Somatostatin Acetate

Somatostatin Acetate
Details:
1.General Specification(in stock)
(1)API(Pure powder)
(2)Tablets
(3)Injection
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Internal Code: KP-3-48/004
Somatostatin CAS 51110-01-1
Molecular formula: C76H104N18O19S2
Molecular weight: 1637.88
Manufacturer: BLOOM TECH Wuxi Factory
Analysis: HPLC, LC-MS, HNMR
Main market: USA, Australia, Brazil, Japan, Germany, Indonesia, UK, New Zealand , Canada etc.
Technology support: R&D Dept.-4
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Description
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Somatostatin Acetate is the acetate salt form of endogenous somatostatin. Its key feature is that the introduction of the acetate moiety optimizes its physicochemical properties and pharmaceutical value. Compared with conventional somatostatin, it exhibits higher water solubility, stability, and bioavailability. It appears as a white powder. The acetate content is controlled within a reasonable range by HPLC, ensuring product purity and stability, with purity above 98.0% and single impurity ≤ 1.0%. 

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Method of Analysis

Somatostatin Acetate COA

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Applications-

Application in the Treatment of Dumping Syndrome

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Mechanism of Action

 

Dumping syndrome occurs mostly after subtotal gastrectomy. Its core pathophysiology is rapid gastric emptying, in which hypertonic food quickly enters the small intestine, triggering massive release of gastrointestinal hormones, vasodilation, and severe blood glucose fluctuations, leading to abdominal distension, diarrhea, palpitations, dizziness, and other symptoms.

Somatostatin Acetate acts precisely through a dual mechanism:First, it directly inhibits gastric smooth muscle contraction and delays gastric emptying, preventing rapid influx of hypertonic contents into the intestine.Second, it broadly suppresses the release of gastrointestinal hormones, including gastrin, vasoactive intestinal peptide (VIP), glucagon, insulin, etc., blocking hormone‑mediated intestinal hypersecretion and vasodilation. It also prolongs small intestinal transit time and reduces intestinal irritation.In addition, it inhibits excessive insulin secretion and prevents hypoglycemia characteristic of late dumping syndrome.

Clinical Application and Evidence of Efficacy

 

Somatostatin Acetate is the first‑line drug for dumping syndrome when dietary modification and acarbose fail, and it significantly improves both early and late symptoms.

Multiple authoritative clinical studies confirm its efficacy:A double‑blind prospective study including patients with severe post‑gastrectomy dumping syndrome showed that octreotide acetate (a long‑acting analog of somatostatin acetate) completely eliminated postprandial vasomotor and gastrointestinal symptoms, prolonged gastric emptying time from 76±23 minutes in the placebo group to 578±244 minutes, and completely suppressed diarrhea.

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During the 12‑month treatment period, the average body weight of patients increased by 11%, and most returned to normal work.

The International Consensus on the Diagnosis and Management of Dumping Syndrome (2020) clearly states that somatostatin analogs (including Somatostatin Acetate) have definite efficacy in refractory dumping syndrome. Short‑acting formulations provide rapid relief of acute symptoms, while long‑acting agents (such as octreotide acetate microspheres) have become the mainstream clinical choice due to convenient administration (once monthly) and superior long‑term weight improvement.

Key Clinical Application Points

 

Short‑acting Somatostatin Acetate is commonly administered intravenously or subcutaneously for rapid control during acute episodes. Long‑acting octreotide acetate is recommended for chronic maintenance to reduce dosing frequency.Blood glucose should be monitored during treatment to avoid fluctuations caused by excessive insulin inhibition. Gastrointestinal adverse reactions (e.g., nausea, abdominal distension) are usually transient and resolve with tolerance.

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Information source: PubMed (PMID:2256759), International Consensus on the Diagnosis and Management of Dumping Syndrome (2020), NCBI Bookshelf (StatPearls)

Application in the Treatment of Secretory Diarrhea

Secretory diarrhea is one of the most challenging digestive system diseases in clinical practice, characterized by the continuous secretion of large amounts of water and electrolytes from the intestine, resulting in daily bowel movements exceeding 1000 grams or even more. Conventional antidiarrheal drugs often have little effect. Among various treatment methods, somatostatin (SS) and its analog Octreotide are like precise "molecular surgical knives", with their comprehensive inhibitory effect on gastrointestinal secretion function, becoming the core weapons for treating refractory secretory diarrhea. 

