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ABSTRACT Bilateral acute depigmentation of the iris and bilateral acute iris transillumination (BAIT) are similar clinical entities. The former causes acute-onset depigmentation of the iris stroma without transillumination, whereas the latter causes depigmentation of the iris pigment epithelium with transillumination. The etiopathogenesis of these conditions is not yet fully understood, but the proposed causes include the use of systemic antibiotics (especially moxifloxacin) and viral triggers. We present a case series of five female patients with a mean age of 41 (32-45) years, all of whom suffered acute onset of bilateral pain and redness of the eyes after moxifloxacin use (oral or topical). It is important for ophthalmologists to be aware of the two forms of iris depigmentation since this case series suggests that SARS-CoV-2 or its empirical treatment with moxifloxacin may trigger iris depigmentation. If this is the case, clinicians will likely see increased incidences of bilateral acute depigmentation of the iris and bilateral acute iris transillumination during and after the COVID-19 pandemic.
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Moxifloxacin (MOX) is a fluoroquinolone antibiotic, a second-line anti-TB drug widely used in the treatment of multidrug-resistant tuberculosis (MDR TB) and drug-susceptible TB. MOX have taste and smell issues with low patient compliance, especially in the pediatric population. MOX taste-masked dispersible tablets were developed by direct compression method using mannitol, aspartame as a sweetening agent and lemon flavor as a flavoring agent. The prepared granules were evaluated for flow properties and compressed tablets for hardness, friability, content uniformity, weight variation, DT and in-vitro drug release. Instrumental analysis like FTIR, DSC and XRD was also performed. The flow properties of the granules of batch F6 were found to be excellent based on the results obtained. The weight variation and content uniformity of the tablets was found to be excellent F6 due to the excellent flow properties of the granules. All of the tablets in the study disintegrated between 22 (F6) to 135 seconds (F1), meeting the official requirement (3 minute) for dispersible tablets. The optimized batch showed complete drug release within 10 minutes time period. The FTIR and DSC study found no incompatibility between the drug excipients. The MOX in the final formulation was present in crystalline form, as shown by XRD. The dispersible MOX tablets could be a better option for treating pediatric TB.
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BACKGROUND: Endophthalmitis is a serious infectious complication of cataract surgery, which may lead to vision loss. Aim: To evaluate the effectiveness of intracameral moxifloxacin in reducing endophthalmitis after cataract surgery in Chilean patients. MATERIAL AND METHODS: We reviewed all phacoemulsification surgeries performed between 2012 and 2020 at a public hospital. The use of intraoperative intracameral moxifloxacin and possible surgical complications were recorded. In patients with postoperative endophthalmitis, we reviewed their risk factors and clinical characteristics. RESULTS: In the study, 22,869 phacoemulsification surgeries were registered, with an annual average of 2,541. The use of prophylactic intracameral moxifloxacin started progressively in 2014. In 2018 it was used in 88% of the surgeries. Fifteen eyes evolved with postoperative endophthalmitis, but none of these surgeries used intracameral moxifloxacin. Five and seven cases occurred in 2012 and 2013, respectively. There was a trend favoring moxifloxacin use, as a preventive measure for endophthalmitis, but the difference between groups was not significant (p = 0.56). In the group with endophthalmitis, 33.3% of the eyes were from patients with type 2 diabetes mellitus, in 13.3% there was rupture of the posterior capsule and 60% of the eyes corresponded to female patients. Since 2018 there is no record of endophthalmitis after cataract surgery performed in this center. Conclusions: Intracameral moxifloxacin showed a tendency to reduce the frequency of endophthalmitis after phacoemulsification surgery, but a longer observation period is required to reach statistical significance, due to the low frequency of this complication.
