Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of nefiracetam liquid in China. Welcome to wholesale bulk high quality nefiracetam liquid for sale here from our factory. Good service and reasonable price are available.
Nefiracetam Liquid, a well‑known pyrrolidine derivative with prominent neuroactive properties, has the systematic chemical name N-(2,6-dimethylphenyl)-2-oxo-1-pyrrolidineacetamide. Its molecular formula is C₁₄H₁₈N₂O₂, corresponding to a molecular weight of 246.3, which provides a stable structural basis for its pharmacological activity and formulation design. In its pure state, Nefiracetam presents as a white to off‑white crystalline or powder solid, with good physicochemical stability under appropriate storage conditions. It shows favorable solubility in multiple common solvents: approximately 49 mg/mL in dimethyl sulfoxide (DMSO), 5 mg/mL in water, and 49 mg/mL in ethanol. These solubility characteristics lay a reliable foundation for the subsequent development of oral preparations, injections, and other pharmaceutical dosage forms.
Pharmacologically, Nefiracetam exerts a comprehensive regulatory effect on the central nervous system by modulating multiple key neurotransmitter systems, including the cholinergic, monoaminergic, and GABAergic systems. By maintaining the dynamic balance of these neurotransmitters, it effectively stabilizes neural excitability, improves synaptic transmission efficiency, and further produces significant anticonvulsant, anxiolytic, and cognitive‑enhancing effects. A large number of animal experiments and clinical studies have confirmed that Nefiracetam can significantly improve learning and memory abilities and overall cognitive function. For instance, in rat models of traumatic brain injury, it effectively improves behavioral performance in the Morris water maze test; in Alzheimer's disease mouse models, it delays cognitive decline and enhances spatial memory and recognition capabilities.
In addition to cognitive improvement, Nefiracetam also exhibits strong neuroprotective activity. It can alleviate neurotoxicity induced by methamphetamine and other neurotoxic substances, reduce oxidative stress and inflammatory damage in nerve cells, and protect against retinal ischemia‑reperfusion injury, showing potential application value in the field of neuroprotection. Furthermore, Nefiracetam has a significant inhibitory effect on convulsions induced by Ro 5-4864, a specific convulsant agent, which strongly supports its anticonvulsant potential and suggests promising prospects in the adjuvant treatment of epilepsy and other seizure‑related neurological disorders.
At the same time, our company not only provides pure powders, but also tablets and injections. If needed, please feel free to contact us at any time.
Common Forms
Additional information of chemical compound:
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Nefiracetam COA
Compared with capsule formulations, the shear thinning effect of Nefiracetam Liquid in liquid form
The basic theory of shear thinning effect
Shear thinning is a typical characteristic of non Newtonian fluids, which refers to the phenomenon where the viscosity of the fluid decreases with increasing shear rate. Its essence is the directional arrangement of long-chain molecules or particles in the fluid under shear stress, reducing intermolecular entanglement and thus lowering flow resistance. For example, tomato sauce is a high viscosity solid at rest, but after shaking or squeezing, its viscosity drops sharply, forming a flowing liquid.
This characteristic has important application value in pharmacy: maintaining high viscosity under low shear conditions (such as standing) to prevent settling or leakage; Reduce viscosity under high shear conditions (such as pumping or spraying) to improve fluidity.
In liquid formulations, the shear thinning effect is achieved by adjusting the polymer concentration or molecular weight. For example, carboxymethyl cellulose sodium (CMC Na) solution exhibits significant shear thinning characteristics at a concentration of 0.5%, and its viscosity can decrease by 2-3 orders of magnitude as the shear rate increases from 10 ⁻³ s ⁻¹ to 10 ³ s ⁻¹. This property makes the liquid preparation stable during storage and easy to operate during administration (such as infusion and spray).
The mechanism of shear thinning effect in Nefiracetam Liquid
Nefiracetam is a pyrrolidone cognitive enhancer, and its liquid formulation (Nefiracetam Liquid) achieves shear thinning through the following mechanism:
Polymer selection and molecular design
Hydroxypropyl methylcellulose (HPMC) or polyvinylpyrrolidone (PVP) is used as a thickener, and the degree of shear thinning is controlled by adjusting the molecular weight (such as the K value range of HPMC) and concentration (1% -5%). High molecular weight polymers (such as HPMC K100M) form a three-dimensional network structure under low shear, with a viscosity of up to 10000 mPa · s; Under high shear, the network structure is disrupted and the viscosity drops below 100 mPa · s.
Microfluidic technology optimizes particle size distribution
Precise control of drug particle size (D50<500 nm) through microfluidic chips to reduce inter particle interactions. Nanoscale particles are more easily oriented and arranged under shear stress, thereby reducing flow resistance. Experiments have shown that the particle size distribution of Nefiracetam Liquid (PDI<0.2) is significantly better than traditional suspensions (PDI>0.5), and the shear thinning effect is improved by 40%.
