AIM　To predict skin permeability of drugs with theoretical parameters. METHODS　The semiempirical self-consistent field molecular calculation AM1 method is utilized to obtain the structural parameters of drug molecules. Stepwise multiple regression analysis or BP neural network is then utilized to establish the correlation between skin permeability of drugs and their structural parameters. RESULTS　The calculated human skin permeability coefficients (kp) of 22 model drugs in vitro or the R values (R=absorbed/unabsorbed) of 17 drugs in vivo are in good agreement with their observed values. CONCLUSION　Theoretical parameters can be used to predict skin permeability of drugs.

Objective To investigate nursing care needs of elderly nursing homes residents in Fuzhou, to help to improve nursing care quality provided by elderly nursing homes. Methods A total of 120 elderly residents from 10 elderly nursing homes in Fuzhou were investigated with a self-developed questionnaire focusing on nursing care needs of elderly nursing home residents. The questionnaire included the following two parts: the general information of the elderly residents and the needs of disease care, basic nursing care, daily life care as well as psychological care. Results The retrieving rate was 95.8%(115/120). The overall nursing care needs of elderly nursing home residents was at the middle level (2.59 ±0.80), the highest demand for nursing care was disease care (3.34±1.07), followed by psychological care (2.56±0.93), basic nursing care (2.20±1.15) and daily life care (2.23±0.97). The single living elderly residents got lower scores than the couple living elderly residents in disease care, basic nursing care 3.19±1.07, 2.06±1.10 vs. 3.78±0.96, 2.62±1.20 (t=2.656, t=2.311, P<0.05). Over 90 years old age groups got lower scores than the other age groups in the disease care, 2.25 ±0.69, 3.80 ±0.72, 3.35 ±1.09, which showed significant difference (F=7.10, P < 0.05). The elderly suffering from hypertension, diabetes, cardiovascular disease varied in the demand for different care. Conclusions The overall nursing care needs of elderly nursing home residents was at the middle level. Staying with spouse, age, disease state are the influencing factors of nursing care needs of elderly nursing home residents.

OBJECTIVE:To explore the similarity of dissolution profiles of self-development and original preparation of Solife-nacin succinate tablet,and provide reference for the prescription and process screening of the former one and the quality similarity evaluation of the latter one. METHODS:The paddle method was adopted with rotational speed of 50 r/min,using water,pH1.2 hy-drochloric acid solution,pH4.0 acetate buffer solution and pH6.8 phosphate buffer solution as dissolution media,HPLC was used to determine the cumulative dissolution of main components of self-development and original preparation of Solifenacin succinate tablet at different time points,dissolution profile was drew,then f2 was used to evaluate its similarity. RESULTS:In the 4 dissolu-tion media,the f2 of both self-development and original preparation of Solifenacin succinate tablet was higher than 50,which indi-cated that the dissolution profiles showed similarity. CONCLUSIONS:The established HPLC is suitable for the dissolution determi-nation of Solifenacin succinate tablet;the dissolution profiles of the self-development and original preparations are basically simi-lar,which indicates the prescription and technology of self-development preparation are feasible.

OBJECTIVETo optimize the extracting process of ethanol extract with hypouricemic effect from Rhizoma Alismatis.

METHODOrthogonal design was utilized to optimize the preparing conditions including the concentration of ethanol, amount of ethanol, extraction times and extraction duration per time while alisol B 23-acetate was selected as the evaluation index. Both the alisol B 23-acetate and the serum uric acid levels were measured by HPLC.

RESULTThe ethanol extract had hypouricemic action. Only extraction times had significant effect on the content of alisol B 23-acetate in ethanol extract.

CONCLUSIONThe optimal extraction process is to extract two times using sevenfold 70% ethanol and 1 h per time.

Alismataceae ; chemistry ; Animals ; Chemical Fractionation ; methods ; Disease Models, Animal ; Ethanol ; chemistry ; Humans ; Hyperuricemia ; blood ; drug therapy ; Mice ; Plant Extracts ; administration & dosage ; Rhizome ; chemistry ; Uric Acid ; blood ; Uricosuric Agents ; administration & dosage

OBJECTIVETo study the influence of the different combinations of the main active parts in Yangyintongnao granule on the pharmacokinetics parameters of the two active components--ligustrazine and puerarin using the method of total amount statistic moment for pharmacokinetics.

METHODCombinations were formed according to the dosages of the four active parts (alkaloid, flavone, saponin, naphtha) by orthogonal experiment L9 (3(4)). Blood concentrations of ligustrazine and puerarin were determinated by HPLC at different time. Zero rank moment (AUC) and one rank moment (MRT, mean residence time) of ligustrazine and puerarin have been worked out to calculate the total amount statistic moment parameters was analyzed of Yangyintongnao granule by the method of the total amount statistic moment. The influence of different compatibilities on the pharmacokinetics parameters was analyzed by orthogonal test.

RESULTFlavone has the strongest effect than saponin on the total AUC. Ligustrazine has the strongest effect on the total MRT. Saponin has little effect on the two parameters, but naphtha has more effect on both of them. It indicates that naphtha may promote metabolism of ligustrazine and puerarin in rat.

CONCLUSIONTotal amount statistic moment parameters can be used to guide for compatibilities of TCM.

Animals ; Data Interpretation, Statistical ; Disease Models, Animal ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; Humans ; Male ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Reperfusion Injury ; drug therapy

Colorectal cancer (CRC) is one of the leading causes of death worldwide. Thus, the development of new therapeutic targets for CRC treatment is urgently needed. SGK1 is involved in various cellular activities, and its dysregulation can result in multiple cancers. However, little is known about its roles and associated molecular mechanisms in CRC. In present study, we found that SGK1 was highly expressed in tumor tissues compared with peri-tumor samples from CRC patients. In vitro experiments revealed that SGK1 overexpression promoted colonic tumor cell proliferation and migration and inhibited cell apoptosis induced by 5-fluorouracil (5-FU), while SGK1 shRNA and inhibitors showed the inverse effects. Using CRC xenograft mice models, we demonstrated that knockdown or therapeutic inhibition of SGK1 repressed tumor cell proliferation and tumor growth. Moreover, SGK1 inhibitors increased p27 expression and promoted p27 nuclear accumulation in colorectal cancer cells, and p27 siRNAs could attenuate the repression of CRC cell proliferation induced by SGK1 inhibitors. Collectively, SGK1 promotes colorectal cancer development via regulation of CRC cell proliferation, migration and survival. Inhibition of SGK1 represents a novel strategy for the treatment of CRC.
Animals ; Apoptosis ; Cause of Death ; Cell Proliferation ; Colon ; Colorectal Neoplasms* ; Fluorouracil ; Heterografts ; Humans ; In Vitro Techniques ; Mice ; Repression, Psychology ; RNA, Small Interfering