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Humanos , Catarata/tratamiento farmacológico , Endoftalmitis/etiología , Endoftalmitis/prevención & control , Endoftalmitis/tratamiento farmacológico , Complicaciones Posoperatorias/prevención & control , Profilaxis Antibiótica , Fluoroquinolonas/uso terapéutico , Moxifloxacino , Antibacterianos/uso terapéuticoRESUMEN
OBJECTIVE To compare the efficacy, safety and economics of bid-winning and original Moxifloxacin hydrochloride tablets in the treatment of outpatient community-acquired pneumonia (CAP). METHODS A retrospective cohort study was conducted to screen and include CAP outpatients during the period of January to December 2021 in Lianyungang First People’s Hospital. They were divided into generic drug group (1 058 cases) and bid-winning drug group (1 121 cases) according to the drug source. Two groups were respectively given original and bid-winning Moxifloxacin hydrochloride tablets, 0.4 g each time, once a day. The efficacy indexes (clinical effective rate, remission time, treatment course, revisiting rate) and safety indexes (allergy, nervous system symptoms, etc.) were compared between the two groups; and the influence factors of clinical treatment failure were analyzed with multi-factor modified Poisson regression model. The economic indicators of the two drugs [quantity, consumption sum, defined daily doses (DDDs), defined daily dose cost (DDDc), price ratio, replacement rate] were compared. RESULTS There were no significant differences in the clinical effective rate, treatment course, revisiting rate, the incidence of nervous system symptoms and Q-T interval prolongation between the two groups (P>0.05). The remission time of original drug group was significantly shorter than that of bid-winning drug group, and the incidence of total adverse drug reaction, allergy reaction, gastrointestinal symptom reaction and hyperglycemia were significantly lower than those in bid-winning drug group(P<0.05). Multivariate Poisson regression analysis showed that bid-winning drug did not increase the risk of clinical treatment failure in CAP outpatients [RR=1.132, 95%CI (0.883, 1.542), P=0.327]. However, antibiotic exposure history, more than 2 items of abnormal clinical manifestations and auxiliary examination all increased the risk of clinical treatment failure (P<0.05). Compared with before the implementation of centralized volume-based procurement policy, the quantity and DDDs of Moxifloxacin hydrochloride tablets increased significantly, while the consumption sum decreased significantly, DDDc of bid-winning drug decreased significantly, the price ratio of it to original drug decreased to 0.117, and the replacement rate increased to 69.44% after the implementation of centralized volume- based procurement policy. CONCLUSIONS Compared with original drug, bid-winning Moxifloxacin hydrochloride tablet shows reliable efficacy and obvious price advantage in the treatment of outpatient CAP, but the incidence of adverse drug reactions is higher.
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Based on the dual needs of analgesia and anti-inflammation in trauma treatment, this study uses acetaminophen and moxifloxacin hydrochloride as active pharmaceutical ingredients and develops a composite bilayer tablet with a dual-phase drug release system by using binder jet 3D printing technology. Due to the complexity of the 3D printing process, there is an interaction between the various parameters. Through the optimization of the process, the relationship between the key process parameters can be determined more intuitively. In this study, the process of extended-release tablets was optimized to maintain the mechanical properties of the tablets while realizing the regulation of release. The full-factor experimental design of three central points 23 was used to analyze the factors that significantly affect the quality attributes of extended-release tablets and the interaction between factors. The optimal extended-release process parameters were obtained by the response optimizer: the inkjet quantity of the printing ink was 10 (about 13.8 pL), the powder thickness was 180 μm, and the running speed was 360 mm·s-1. The in vitro of release of 3D printed composite bilayer tablets showed that the in vitro of release of 3D printed tablets and commercially available tablets conformed to the Ritger-Peppas release model. The results of porosity showed that the immediate-release layer of the preparation has many pores and large pore size, and the dissolution of the immediate release layer within 15 min was greater than 85%. The internal pore size of the extended release layer is large, but it can still release slowly for up to 8 h, the mechanism may be related to the extended release of HPMC gelation. On the basis of verifying the rationality of the design goal of 3D printed composite bilayer tablets, this study also provides a theoretical basis for the preparation of 3D printing complex preparations.
