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Tianeptine sodium tablet is an oral medication containing the active ingredient tianeptine sodium (stablon). It belongs to the category of antidepressants and is mainly used to treat depression and related mood disorders. Sodium tianeptin improves mood and alleviates depressive symptoms by enhancing the reuptake of serotonin in the brain, while slightly affecting the dopamine and noradrenaline systems. Most antidepressants, such as SSRIs, increase their concentration by inhibiting neurotransmitter reuptake, while the mechanism of action of tianeptin sodium is opposite but equally effective. It can have auxiliary effects on chronic pain, fibromyalgia, or stress-related disorders, strictly follow medical advice. It can cause adverse reactions such as dry mouth, constipation, dizziness, drowsiness, insomnia, nausea, or indigestion.
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.
Additional information of chemical compound:
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Tianeptine Sodium COA
Tianeptine sodium tablet is an antidepressant drug used to treat depression and related mood disorders, with its core active ingredient being stablon. The following is a detailed explanation of its manufacturing information:
Preparation of raw materials and auxiliary materials
Preparation of Active Ingredients (API)
The synthesis of tianeptin sodium requires multiple organic reactions, and the main raw materials include:
Starting materials: such as o-chloroaniline, cyclohexanone, etc., must meet pharmaceutical grade standards (purity ≥ 99%).
Intermediate: Prepared through condensation, cyclization, chlorination and other reactions, with strict control of impurity content (such as unreacted raw materials and by-products).
Salt formation reaction: The free acid of thiamethoxam is reacted with sodium hydroxide to form a sodium salt, and the pH (7.0-8.0) needs to be controlled to avoid excessive salt formation or decomposition.
Key control points: The reaction conditions (temperature, pressure, catalyst dosage) need to be precisely controlled to avoid side reactions. Purification processes (such as recrystallization and chromatographic separation) require the removal of genotoxic impurities (such as nitrosamines). The drying process should avoid API degradation caused by high temperature.
Selection and preparation of auxiliary materials
The excipients must comply with the Chinese Pharmacopoeia or USP/EP standards, and commonly used excipients include:
Fillers: lactose, microcrystalline cellulose (to increase tablet volume).
Adhesive: polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC) (promotes particle formation).
Disinfectant: Crosslinked carboxymethyl cellulose sodium (CCNa), carboxymethyl starch sodium (CMS Na) (accelerates tablet disintegration).
Lubricants: Magnesium stearate, talc powder (to reduce friction during compression).
Coating materials: Hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG) (to improve appearance and mask odors).
Screening principle: There is no interaction between excipients and APIs (such as avoiding the use of sulfite containing excipients to prevent oxidative degradation). Consider patient specificity (such as lactose intolerance requiring replacement with other fillers).
Synthesis process and formulation preparation
The synthetic route of tianeptin sodium
The typical synthesis route is divided into the following steps:
Cyclization reaction: The condensation of o-chloroaniline with cyclohexanone produces the intermediate dihydrodibenzothiazine.
Chlorination reaction: Introducing chlorine atoms under the action of a catalyst (such as FeCl ∝) to form 3-chloro compounds.
Methylation reaction: Introducing a methyl group at position 6 through a methylation reagent such as iodomethane.
Amino side chain introduction: reacts with 7-aminoheptanoic acid to form the target molecule.
Salt formation and purification: Reacts with sodium hydroxide to produce sodium salt, which is then purified by recrystallization or chromatography to obtain high-purity API.
Process optimization direction:
Adopting continuous flow reaction technology to improve yield (currently the laboratory stage yield is about 65-70%).
Develop green catalysts (such as biocatalysis) to reduce waste.
Tablet preparation process
Wet granulation and compression method (mainstream process)
1
Pre mixing
Pre mix API with some fillers (such as microcrystalline cellulose) to ensure uniformity.
2
Wet granulation
Add adhesive solution (such as 5% PVP ethanol solution) and form wet particles through high-speed stirring granulator.
3
Drying and granulation
Fluidized bed drying (inlet temperature 50-60 ℃), sieving (20-60 mesh) to obtain uniform particles.
4
Total mixing
Add disintegrant and lubricant, mix for 10-15 minutes.
5
Tablet pressing
Control the difference in tablet weight (± 5%), hardness (50-100 N), and brittleness (≤ 1%).
6
Direct compression method (applicable to API sensitive to moisture and heat)
The auxiliary materials with good compressibility (such as spray dried lactose and pregelatinized starch) need to be screened.
It is necessary to control the environmental humidity (RH ≤ 40%) to prevent particles from absorbing moisture and clumping.
7
Coating process
Purpose: To mask unpleasant odors, prevent moisture, and control drug release.
Composition of coating solution: HPMC (3-5%), PEG 400 (1-2%), titanium dioxide (1-2%), talc powder (0.5-1%).
Process parameters: Inlet air temperature of 60-70 ℃, coating weight gain of 3-5%.
