Drug loading is an important index to evaluate the quality of solid preparation of traditional Chinese medicine. Drug loading is restricted by drug characteristics, dosage form, process, and drug delivery in vivo, which affects the preparation process, therapeutic effect, and drug release rate. By consulting domestic and foreign literature, this paper put forward the significance of increasing the drug loading: improving the compliance of patients, reducing the production cost, reducing the risk of the excipients. In this review, the possible approaches to increase drug loading, such as the selection of high-efficiency excipients, suitable drug preparation techniques, and modification of the physical properties of drugs are summarized. It will provide theoretical basis through this review for the development of high drug loading and high-quality formulations.

Objective:To investigate the impacts of gantry rotation angle errors, monitor unit (MU) errors, collimator and multi-leaf collimator (MLC) position errors upon the γ passing rate of dose verification in volumetric modulated arc therapy (VMAT).Methods:Ten patients with rectal cancer and 10 patients with uterine tumors were selected. The operating errors of accelerator parameters were introduced during the VMAT execution. By comparing the γ passing rates during dose verification between the simulating and original plans, the impact and sensitivity of the operating errors of each accelerator parameter on γ passing rate were analyzed.Results:When the γ criteria were set as 3%/3 mm, 3%/2 mm and 2%/2 mm, the γ passing rate decreasing gradient was less than 7.0% after the introduction of gantry rotation angle, MU and collimator position errors, respectively. However, after the reverse, opposite, and co-directional motion errors of the MLC blades on both sides were introduced, the γ passing rate decreasing was less than 19.13 %, 18.53%, 0.19 %; 19.87%, 20.01%, 0.42 % and 23.11%, 23.45%, 0.65 % for absolute dose verification, respectively.Conclusion:During VMAT, the reverse and opposite motion errors of MLC blades exert more significant effect on the γ passing rate compared with the gantry rotation angle errors, MU errors, collimator position errors and co-directional motion errors of the MLC blades. When the γ criteria of 3%/3 mm, 3%/2 mm and 2%/2 mm are adopted, the impact of accelerator operating errors upon the γ passing rate is strengthened in sequence. Therefore, when performing dose verification for a specific patient, appropriate γ criteria should be chosen and absolute dose verification should be taken as the reference index to evaluate the consistency between the calculated and measured dose distribution.

Objective To investigate the supernatant of umbilical cord-derived mesenchymal stem cells (UCMSCs) on tumor necrosis factor-α(TNF-α) and apoptosis protein caspase-3 in diabetic rats model with skin ulcer. Methods 45 Sprague-Dawley rats were randomly divided into control group (acute wounds group), phosphate buffered saline (PBS) group and UCMSCs supernatant group. The diabetic rat model was constructed by injecting with alloxan by tail vein and feeding with high-fat diet. Diabetic skin ulcer (DSU) rat model was constructed by scratching a wound and infusing suspension of Staphylococcus aureus. In the control group, the diabetic rats (n=15) were scratched to form a wound and treated by tail vein injection of 100μl PBS. In the PBS group, DSU rats (n=15) were treated by tail vein injection of 100μl PBS, and then 100μl PBS was dropped at the ulcer site. In the UCMSCs supernatant group, freeze-dried powder of UCMSCs supernatant was dissolved in 200μl PBS, 100μl of which was injected into the tail vein of DSU rats (n=15), and other 100μl was dropped at the ulcer site. After 5 days of the treatments, the levels of serum TNF-αwere detected by radioimmunoassay method, and the expression of TNF-αand caspase-3 in the ulcer tissues of rats was detected by polymerase chain reaction and Western Blot. Results The levels of TNF-αin the PBS group [(35.9±3.7)μg/L] were significantly higher than that of the control group [(11.4±4.9)μg/L] and the UCMSCs group [(14.7±6.6)μg/L] (all P<0.05). The levels of mRNA and protein expression of TNF-αand caspase-3 in the UCMSCs group were significantly lower than those of the PBS group (all P<0.05), and have no significant differences with respect to those of the control group (all P>0.05). Conclusions UCMSCs supernatant treatments can effectively down-regulate the expression of TNF-αand caspase-3 in ulcer tissue of DSU rats, and play an anti-inflammatory and anti-apoptotic effect.

BACKGROUND:The OPG-RANKL-RANK transport system plays a crucial role in bone resorption mechanism of osteoclasts. OBJECTIVE:To observe the expression of OPG-RANKL-RANK signaling system in osteoclasts, osteoporosis, and the targeted therapy of OPG-RANKL-RANK signaling system. METHODS:We retrieved related literatures in the periodicals database with the key words of“osteoprotegerin, RANKL, RANK, osteoclasts, osteoporosis”in English and Chinese. According to the inclusion criteria, the literatures were included in this study after the evaluation of quality. RESULTS AND CONCLUSION:The mature of osteoclasts is mediated via OPG-RANKL-RANK signaling system and its associated signaling pathways. This signal pathway leads to the mechanism of osteoporosis. At the genetic and molecular levels, the targeted therapy of osteoporosis has become the focus. OPG-RANKL-RANK signaling system can provide a research platform for targeted treatment of osteoporosis, and OPG-RANKL-RANK signaling system is an important way to the regulation of osteoclasts and osteoporosis.