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Purpose: To compare different endophthalmitis prophylaxis methods adopted in cataract surgery (manual small-incision cataract surgery and phacoemulsification) between the years 2013 and 2021 in the community eye care section of a tertiary eye care hospital in South India and report their outcomes. Methods: All cataract surgeries performed from January 2013 to December 2021 (2,46,874 surgeries) at a single center were included in this retrospective study. The different endophthalmitis rates with each regimen were analyzed and evaluated. Results: 70,081 surgeries were performed from January 2013 to February 2015, where Tobramycin was added to Balanced Salt Solution (BSS) (Group A). From March 2015 to January 2017, 63,245 surgeries were performed when intracameral Moxifloxacin was given (Group B). From February 2017 to December 2021, 1,13,548 surgeries were performed were Amikacin was added to BSS (Group C). In total, 42 cases of postoperative endophthalmitis were reported during the study period (0.02%). There was no significant difference in the endophthalmitis rates between groups A and B (P = 0.4152); however, there was a significant decrease in endophthalmitis rates in group C when compared with group A (P = 0.04) and group B (P = 0.006). Conclusion: There was a significant reduction in the rates of endophthalmitis following the addition of amikacin in irrigating BSS. Nocardia was one of the predominant organisms isolated from these endophthalmitis patients. This is the first single-center study to report a comparative analysis of different endophthalmitis prophylactic measures in a community eye care set up with a high incidence of Nocardia endophthalmitis prevented with amikacin in BSS irrigating solution.
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Background: Antimicrobials are routinely prescribed in several disease conditions in which infections are established or suspected to be the reason for the illness. Excessive and irrational use of antimicrobials leads to development of drug resistance in microorganisms, besides increasing health-care expenditure. Antimicrobial resistance (AMR) leads to increase in morbidity and mortality. The rational use of antimicrobials is a major health need in all countries. Hence, assessment of prescribing pattern of antimicrobials is essential for clinical, educational, and economic purposes. Aims and Objectives: The objectives of the study were to evaluate and compare the prescribing pattern of antimicrobials by assessing – (i) commonly used antimicrobials; and (ii) disease conditions for which they were prescribed. Materials and Methods: It was a prospective observational study done for a period of 1 month. All the prescriptions in which antimicrobials were prescribed in the outpatient departments (OPD) and in-patient wards (IP) were included in the study. Prescriptions were analyzed for demographic and antibiotic data. Results: 1092 prescriptions were collected and analyzed. Among them, 690 prescriptions were from OPD and 382 prescriptions from in patient wards. Out patient data: Cefixime (21.30%) was commonly prescribed followed by fixed dose combination of Amoxicillin + Clavulanic acid (14.64%) and Ciprofloxacin (8.84%). Cefixime was commonly prescribed for URTI (13.43%). Oral route (82.17%) was the preferred route of administration. IP data: Cefotaxime (26.45%) was commonly prescribed followed by fixed dose combination of Piperacillin + Tazobactum (15.29%) and Ceftriaxone (14.46%). Cefotaxime was commonly prescribed preoperatively for most of the surgeries (76.56%). Intravenous route (46.86%) was the preferred route of administration. Single antimicrobial therapy (81.41%) was preferred followed by double (17.80%) and triple (0.79%) antimicrobial therapy. Conclusion: Cefixime and cefotaxime were commonly used in OPD and in patient wards, respectively. Oral route and intravenous route were the preferred route in OPD and IP wards, respectively. Single antimicrobial therapy was commonly preferred in both IP and out-patient wards. Although double and triple antimicrobial therapy was prescribed in small number of patients, it should be cautiously used to prevent AMR.
