OBJECTIVE:To screen the effective antioxidant in tretinion ointment METHODS:The six tretinion ointments were prepared with different antioxidants and the same base Based on the accelerated test design,the tretinion concentration was determined by HPLC RESULTS:The ointment with the antioxidant D exhibited the least oxidation rate CONCLUSION:Data from accelerated test demonstrated that the compound antioxidant D was the best one in this formula

OBJECTIVE: To study the dissolution amounts of aciclovir (ACV) from differently based preparations and provide the evidence for the development of new preparation of ACV. METHOD: The dissolution tester was applied for the quantitative determination of ACV released from 3 based formulations and 5 concentrations samples. The release amount per unit area (M) and the accumulative release percentage (Q) were compared respectively. RESULTS: The value for M was raised with the increase of the concentration of aciclovir in preparations, and for Q was reduced. The release rates of the aciclovir gel were at least two times faster than the creams and the ointment. CONCLUSION: The drug dissolution from ACV gel was better than the creams and the ointment. 10 gkg-1 ACV in prearation was the suitable concentration.

Adolescent ; Adult ; Aged ; Facial Nerve ; anatomy & histology ; pathology ; Female ; Humans ; Male ; Microsurgery ; Middle Aged ; Parotid Neoplasms ; surgery ; Young Adult

OBJECTIVETo observe the efficacy of combination therapy of clomiphene and Chinese drugs for nourishing Shen and activating blood circulation (NSABC) in treating Stein-Leventhal syndrome caused sterility.

METHODSSixty-two patients with anovulation caused sterility were randomly divided into the treated group (n = 32) and the control group (n = 30). The treated grop was treated with the combination therapy and the control group treated by the same dosage of clomiphene alone.

RESULTSAfter treatment, when comparing with that before treatment, the endocrine hormones in the treated group improved significantly, showing a markedly decrease of androgen and luteotropic hormone, and increase of estrogen (P < 0.001). The periodic ovulation rate in the treated group reached 87%, the total pregnancy rate being 65.6%, with no occurrence of ovarian hyperstimulation syndrome (OHSS) and luteinized unruptured follicle syndrome (LUFS), while in the control group, the periodic ovulation rate was 66%, the total pregnancy rate 36.6%, with LUFS occurred in 4 patients. Comparison of the therapeutic effects between the two groups showed significant difference (P < 0.05).

CONCLUSIONThe combination therapy of clomiphene and NSABC has a better therapeutic effect in treating Stein-Leventhal syndrome caused sterility than that of using clomiphene alone.

Adult ; Androgens ; blood ; Anovulation ; blood ; etiology ; Clomiphene ; therapeutic use ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Infertility, Female ; blood ; drug therapy ; etiology ; Ovarian Hyperstimulation Syndrome ; prevention & control ; Ovulation Induction ; Phytotherapy ; Polycystic Ovary Syndrome ; blood ; complications ; drug therapy ; Progestins ; blood

To investigate the antitumor activities of the immunoconjugates composed of anti-type IV collagenase monoclonal antibody Fab' fragment and lidamycin (LDM) prepared with different linkers. The immunoconjugates were prepared by linking Fab' to lysine-69 of LDM apoprotein by SPDP, LCSPDP, SMBS or SSMPB as the intermediate drug linkers. Immunoreactivities of the conjugates were determined by ELISA. The cytotoxicities of the conjugates were examined by clonogenic assay. In vivo antitumor effects of the conjugates were evaluated in nude mice bearing subcutaneously implanted HT-1080 tumor. ELISA assay showed that the conjugates retained part of the immunoreactivity of 3G11 against the antigen. The cytotoxicities of the Fab'-SMBS-LDM and Fab'-SSMPB-LDM to HT-1080 cells were significantly potent, compared with Fab'-SPDP-LDM, Fab'-LCSPDP-LDM and free LDM. In animal models at the same condition, free LDM, Fab'-SPDP-LDM and Fab'-LCSPDP-LDM inhibited the growth of HT-1080 tumor by 70.9%, 74.8% and 72.3%, while Fab'-SMBS-LDM and Fab'-SSMPB-LDM reached 78.0% and 87.7%, respectively. The median survival time of the mice treated with free LDM, Fab'-SPDP-LDM and Fab'-LCSPDP-LDM were prolonged by 71.9%, 82.2% and 107.5%, respectively, compared with that of untreated group. Whereas, the median survival time of Fab'-SMBS-LDM and Fab'-SSMPB-LDM were prolonged by 145.2% and 165.8%, respectively, indicating that Fab'-SSMPB-LDM was more effective than Fab'-SMBS-LDM in tumor suppression and life span prolongation. Fab'-SSMPB-LDM has more marked selective antitumor efficacy and lower toxicity, and might be a novel candidate for cancer therapy.