Quality Control and Testing Methods
API Quality Control
| Testing items | Method | Standard |
| HPLC | HPLC (C18 column, acetonitrile phosphate buffer mobile phase) | 98.0%-102.0% |
| Regarding substances | HPLC (gradient elution) | Single impurity ≤ 0.5%, total impurity ≤ 1.5% |
| Residual solvent | GC (headspace injection) | Ethanol ≤ 0.5%, methanol ≤ 0.3% |
| Moisture content | Karl Fischer method | ≤3.0% |
| Heavy metal | Atomic absorption spectroscopy | ≤20 ppm |
Tablet quality control
| Testing items | Method | Standard |
| Content uniformity | UV-Vis spectrophotometry | A+1.8S≤15(n=10) |
| dissolution rate | Paddle method (50 rpm, 0.1N HCl 900 mL) | 30 minutes ≥ 80% |
| Microbial limit | General Rule 1105 of the Chinese Pharmacopoeia | Total aerobic bacteria ≤ 1000 CFU/g, total mold and yeast ≤ 100 CFU/g |
| Weight difference | Weighing method | ± 5% (average tablet weight below 0.3 g) or ± 7.5% (0.3 g and above) |
Research progress on Tianeptine Sodium as a key executor and intervention target in tumor invasion behavior
Tumor invasion and metastasis are the core markers of malignant progression in cancer, involving multiple processes such as extracellular matrix (ECM) degradation, cell migration, and angiogenesis. Among them, the matrix metalloproteinases (MMPs) family provides key conditions for tumor cells to break through the basement membrane and invade surrounding tissues by degrading ECM components such as collagen, gelatin, and laminin. MMP-9 (gelatinase B), as an important member of the MMPs family, is recognized as a "key executor" of tumor invasion due to its efficient hydrolytic activity on type IV collagen (the main component of the basement membrane).
Traditional broad-spectrum MMP inhibitors are limited in clinical application due to their lack of selectivity, leading to serious side effects such as musculoskeletal pain. In recent years, specific intervention strategies targeting MMP-9 have become a research hotspot. Tianeptine Sodium Tablet, as a novel antidepressant, provides a new approach for tumor treatment by inhibiting MMP-9 expression and exerting anti-tumor invasion effects.
The core mechanism of MMP-9 in tumor invasion
ECM degradation and structural damage
The degradation of type IV collagen by MMP-9 is the initial step in tumor invasion.
In breast cancer, colorectal cancer, non-small cell lung cancer and other malignant tumors, the expression level of MMP-9 is significantly related to tumor stage, metastasis potential and patient prognosis. For example, in invasive pituitary adenomas (IPA), MMP-9 leads to plaque instability by degrading fibrous cap ECM, promoting tumor cell infiltration into surrounding tissues.
Inflammation and immune microenvironment regulation
MMP-9 regulates inflammatory cytokine activity through protein hydrolysis:
Chemokine splicing: MMP-9 splicing of IL-8 (CXCL8) enhances its chemotactic activity by 10 times, promoting neutrophil infiltration and inflammatory response.Cytokine activation: Enzymatic cleavage of TGF - β precursor releases active TGF - β, inducing epithelial mesenchymal transition (EMT) and immune suppression.
Adhesion molecule regulation: Cutting ICAM-1 affects leukocyte adhesion and extravasation, promoting tumor immune escape.
Angiogenesis promotion
MMP-9 activates tumor angiogenesis by degrading ECM and releasing stored VEGF. In ovarian cancer, the co expression levels of MMP-9 and VEGF are negatively correlated with microvascular density and patient survival rate.
Regulation of cellular mechanical properties
The latest research reveals that the expression level of MMP-9 is closely related to the biophysical properties (size, stiffness) of tumor cells.
In MDA-MB-231 breast cancer cells, MMP-9 overexpression cells showed stronger spreading ability and aggressiveness, while knockdown of MMP-9 led to cell rounding and cortical softening. This mechanical heterogeneity significantly enhances collective invasion ability by promoting the enrichment of high MMP-9 cells at the invasion front and the squeezing effect of low MMP-9 cells.
Molecular mechanism of Tianeptine Sodium inhibiting MMP-9
Inhibit the PI3K/Akt/NF - κ B signaling pathway
Tianeptine sodium tablet inhibits MMP-9 expression through the following mechanisms:
Inhibition of PI3K/Akt phosphorylation: Blocking Akt kinase activity reduces I κ B degradation, thereby inhibiting NF - κ B nuclear translocation.
Downregulation of MMP-9 promoter activity: By inhibiting the binding of NF - κ B to MMP-9 promoter, transcriptional activation is reduced.
Dose dependent inhibition: Stablon significantly reduced TNF - α - induced MMP-9 activity and expression in LNCaP prostate cancer cells at a concentration gradient (10-50 μ M).
Block the invasion induced by inflammatory factors
TNF - α is an important pro-inflammatory factor in the tumor microenvironment, which upregulates MMP-9 expression by activating the NF - κ B signaling pathway. Stablon significantly reduces the invasive ability of tumor cells under TNF - α stimulation by inhibiting this pathway. For example, in Matrigel invasion experiments, stablon treatment reduced the invasion rate of LNCaP cells by over 60%.
