The molecular formula of nitazoxanide powder is C12H9N3O5S, CAS 55981-09-4, and the molecular weight is 307.28 g/mol. It is a white to off white crystalline powder with the chemical name 2- [(5-nitro-1,3-thiazol-2-yl) carbamoyl] phenol acetate, which belongs to the derivatives of nitrothiazide. Although its actual mechanism of action is not yet clear, it is believed to be related to the enzyme dependent electron transfer reaction that inhibits pyruvate and iron redox protein oxidoreductase, the latter of which is crucial for anaerobic energy metabolism.
This product is active not only against Cryptosporidium and Giardia, but also against many intestinal parasites such as Babesia and other sporozoites, amoebic protozoa, human roundworms, hookworms, flagellates, beef tapeworms, short membrane shell tapeworms, and liver flukes. It has anti parasitic, anti intestinal parasitic, antibacterial, antiviral and other pharmacological effects, and its anti parasitic spectrum and antibacterial spectrum are more extensive than that of albendazole, metronidazole and metronidazole, and its application fields are also more extensive than other drugs.
This product is also active against certain anaerobic and microaerophilic bacteria, such as Helicobacter pylori. According to an article published in the renowned British medical journal The Lancet on June 13, 2006, nitrozotocinide also has a good therapeutic effect on childhood diarrhea caused by rotavirus.
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Additional information of chemical compound:
| Product Name | Nitazoxanide Tablets | Nitazoxanide Powder |
| Product Type | Tablets | Powder |
| Product Purity | HPLC≥99.0% | ≥99% |
| Product Specifications | Customizable | Customizable |
| Product Package | Customizable | Customizable |
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Nitazoxanide+. COA
Nitazoxanide powder, as a broad-spectrum antibacterial, anti parasitic, and antiviral drug, plays an important role in clinical treatment. Its unique chemical structure and mechanism of action make it an effective choice to treat a variety of infectious diseases.
Antiparasitic use
1.Treatment of Cryptosporidiosis
Nizopanib is the first and only drug approved by the US Food and Drug Administration (FDA) for the treatment of cryptosporidiosis. Cryptosporidium is a common intestinal parasite, which can cause diarrhea and other symptoms. Especially in patients with weak immune system, such as AIDS patients, cryptosporidium infection may lead to severe chronic diarrhea. Nizonide achieves therapeutic goals by inhibiting the energy metabolism process of Cryptosporidium, interfering with its growth and reproduction. Research has shown that nitrozotocinide has significant therapeutic effects on diarrhea caused by cryptosporidium, effectively alleviating symptoms, reducing the frequency and duration of diarrhea.
2. Treating Giardia disease
Giardia is another common intestinal parasite that can cause Giardia disease, characterized by abdominal pain, diarrhea, nausea, vomiting, and other symptoms. Nizonide has a strong inhibitory effect on Giardia, and its mechanism of action is related to the inhibition of Giardia 'energy metabolism. In clinical trials, nitrozotocinide has shown significant efficacy in treating Giardia lamblia, effectively clearing the body of Giardia lamblia, relieving symptoms, and having good tolerability.
3. Treat other intestinal parasitic infections
Nizonide is active against various intestinal parasitic infections, including sporozoites such as Babesia, amoebas, roundworms, hookworms, whipworms, beef tapeworms, short membrane tapeworms, and liver flukes. For infections caused by Bacillus subtilis and other sporozoites, nitrozotocinide can inhibit their growth and reproduction, and alleviate symptoms of infection. For amoebic infection, nitrozotocinide can effectively inhibit the reproduction and spread of amoebic parasites, reduce inflammatory reactions, and alleviate related symptoms. When treating intestinal parasitic infections such as roundworms, hookworms, whipworms, beef tapeworms, short membrane tapeworms, and liver flukes, nitrozotinib also shows good efficacy in clearing parasites from the body and improving the health status of patients.
4. Treating parasitic infections in children
Nizopanib has significant value in the treatment of parasitic infections in children. For example, in the treatment of childhood roundworm disease and tapeworm disease, nitrozotocinide can have a similar effect to albendazole and praziquantel. Its dosage forms are diverse, including tablets and dry suspensions, making it convenient for children of different ages to take. For younger children, dry suspension can facilitate dosage adjustment and improve medication adherence. Clinical studies have shown that nitrozotocinide has good safety and fewer adverse reactions in treating parasitic infections in children. It can effectively eliminate parasites in children's bodies and promote their healthy growth.