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1. Mechanism of action: multi-target, all-round inhibition network
Somatostatin is a peptide hormone secreted by D cells in the hypothalamus and pancreas. There are two molecular forms in the body, SS-14 (14 peptide) and SS-28 (28 peptide), with SS-28 being the main form in plasma due to its slower degradation rate. Its anti diarrhea mechanism can be described as a "multi pronged approach":

Firstly, it effectively inhibits intestinal secretion. By acting on the surface of intestinal mucosal cells with somatostatin receptors (SSR1-5 subtypes have been cloned), the secretion of gastric acid, pepsinogen, trypsin, bicarbonate, and bile is significantly inhibited. At the same time, the release of various gastrointestinal hormones such as vasoactive intestinal peptide (VIP), gastrin, glucagon, intestinal glucagon, cholecystokinin, etc. is inhibited, cutting off the "faucet" of diarrhea from the source.

2. Secondly, inhibit intestinal peristalsis. It can prolong the passage time of the digestive tract, reduce the effective utilization of the small intestine absorption area, and inhibit the contraction of intestinal smooth muscle, slowing down the propulsion speed of intestinal contents and buying valuable time for water reabsorption.

Thirdly, reduce visceral blood flow. It can reduce portal vein blood flow and visceral blood flow, which is particularly important in patients with gastrointestinal bleeding combined with diarrhea, and can achieve the dual goals of stopping bleeding and stopping diarrhea at the same time.

Naturally, its half-life is only about 2-3 minutes, so it can only be administered through continuous intravenous infusion; The half-life of artificially synthesized octreotide is extended to about 100 minutes, and its ability to inhibit growth hormone release is 70 times that of natural somatostatin, and its ability to inhibit gastric acid secretion is up to 80 times, making clinical application more convenient.

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Clinical indications: covering multiple types of refractory diarrhea

1. Neuroendocrine tumor associated diarrhea (core indication)
This is the most classic and precise application field. In VIP tumor patients, an initial dose of 50-150 μ g of octreotide, administered subcutaneously 2-3 times a day, can control diarrhea symptoms in approximately 85% of patients; If desensitization occurs after long-term medication, the dosage can be increased to 450 μ g each time, 3 times a day, and combined with adrenal corticosteroids can further improve the efficacy. In cancer like syndrome, a 24-hour dose of 50-1000 μ g of octreotide can effectively alleviate symptoms such as diarrhea, facial flushing, and skin flushing. For glucagon tumors, octreotide can suppress diarrhea symptoms by inhibiting glucagon production.

It is worth noting that it can cause diarrhea itself - the excessive secretion of somatostatin inhibits the secretion of pancreatic enzymes and bile, leading to the disorder of fat digestion and absorption, and the appearance of characteristic fatty diarrhea, accompanied by diabetes and cholelithiasis (clinical triad). At this point, the treatment is quite contradictory: it is necessary to use somatostatin analogs to control tumors, while also being alert to their side effects of exacerbating diarrhea.

2. Diarrhea due to diabetes
Up to 8%~22% of diabetes patients suffer from diarrhea, especially type 1 diabetes patients with a long course of disease, who are characterized by chronic secretory diarrhea that persists 24~48 hours after fasting and has no osmotic pressure difference in stool. Octreotide can effectively control such diarrhea symptoms and is an important choice in addition to opioid drugs.

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3. Diarrhea caused by radiation enteritis
Radiation enteritis may not show symptoms until several years after radiotherapy, presenting as refractory diarrhea or even hemorrhagic diarrhea. Octreotide can cure or improve various symptoms, including refractory diarrhea, especially for patients who have relapsed after treatment with other methods. Prophylactic use of long-acting octreotide (Shanlong) before radiotherapy may achieve a dual effect of prevention and treatment.

4. AIDS related diarrhea
Diarrhoea in AIDS patients is usually caused by cryptosporidium infection, which lacks effective antibiotics and requires long-term symptomatic treatment. Octreotide at a dose of 50-1500 μ g per day can significantly reduce bowel movements in approximately 50% of patients.

5. Short bowel syndrome and chemotherapy related diarrhea
The use of octreotide in patients with short bowel syndrome can reduce intestinal fluid secretion by 1-2 liters per day, while also reducing the amount of intravenous fluid (but cannot completely replace intravenous infusion). Severe diarrhea in cancer chemotherapy and organ transplant patients is often difficult to control with loperamide, at which point octreotide can play a crucial role.

6. Idiopathic secretory diarrhea
For various types of refractory diarrhea that are ineffective with conventional treatment, somatostatin is equally effective. A clinical observation of 37 cases of refractory diarrhea showed that after treatment with 300~1200 μ g/d octreotide for 1~12 days, about 3/4 of patients' symptoms disappeared within 2 days, with a total effective rate of 75.7%.

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Core Precautions for Somatostatin Acetate Use

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In clinical practice, strict attention must be paid to indications, dosage, and monitoring to ensure efficacy and safety.Before use, exclude patients with a history of hypersensitivity. Use is contraindicated in individuals allergic to somatostatin or acetate excipients.Although it has good water solubility and stability, intravenous administration must follow strict preparation requirements. Avoid mixing with other drugs during infusion to prevent physicochemical changes that impair efficacy.