Regulating cellular mechanical properties
The latest research suggests that stablon may indirectly regulate the mechanical properties of tumor cells by affecting MMP-9 expression. In MDA-MB-231 cells, knocking down MMP-9 leads to a decrease in cell stiffness, while stablon treatment may inhibit the mechanical force required for cell invasion through a similar mechanism.
Pharmacological Mechanism
Tianeptine sodium tablet is an atypical tricyclic antidepressant whose pharmacological mechanism is completely opposite to mainstream SSRI antidepressants, challenging the established monoamine neurotransmitter hypothesis of depression. Its therapeutic effects are mediated through three core signaling pathways.
First, modulation of the serotonin (5-HT) system. Conventional antidepressants inhibit 5-HT reuptake to raise neurotransmitter concentrations within the synaptic cleft. In contrast, this agent selectively facilitates 5-HT reuptake in the cerebral cortex and hippocampus, lowering synaptic 5-HT levels to normalize dysregulated serotonergic neural circuits.
It barely interferes with basal norepinephrine and dopamine transport and exerts no antagonistic activity against muscarinic cholinergic or histaminic receptors. Accordingly, it produces far fewer sedative, xerostomic, and cardiovascular adverse reactions than classic tricyclic antidepressants.Second, modulation of glutamatergic neuroplasticity, the primary driver of its antidepressant and anti-stress effects. Chronic stress induces hippocampal neuronal atrophy and excessive glutamate release, triggering excitotoxic neuronal damage.Stablon suppresses stress-evoked glutamate overrelease, modulates the function of NMDA and AMPA receptors, repairs injured hippocampal neurons, and reverses structural brain lesions caused by persistent stress.
This alleviates somatic pain, anxiety, and cognitive impairment comorbid with depressive disorders.Furthermore, contemporary research confirms that this drug activates μ-opioid and δ-opioid receptors, which accounts for its rapid mood-relieving efficacy as well as its risk of abuse and dependence. Unlike agents that rely solely on monoamine modulation, stablon exerts therapeutic effects via a multi-target network encompassing neurotransmitter homeostasis, neural repair, and opioid receptor agonism. It avoids SSRI-characteristic side effects such as sexual dysfunction and weight gain, rendering it more suitable for patients with depression accompanied by somatization symptoms. Long-term administration sustains stable function of cerebral mood-regulating circuits.
Research and development of stablon commenced in the 1960s through a collaborative synthetic program conducted by the French National Institute of Medical Research and Servier Laboratories. At that time, the medical community universally endorsed the monoamine depletion hypothesis of depression, and the research team aimed to develop a novel tricyclic antidepressant with reduced side effects.
The core chemical scaffold of the compound was synthesized in 1970, followed by the patent authorization of the full molecular synthetic route in 1971. Early animal studies serendipitously uncovered its unique property of inverse 5-HT transport modulation, overturning the prevailing paradigm for antidepressant drug development at the time.
Over a decade of clinical trials validated its efficacy and safety profile, leading to its official marketing approval in France in 1987 under the brand name Stablon, with subsequent rollout across numerous European and Asian countries. Upon initial launch, only its serotonergic regulatory activity was recognized by clinicians; the mechanisms of glutamatergic neural repair and opioid receptor agonism were progressively elucidated in the 21st century.
Due to dependence and abuse risks stemming from opioid receptor activation, the United States has never approved its indication for depression, and multiple countries have since tightened regulatory controls over its distribution. The drug entered the Chinese market after 2000 for clinical use as a prescription antidepressant, emerging as a niche yet distinct atypical antidepressant agent.
FAQ
How does the product differ from common SSRIs?
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Most SSRIs inhibit serotonin reuptake to raise serotonin levels in synaptic clefts. By contrast, tianeptine sodium accelerates serotonin reuptake to balance overactive serotonergic pathways. Besides, it regulates glutamatergic system and binds to opioid receptors, while SSRIs have no opioid affinity. It also causes fewer side effects like weight gain and sexual dysfunction compared with SSRIs.
What is the exact mechanism of action?
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It works through three core pathways: 1) Enhances serotonin reuptake to stabilize abnormal mood circuits; 2) Modulates glutamate receptors to repair hippocampal neuronal damage caused by chronic stress and relieve stress-induced cognitive decline; 3) Acts as a weak agonist for mu and delta opioid receptors, bringing rapid anxiolytic and mood-lifting effects, which also leads to its abuse potential.
What symptoms can the product treat clinically?
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It is mainly indicated for major depressive disorder, persistent low mood, generalized anxiety disorder, and depression accompanied by somatic symptoms such as chronic physical pain, gastrointestinal discomfort and palpitations. It performs better than SSRIs in improving stress-induced physical discomfort and emotional collapse.
What are the common side effects?
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Mild and transient side effects include dizziness, mild nausea, dry mouth and insomnia, which usually disappear within 1-2 weeks after medication. Rare adverse reactions contain slight liver function fluctuation and tachycardia. It has almost no anticholinergic side effects compared with traditional tricyclic antidepressants.
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