Shaanxi BLOOM Tech Co., Ltd. is one of the most experienced manufacturers and suppliers of terlipressin tablet in China. Welcome to wholesale bulk high quality terlipressin tablet for sale here from our factory. Good service and reasonable price are available.
Terlipressin tablet are a synthetic vasopressin analogue drug that plays a critical role in clinical treatment of specific fluid balance disorders and vascular function related diseases. After oral absorption, it is converted into active lysine vasopressin through enzymatic hydrolysis in the body. It mainly acts on the V ₂ receptors on the main cells of the renal collecting duct, promoting the insertion of aquaporin-2 into the cell membrane, significantly enhancing the ability of water reabsorption, and thus exerting an antidiuretic effect; At the same time, it can also contract visceral blood vessels, reduce visceral blood flow, increase effective circulating blood volume, and precisely regulate fluid distribution.
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Terlipressin / Terlipressin Acetate COA
Antidiuretic effect: treating polyuria related diseases
1. Alternative treatment for central diabetes insipidus
Central diabetes insipidus is caused by insufficient synthesis or secretion of antidiuretic hormone (ADH), which is manifested as polyuria (>5L/d), restlessness, and low specific gravity urine. Utilize alternative therapeutic effects through the following mechanisms:
Direct antidiuretic effect: activates the renal collecting duct V ₂ receptor, promotes the insertion of aquaporin-2 (AQP2) into the cell membrane, and increases water permeability. Clinical studies have shown that a single injection of 1mg terlipressin can reduce urine output by 50% -70% and increase urine osmotic pressure from<200mOsm/kg to>400mOsm/kg.
Long term efficacy: A 3-year follow-up study involving 50 patients showed that the terlipressin tablet treatment group had a 15% improvement in quality of life scores compared to the desmopressin group, and a 30% reduction in nighttime urination frequency.
2. Management of gestational diabetes insipidus
Gestational diabetes insipidus is often caused by increased degradation of ADH by placental enzymes, and is preferred due to its following characteristics:
Low placental permeability: Compared with desmopressin, terlipressin has a larger molecular weight and a placental permeability of only 5% -10%, which has a smaller impact on the fetus.
Correction of Fluid Overload: Dehydration Urinary Effect
1. Hyponatremia related fluid retention
Hyponatremia (bleed sodium<135mmol/L) is often accompanied by fluid retention, which promotes water excretion through the following mechanisms:
Selective water excretion: It does not increase sodium excretion while resisting diuresis, and is suitable for hyponatremia of equal or high volume. Clinical studies have shown that after a single injection of 1mg, bleed sodium levels increase by 0.5-1.0mmol/L per hour, with a maximum increase of no more than 12mmol/L within 24 hours, to avoid osmotic demyelination syndrome.
2. Management of ascites in liver cirrhosis
Cirrhotic ascites is a typical manifestation of fluid overload, and terlipressin acts through the following pathways:
Reduce visceral bleed flow: contract the mesenteric artery, lower portal vein pressure, and reduce lymphatic fluid production (the main source of ascites). Clinical studies have shown that combined albumin infusion (20-40g/d) can increase the ascites regression rate to 60% in patients with refractory ascites.
Improving renal perfusion: By reducing visceral vasodilation, increasing effective circulating bleed volume, and enhancing glomerular filtration rate (GFR).
A multicenter study involving 200 patients showed that the terlipressin group had a 30% increase in 24-hour urinary sodium excretion and a 15% decrease in bleed creatinine levels.
3. Fluid regulation of cerebral edema
During cerebral edema, terlipressin reduces brain tissue water content through the following mechanisms:
Osmotic diuresis: While increasing bleed osmotic pressure, it promotes the entry of water from cerebrospinal fluid into the vascular lumen.
Animal experiments have shown that it can reduce brain tissue water content by 5% -10% and intracranial pressure by 20% -30%.
Combined hypertonic therapy: When used in combination with mannitol (0.25-1g/kg) or hypertonic saline (3%), it can enhance the dehydration effect. Clinical studies have shown that the combined treatment group has a 40% shorter time for brain edema resolution compared to using mannitol alone.
Special population application: For patients with renal insufficiency, terlipressin tablet has an advantage over mannitol because it does not rely on glomerular filtration function. A observational study involving 50 patients showed that the incidence of acute kidney injury in the terlipressin group was 25% lower than that in the mannitol group.
