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1.

Objectives:

Magnesium historically has been used for treatment and/or prevention of eclampsia. Considering the low body mass index of Indian women, a low-dose magnesium sulfate regime has been introduced by some authors. Increased blood levels of magnesium in neonates is associated with increased still birth, early neonatal death, birth asphyxia, bradycardia, hypotonia, gastrointestinal hypomotility. The objective of this study was to assess safety of low-dose magnesium sulfate regimen in neonates of eclamptic mothers treated with this regimen.

Materials and Methods:

This was a cross-sectional observational study of 100 eclampsia patients and their neonates. Loading dose and maintenance doses of magnesium sulfate were administered to patients by combination of intravenous and intramuscular routes. Maternal serum and cord blood magnesium levels were estimated. Neonatal outcome was assessed.

Results:

Bradycardia was observed in 18 (19.15%) of the neonates, 16 (17.02%) of the neonates were diagnosed with hypotonia. Pearson Correlation Coefficient showed Apgar scores decreased with increase in cord blood magnesium levels. Unpaired t-test showed lower Apgar scores with increasing dose of magnesium sulfate. The Chi-square/Fisher''s exact test showed significant increase in hypotonia, birth asphyxia, intubation in delivery room, Neonatal Intensive Care Unit (NICU) care requirement, with increasing dose of magnesium sulfate. (P ≤ 0.05).

Conclusion:

Several neonatal complications are significantly related to increasing serum magnesium levels. Overall, the low-dose magnesium sulfate regimen was safe in the management of eclamptic mothers, without toxicity to their neonates.KEY WORDS: Eclampsia, low-dose magnesium sulfate, serum magnesium level, neonatal outcome  相似文献   

2.

Objective:

To study the anticonvulsant activity and neurotoxicity of ethanolic extract and ethyl acetate fraction of the rhizome of Smilax china (EESC and EAF, respectively) in mice.

Materials and Methods:

The anticonvulsant activities of EESC and EAF were studied against maximal electroshock (MES) and pentylenetetrazole (PTZ)-induced seizures in mice and neurotoxicity was determined using rotarod test.

Results:

The duration of hindleg extension in MES test was reduced significantly (P < 0.001) by EESC at a dose level of 400 mg/kg and EAF at both higher dose levels (200 and 400 mg/kg). In PTZ model, the seizure latency was prolonged by all the test groups.

Conclusion:

The EESC and EAF may help to control petit mal and grand mal seizures.  相似文献   

3.

Background and the purpose of the study

The objective of the present work was to improve bioavailability of cepodoxime proxetil through gastroretentive microballoon formulation.

Methods

Microballoons of cefpodoxime proxetil were formulated by solvent evaporation and diffusion method employing hydroxypropylmethyl cellulose (HPMC) and ethyl cellulose (EC) polymers and characterized for particle size, surface morphology, incorporation efficiency, floating behavior, in vitro drug release study and differential scanning calorimetry (DSC).

Results

The average particle size of formulated microballoons was in the range of 54.23±2.78–95.66±2.19µm. Incorporation efficiencies of over 83.77±0.85% were achieved for the optimized formulations. Most of formulations remained buoyant (having buoyancy percentage maximum of 81.36±1.96%) for more than 12 hrs indicating good floating behavior of microballoons. Higher values of correlation coefficients were obtained with Higuchi''s square root of time kinetic treatment heralding diffusion as predominant mechanism of drug release.

Conclusion

Inferences drawn from in vitro studies suggest that microballoons may be potential delivery system for cefpodoxime proxetil with improvement in bioavailability in comparison to conventional dosage forms.  相似文献   

4.

Objective:

To investigate the anticonvulsant and muscle relxant activity of ethanolic extract of stems of Dendrophthoe falcata in mice.

Materials and Methods:

The ethanolic extract of stems of D. falcata (100, 300 and 500 mg/kg, p.o.) was studied for its anticonvulsant effect on maximal electroshock-induced seizures and muscle relaxant activity at the same dose level using rota rod and traction test in mice.

Results:

Preliminary phytochemical analysis revealed presence of proteins, carbohydrates, glycosides, steroids, triterpenes, flavonoids, tannins and phenolic compounds. D. falcata ethanolic extract (DFEE) (100, 300 and 500 mg/kg, p.o.) significantly (P<0.001) inhibited seizures induced by MES, reduced the duration of Hind limb tonic extensor phase (HLTE) and a decline in motor coordination.