Objective To evaluate the effect of schistosomiasis control in Yunnan Province since achieving the transmission control standards,so as to provide the evidence for formulating the next prevention and control strategy. Methods The schistoso-miasis epidemic monitoring reports,annual reports,relevant information about Oncomelania hupensis snails,and schistosomiasis patient conditions were collected and analyzed for epidemic condition and characteristics of schistosomiasis in Yunnan Province from 2009 to 2012. Results The various epidemic monitoring indicators all decreased. In 2012,compared with 2009,the preva-lence reduced by 33.33%after correction;the number of villages with schistosomiasis patients reduced by 55.56%;the adjusted positive rate of livestock stool tests reduced by 45.45%;the number of villages with infected cow reduced by 42.25%;the actual area with snails reduced by 13.58%;the density of living snails reduced by 25.66%,and no schistosome infected snails were found in 2012. Conclusion There still exist schistosome infections in human and animals in some local areas of Yunnan Prov-ince,and it is difficult to achieve the standard of schistosomiasis transmission interrupted in a short period.

Bronchial Diseases ; diagnosis ; Child ; Female ; Humans ; Infant ; Male ; Tuberculosis, Pulmonary ; diagnosis

Animals ; Bone and Bones ; chemistry ; Female ; Ovariectomy ; adverse effects ; Ovary ; surgery ; Rats ; Rats, Sprague-Dawley ; Receptors, Estrogen ; analysis ; Transforming Growth Factors ; analysis

AIMTo establish the fundamentals for the design of scutellarin prodrug and formulation with feasible physicochemical and biopharmaceutical properties by esterifying scutellarin, an active component with poor absorption extracted from Erigeron breviscapus of Chinese medicine.

METHODSWith the method of salifying followed by esterifying, ethyl and benzyl ester of scutellarin were synthesized. Glycolamide ester of scutellarin was also synthesized with an improved method. Their structures were confirmed by MS and 1H NMR. The solubility and partition coefficient of the prodrugs were determined and their degradations were investigated in various buffers and in human plasma. The emulsion and cyclodextrin complex of glycolamide ester were prepared and the protection of the ester from degradation was compared in the intestinal tract contents. Furthermore, the degradation of glycolamide ester in the homogenates of various intestinal segments was studied. Results Three prodrugs were synthesized successfully and their structures were confirmed. Glycolamide ester of scutellarin showed better stability in the aqueous solution (t(1/2) approximately =16 d, pH 4.2) and the shortest half-life in the human serum (t(1/2) approximately =7 min). Compared with scutellarin, the solubility of glycolamide ester was increased about ten times in pH 4.0 buffer, and about thirty five times in water. Partition coefficient of the glycolamide ester increased significantly from -2.56 to 1.48. However, the ester degradation in the homogenates of intestinal mucus would be an obstacle for its absorption. The degradation rates were in the order duodenum > ileum > or = jejunum > colon. The emulsion showed a better protection of glycolamide ester from the degradation than cyclodextrin complex.

CONCLUSIONGlycolamide ester of scutellarin shows better physicochemical properties than ethyl and benzyl eater of scutellarin, but its stability in intestinal tract needs to be improved. The emulsion or / and colon-targeted delivery may be selected as one of strategies to decrease the presystemic degradation.

Animals ; Apigenin ; chemistry ; isolation & purification ; pharmacokinetics ; Emulsions ; Erigeron ; chemistry ; Esters ; Flavones ; chemical synthesis ; chemistry ; pharmacokinetics ; Glucuronates ; chemistry ; isolation & purification ; pharmacokinetics ; Glucuronides ; chemical synthesis ; chemistry ; pharmacokinetics ; Humans ; Intestinal Mucosa ; metabolism ; Intestines ; metabolism ; Male ; Plants, Medicinal ; chemistry ; Prodrugs ; chemical synthesis ; chemistry ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley

Objective To investigate the mechanism of hypoxia regulate osteopontin (OPN) secreting by mature dendritic cells (mDCs). Methods CD14 + cells were enriched using anti-CD14 immunomagnetic beads, for inducing to mDCs, CD14 + cells were cultured with GM-CSF and IL-4 in hypoxia or normoxiain vitro. Concentration of OPN and TGF-β1 in supernatant were detected by sandwich ELISA, OPN mRNA detected by RT-PCR. Approach regulating function of A2 R in expressing of OPN by mDCs by using NECA (surrogate of adenosine), A2R agonist (CGS21680), A2R antagonist (SCH58261) and investigate role of TGF-β1 in this process by using rhTGF-β1 and anti-TGF-β1 Ab. Results Hypoxia inreased the level of OPN and OPN mRNA in mDCs, and this effect could be reversed by A2 R antagonist. Under normoxia,both NECA and A2R agonist (CGS21680) could upregulate the level of OPN and OPN mRNA in mDCs significantly, but this positive effect could be reversed by A2 R antagonist. A2 R played a role in regulating TGF-β1, and confirmed TGF-β1 involved in regulation of OPN by using rhTGF-β1 and anti-TGF-β1 Ab. Conclusion High adenosine induce the generation of TGF-β1 through the A2R on mDCs, and then TGF-β1 raise the OPN secreting by mDCs.