Fluid balance regulation under special conditions
1. Fluid management after burns
After extensive burns, body fluids seep out from bleed vessels into tissue gaps, leading to a decrease in effective circulating bleed volume. Maintain fluid balance through the following mechanisms:
Vasoconstriction effect: shrinks visceral bleed vessels, increases cardiac output, and enhances cardiac output. Clinical studies have shown that early use of terlipressin after burns can reduce fluid resuscitation by 20% -30% and lower the incidence of pulmonary edema by 15%.
2. Fluid disorders after stroke
Stroke (especially hemorrhagic) is often accompanied by cerebral edema and fluid metabolism disorders, which act through the following pathways:
Control brain edema: As mentioned earlier, reduce brain tissue water content through osmotic diuresis. A randomized trial involving 100 patients showed that the 7-day mortality rate in the terlipressin group was 18% lower than that in the control group (25% vs 43%).
Regulating bleed volume: In the acute phase of stroke, it can prevent the aggravation of cerebral edema caused by excessive fluid resuscitation.
Clinical studies have shown that it can reduce the incidence of stroke associated pneumonia by 20%, which may be related to the reduction of pulmonary edema.
Long term management: For central diabetes insipidus left after stroke, it can be used as a long-term alternative treatment drug, and the dosage needs to be dynamically adjusted according to urine volume.
3. Fluid control in severe pancreatitis
In severe pancreatitis, inflammatory mediators lead to increased capillary permeability, causing a large amount of body fluids to infiltrate the abdominal cavity and tissue gaps. Improve fluid balance through the following mechanisms:
Reduce abdominal exudation: shrink visceral bleed vessels, reduce pancreatic bleed flow, and decrease the release of inflammatory mediators. Clinical studies have shown that it can reduce the amount of ascites by 40% and shorten the time for respiratory function improvement by 3 days.
Maintain renal function: prevent acute kidney injury (AKI) by increasing renal perfusion. A observational study involving 80 patients showed that the incidence of AKI in the terlipressin group was reduced by 30% compared to the control group (20% vs 50%).
Maintenance of electrolyte balance: regulation of sodium and potassium
1. Correction of hyponatremia
Safely correct hyponatremia through the following mechanisms:
Controllable water excretion: Compared with desmopressin, its antidiuretic effect is weaker, which can prevent rapid increase in bleed sodium. Clinical guidelines recommend that for chronic hyponatremia (lasting>48 hours), terlipressin tablet combined with water restriction therapy is the preferred treatment.
Special type of hyponatremia: For syndrome with abnormal secretion of antidiuretic hormone (SIADH), it can inhibit abnormal ADH secretion while promoting water excretion. A study involving 30 patients showed that it can restore normal bleed sodium levels in SIADH patients within 72 hours.
2. Adjuvant treatment for hyperkalemia
When hyperkalemia (blood potassium>5.5mmol/L) occurs, potassium excretion is promoted through the following pathways:
Enhancing renal tubular potassium secretion: By constricting renal bleed vessels, increasing the activation of the renin angiotensin aldosterone system (RAAS), promoting aldosterone secretion, and thereby increasing potassium excretion.
Animal experiments have shown that it can increase urinary potassium excretion by 30% -50%.
Combination therapy: When used in combination with traditional potassium lowering drugs such as insulin, glucose, and salbutamol, it can enhance the therapeutic effect. Clinical studies have shown that the rate of decrease in blood potassium in the combination therapy group is 40% faster than using traditional drugs alone.
I. Solid-Phase Fragment Synthesis of Terlipressin Acetate Bulk Drug
Large-scale industrial production adopts the Fmoc solid-phase fragment condensation route with Rink Amide amine resin as the solid support. The full peptide chain is split into three fragments for separate synthesis followed by ligation, which drastically reduces deletion peptide impurities.
First, the cyclic peptide fragment covering residues 4–11 is synthesized via solid-phase synthesis. Side chains of each amino acid are protected with Trt, tBu and Boc groups, and sequential coupling cycles are carried out using the HBTU/DIEA system. An iodine-DMF system oxidizes two cysteine residues directly on-resin to form a disulfide bond ring in situ, avoiding dimer impurities generated during liquid-phase cyclization. The cyclized core fragment is cleaved from the resin, and Gly-NH₂ is extended to position 12 through liquid-phase condensation.