Conclusion:

The ethanolic extract possesses anticonvulsant activity and muscle relaxant activity.KEY WORDS: Anticonvulsant, Dendrophthoe falcate, mice, muscle relaxant  相似文献   

5.

Background:

To study the anticonvulsant effect of different extracts of Centella asiatica (CA) in male albino rats with reference to Na+/K+, Mg2+ and Ca2+-ATPase activities.

Materials and Methods:

Male Wistar rats (150±25 g b.w.) were divided into seven groups of six each i.e. (a) control rats treated with saline, (b) pentylenetetrazol (PTZ)-induced epileptic group (60 mg/kg, i.p.), (c) epileptic group pretreated with n-hexane extract (n-HE), (d) epileptic group pretreated with chloroform extract (CE), (e) epileptic group pretreated with ethyl acetate extract (EAE), (f) epileptic group pretreated with n-butanol extract (n-BE), and (g) epileptic group pretreated with aqueous extract (AE).

Results:

The activities of three ATPases were decreased in different regions of brain during PTZ-induced epilepsy and were increased in epileptic rats pretreated with different extracts of CA except AE.

Conclusion:

The extracts of C. asiatica, except AE, possess anticonvulsant and neuroprotective activity and thus can be used for effective management in treatment of epileptic seizures.  相似文献   

6.

Background and the purpose of the study

Microemulsions are thermodynamically stable, clear dispersions of water, oil, surfactant, and cosurfactant. This study was aimed to develop flurbiprofen microemulsion for enhanced transdermal delivery and investigate the effects of different surfactants and cosurfactants on its delivery and phase behavior.

Method

Various surfactant-cosurfactant mixtures in ratio of 2:1 (Smix) along with oleic acid (oil) were selected and phase diagrams were constructed. Six microemulsions each containing 5% drug, 5% oil, 56% Smix and 34% water, were prepared and compared for their permeation and phase behaviors to determine the effects of the type of Smix.

Results

In vitro transdermal permeation through rabbit skin of all microemulsions was high than saturated aqueous drug solution. Tween 20 and ethanol as Smix produced the highest flux amongst all the Smix, and were used to prepare formulations with different values of oil and Smix. While the type of surfactant did not affect the droplet size, propylene glycol as cosurfactant produced the largest droplets and highest viscosity. Decrease in oil or Smix concentration resulted in decrease of the droplet size and increase in permeation flux while decrease in viscosity also increased the permeation flux of microemulsions. Finally the selected microemulsion formulation comprising 5% flurbiprofen, 5% oleic acid, 46% Tween 20:ethanol (2:1) and 44% water, showed the highest transdermal flux and caused no skin irritation.

Conclusion

Type of surfactant and cosurfactant affect both the phase behavior and transdermal drug delivery of microemulsion; and results of this study showed that they are promising vehicles for improved transdermal delivery and sustained action of flurbiprofen.  相似文献   

7.

Objective:

The Delhi State Drug Policy was adopted in 1994 following which the first Essential Medicines List (EML) was developed in 1996. The Delhi State Essential Medicines Formulary was brought out in 1997. A need was felt to revise the formulary to match with the EML as the EML is renewed every 2 years.

Materials and Methods:

A survey was undertaken to elicit the opinions of the doctors practicing in the state on the usefulness of the formulary before revising and printing the updated version. The survey covered dispensaries, 10–20 bedded hospitals, 100-bedded hospitals and two tertiary care hospitals. Discussions were focused on questionnaires on attitudes toward adopting Essential Medicines Formulary using a 10-point scale.

Results:

Of the 200 doctors approached, only 90 doctors completed the questionnaire. Sixty-nine respondents (76.6%) had received the copy of the formulary. Most practitioners welcomed the formulary and were satisfied with the coverage and selection of the medicines. Most respondents (76.9%) agreed that a well-developed formulary would improve the quality of the public health care system, although they had reservations about the authority, relevance and effect on professional autonomy.

Conclusion:

About 74% of the respondents used the formulary in clinical practice as a source of medicine information, which makes its regular revision necessary.  相似文献   

8.