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Purpose: This study aimed to analyze the clinical presentations, microbiology, and management outcomes of post–cataract surgery endophthalmitis, with and without intracameral moxifloxacin prophylaxis. Methods: This study was designed as a retrospective, consecutive, comparative case series. Records of consecutive cataract surgery from January 1, 2015, till June 30, 2020, were analyzed. The cases that developed endophthalmitis were analyzed. The endophthalmitis cases were divided by their prophylaxis treatment into two groups: with intracameral moxifloxacin (ICM) and without (N?ICM). Inclusion criteria were (1) age ? 18 years, (2) cataract surgery with intraocular lens implantation, (3) endophthalmitis within 6 weeks of cataract surgery, and (4) cataract surgery in the institute by any of the three methods—phacoemulsification, manual small incision cataract surgery, and extracapsular cataract extraction. Results: In the study period, 66,967 cataract surgeries were performed; 48.7% (n = 32,649) did not receive ICM. There was no difference between the N?ICM and ICM groups in the incidence of clinical (n = 21, 0.064% and n = 15, 0.043%; P = 0.23) and culture proven (n = 19, 0.033% and n = 11, 0.023%; P = 0.99) endophthalmitis, respectively. Greater number of patients in the N?ICM group had lid edema (76.2% vs. 40%; P = 0.03), corneal edema (71.4% vs. 33.3%; P = 0.03) and lower presenting vision with available correction (logMAR [logarithm of the minimum angle of resolution] 1.26 ± 1.2 vs. logMAR 0.54 ± 0.85; P = 0.02). The final best?corrected visual acuity following treatment was worse in the N?ICM group (logMAR 1.26 ± 1.2 vs. 0.54 ± 0.85; P = 0.02). Conclusion: Endophthalmitis after intracameral moxifloxacin may have relatively milder signs and symptoms and may respond better to treatment.
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Postoperative endophthalmitis (POE) is a serious vision-threatening complication of cataract surgery, with an incidence rate of 0.033%-0.11% in China.In recent years, numerous retrospective studies and data analyses have reported that intracameral injection of antibiotics can effectively reduce the incidence of bacterial endophthalmitis, which commonly include cefuroxime, vancomycin and moxifloxacin.Globally, due to factors such as the availability, cost-effectiveness, and types of pathogens of POE, the drug choice varies to a large extent.Adverse events caused by antibiotics in the intracameral injection often occur, including macular edema, retinal vascular leakage, and uveitis caused by overdose of cefuroxime, and complications such as hemorrhagic retinal vasculitis obliterans due to vancomycin.Moxifloxacin, as a fourth-generation fluoroquinolone, has a significant effect on the prevention of bacterial endophthalmitis.Studies in the past five years related to moxifloxacin, and the significant advantages of moxifloxacin in the prevention of bacterial endophthalmitis, drug safety, duration of intracameral drug, and cost-effectiveness were summarized in this article.
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Objective:To investigate the clinical effects of moxifloxacin combined with biapenem on controlling inflammatory responses and improving immune function in older adult patients with severe pneumonia.Methods:120 older adult patients with severe pneumonia, who received treatment in the Second People's Hospital of Lishui from February 2017 to March 2020, were included in this study. They were randomly assigned to receive either biapenem (control group, n = 55) or moxifloxacin combined with biapenem (observation group, n = 65) for 7 days. Inflammatory response control, immune function improvement, and adverse reactions were assessed in each group after treatment. Results:After treatment, levels of interleukin-6 (IL-6), high-sensitivity C-reactive protein (hs-CRP) and procalcitonin (PCT) in the observation group were (24.51 ± 4.24) ng/L, (12.51 ± 3.15) mg/L and (4.62 ± 1.05) μg/L, respectively, which were significantly lower than those in the control group [(48.74 ± 4.67) ng/L, (26.80 ± 4.24) mg/L, (8.92 ± 1.10) μg/L, t = 29.77, 21.14, 21.87, all P < 0.001). The proportion of CD 3+ and CD 4+ cells and CD 4+ / CD 8+ ratio in the observation group were (63.27 ± 3.72)%, (39.97 ± 2.18)%, 1.79 ± 0.16, respectively, which were significantly higher than those in the control group [(55.58 ± 2.28)%, (35.18 ± 2.62)%, 1.41 ± 0.15, t = 17.08, 10.93, 13.34, all P < 0.001). Total effective rate was significantly higher in the observation group than in the control group [96.92% (63/65) vs. 83.64% (46/55), χ2 = 6.32, P < 0.05]. There was no significant difference in the incidence of adverse reactions between observation and control groups [10.77% (7/65) vs. 9.09% (5/55), χ2 = 0.09, P > 0.05]. Conclusion:Moxifloxacin combined with biapenem based on routine treatment for severe pneumonia in older adult patients can greatly strengthen anti-inflammatory effects, improve immune function, and enhance clinical efficacy without increasing adverse drug reactions.
