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|2.Nifuratel Reviews–Technological Informations|
| 3. Nifuratel Dosage
| 4.Nifuratel Application
| 5. Nifuratel Effects–How Does It Work？
|6.Nifuratel Side Effects|
| 7. Buy Nifuratel Powder Online
Nifuratel powder video
I.Raw Nifuratel powder basic Characters:
|Storage Temp:||-20°C Freezer|
|Color:||White to off white Crystalline powder|
Nifuratel(CAS: 4936-47-4) is an antibacterial, antifungal, and antiprotozoal compound with activity against Trichomonas. It is a local antiprotozoal and antifungal agent that may also be given orally. Nifuratel is not approved for use in the United States.
Nifuratel appears to have a broad antibacterial spectrum of action and is effective against Chlamydia trachomatis and Mycoplasma spp. as well as fungal infections from Candida spp.
Taken orally, or as a vaginal pessary, it is used in the treatment of a wide range of infections of the genito-urinary tract, especially if there is no accurate diagnosis available. For example, it may be used in the treatment of women exhibiting vaginal discharge where there is uncertainty as to whether the cause is Trichomonas vaginalis or Candida strains such as Candida albicans.Side effects appear to be minimal or non-existent and it has a safe toxicological profile.
|Chemical properties||Nifuratel – the anti-inflammatory, antibacterial agent derivative of nitrofuran. The molecular mass of a chemical compound = 285,3 grams on mol. Substance is let out in the form of tablets for intake, Nifuratel is a part of candles and ointments for local use.|
|Pharmacodynamics and pharmacokinetics||Nifuratel – antibacterial agent of a broad spectrum of activity. Drug is active concerning gram-positive and gram-negative microorganisms: stafilokokk, Citrobacter spp., Enterococcus faecium, salmonellas, Escherichia coli, klebsiyella, Enterococcus faecalis, Bacillus subtilis, Shigella flexneri, Enterobacter spp., Shigella sonnei, Serratia spp., Morganella spp., Pragia fontium, Rachnella aquatilis; lyambliya and protozoa; Rettgerella spp., Budvicia aquatica, Acinetobacter spp.; sort mushrooms Candida and Trichomonas vaginalis.
Medicine is less active in relation to Pseudomonas aeruginos, Proteus mirabilis and Proteus vulgaris.
|Nifuratel Application||Nifuratel is a drug used as an antibacterial, antifungal, antiprotozoal (Trichomonas). Nifuratel appears to have a broad antibacterial spectrum of action and is effective against Chlamydia trachomatis and Mycoplasma spp. as well as fungal infections from Candida spp.|
Drug is appointed inside. Depending on a disease a dosage and the scheme of treatment various.
Standard daily dosage for the adult – from 600 mg to 1,2 g. The quantity of medicine which the child needs to accept within a day is calculated by the principle of 10-30 mg on weight kg.Duration of treatment and frequency of reception depends on indications and is defined by the attending physician.Other dosage forms (candles and ointment) use according to recommendations of the producer.
Nifuratel (brand name Macmiror, or — in combination with nystatin, — Macmiror Complex) is a drug used in gynecology.
|Combined product for local use in gynecology, consisting of the derived nitrofuran (nifuratel) and antibiotic group of polyanov (nystatin).|
|2.Description pharmacological action:|
|Active against Trichomonas vaginalis and Candida fungi, protozoa, gram-positive and gram-negative microorganisms.|
|3.Method of application and dose:|
|Any contraindications to the use of the drug during pregnancy and lactation (breastfeeding) no.
Method of application and dose:
Vaginally, before bed — within 8 days 1 supp. or 2.5 g of cream 1-2 times a day (using the applicator). If necessary, repeat the treatment after menstruation.
To achieve maximum therapeutic effect you should insert the suppository into the upper part of the vagina.
Suppositories is used to treat in children, it is recommended to apply vaginal cream complete with applicator (graduated syringe).
|A simultaneous treatment of sexual partner because of the risk of re-infection. During the period of treatment should avoid sexual contacts.
The method of using the graduated applicator: screw the graduated applicator to the tube of cream. To gain the necessary amount of cream (in accordance with scale lines indicating the number of grams), pushing the tube. Disconnect from the tube, introduced into the vagina, squeeze out the contents, pressing down on the rod.
A special nozzle allows you to enter the cream without damaging the hymen. It is necessary to remove the cannula from the upper part of the rod and screwed onto the head of the syringe from the opposite side before you enter the cream in the vagina.
Nifuratel can effectively kill those bacteria, protozoa and molds that lead to vaginal infections without any acute or chronic side effects. Due to its pleiotropic effects, nifuratel can be used for all kinds of vaginitis caused by bacteria, trichomonas and molds infection. Nifuratel, a variety of broad- spectrum antimicrobial agents with two methods of application: oral and external application, was developed by Doppel Farmaceutici. S. r. l. with the trade name of Macmiror/ Macmiror. In 2001, SFDA approved nifuratel made by Doppel Farmaceutici. S. r. l. to be sold in China with such main species as sugarcoated tablets, vaginal tablets and vaginal suppositories under the trade names of Macmiror and Macmiror Complex. Nifuratel effects develops fast after entering China with annual sales rising from CNY 53.2 thousand in 2005 to CNY 38.03 million in 2014 and CAGR reaching 24.43% and some Chinese enterprises have also started to make generic drugs.
