OBJECTIVE: To investigate the effect of solvent pH on the physical/chemical properties and clinical use of four drugs commonly used in gynecology and obstetrics, including aminophylline, ambroxol, labetalol and ritodrine, through simulation and evidence-based evaluation to provide theoretical guidance and quantitative reference for clinical use. METHODS: By searching PubMed compound and Martindale: The Complete Drug Reference, the physical/chemical and clinical information of the four drugs were obtained. The logP, pKa, logD, and solubility were simulated using ACD/LAB 6.0 software. RESULTS: The solvent pH had effects on the logD and solubility of the four drugs to a certain degree in an exponential manner. The four drugs are compatible with dextrose injection or 0.9% sodium chloride injection, but special care needs to be taken in the clinical use. CONCLUSION: Solvent pH has influence on the dissolution balance of the four drugs. Simulation of the physical/chemical properties of drugs will provide theoretical guidance and reference for clinicians with more detailed information.

BACKGROUND: Studies are very few regarding the specific reaction of bone marrow mesenchymal stem cells (BMSCs) to activated microglia. Moreover, it remains unclear how MSCs maintain dopaminergic neuronal survival under specific microenvironment.OBJECTIVE: To explore the effect of BMSCs stimulated by activated microglia on dopaminergic neuron survival.METHODS: BMSCs were isolated from Wistar rats by attachment method, and in vitro cultured; microglia was activated, and dopaminergic neurons were cultured by enzyme digestion method. The experiment included 5 groups: BMSCs, microglia, lipopolysaccharide (LPS)+microglia; BMSCs+LPS+microglia groups, in which the dopaminergic neurons were cultured with corresponding culture medium; the dopaminergic neurons alone group was cultured with 10% fetal bovine serum+ DMEM/F12. The effect of different microenvironment on dopaminergic neuron survival and gliocyte-derived neurotrophic factor released from BMSCs were detected by immunofluorescence technique.RESULTS AND CONCLUSION: The release of gliocyte-derived neurotrophic factor in groups involving BMSCs was greater than corresponding control group. Tyrosine hydroxylase immunofluorescence showed that neuronal survival of dopaminergic neurons alone group was 15%, microglia group was 10%, LPS+microglia was 5%, but BMSCs+LPS+microglia group was 28%, significantly greater than the other groups (P < 0.05). In addition, survival of in vitro cultured dopaminergic neurons was decreased with increasing culture duration, but the survival of dopaminergic neurons in group involving BMSCs was significantly greater than corresponding control group. This indicates that microglia activation stimulated BMSCs to upregulate gliocyte-derived neurotrophic factor to prevent dopaminergic neurons from toxic injury, and inhibit delayed death of dopaminergic neurons.

OBJECTIVE: To investigating the Pregnancy, Lactation, and Reproductive Potential: Labeling for Human Prescription Drug and Biological Products-Content and Format, and we provide lessons for China's future revolution for the use of drug for pregnant women. METHODS: We analyzed and summarized the materials about the new system, and discussed history, letter risk categorization system, the preparation, new system, the effects of new rule. RESULTS: The new rule eliminates letter risk categorization system (ABCDX). The new system not only combines different parts of the previous rule but also adds a new part-"Females and Males of Reproductive Potential". CONCLUSION: Clinical pharmacists will work better with the new rule, thus should take lessons of FDA's revolutions for rules on pregnancy, and take steps to improve the safety measures for pregnant women.

OBJECTIVE: To investigate whether there is necessity for carrying out pharmaceutical care for advanced maternal aged multiparous women as the number of this special population in our country growing greatly under the "universal two-child" policy. METHODS: We compared the pregnancy outcomes of the advanced maternal aged multipara with advanced maternal aged primipara and right aged multipara to investigate the characteristics of advanced maternal aged pregnancy outcomes. Through analyzing the importance and urgency of pharmaceutical care for advanced maternal aged multipara, we explored current status and challenges, and analyzed pregnancy drug risk category and pregnancy drug registry. RESULTS: Compared with advanced maternal aged primipara and right aged multipara, pregnancy outcomes and exposure risk are different in advanced maternal aged multipara. Pregnancy drug risk category and pregnancy drug registry are crucial measures in observing study of pharmaceutical care. CONCLUSION: It is necessary to carry out pharmaceutical care for advanced maternal aged multipara. Pregnancy drug risk category and pregnancy drug registry can provide basis for designing interventional study of pharmaceutical care.

OBJECTIVE: To analyze 13 judicial precedents involving off-label drug use and explore the legal interpretation on off-label drug use in China in order to provide experience for establishment of off-label drug use and clinical application. METHODS: Based on the law databases (China Judgements Online, Chinalawinfo, Jufaanli, Itslaw), 13 cases were searched and screened involving legal off-label drug use. The relationship was investigated and discussed between different results and characteristics of the 13 cases. RESULTS: In 13 cases, there are 2 cases probably reasonable for off-label use, 2 cases unreasonable but not correlated with patients′ outcomes, 9 unreasonable and with a causal relationship with patients′ outcomes. In the 9 unreasonable cases, there are 4 cases without sufficient evidence, 3 cases without informed consent, 1 case lack of monitoring after off-label use, 1 case with idiosyncratic reaction, and 1 case not consistent with the label of the drug used. CONCLUSION: Major deficiencies of off-label drug use in China are without sufficient evidence, lack of informed consent and with uncompleted system on off-label drug use. Establishing more completed and detailed system, investigating enough clinical evidence, better informed consent and monitoring after off-label use are important measurements to ensure safety on off-label drug use.