Antibacterial use
1. Treating anaerobic bacterial infections
Nitrozotocin exhibits broad-spectrum antibacterial activity against various anaerobic bacteria, including Bacteroides fragilis, Clostridium difficile, Campylobacter jejuni, Clostridium difficile, and Clostridium perfringens. Anaerobic bacterial infection can cause infections in the abdominal cavity, pelvic cavity, oral cavity, and vagina, leading to symptoms such as abscess formation, tissue necrosis, and overall discomfort. Nitrozotocin achieves antibacterial effects by inhibiting the energy metabolism process of anaerobic bacteria, interfering with their growth and reproduction. Nizopanib can be used in combination with other antibiotics to improve treatment efficacy in the treatment of abdominal and pelvic infections. For oral infections, nitazonide can be made into oral lozenges or mouthwashes, which can be directly applied to the infected area to reduce inflammatory reactions. When treating vaginal infections, nitrozotocin can be made into vaginal suppositories or washes, effectively removing anaerobic bacteria from the vagina and relieving symptoms.
2. Treatment of Helicobacter pylori infection
Helicobacter pylori is a common pathogenic bacterium in the stomach that can cause diseases such as gastritis, gastric ulcers, and duodenal ulcers. Nitazoxanide powder has activity against Helicobacter pylori and can inhibit its growth and reproduction. When treating Helicobacter pylori infection, nitrozotocin is usually used in combination with other antibiotics such as clarithromycin, amoxicillin, etc., forming a triple or quadruple therapy. This combination therapy can improve the eradication rate of Helicobacter pylori and reduce the development of drug resistance. Clinical studies have shown that the combination of nitrozotocinide and other antibiotics has significant efficacy in treating Helicobacter pylori infection, effectively alleviating patients' symptoms and promoting the healing of gastric diseases.
3. Treat other bacterial infections
Nizopanib also has certain therapeutic effects on some other bacterial infections, such as pseudomembranous colitis caused by Clostridium difficile. Clostridium difficile is a common intestinal pathogen that can produce toxins, leading to intestinal mucosal damage and inflammatory reactions. Nizopanib alleviates symptoms of pseudomembranous colitis by inhibiting the growth and reproduction of Clostridium difficile, reducing toxin production. During the treatment process, nitrozotocinide can be used in combination with other drugs to improve treatment efficacy and shorten the course of the disease.
Antiviral use
1. Treatment of rotavirus gastroenteritis
Rotavirus is one of the main pathogens causing acute gastroenteritis in children, which can lead to severe symptoms such as diarrhea, vomiting, and dehydration. Nizopanib has a good therapeutic effect on rotavirus gastroenteritis. Research has shown that nitrozotocinide can inhibit the replication of rotavirus, alleviate intestinal inflammation caused by viral infection, and alleviate symptoms such as diarrhea and vomiting. In clinical trials, the use of nitrozotocinide to treat children with rotavirus gastroenteritis significantly shortened the time to symptom relief and the course of the disease, and the treatment effect was significant.
2. Treatment of chronic hepatitis C
Nixostat has also shown certain therapeutic effects on chronic hepatitis C. Its metabolite, Tenzomib, has a unique inhibitory effect on HCV replication. A multicenter double-blind randomized controlled trial investigated the efficacy of nitazonide in the treatment of chronic hepatitis C, with a treatment regimen of nitazonide 500mg po bid or placebo for 24 weeks. As a result, at the end of the treatment, the HCV RNA seroconversion rates in the nitrozotocinide group and placebo group were 30.4% (7/23) and 0% (0/24), respectively; After 24 weeks of follow-up after the course of treatment, the continuous negative conversion rate of HCV RNA in the nitrozotocinide group was 17.4% (4/23). This indicates that nitrendipine has certain potential in the treatment of chronic hepatitis C, as it can reduce viral load and improve the treatment response rate of patients.
3. Inhibition of other viruses
In recent years, studies have found that nitazone also has inhibitory effects on certain other viruses, such as influenza virus, coronavirus, etc. In animal models, nitrozotocinide showed activity against Japanese encephalitis virus, reducing the mortality rate of infected mice and protecting them from lethal doses of the virus challenge. Although there is currently relatively little clinical research on the effects of nitrozotocinide on these viruses, these findings provide new ideas and directions for the application of nitrozotocinide in antiviral therapy.