With the fast development of Chinese economy and the improvement of national health insurance system, many kinds of gynecological inflammation drugs, driven by new concepts of treatment, have become affordable to civilians. In general, the gynecological anti- infective market in sample hospitals is dominated by pharmaceutical preparations which operate quickly. On the other hand, Chinese patent medicine made by local enterprises fail to enter the market, instead, they are widely used in mother and child healthcare hospitals, medical institutions based in communities as well as the rural market.
（1）The effect of nifuratel on gastric cancer cell proliferation by the MTT and colony formation assays
To investigate the effect of nifuratel on human gastric cancer cell lines, cell viability was evaluated by the MTT assay. The SGC-7901 and BGC-823 cell lines were treated with increasing doses of nifuratel for 48 hours, and the cell viability was evaluated by the MTT assay. The results in Figure 1B show that cell viability was suppressed in a dose-dependent manner in the SGC-7901 and BGC-823 cell lines, with IC50 values of 169.7±2.2 μM in SGC-7901 cells and 133.7±0.85 μM in BGC-823cells.
Also, as shown in Figure 1C, compared with control cells, a dose-dependent decrease in colony formations by SGC-7091 and BGC-823 cells was detected using a colony formation assay. These results suggest that nifuratel significantly inhibited the growth and the proliferation of human gastric cancer cells, inducing cell death in a dose-dependent manner.
（2）Nifuratel induces G2/M cell cycle arrest in human gastric cancer cells
The cell cycle is a process involving a series of cellular events that lead to cell division and ultimately to proliferation. The entire cell cycle can be divided into four stages including the G1 phase, S phase, G2 phase, and M phase (the division stage).20 To evaluate the cell cycle arrest associated with nifuratel, SGC-7901 and BGC-823 cell lines were treated with nifuratel for 24 hours. The percentage of nifuratel-treated and untreated gastric cancer cells in the G2/M phase was measured by flow cytometry analysis. As show in Figure 2A and B, nifuratel significantly induced the arrest of gastric cancer cells in the G2/M phase of the cell cycle compared with the untreated control group.
Notes: (A) Induction of cell cycle arrest in human gastric cancer cells analyzed by ﬂow cytometry after treatment with a concentration gradient of nifuratel for 24 hours; DMSO is used as a loading control. (B) Representative histograms from flow cytometry analysis in the two human gastric cancer cells treated with various concentrations of nifuratel. Assays were performed in triplicate.
（3）Nifuratel induces apoptosis in human gastric cancer cells
To evaluate the apoptosis-inducing effect of nifuratel in human gastric cancer cell lines, the cancer cells were treated with nifuratel for 24 hours, stained with Annexin V-FITC and PI, and apoptotic cells were evaluated by flow cytometry analysis. The data showed that nifuratel dose-dependently induced cell apoptosis (Figure 3A). In addition, Western blot analysis data further revealed that nifuratel increased the expression of the proapoptotic protein Bax and decreased the level of the antiapoptotic protein Bcl-2 in human gastric cancer cells in a dose-dependent manner (Figure 3B). Our results also revealed that nifuratel could regulate the expression of cell death-related proteins, which blocks the process of human gastric cancer cell proliferation.
Notes: (A) SGC-7901 and BGC-823 cell lines were treated with a concentration gradient of nifuratel for 24 hours and stained with Annexin V and propidium iodide. The results were assessed by flow cytometry analysis. (B) Western blot analysis of apoptosis-related proteins. The expression of Bcl-2 and Baxin in SGC-7901 and BGC-823 cells were measured by Western blotting after incubation with nifuratel for 24 hours.
（4）Nifuratel inhibits the STAT3 signaling pathway
A number of studies have shown that overexpression of the STAT3 protein may be associated with the progression of gastric cancer.21 Our results indicated that treatment with 300 μM nifuratel markedly reduces the phosphorylated STAT3 (P-STAT3) protein level in SGC-7901 and BGC-823 cell lines. As show in Figure 4, nifuratel decreased P-STAT3 protein expression in SGC-7901 and BGC-823 cell lines in a concentration-dependent manner after 24-hour treatment. Notably, the 300 μM dose of nifuratel also markedly decreased P-STAT3 protein expression after 6 hours in the SGC-7901 cell lines and after 3 hours in the BGC-823 cell lines.
Notes: (A) SGC-7901 and BGC-823 cell lines were treated with a concentration gradient of nifuratel, the expression of P-STAT3 is shown by Western blot analysis. (B) The expression of P-STAT3 time dependently induced by nifuratel is shown by Western blot analysis in SGC-7901 and BGC-823 cell lines.
Abbreviations: DMSO, dimethyl sulfoxide; NIFU, nifuratel; STAT3, signal transducer and activator of transcription 3; P-STAT3, phosphorylated STAT3.
