablet shows good properties of fast and sustained release and clinic application is achieved.

Objective To prepare the long-circulating liposomes of paraoxonase(PON).Methods The long-circulating liposomes of paraoxonase were prepared by film dispersion method.The encapsulation efficiency was determined by gel column.The effects of the factors on the encapsulation efficiency,such as the weight ratio of paraoxonase to phospholipid,cholesterol(Choi) to phospholipid,PEG-cholesterol (PEG-Chol) and the iron strength of water phase,were investigated respectively.Then the formulation was optimized by orthogonal design.Results The encapsulation efficiency of the paraoxonase liposomes was 87.66±3.46%,and the average diameter of the liposomes was about 126 nm.There was no significant change on encapsulation efficiency on 15 d at 4 ℃,and the activity of paraoxonase was maintained basically stable.Conclusion The preparation of PEG-modified paraoxonase liposomes was easy and practicable,and the property investigation in vitro showed that the paraoxonase liposomes were stable.

The free membrane of Eudragit L100/S100 which is pH-sensitive, colon-specific was prepared by plane casting films. The film humidity, species and amount of plasticizers, the ratio of membrane material was investigated. The rate of membrane permeability and mechanical properties were used as indicators of orthogonal experiment, and its related properties were studied. The results show that the mechanical properties of the membrane and phragmoid capacity are the best when 30% TEC was used as plasticizer; the ratio of membrane material have little effect on the rate of membrane permeability and mechanical properties. By adjusting the species and amount of plasticizers, the ratio of Eudragit L100/S100, the free membrane which is colon-specific can be obtained.

OBJECTIVETo prepare Qixian decoction pellets.

METHODThe formulation and technological factors influencing the preparation of Qixian decoction were investigated in tangential spray fluid bed choosing the yield of pellets, particle diameter distribution, repose angle, bulk density as inspecting indexes.

RESULTthe technological parameters for the preparation of blank pellets were as follows: the ratio of starch and dextrin was 2:1, the adhesive agent was 70% syrup, the rotating speed was 200 r x min(-1), the air blow flow was 15 x 20 L x min(-1), the rate of air flow was 15 L x min(-1), the spay air pressure was 0.15 MPa, and the rotating rate of spray solution pump was 20-50 r x min(-1); The optimized technological parameters for the preparation of Qixian decoction were as follows: the relative density of the extract was 1.12-1.15 g x min(-1), the diluent was MCC and its quantity was 8%, the rotating rate of spray solution pump was 10-12 mL x min(-1), the frequency of the rotor disc was 18-20 Hz, the atomizing pressure was 0.2 MPa, the frequency of the fan was 22 Hz, and the spheronisation and drying time was 30 mins.

CONCLUSIONthe appearance of the Qixian decoction pellets prepared in tangential spray fluid bed are smoothing and round, the yield of pellets are high, and pellets of the particle size between 500-700 microm is 90.6%.

Adhesives ; chemistry ; Drug Compounding ; instrumentation ; methods ; Drug Implants ; Drugs, Chinese Herbal ; chemistry ; Rotation ; Temperature ; Time Factors

The quality control of traditional Chinese medicine (TCM) preparations is a key issue related to their curative effect, safety and stability. The application of modern analytical means and the development of new disciplines improve the quality control of TCM preparations to some extent. For a long time, however, the quality control level of TCM preparations remains low and the quality standards exist in name only unable to effectively control drug quality and ensure therapeutic effect and safety. The essay makes a systematic analysis on possible factors impacting TCM preparations and current situation of quality control and discusses possible approaches and new methods for improving quality control of TCM preparations, in order to give an impetus to the quality control standards and the mode evolvement of TCM preparations and ensure safety, efficiency and quality controllability of TCM preparations.
Drugs, Chinese Herbal ; Medicine, Chinese Traditional ; methods ; Quality Control

OBJECTIVETo prepare enteric coated pellets containing panax notoginseng saponins.

METHODPanax notoginseng saponins loaded pellets were prepared by Extrusion-Spheronization method, and coated by Eudragit L30D-55 using Glatt fluid bed with the bottom spray process, central composite design was used to optimize the coating prescription.

RESULTThe drug release of enteric coated pellets of panax notoginseng saponins pellets would be lower than 5% in 2 h in simulated gastric fluid, but reach above 85% in 3 h in simulated human gastroenteric environment.

CONCLUSIONThe enteric coated pellets of panax notoginseng saponins have good acid residence to avoid panax notoginseng saponins from degrading in gastric acid.

Chemistry, Pharmaceutical ; methods ; Drug Stability ; Gastric Acid ; chemistry ; Gastrointestinal Tract ; drug effects ; Humans ; Models, Biological ; Panax notoginseng ; chemistry ; Saponins ; chemistry ; pharmacokinetics ; Tablets, Enteric-Coated ; chemistry

Objective To explore the synthesis of photographic developer 2-18 F-fluoropropionic acid(18 F-FPA) and its imaging value in prostate cancer-bearing nude mice.Methods 18F-FPA was automatically synthesized by using the CFN-multi-200 multifunctional drug synthesis module,then the quality control were performed.The PC3 prostate cancer-bearing nude mice models(16 cases) and 22RV1 prostate cancer-bearing nude mice models(4 cases) were constructed.Then 18F-FPA imaging was conducted in these models,which were compared with those by 2-deoxy-2-18 F fluoro-D-glueose(18 F-FDG) and 11C-choline for evaluating the imaging value of 18F-FPA in prostate cancer.The mice bearing PC3 prostate cancer were randomly divided into 4 group for conducting the biodistribution measurement.The percentage rate of injection dose per gram tissue(％ID/g) and tumor/non-tumor tissue ratio was calculated.Results The synthetic process of 18 F-FPA was about 40 min,the yield rate was (38 ± 2) ％ (without time correction),the radiochemical purity was more than 97 ％,with good in vitro stability.After 18F-FPA injection,the tumor image in two kinds of tumor-bearing nude micecould was developed clearly,while a slight uptake was detected in developed tumor with 18 F-FDG and n C-choline imaging.The biodistributions of tumor in PC3 prostate cancer bearing nude mice were (6.91 ± 0.72),(6.99 ±0.55),(7.17 ± 0.25),(6.49 ± 0.74) ％ ID/g at 0.5,1.0,2.0 and 4.0 h after 18 F-FPA injection,respectively,the difference was not statistically significant(P＞0.05).Conclusion 18 F-FPA is simply synthesized,has better imaging effect for the nude mice bearing prostate cancer and is expected to be used for clinical detection of prostate cancer.