Other potential uses
1. Regulating autophagy and inhibiting mTORC1 signaling
Nizopanib can also regulate autophagy and inhibit mTORC1 signaling. Autophagy is an intracellular degradation process that plays an important role in maintaining the stability of the cellular environment and the survival of cells. The mTORC1 signaling pathway plays a crucial role in processes such as cell growth, proliferation, and metabolism. Nizopanib may have therapeutic effects on some diseases related to cell growth and metabolic abnormalities, such as tumors, by regulating autophagy and inhibiting mTORC1 signaling. However, current research on the role of nitrozotocinide in these areas is still in its early stages, and further studies are needed to reveal its specific mechanism of action and potential clinical application value.
2. Treatment of hepatitis B
Studies have shown that nitazone also exhibits effective inhibition of HBV replication. Nixostat induces a decrease in the production of several HBV proteins (HBsAg and HBeAg, core antigens) in 2.2.15 cells, but does not affect the transcription of HBV RNA. Some preliminary research results show that the negative conversion rate of HbeAg and HBsAg in the treatment of hepatitis B with Nizoxanide is significantly higher than that of any other approved treatment drugs for hepatitis B, including interferon. This suggests that Nitazoxanide powder may have potential application prospects in the treatment of hepatitis B, but more clinical trials are needed to verify its efficacy and safety.
Polycrystalline phenomenon
This substance exists in two crystal forms: crystal form I melts at 198 ° C, and crystal form II melts at 201 ° C. There is a displacement difference of 2 cm ⁻ ¹ in the ester carbonyl stretching vibration peak of the infrared spectra of the two crystal forms at 1720 cm ⁻ ¹. Research on crystal transformation has shown that pure crystal form I can be obtained by recrystallization in ethanol solution, while crystal form II tends to form in ethyl acetate. Strict monitoring of crystal form is required in formulation development, as the dissolution rate of crystal form II is 15-20% lower than that of crystal form I.
The ability of this substance to penetrate the crystal barrier of Natron salt (Na2CO3 · NaHCO3)
Trona (Na ₂ CO ∝ · NaHCO ∝) is a naturally occurring carbonate bicarbonate composite mineral, whose crystalline structure may form a physical barrier that affects the permeability of drug molecules. Nitazoxanide (NTZ) is a broad-spectrum antiparasitic and antiviral drug, and its powder form needs to penetrate such crystal barriers in specific application scenarios, such as local treatment of salt lake related infections or drug delivery system development.
Characteristics of Trona Crystal Barrier
Crystal Structure
The crystal structure of Trona belongs to the monoclinic system, with the space group C2/c. Its lattice is composed of Na ⁺, CO ∝ ² ⁻, and HCO ∝ ⁻ ions connected by ionic and hydrogen bonds to form a layered structure (Figure 1). Each layer is alternately arranged with Na ⁺ and CO ∝ ² ⁻/HCO ∝⁻, and stable physical barriers are formed between layers through hydrogen bonding and van der Waals forces interactions. This structure endows Natron salt with the following characteristics:
High mechanical strength: Interlayer forces make it difficult for crystals to be physically broken.
Low permeability: Molecules need to overcome interlayer energy barriers to penetrate the barrier.
Environmental responsiveness: Changes in humidity, temperature, or pH may alter crystal morphology and affect barrier performance.
Crystal morphology and barrier function
The crystalline morphology of Trona (such as particle size and morphology) directly affects the permeability of the barrier:
Microcrystalline (<10 μ m): with a large specific surface area, numerous interlayer gaps, and high permeability.
Large crystals (>100 μ m): have a dense structure and low permeability, but may provide permeation channels due to cracks or defects.
Porous structure: By synthesizing or naturally forming pores (such as mesopores and macropores), permeability can be significantly improved.
FAQ
1. Besides anti-parasitic treatment, what are some emerging research directions?
The research has found that it has in vitro inhibitory effects on various viruses (such as rotavirus, norovirus, and influenza virus). The core mechanism lies ininterfering with the host cell's enzyme system, thereby inhibiting virus replication. However, this application is still in the research stage and is not yet a routine clinical application.
2. Why not simply use the powder, but instead need to formulate it into a preparation?
This drug is extremely insoluble in water and has an extremely low oral bioavailability. It can only be effectively absorbed by the human body through specializeddrug formulation processes (such as being made into micronized particles or specific crystal forms) and by adding excipients. Taking the raw powder directly is ineffective and poses risks.
3. What is the biggest limitation of this application?
Its efficacy is highly dependent on the patient's immune function. As an antibacterial/viral inhibitor, it mainly works by weakening the pathogen, creating a window for the immune system to clear the infection. Therefore, it has limited effectiveness for patients with severely compromised immune function, and is not applicable to bacterial infections.
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