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This study is to establish and validation in vivo models of moxifloxacin based on the theory of physiologically based pharmacokinetics (PBPK), and then to predict the distribution of moxifloxacin in human venous return and organ such as lung, spleen and so on. The efficacy of moxifloxacin and its pharmaceutical preparations were quantified by comparing the pharmacokinetic parameters with the minimum inhibitory concentration of related pathogenic bacterium. The results showed that the anti-infection efficacy of pharmaceutical moxifloxacin preparation in the corresponding organs was basically the same. The PBPK model of moxifloxacin preparations can be more accurately described the pharmacokinetic of anti-infective drugs in human, it is suitable for the efficacy evaluation of anti-infective drugs and provides a strong basis for the corresponding scientific research and scientific supervision.
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Objective:To investigate outcomes and safety of doxycycline-moxifloxacin sequential regimen in the treatment of Mycoplasma genitalium urethritis/cervicitis. Methods:From June 2019 to December 2020, patients with Mycoplasma genitalium urethritis/cervicitis confirmed by nucleic acid amplification testing were successively recruited at Department of Sexually Transmitted Diseases, Hospital of Dermatology, Chinese Academy of Medical Sciences, and received sequential therapy with oral doxycycline for 7 days followed by oral moxifloxacin for 7 days. Clinical and/or etiological assessment was conducted 2 to 3 weeks after the end of treatment. Fisher′s exact test was used to analyze factors influencing the treatment outcome. Results:Totally, 36 eligible subjects were enrolled, including 30 males and 6 females. Among them, 18 (50%) patients completed post-treatment etiological assessment, which showed that 12 achieved microbiological cure, and treatment failures occurred in 6; another 18 patients achieved clinical cure. The overall response rate to doxycycline-moxifloacin sequential therapy was 83.3% (30/36, 95% confidence interval[ CI]: 70.5%, 96.1%) . The treatment outcome showed no significant association with the patients′ age, gender, marital status, number of sexual partners in the past 1 month, history of sexually transmitted diseases, history of antibiotic use in the past 1 month, or co-infections (all P > 0.05) . Conclusion:The efficacy of doxycycline-moxifloacin sequential regimen is limited in the treatment of Mycoplasma genitalium infections in Nanjing area, and clinicians should be alerted to the possibility of treatment failure in clinical practice.
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Abstract Fluoroquinolones are an important class of antimicrobial agents to manage infectious diseases. However, knowledge about how host bile acids are modified by fluoroquinolones is limited. We investigated and compared the impact of fluoroquinolones on circulating bile acid profiles and gut microbiota from in vivo studies. We administered ciprofloxacin (100 mg/kg/day) or moxifloxacin (40 mg/kg/day) orally to male Wistar rats for seven days. Fifteen bile acids (BAs) from the serum and large intestine were quantified by HPLC-MS/MS. The diversity of gut microbiota after ciprofloxacin and moxifloxacin treatment was analyzed using high-throughput, next-generation sequencing technology. The two fluoroquinolone-treated groups had different BA profiles. Ciprofloxacin significantly reduced the hydrophobicity index of the BA pool, reduced secondary BAs, and increased taurine-conjugated primary BAs in both the serum and large intestine as compared with moxifloxacin. Besides, ciprofloxacin treatment altered intestinal microbiota with a remarkable increase in Firmicutes to Bacteroidetes ratio, while moxifloxacin exerted no effect. What we found suggests that different fluoroquinolones have a distinct effect on the host BAs metabolism and intestinal bacteria, and therefore provide guidance on the selection of fluoroquinolones to treat infectious diseases.