Background and the purpose of the study

Diclofenac sodium is a non-steroidal anti-inflammatory agent with a short biological half-life (1–2 hr) and requires multiple dosing. This research was carried out to develop and optimize diclofenac sodium loaded alginate-PVP K 30 microbeads to eliminate the need for multiple dosing and adverse effects.

Methods

Diclofenac sodium loaded alginate-PVP K 30 microbeads were prepared by ionotropic gelation. Particle size, drug release, swelling, FTIR and SEM analyses were performed.

Results

Optimized microbeads showed particle size of 0.589±0.054 to 0.620±0.067 mm, and drug entrapment efficiency of 97.88±2.86 to 98.60±3.55%. The in vitro drug release from microbeads was sustained over 10 hrs and followed controlled-release pattern. FTIR analysis indicated the possibility of intermolecular hydrogen bonding interactions, i.e., –OH…O=C in microbeads.

Conclusion

Microbeads for oral controlled delivery of diclofenac sodium were successfully developed by ionotropic gelation.  相似文献   

9.

AIMS

To investigate the transfer of chloroquine and its major bioactive metabolite desethylchloroquine across the placenta and into breast milk.

METHODS

In Papua New Guinea, chloroquine (CQ; 25 mg base kg−1) is recommended for prophylaxis of malaria during pregnancy, and at the Alexishafen Health Centre women are routinely prescribed CQ at the time of delivery. Fetal-cord and maternal serum samples were collected at delivery (n = 19) and milk samples were collected from day 3 to day 17–21 after delivery (n = 16). CQ and its primary active metabolite desethylchloroquine (DECQ) were quantified by high-performance liquid chromatography. For both CQ and DECQ cord/maternal ratios (C/M) were calculated to characterize placental transfer, and infant exposure via milk was estimated by standard methods.

RESULTS

The median (interquartile range) C/M was 1.1 (0.9, 1.6) for CQ and 1.2 (0.5, 1.8) for DECQ. The average concentration in milk over the time of sampling was 167 μg l−1 (27, 340) for CQ and 54 μg l−1 (22, 106) for DECQ. Estimated absolute and relative infant doses were 34 μg kg−1 day−1 (7, 50) and 15 μg kg−1 day−1 (4, 26), and 2.3% (0.5, 3.6) and 1.0% (0.4, 2.0) for CQ and DECQ (as CQ equivalents), respectively.

CONCLUSION

Infant exposure to CQ and DECQ during pregnancy will be similar to that in the maternal circulation, and dependent on maternal dose and frequency. The median CQ + DECQ relative infant dose of 3.2% (as CQ equivalents) was low, confirming that use of CQ during lactation is compatible with breastfeeding.

WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT

  • The literature on placental and milk transfer of chloroquine and its major bioactive metabolite desethylchloroquine is sparse and incomplete.

WHAT THIS STUDY ADDS

  • We have provided data on the transplacental transfer of chloroquine and desethylchloroquine in Melanesian women (n = 19), measured transfer of these drugs into breast milk (n = 16) and estimated absolute and relative infant doses for the breastfed infant.
  • The data for desethylchloroquine are novel.
  • In all three areas we have significantly increased both quantity and quality of the available database.
  相似文献   

10.

Background and the purpose of the study

Budesonide is the drug of choice for treatment of active inflammatory bowel disease (IBD). The aim of this study was to develop budesonide pellets based on a novel colon drug delivery system (CODES).

Methods

Pellet cores containing lactulose or mannitol were prepared by extrusion/spheronization and coated with an acid soluble polymer (Eudragit E100), hydroxypropylmethyl cellulose (HPMC) and an enteric coat (Eudragit FS 30D) sequentially. In vitro drug release of coated pellets was studied using USP dissolution apparatus type II in buffers of pH 1.2 (2 hrs), pH of 7.4 (4 hrs) and pH of 6.8 containing 8% rat cecal contents (RCC) (18 hrs). The efficacy of the optimized formulation (containing 50% lactulose coated with Eudragit E (30% w/w) and Eudragit FS 30D (12% w/w)) was evaluated against 2, 4, 6-trinitrobenzenesulfonic acid (TNBS)-induced colitis in rats.