OBJECTIVE: The aim of this study is to investigate labelings on dermatologic drugs for pregnant women and provide qualitative and quantitative pharmaceutical support for clinical use. METHODS: Labelings and formularies on pregnancy of topical drugs were analyzed and sorted according to classification on pregnancy use. Transdermal abilities of the drugs not forbidden nor avoided were evaluated through ACD/LAB 6.0 software and Potts-Guy formulation. Through TOXNET database and dose conversion equation, toxicities on animals were collected and human doses for pregnant women were calculated. RESULTS: In dermatologic drugs, there are 16 drugs forbidden, 8 not recommended/avoided/should not be used, 14 used with caution/weighed pros and cons, 7 used under instruction, 16 unclear or with no statement. In topical drugs not forbidden nor avoided, there are 9 drugs' logKp above-5, butenafine and sertaconazole with strongest transdermal abilities, 7 drugs' logKp influenced under pH5.5 or pH7.0, with a decline in logK'p compared with logKp, still 15 drugs not influenced by pH, 7 drugs' toxicities on animals unknown, 14 drugs' pregnancy human doses under 10 mgkg-1. CONCLUSION: Currently,only a few topical drugs' instructions on pregnancy are clear. With properties and animal experiments, better pharmaceutical support can be provided for clinical use on qualitative or quantitative reference.

Objective To investigate the expression of vascular endothelial growth factor(VEGF)in synovium of rats with adjuvant arthritis and the relationship between the histopathologic score and the expression of VEGF.Methods Adjuvant arthritis was established in Wistar rats by inoculating complete Freund's adjuvant(CFA). We calculated the arthropathologic score and the expression of VEGF mRNA and protein at different stages after CFA inoculation.Results In model group the arthropathologic score and expression of VEGF protein in synovium increased significantly all the time (P

To study the influence of hypercholesterolemia with caveolin-1 on the plasmalemma of vascular endothelium, we used the methods of immunohistochemistry to detect the dynamic changes of caveolin-1 in cultured ECV-304 cells which were stimulated high cholesterol serum and the arterial endothelium of hypercholesterolemia rats. It is resulted that high cholesteorol level can upregulate the expression of caveolin-1 both in vitro and in vivo. In the initial stage of hypercholesterolemia model, the expression of caveolin-1 increased as the time of high cholesterol level added, but in the later period it was decreased slightly.
Animals ; Aorta ; pathology ; Caveolin 1 ; Caveolins ; biosynthesis ; genetics ; Cells, Cultured ; Cholesterol ; blood ; Endothelium, Vascular ; cytology ; metabolism ; Female ; Humans ; Hypercholesterolemia ; metabolism ; Male ; Rabbits ; Rats ; Rats, Sprague-Dawley ; Umbilical Veins ; cytology

Xingnaojing (XNJ) is an effective clinical drug used to treat acute stroke. Compared with injection administration, its nasal administration has better brain targeting. Therefore, through nasal administration, XNJ microemulsion could help solve the drug load of compound components of different polarities contained in large-dose and high-concentration traditional Chinese medicines, and reduce irritation to nasal mucosa In this study, the modified volume correction method and the improved rat in situ nasal perfusion model were adopted to compare the nasal absorption of geniposide contained in different XNJ preparations. The results showed that the constant absorption rate of geniposide (GE) in XNJ-D was (2.95 +/- 0.25) x 10(-3) min(-1), whereas the constant absorption rate of GE in XNJ-M was (2.16 +/- 0.21) x 10(-3) min(-1). This indicated that the rat nasal absorption of GE in different XNJ preparations complied with the first-order process and could be considered as passive absorption. GE in XNJ-D was absorbed faster than that in XNJ-M, which provided basis for the development of nasal preparations of XNJ.
Absorption ; Administration, Intranasal ; Animals ; Drugs, Chinese Herbal ; pharmacokinetics ; Emulsions ; Iridoids ; pharmacokinetics ; Male ; Nose ; metabolism ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo conduct a molecular epidemiological survey on the mitochondrial DNA C1494T mutation in non-syndromic hearing loss patients in Chinese population.

METHODSPolymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) were used to screen the mitochondrial DNA 12S rRNA C1494T mutation in 20 patients with aminoglycoside antibiotic induced hearing loss, 136 sporadic non-syndromic hearing loss patients and 50 probands of pedigrees with non-syndromic hearing loss.

RESULTSThe C1494T mutation did not appear in all cases except for the positive control.

CONCLUSIONIncidence of mitochondrial DNA C1494T mutation is much lower than that of mitochondrial DNA A1555G mutation in non-syndromic hearing loss of Chinese population. Mitochondrial DNA C1494T mutation may be a rare variation in non-syndromic hearing loss and is not the main cause of aminoglycoside antibiotic induced-deafness.

Adolescent ; Aminoglycosides ; adverse effects ; Anti-Bacterial Agents ; adverse effects ; Asian Continental Ancestry Group ; genetics ; Child ; China ; DNA, Mitochondrial ; genetics ; Female ; Hearing Loss ; chemically induced ; ethnology ; genetics ; Humans ; Male ; Point Mutation ; Polymerase Chain Reaction ; Polymorphism, Restriction Fragment Length ; RNA, Ribosomal ; genetics