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Animales , Masculino , Ratas , Ácidos y Sales Biliares , Estudio Comparativo , Ciprofloxacina/análisis , Ratas Wistar , Microbioma Gastrointestinal , Moxifloxacino/análisis , Cromatografía Líquida de Alta Presión/métodos , Secuenciación de Nucleótidos de Alto Rendimiento , Interacciones Hidrofóbicas e Hidrofílicas , Intestino Grueso/anomalías , Antiinfecciosos/farmacologíaRESUMEN
Objective:To investigate the safety and efficacy of moxifloxacin in children with severe Mycoplasma pneumoniae pneumonia (SMPP).Methods:The patients with SMPP in the Pediatric Intensive Care Unit of Beijing Children's Hospital between January 2017 and April 2020 were retrospectively analyzed. Clinical data were collected to assess therapeutic efficacy, analyze drug safety and summarize positive rate of macrolide-resistant Mycoplasma pneumoniae genes mutation.Results:Thirty-nine children diagnosed SMPP treated with moxifloxacin were included. The positive rate of macrolide-resistant Mycoplasma pneumoniaegenes mutation was 95.2%. In the 39 patients, 6 (15.4 %) were cured, 29 (74.4 %) were effective, 2 (5.1 %) were no response, 2 (5.1 %) were discharged automatically during treatment with moxifloxacin, and the overall response rate was 89.8 %. The situations of consciousness, skin, joint, heart rhythm and gastrointestinal function were carefully observed; Blood routine test, liver and kidney function were closely monitored. There were no adverse drug reactions in the period of medication. No children were discontinued due to adverse reactions.Conclusions:Moxifloxacin can improve efficacy and prognosis for pediatric patients with SMPP. There are no drug adverse reactions during treatment with moxifloxacin, indicating that short-term medication is safe. The application of quinolones in pediatric patients is off-label drug use, and clinical pharmacists should assist clinicians in reducing medical risks.
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AIM: To study the pharmacokinetic characteristics of single-dose oral moxifloxacin hydrochloride tablets under fasting and fed conditions, and use moxifloxacin hydrochloride tablets produced by Bayer Pharma AG as a reference to compare the pharmacokinetic parameters of the two preparations, and evaluate the human bioequivalence of the two preparations. METHODS: A single-center, randomized, open, two-period, and self-crossover design was adopted to conduct a fasting and fed bioequivalence study of 23 healthy subjects each. The 0.4 g dose preparations were taken orally per cycle on fasting or fed administration. The plasma concentrations of moxifloxacin at different times after administration were determined by HPLC-MS/MS. The main pharmacokinetic parameters were calculated, and the bioavailability of the test preparation relative to the reference preparation was evaluated. RESULTS: After subjects in the fasting group took the test preparation T and the reference preparation R, the main pharmacokinetic parameters of moxifloxacin hydrochloride were: C
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Objective@#To explore the clinical effect of Kangfu Xiaoyan suppository combined with moxifloxacin in the treatment of chronic pelvic inflammatory disease.@*Methods@#From November 2016 to November 2018, a total of 216 patients with chronic pelvic inflammatory disease admitted to the Maternal and Child Health Care Hospital of Lishui were enrolled.The patients were divided into control group and observation group according to the digital table, with 108 cases in each group.The patients in the control group were treated with quinolone antibacterial agent moxifloxacin hydrochloride tablets.The patients in the observation group were treated with Kangfu Xiaoyan suppository and moxifloxacin hydrochloride tablets.The disappearance time of clinical signs, clinical treatment effects and adverse reactions in the two groups after treatment were observed and compared.@*Results@#The disappearance time of fever[(5.15±2.46)h], lower abdominal pain[(7.62±2.77)h], leucorrhea abnormality[(9.16±3.13)h], and pain[(6.38±2.03)h] in the observation group were significantly shorter than those in the control group[(8.09±2.28)h, (10.45±2.68)h, (12.20±2.96)h, (9.49±2.27)h](t=8.231, 7.631, 7.334, 10.613, all P=0.000). The total effective rate of the observation group (93.51%) was significantly higher than that of the control group (86.11%), the difference was statistically significant (χ2=6.983, P=0.008). The overall incidence of adverse reactions of the observation group (3.70%) was significantly lower than that of the control group (11.11%), and the difference was statistically significant (χ2=4.32, P=0.038).@*Conclusion@#Compared with the simple use of moxifloxacin, Kangfu Xiaoyan suppository combined with moxifloxacin in the treatment of gynecological chronic pelvic inflammatory disease has a better clinical treatment effect and a lower incidence of adverse reactions.It is recommended to apply in clinical treatment in the future.