Results

The results of the kind of bacteria in vitro dissolution tests indicated absence of drug release in pHs of 1.2 and 7.4 and controlled release in buffer of pH 6.8 containing RCC. It was found that release rate was controlled by the type and amount of polysaccharide and the thickness of the acid soluble layer. The prepared formulation showed promising results in alleviating the conditions of experimental model of colitis.

Conclusion

The results of this study suggest that pellets based on CODES technology could be useful for colonic delivery of budesonide.  相似文献   

11.

Aim:

As injection is not an ideal means for insulin delivery, various attempts have been made to administer insulin orally until now. The development of an oral dosage form of insulin would help diabetic patients and make the treatment more convenient. The aim of the present study is to evaluate the effectiveness of an oral insulin formulation containing polar and non-polar ingredients.

Materials and Methods:

New excipient for oral insulin administration in normal and diabetic rats was evaluated by measuring blood glucose concentrations in two groups (10 rats each) of normal and streptozotocin-induced diabetic rats. Oral insulin was administrated and blood glucose was measured by glucometer at 0, 1, 2, 3 and 4 h post-feeding. The data was compared by Student''s t test.

Results:

Oral insulin formulation significantly (P<0.05) reduced blood glucose from 100 mg/dl to 33.73 mg/dl and 451.66 mg/dl to 200.83 mg/dl at 4 h in normal and diabetic rats, respectively.

Conclusion:

The novel excipient used could protect insulin from gastric and pancreatic enzymes and reduce blood glucose concentration in both healthy and diabetic rats suggesting that oral delivery of insulin is feasible in a near future.KEY WORDS: Blood glucose, normal and diabetic rats, oral insulin  相似文献   

12.

Context:

Nanotechnology is an empowering technology that holds promise in cancer therapeutics by increasing the ratio of tumor control probability to normal tissue complication probability. It can increase the bioavailability of the drug at the target site, reduce the frequency of administration and reach otherwise lesser-accessible sites. The present study shows the feasibility of the cisplatin-loaded albumin nanoparticle as a sustained delivery system.

Aims:

Cisplatin is one of the most widely used chemotherapeutic agents for the treatment of malignant disorders. Conventional cisplatin formulation given as intravenous infusion has low bioavailability to the target organ in addition to significant side-effects, like ototoxicity and nephrotoxicity. The aim of this study was to develop a protein-based nanoparticulate system for sustained release of cisplatin.

Materials and Methods:

Nanoparticles were prepared by the coacervaton method of microcapsulation and chemical cross-linking with glutaraldehyde. Particle size was characterized by dynamic light scattering and transmission electron microscopy.

Results and Conclusions:

Using the coacervation method, nanoparticles of less than 70 nm diameter were produced. Drug encapsulation measured by ultraviolet spectroscopy varied from 30% to 80% for different ratios of cisplatin and protein. In vitro release kinetics shows that the nanoparticle-based formulation has biphasic release kinetics and is capable of sustained release compared with the free drug (80% release in 45 h). The study proves the feasibility of the albumin-based cisplatin nanoparticle formulation as a sustained release vehicle of cisplatin.  相似文献   

13.

Objective:

Depression is a dilapidating disorder, which may occur during pregnancy. Citalopram is an antidepressant drug often prescribed to pregnant women. The purpose of the present study is to determine whether maternal administration of citalopram affects fetal liver histology.

Materials and Methods:

Pregnant Wistar albino rats were treated with citalopram (10 or 20 mg/kg/day). A control group received no treatment. Rat fetal liver samples were obtained on day 18 of gestation and evaluated morphologically and histologically.

Results:

Statistical evaluation of data showed that there were no differences in liver weight and relative liver weight between control and citalopram treatment groups. Liver histology changes (such as increases in the number of Kupffer cells and lymphocytes) were seen in the fetuses of the group receiving a high dose of citalopram during gestation. Degeneration of hepatocytes was not seen and the megakaryocyte number did not change significantly in the citalopram treated groups.

Conclusion:

This study showed that citalopram administration during gestation may have some adverse effects on the phagocytic cell population in the fetal liver of rats.KEY WORDS: Citalopram, depression, fetus, histology, liver  相似文献   

14.

Aim(s)

The current investigation aims to provide new insights into fetal exposure to tacrolimus in utero by evaluating maternal and umbilical cord blood (venous and arterial), plasma and unbound concentrations at delivery. This study also presents a case report of tacrolimus excretion via breast milk.