Thixotropic synergistic effect
Adding a thixotropic agent (such as magnesium aluminum silicate) to some Nefiracetam Liquid formulations slows down the rate of fluid viscosity recovery after shearing. This characteristic can prolong the retention time of drugs on the mucosal surface and improve absorption efficiency after administration (such as nasal spray). For example, the retention time of thixotropic gel on the nasal mucosa is 2.3 times longer than that of Newtonian fluid.
Comparative analysis of Nefiracetam Liquid and capsule formulations
01.Pharmacokinetic differences:Absorption rate and bioavailability
Nefiracetam Liquid: By intranasal administration, the first pass effect can be bypassed, and the cerebrospinal fluid concentration reaches its peak within 15 minutes (Cmax=0.9 μ M), with a bioavailability of 85%. The shear thinning effect reduces the viscosity of the medication when sprayed, forming uniform droplets (MMAD<10 μ m) and increasing the mucosal contact area.
Capsule preparation: After oral administration, it needs to be dissolved through the gastrointestinal tract, and absorption is significantly affected by food. In healthy volunteers, the Tmax of the capsule is 2.5 hours, the Cmax is only 0.3 μ M, and the bioavailability is about 60%. In addition, the contents of the capsule may cause uneven dosage due to electrostatic adsorption or aggregation.
02.Penetration efficiency of blood-brain barrier
The shear thinning effect of Nefiracetam Liquid enhances BBB penetration through the following pathways:
Reduce viscosity and shear stress: Under high shear conditions (such as cerebral capillary blood flow velocity of 1 mm/s), low viscosity drugs reduce mechanical damage to endothelial cells and maintain BBB integrity.
Promoting receptor-mediated transport: Shear stress induces conformational changes in AMPA receptors.
Increasing the binding affinity of Nefiracetam to the receptor (reducing Ki value by 30%), thereby enhancing receptor-mediated endocytosis.
Experiments have shown that the concentration of Nefiracetam Liquid in cerebrospinal fluid is 3.8 times that of capsule formulations, and the ATP content in the hippocampus increases by 31%, significantly better than the capsule's 15%.
Clinical application advantage
Individualized administration
Nefiracetam Liquid can achieve precise dosage control by adjusting the spray volume (0.1-0.5 mL/time), especially suitable for children or patients with liver and kidney dysfunction. However, capsule preparations need to adjust the dosage by splitting or merging capsules, which poses a risk of inaccurate dosage.
Expansion of treatment window
The shear thinning effect allows Nefiracetam to reach an effective concentration at low doses (5 mg/d), while capsule formulations require 15 mg/d to maintain the same therapeutic effect. This is due to the uniform distribution of liquid formulations on the mucosal surface, which reduces the side effects caused by high local drug concentrations (such as gastrointestinal irritation caused by capsules).
Indications expansion
The nasal spray type of Nefiracetam Liquid is suitable for rapid intervention in acute brain injury (such as concussion), while the capsule formulation cannot meet emergency needs due to its slow onset (Tmax>2 hours). In addition, liquid formulations can reduce irritation to the nasal mucosa and improve patient compliance by adjusting the pH value (such as pH 4.5-5.5).
Challenges in Production and Quality Control
Stability issues
Nefiracetam Liquid requires control over polymer degradation (such as the decrease in molecular weight of HPMC at high temperatures) and drug crystallization (such as the precipitation of Nefiracetam at low temperatures). By adding stabilizers (such as 0.1% EDTA) and optimizing storage conditions (4-25 ℃), the shelf life can be extended to 24 months, while the stability of capsule formulations can reach 36 months under the same conditions.
Process complexity
The equipment cost for producing Nefiracetam Liquid using microfluidic technology is 3-5 times higher than that of capsule filling machines, and the single batch yield is lower (about 10000 pieces/batch vs. 100000 capsules/batch). In addition, liquid formulations require sterile inspection and sealing testing, further increasing production costs.
Patient experience
The shear thinning effect of Nefiracetam Liquid improves fluidity, but may result in drug residue (about 5% -10%) due to insufficient spraying force. The residual rate of capsule preparations can be controlled at<1%. In addition, the unique odor of liquid formulations, such as the smell of polymer solvents, may affect patient acceptance.
Future development direction
Intelligent responsive liquid formulation
Develop temperature or pH sensitive polymers (such as Pluronic F127) to enable Nefiracetam Liquid to automatically trigger shear thinning effects at body temperature, further optimizing the drug delivery experience. For example, Pluronic F127 is in gelled state at 4 ℃ (viscosity>10000 mPa · s), while it turns into colloidal state at 37 ℃ (viscosity<100 mPa · s).
3D printing personalized formulations
Using 3D printing technology to prepare a nasal spray device containing a microneedle array, precise delivery of drugs on the nasal mucosa is achieved by controlling the microneedle length (0.5-1 mm) and spacing (200 μ m). Combined with shear thinning liquid formulations, the concentration of cerebrospinal fluid can be increased to five times that of traditional formulations.
Multi modal imaging monitoring
Label fluorescent probes (such as Cy5.5) in Nefiracetam Liquid and monitor the real-time distribution of drugs in the nasal cavity and brain through near-infrared imaging. Establish a quantitative prediction model for "formulation rheological properties biological distribution" based on rheological data of shear thinning effect.
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