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Objective To compare the pharmacokinetics of moxifloxacin (MXF) administered orally in the plasma and lung tissues of rats with pneumonia infected by Streptococcus pneumoniae (S.p) and normal rats. Methods To establish a model of Streptococcus pneumoniae pneumonia rats and normal rats. Moxifloxacin was administered by intragastric administration at 42 mg/kg. Microdialysis technique was used to sample the blood and lung tissues of pneumonia rats and normal rats to determine the free drug concentration of moxifloxacin in each sample, calculate the pharmacokinetic parameters, and compare the pharmacokinetics of oral moxifloxacin in pneumonia rats and normal rats. Results The t1/2 of moxifloxacin in the blood of normal rats and pneumonia rats were (5.27±4.38) h, (2.15±0.07) h (P>0.05), and Cmax were (4.94±0.98) μg/ml, respectively, (4.83±0.05) μg/ml (P>0.05), Clast_obs/Cmax were 0.02±0.03, 0.27±0.04 (P<0.05), AUC0-t were (22.33±2.02)μg/ml·h, (12.88±1.19)μg /ml·h (P<0.05), CL/F are (1.79±0.11)(mg/kg)/(μg/ml)·h, (2.49±0.26)(mg/kg)/(μg/ml)·h (P<0.05); Cmax of lung tissue of normal rats and pneumonia rats were (1.42±0.05) μg/ml, (4.84±0.02) μg/ml (P<0.05), t1/2 are (1.9±0.63)h, (3.39±0.79)h (P>0.05), AUMC are (11.93±5.14)μg/ml·h2, (107.01±25.39)μg/ml·h2 (P<0.05), AUC0-t are (3.06±1.0) 7μg/ml·h, (13.16±0.53)μg/ml·h (P<0.01). Conclusions ① Under the 400 mg/d dose condition, after intragastric administration of moxifloxacin, the concentration of free drugs in the blood and lung tissues is higher, far exceeding the minimum inhibitory concentration (MIC) and anti-drug resistance concentration (MPC), can effectively remove Streptococcus pneumoniae. ②The free concentration of moxifloxacin in the lung tissue of rats infected with Streptococcus pneumoniae is always higher than that of normal rats, and the Cmax is about 3.4 times that of normal rats. The penetration rate of moxifloxacin in lung tissue of pneumonia rats is significantly higher than that of normal rats.
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Objective To explore theclinical effect of Kangfu Xiaoyansuppositorycombined with moxifloxacin in the treatment of chronic pelvic inflammatory disease.Methods From November 2016 to November 2018,a total of 216 patients with chronic pelvic inflammatory disease admitted to the Maternal and Child Health Care Hospital of Lishui were enrolled .The patients were divided into control group and observation group according to the digital table , with 108 cases in each group .The patients in the control group were treated with quinolone antibacterial agent moxifloxacin hydrochloride tablets .The patients in the observation group were treated with Kangfu Xiaoyan suppository and moxifloxacin hydrochloride tablets .The disappearance time of clinical signs ,clinical treatment effects and adverse reactions in the two groups after treatment were observed and compared .Results The disappearance time of fever [(5.15 ±2.46)h],lower abdominal pain[(7.62 ±2.77)h],leucorrhea abnormality[(9.16 ±3.13)h],and pain [(6.38 ±2.03) h] in the observation group were significantly shorter than those in the control group [(8.09 ± 2.28)h,(10.45 ±2.68)h,(12.20 ±2.96)h,(9.49 ±2.27)h](t=8.231,7.631,7.334,10.613,all P=0.000). The total effective rate of the observation group (93.51%) was significantly higher than that of the control group (86.11%),the difference was statistically significant (χ2 =6.983,P=0.008).The overall incidence of adverse reactions of the observation group (3.70%) was significantly lower than that of the control group (11.11%),and the difference was statistically significant (χ2 =4.32,P =0.038).Conclusion Compared with the simple use of moxifloxacin ,Kangfu Xiaoyan suppository combined with moxifloxacin in the treatment of gynecological chronic pelvic inflammatory disease has a better clinical treatment effect and a lower incidence of adverse reactions .It is recommended to apply in clinical treatment in the future .