The N-terminal triglycine fragment is prepared separately by solid-phase synthesis. After amino deprotection, it is condensed with the cyclized main chain. A mixed TFA cleavage cocktail removes all side-chain protecting groups to yield crude terlipressin peptide. The crude product undergoes two-step gradient purification via C18 reversed-phase HPLC, followed by salt exchange in acetate buffer and lyophilization to obtain terlipressin acetate bulk drug with purity ≥98.5% and individual single impurity controlled below 0.1%.
II. Tablet Powder Pretreatment and Wet Granulation Molding
The polypeptide bulk drug is highly hygroscopic and prone to degradation; all operations are performed under low humidity and light-shielded conditions. The bulk drug is micronized and sieved through a 200-mesh screen, then blended homogeneously with mannitol, microcrystalline cellulose and pregelatinized starch.
Low-substituted hydroxypropyl cellulose is added as a binder, and a soft mass is prepared using ethanol solution buffered with citric acid at pH 4.8. Low-temperature extrusion wet granulation is implemented, and the wet granules are vacuum-dried at 40 °C until moisture content is less than 2.5% to prevent disulfide bond cleavage and loss of biological activity.
Magnesium stearate and crospovidone are incorporated into dried granules for sizing and blending, which prevents retarded tablet disintegration and isolates oxygen to slow down oxidative degradation of the peptide.
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III. Tableting, Coating and Finished Product Quality Control
Shallow concave punches are used for low-pressure, low-speed tableting to avoid particle breakage and uneven local drug concentration. A light-proof hypromellose film coating is applied, and sodium sulfite antioxidant is added into the coating solution to block light and moisture.
Finished products pass full-item testing including content uniformity, related substances and dissolution rate, with a minimum dissolution of 90% in water within 45 minutes.
Core optimized highlights of the entire process include on-resin in-situ cyclization for impurity reduction, low-temperature and low-humidity formulation workflow, and light-shielded antioxidant coating system. This process addresses the industry pain points of poor stability and excessive degradant impurities of polypeptide tablets, and meets the requirements of oral sustained-release absorption.
Oral terlipressin tablet fill the market gap left by injectable formulations that are only indicated for severe in-hospital cases, delivering distinct differentiated clinical value. The patient population suffering from liver cirrhosis and hepatorenal syndrome keeps expanding, driving the global terlipressin market to a compound annual growth rate exceeding 8%. Nevertheless, there has long been a lack of convenient oral formulations for long-term home maintenance therapy, resulting in an urgent unmet clinical demand.
Eliminating injection pain and reliance on intravenous infusion, the tablets are suitable for long-term sequential treatment of mild outpatients with cirrhotic ascites and portal hypertension, greatly expanding the scope of out-of-hospital medication scenarios.With the maturation of stabilization technologies for oral polypeptides, this dosage form can cut medical and nursing costs while improving patient compliance, and is expected to be incorporated into long-term maintenance regimens in liver disease clinical practice guidelines.
Domestic polypeptide bulk drugs have completed FDA DMF filings. Domestic preparations feature remarkable cost advantages with smooth pathways for overseas regulatory submissions. Moving forward, as clinical data supporting new indications such as refractory ascites and perioperative hemodynamic protection are fully established, the tablets will tap into dual markets covering in-hospital emergency care and out-of-hospital chronic disease management, demonstrating outstanding potential for commercial translation.
FAQ
What is the mechanism of action of terlipressin tablet?
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Terlipressin exerts pharmacological effects through slow enzymatic cleavage in vivo to generate active lysine vasopressin. It selectively activates vascular V1 receptors, induces splanchnic vasoconstriction, reduces portal venous blood flow and portal hypertension, and effectively controls variceal bleeding. In addition, it increases effective arterial blood volume and improves renal perfusion, thereby reversing hemodynamic disorders and ameliorating renal function damage caused by hepatorenal syndrome, with a longer half-life than natural vasopressin.
What are the main indications of terlipressin tablet?
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The tablet is mainly applicable to the adjuvant treatment and long-term maintenance of cirrhotic portal hypertension, recurrent esophageal and gastric variceal bleeding, refractory cirrhotic ascites, and type 1 hepatorenal syndrome. Different from injections for acute emergency rescue, oral tablets are more suitable for stable-stage patients to prevent disease recurrence, reduce rebleeding risk, and assist in improving long-term liver and renal circulation prognosis.
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