Methods

Maternal and umbilical cord (venous and arterial) samples were obtained at delivery from eight solid organ allograft recipients to measure tacrolimus and metabolite bound and unbound concentrations in blood and plasma. Tacrolimus pharmacokinetics in breast milk were assessed in one subject.

Results

Mean (±SD) tacrolimus concentrations at the time of delivery in umbilical cord venous blood (6.6 ± 1.8 ng ml−1) were 71 ± 18% (range 45–99%) of maternal concentrations (9.0 ± 3.4 ng ml−1). The mean umbilical cord venous plasma (0.09 ± 0.04 ng ml−1) and unbound drug concentrations (0.003 ± 0.001 ng ml−1) were approximately one fifth of the respective maternal concentrations. Arterial umbilical cord blood concentrations of tacrolimus were 100 ± 12% of umbilical venous concentrations. In addition, infant exposure to tacrolimus through the breast milk was less than 0.3% of the mother''s weight-adjusted dose.

Conclusions

Differences between maternal and umbilical cord tacrolimus concentrations may be explained in part by placental P-gp function, greater red blood cell partitioning and higher haematocrit levels in venous cord blood. The neonatal drug exposure to tacrolimus via breast milk is very low and likely does not represent a health risk to the breastfeeding infant.  相似文献   

15.

Objective:

Cutaneous drug reactions are the most common type of adverse drug reactions. Adverse cutaneous drug reactions form 2-3% of the hospitalized patients. 2% of these are potentially serious. This study aims to detect the drugs commonly implicated in Steven Johnson Syndrome-Toxic Epidermal Necrosis (SJS-TEN).

Materials and Methods:

A retrospective analysis was done in all patients admitted in the last five years in SDM hospital with the diagnosis of SJS-TEN.

Results:

A total of 22 patients with SJS-TEN were studied. In 11 patients anti-epileptics was the causal drug and in 7, anti-microbials was the causal drug. Recovery was much faster in case of anti epileptics induced SJS-TEN as compared to that induced by ofloxacin.

Conclusion:

SJS-TEN induced by ofloxacin has a higher morbidity and mortality compared to anti convulsants.KEY WORDS: Anti-epileptics, ofloxacin, Stevens Johnson syndrome, toxic epidermal necrosis  相似文献   

16.

Background:

Patients admitted to cardiology department are mostly on polypharmacy. So drug-drug interactions and adverse effects of drugs are quite common. Yet, there is a paucity of data regarding adverse drug reaction (ADR) monitoring in cardiology department in India. The present study is an effort to fill up these lacunae.

Materials and Methods:

A prospective, observational study registering 966 indoor cardiology patients according to predetermined inclusion and exclusion criteria was conducted for one year. ADR profile was noted by spontaneous reporting and intensive monitoring. Naranjo ADR probability scale was used to establish the causality.

Results:

A total of 208 ADRs were reported from 188 patients (19.5%). Of these 188 patients, 62 patients (33%) were hospitalized primarily due to the development of ADRs, while 126 (67%) patients developed ADRs during hospital stay. Nitrates were the most common offender drug group (17.8%).

Conclusion:

Development of ADR in one of every five cardiac patient points toward a grave situation, but a higher incidence of Type A reactions in cardiology department means that these can be avoided.  相似文献   

17.

Background:

Magnesium sulphate is a high-risk medication that is used extensively for prophylaxis and treatment of eclampsia. To accommodate recommendations related to fluid restrictions and patient safety, a protocol was developed for the administration of 20% magnesium sulphate.

Objectives:

To determine whether administration of 20% magnesium sulphate increased the risk of phlebitis relative to 2% to 8% magnesium sulphate solutions, to determine if the institution’s protocol for administration of 20% magnesium sulphate reduced errors during administration, and to identify strategies to further reduce potential errors.

Methods:

A retrospective chart audit was undertaken for patients who had received magnesium sulphate for prophylaxis of eclampsia from December 2004 to December 2007. A failure mode and effect analysis was used to identify additional safety strategies.