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Objective@#Moxifloxacin (MFX) shows good activity against and can be a possible antibiotic therapy to treat infection; however, other studies have shown a lower or no activity. We aimed to evaluate MFX activity against using zebrafish (ZF) model .@*Methods@#A formulation of labeled with CM-Dil was micro-injected into ZF. Survival curves were determined by recording dead ZF every day. ZF were lysed, and colony-forming units (CFUs) were enumerated. Bacteria dissemination and fluorescence intensity in ZF were analyzed. Inhibition rates of MFX and azithromycin (AZM, positive control) were determined and compared.@*Results@#Significantly increased survival rate was observed with different AZM concentrations. However, increasing MFX concentration did not result in a significant decrease in ZF survival curve. No significant differences in bacterial burdens by CFU loads were observed between AZM and MFX groups at various concentrations. Bacterial fluorescence intensity in ZF was significantly correlated with AZM concentration. However, with increasing MFX concentration, fluorescence intensity decreased slightly when observed under fluorescence microscope. Transferring rates at various concentrations were comparable between the MFX and AZM groups, with no significant difference.@*Conclusion@#MFX showed limited efficacy against using ZF model. Its activity needs to be confirmed.
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Animales , Antibacterianos , Farmacología , Modelos Animales de Enfermedad , Moxifloxacino , Farmacología , Infecciones por Mycobacterium no Tuberculosas , Quimioterapia , Mycobacterium abscessus , Pez CebraRESUMEN
We prepared moxifloxacin (MXF) loaded nanoparticles by nano-precipitation/self-assembly method, then compared the antibacterial activity of MXF and MXF loaded nanoparticles, and investigated the antibacterial mechanism of MXF loaded nanoparticles against Pseudomonas aeruginosa in vitro. The physicochemical properties such as particle size and zeta potential were investigated by laser particle size analyzer. The in vitro release characteristics were investigated by high performance liquid chromatography (HPLC). The effect of nanoparticles on HBE cells viability was investigated by CCK-8 assay. In addition, the in vitro antibacterial activity was investigated by minimum inhibitory concentration (MIC) assay, biofilm formation assays and transmission electron microscope (TEM) observation, then the antibacterial mechanism was initially explored. The particle size measurement showed that the nanoparticles had a size of 332.5 ± 2.7 nm, a polymer dispersion index (PDI) of 0.125 ± 0.053, a zeta potential of -24.3 ± 1.7 mV, and a uniform particle size distribution, drug loading content was (6.02 ± 1.27) %, encapsulation efficiency was (16.69 ± 1.17) %. The TEM results show that the nanoparticles have a spheroidal structure, and the particle size and distribution are consistent with the particle size measurement results. The nanoparticles can be effectively and rapidly released in phosphate buffer saline (PBS), releasing about 70% in 24 h, and releasing 87% in 72 h, and almost completely releasing the MXF at 120 h. At the same time, compared with moxifloxacin free drug, its MIC value is 8 μg·mL-1, which is 1/2 of MXF solution, and can significantly inhibit the formation of bacterial biofilms. It has well antibacterial activity in vitro and can be targeted to the surface of bacteria to exert its efficacy and improve the antibacterial effect. The moxifloxacin nanoparticles prepared in this study has a uniform particle size distribution, well drug release performance and antibacterial effect, and provides new ideas and strategies for the treatment of bacterial lung infection and the development of new antibacterial nanoformulations.