Importantly, the previous study found that the IL-6-induced phosphorylation of STAT3 in neoplastic gastric tissue positively correlated with tumor progression.22 It has been established that IL-6-mediated activation of STAT3 signaling pathway can promote the progression of other cancers.23,24 The STAT3 inhibitor inhibited the activation of STAT3, blocking the IL-6 signaling pathway which downregulated cancer cell proliferation, and downregulated the antiapoptotic protein Bcl-2.25 Thus, to further clarify whether nifuratel can block the IL-6-induced phosphorylation of STAT3, we combined the treatment with nifuratel and IL-6. In addition, napabucasin, an orally available STAT3 inhibitor, was used as a positive control group. The results indicated that nifuratel could block the IL-6-induced activation of the STAT3 signaling pathway, but had no effect on the activation of STAT1 mediated by interferon-γ (IFN-γ) (Figure 5). Our results also revealed that nifuratel regulated the expression of the cell death-related protein Bcl-2, induced cell cycle arrest, and inhibited the proliferation of human gastric cancer cells by blocking the IL-6-induced activation of the STAT3 signaling pathway.
Notes: (A) Gastric cancer cells were pretreated with the indicated concentrations of nifuratel and napabucasin for 24 hours and then stimulated with IL-6 (50 ng/μL) for 30 minutes. Whole-cell extracts were prepared and subjected to Western blot analysis using the indicated antibodies. (B) Gastric cancer cells were pretreated with the indicated concentrations of nifuratel for 24 hours and then stimulated with interferon-γ (IFN-γ) (50 ng/μL) for 30 minutes. Whole-cell extracts were prepared and subjected to Western blot analysis using the indicated antibodies.
Abbreviations: NIFU, nifuratel; Napa, napabucasin; P-STAT3, phosphorylated STAT3; STAT3, signal transducer and activator of transcription.
(5) Use Of nifuratel to treat infections caused by clostridium species
The present invention relates to the use of nifuratel, or a physiologically acceptable salt thereof, to treat infections caused by Clostridium species. The invention is further directed to the use of nifuratel to treat Clostridium difficile infection (CDI) and in particular Clostridium difficile associated diarrhoea (CDAD).
The object of the present invention is represented by nifuratel, or a physiologically acceptable salt thereof, for use in the treatment of any infection caused by Clostridium species, such as Clostridium difficile, Clostridium butyricum and Clostridium beijerinckii. More particularly, it is represented by the use of nifuratel, or a physiologically acceptable salt thereof, for treating Clostridium difficile infection (CDI) and, in particular, Clostridium difficile associated diarrhoea (CDAD).
Solid, semi-solid or liquid preparations of nifuratel or of a physiologically acceptable salt thereof, in the form of oral tablets, film-coated tablets, capsules, dragées or syrup, with a content in nifuratel from 10 to 1000 mg per single dose, more preferably from 50 to 800 mg per single dose, most preferably from 100 to 600 mg per single dose, are suitable to treat infections by Clostridium spp.; such preparations may be administered to infected patients according to conventional techniques; according to a preferred embodiment, they are administered on a regular basis, preferably three times daily. Pharmaceutical compositions may be prepared according to conventional techniques, may contain pharmaceutically acceptable excipients, adjuvants and/or carriers, and may also contain, in combination, one or more active principles with complementary or, in any case, useful activity.
The active agents which may be used in combination with nifuratel according to the present invention include, but are not limited to, antibiotics, antidiarrheal agents and probiotics; such active ingredients may be administered together with nifuratel (i.e. they may be for instance contained in the same composition as nifuratel) or they may be administered separately from or in temporal proximity with nifuratel.
Examples of antibiotics include metronidazole, vancomycin, bacitracine, rifaximine, aminoglycosides such as neomycin, gentamycin, amikacin, kanamycin and salts thereof.
Examples of the antidiarrheal agents include: bismuth subsalycilate, aluminium silicate, kaolin, activated charcoal, loperamide, attapulgite, zinc. Examples of probiotics include species of the genus Lactobacillus, Bacillus clausii and Saccharomyces bouillardii. Examples of the compositions prepared according to the present invention include: tablets, film-coated tablets, capsules, dragées or syrup suitable for oral administration.
The pharmaceutical compositions and the uses of the present invention will now be more fully described by the following examples. It should, however, be noted that such examples are given by way of illustration and not of limitation.
GI disturbances; peripheral neuropathy; thrombocytopenic purpura; haemolytic anaemia in patients with G6PD deficiency; hypersensitivity reactions; contact dermatitis; hepatotoxicity; blood dyscrasias; pulmonary reactions.
An indication is a term used for the list of condition or symptom or illness for which the medicine is prescribed or used by the patient. For example, acetaminophen or paracetamol is used for fever by the patient, or the doctor prescribes it for a headache or body pains. Now fever, headache and body pains are the indications of paracetamol. A patient should be aware of the indications of medications used for common conditions because they can be taken over the counter in the pharmacy meaning without prescription by the Physician.
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