BACKGROUND:The V-ATPase a3 transport system plays a crucial role on bone resorption mechanism of the osteoclasts.
OBJECTIVE:To observe the expression of V-ATPase a3 transport system in fracture repair and the effect of V-ATPase a3 transport system inhibitor on fracture healing.
METHODS:We retrieved related literatures in the periodicals database with the key words, and screen them according to the inclusion criteria. The literatures were included in this study after the evaluation of quality.
RESULTS AND CONCLUSION:V-ATPase a3 transport system widely exists in the cytoplasm membrane and organel e membrane of eukaryotic cells. V-ATPase a3 has two structural domains:V0 and V1. V0 structural domain is the proton transport channel, V1 structural domain is mainly the hydrolysis of ATP. V-ATPase a3 transport system focuses on the fril ed edge of osteoclasts, H+is transported to form a high concentration, dissolves inorganic minerals and provides the acidic environment for hydrolytic enzymes, thus being involved in bone resorption. So V-ATPase a3 transport system is selected as the research target in the fracture repair and reshape.

With the deepening of modernization of traditional Chinese medicine (TCM), the method of quantification and standardization of TCM (i.e., quantitative characterization of TCM) has been more and more widely accepted by researchers. Chemometrics processes complicated data of TCM through applied mathematics, statistics and com-puter technology. And multivariable study was introduced into the quantitative characterization of TCM with great achievements. This article reviewed existed problems of quantitative characterization in TCM, the principles, char-acteristics, limitations, commonly used statistical methods and application conditions on quantitative characteriza-tion of TCM. With this review, a reference for further study of quantitative characterization of TCM was provided and a further research idea of combination with main methods of chemometrics was given.

OBJECTIVETo establish an accurate and simple qualitative analytical method in vivo in the study on HPLC characteristic fingerprint of active components of dachuanxiong fang in plasma and cerebrospinal fluid, in order to lay a foundation for studies on components found in plasma and cerebrospinal fluid and provide basis for compatible regularity of initiators.

METHODHPLC characteristic fingerprint of active components of dachuanxiong fang in plasma and cerebrospinal fluid was established.

RESULTThe similarity of fingerprints of all of six batches of samples was above 0.85, RSD of their relative retention times in common peaks was less than 2. 0%.

CONCLUSIONThe fingerprints of active components of dachuanxiong fang in plasma and cerebrospinal fluid were stable and accurate that they can be used in qualitative analysis on in vivo components.

Animals ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; metabolism ; Male ; Medicine, Chinese Traditional ; Plant Extracts ; blood ; cerebrospinal fluid ; Quality Control ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo observe the pharmacokinetic effect of Shaoyao Gancao compound on rats using different decocting methods, and to pharmacokinetically detect the the compatibility of the component compounds of the Shaoyao Gancao compound from the pharmacokinetic viewpoint.

METHODBased on the established HPLC analytical method of plasma effective constituents, rats were orally administered with a single or mixed decoction of Shaoyao and Gancao. Blood at different times after administering these decoctions were collected, and then variance analysis was made for pharmacokinetic parameters.

RESULTThe results of all six rats indicated that the absorption of the mixed decoction of Shaoyao and Gancao was greater than that of the single decoction. While, the absorption of the characteristic peaks at the retention time of 5.2, 11.0, 12.0, 14.6 min had statistical significance.

CONCLUSIONShaoyao Gancao compound was proved better than that of the single decoction from the pharmacokinetic viewpoint.

Administration, Oral ; Animals ; Biological Availability ; Chromatography, High Pressure Liquid ; Drug Compounding ; methods ; Drugs, Chinese Herbal ; administration & dosage ; analysis ; pharmacokinetics ; Male ; Paeonia ; chemistry ; Plasma ; chemistry ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo quantify the physical characteristics of sticks of traditional Chinese medicine (TCM) honeyed pills prepared by the plastic molded method and the correlation of adhesiveness and plasticity-related parameters of sticks and quality of pills, in order to find major parameters and the appropriate range impacting pill quality.

METHODSticks were detected by texture analyzer for their physical characteristic parameters such as hardness and compression action, and pills were observed by visual evaluation for their quality. The correlation of both data was determined by the stepwise discriminant analysis.

RESULTStick physical characteristic parameter l(CD) can exactly depict the adhesiveness, with the discriminant equation of Y0 - Y1 = 6.415 - 41.594l(CD). When Y0 < Y1, pills were scattered well; when Y0 > Y1, pills were adhesive with each other. Pills' physical characteristic parameters l(CD) and l(AC), Ar, Tr can exactly depict smoothness of pills, with the discriminant equation of Z0 - Z1 = -195.318 + 78.79l(AC) - 3 258. 982Ar + 3437.935Tr. When Z0 < Z1, pills were smooth on surface. When Z0 > Z1, pills were rough on surface.

CONCLUSIONThe stepwise discriminant analysis is made to show the obvious correlation between key physical characteristic parameters l(CD) and l(AC), Ar, Tr of sticks and appearance quality of pills, defining the molding process for preparing pills by the plastic molded and qualifying ranges of key physical characteristic parameters characterizing intermediate sticks, in order to provide theoretical basis for prescription screening and technical parameter adjustment for pills.

Dosage Forms ; Drugs, Chinese Herbal ; chemistry ; Medicine, Chinese Traditional ; methods ; Plastics

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.