Results:

A total of 47 patients received magnesium sulphate according to the old administration protocol (2% to 8% solution) and 29 according to the new protocol (20% solution). No evidence of phlebitis was documented for any of these 76 patients. A few errors occurred with changes in rates or concentrations and because of failure to reset the pump after the loading dose, but there was no documented harm to any of the patients. Strategies to further reduce errors in the administration of magnesium sulphate included development of preprinted orders, use of 20% magnesium sulphate for all infusion rates, changes to pump settings to enable use of fractional infusion rates, preparation of magnesium sulphate in mini-bags in the pharmacy, double-check of pump settings by nurses, anesthesiology consult, and distribution of protocols to all areas in the hospital (to limit errors associated with patient transfers).

Conclusions:

There was no documented phlebitis, and fewer errors occurred when 20% magnesium sulphate was used. Several additional strategies were identified to reduce errors in the administration of this high-risk medication.  相似文献   

18.

Background:

The students are in the best position to comment on the effectiveness of any teaching system and they may be regarded as the best judges to assess the teaching and evaluation methods.

Objective:

This study was designed to obtain student feedback on teaching and assessment methods in the subject of pharmacology and use it for improvement.

Materials and Methods:

Based on student feedback from batch 2006, innovative strategies were implemented. To know the effect of these strategies feedback was obtained from subsequent batch 2007 using a written validated questionnaire covering various aspects of teaching and assessment methods.

Results:

Students were satisfied with all teaching methods except lecture, seminars and pharmacy exercises. Majority of the students showed preference for tutorials, short answer questions and revision classes. All students felt that there should be more time for clinical pharmacology and bedside teaching. The performance score of the students (batch 2007) indicated improvement in their scores (12%) when earlier feedback suggestions were implemented. The pass percentage of the subsequent batch in university examinations improved from 90 to 100%.

Conclusion:

The implementation of suggestions obtained from students resulted in improvement in their performance. Hence, it is very essential to synchronize teaching and evaluation methods with special requirements of medical students.  相似文献   

19.

Background

Chitosan has gained considerable attentions as a biocompatible carrier to improve delivery of active agents. Application of this vehicle in the form of nanoparticle could profit advantages of nanotechnology to increase efficacy of active agents.The purpose of this study was to provide detailed information about chitosan–glutathione (Cht-GSH)nanoparticles which are gaining popularity because of their high mucoadhesive and extended drug release properties.

Methods

Depolymerization of chitosan was carried out using sodium nitrite method.Glutathione was covalently attached to chitosan and the solubility of the resulting conjugates was evaluated. Nanoparticles were prepared by ionic gelation method and then the effect of glutathione immobilization on properties of nanoparticles was investigated.

Results

Thiolation efficiency was higher in lower molecular weight chitosan polymers compared to unmodified chitosan nanoparticles. Cht-GSH conjugates of the same molecular weight but with different degrees of thiolation had the same hydrodynamic diameter (995± nm) and surface charge (102± mV) as unmodified chitosan, but comprised of a denser network structure and lower concentration. Cht-GSH nanoparticles also exhibited greater mucoadhesive strength which was less affected by ionic strength and pH of the environment.

Conclusion

Thiolation improves the solubility of chitosan without any significant changes in size and charge of nanoparticles, but affects the nanogel structure.  相似文献   

20.

Objective:

To compare the pattern, efficacy, and tolerability of self-medicated drugs and to assess the adequacy of their dose in primary dysmenorrhea (PD).

Materials and Methods:

A survey using a self-developed, validated, objective, and structured questionnaire as a tool was conducted among subjects with PD. Statistical analysis was carried out using Chi-square test and ANOVA with post-hoc Tuckey''s test.

Results:

Out of 641 respondents, 42% were self-medicated. The pattern of drugs used was: Dicyclomine, an unknown drug, mefenamic acid, mefenamic acid + dicyclomine, and metamizole by 35%, 29%, 26%, 9%, and 1% of respondents, respectively. Mefenamic acid + dicyclomine, the combination was the most efficacious in comparison to other drugs in moderate to severe dysmenorrhea. There was better tolerability with mefenamic acid + dicyclomine group compared to other drugs. Sub-therapeutic doses were used by 86% of self-medicating respondents.

Conclusions:

The prevailing self-medication practices were inappropriate in a substantial proportion of women with inadequate knowledge regarding appropriate drug choice, therapeutic doses, and their associated side effects.KEY WORDS: Efficacy, primary dysmenorrhea, self-medication, survey, tolerability  相似文献   

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