 

Blood glucose should be closely monitored during treatment, as the drug inhibits insulin and glucagon secretion and may cause glucose fluctuations. Patients with abnormal fasting blood glucose or diabetes require intensified monitoring and timely adjustment of antidiabetic regimens to avoid hypoglycemia or hyperglycemia.Long‑term users need regular gallbladder function checks, because inhibition of gallbladder contraction and bile flow may increase the risk of cholestasis and cholelithiasis; choleretic measures may be added if necessary.

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Use in pregnant women, lactating women, children, and patients with hepatic or renal impairment requires careful risk–benefit evaluation and dosage adjustment based on body weight or organ function.Transient adverse reactions such as nausea, abdominal pain, diarrhea, and dizziness usually resolve spontaneously. Severe arrhythmia or allergic reactions require immediate discontinuation and symptomatic treatment.Somatostatin Acetate may affect coagulation; increased monitoring of coagulation parameters is required when combined with anticoagulants to avoid bleeding risk.

Information source: Merck Somatostatin for Injection (Stilamin) Prescribing Information (2021), DailyMed (FDA Label for Octreotide Acetate), China Pharmaceutical Information Query Platform, Hunan Pharmaceutical Affairs Service Network

Application in Pain Management

 

Mechanism of Action

 

The analgesic effect of Somatostatin Acetate is based on dual central and peripheral modulation:At the central level, somatostatin is widely distributed in the substantia gelatinosa of the spinal dorsal horn. It directly inhibits electrical activity of nociceptive neurons and blocks transmission of pain signals to the center. It also suppresses the release of neurotransmitters such as substance P and calcitonin gene‑related peptide (CGRP), reduces pain sensitization, and decreases spinal c‑fos expression (a marker of pain activation), interrupting pain signaling at the neural pathway level.

At the peripheral level, it inhibits the release of inflammatory factors (e.g., prostaglandins, TNF‑α), reduces local inflammatory edema, and relieves inflammation‑mediated pain. For visceral pain, it directly alleviates spastic pain of visceral smooth muscle by inhibiting visceral nerve excitability and reducing abnormal gastrointestinal hormone secretion.

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Clinical Application and Evidence of Efficacy

 

Somatostatin Acetate is mainly used for neuropathic pain and visceral pain, especially refractory pain resistant or unresponsive to opioids.

In neuropathic pain, intrathecal octreotide acetate significantly relieves chronic intractable non‑cancerous neuralgia. A 5‑year clinical follow‑up study showed that two patients with refractory neuralgia receiving continuous intrathecal infusion of octreotide acetate had sustained reduction in pain scores without obvious neurotoxicity, demonstrating good long‑term safety.

 

Animal experiments confirmed that octreotide acetate dose‑dependently inhibits acute inflammatory pain and visceral pain induced by formalin or acetic acid. Although its analgesic effect is weaker than morphine, it lacks adverse effects such as central respiratory depression and addiction, resulting in a higher safety profile.

In visceral pain, Somatostatin Acetate effectively relieves severe visceral pain caused by pancreatitis, intestinal obstruction, gastrointestinal tumors, etc., by suppressing visceral nerves and inflammation, rapidly reducing pain intensity and improving quality of life.

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Key Clinical Application Points

 

Neuropathic pain is usually treated by intrathecal or local administration to minimize systemic side effects. Visceral pain can be relieved by subcutaneous or intravenous injection for rapid onset.Dosing must be individualized, starting low and titrating gradually to avoid reduced efficacy due to somatostatin receptor desensitization. Long‑term users require monitoring of blood glucose and gallbladder function, as well as central and gastrointestinal reactions such as dizziness and nausea.

Information source: PubMed (PMID:8747973), Acta Physiologica Sinica, PMC (PMC8558988)

References

[1] What is the function of somatostatin Bohe Health, August 11, 2025 https://m.bohe.cn/article/mip/1ikv2uzylk08lbo.html

[2] Modern treatment of digestive diseases: diarrhea and octreotide two thousand and one

[3] Practical pediatric gastroenterology: ischemia and diarrhea one thousand nine hundred and ninety-seven

[4] Somatostatin is usually used for a few days 39. Ask the doctor, March 29, 2022 https://ask.39.net/question/107187367.html

[5] Side effects and precautions of somatostatin 39 Health Network, June 10, 2023 https://m-mip.39.net/askar/mipso_k59q2df.html

[6] Chronic diarrhea is associated with NEN, CgA, and somatostatin two thousand and eighteen

[7] What are the symptoms of somatostatin injection that can be used 39 Drug Communication, November 8, 2023 https://wapypk.39.net/saftydrugs/cm22geqz.html

[8] What are the main treatment methods for chronic diarrhea There is a doctor here, June 30, 2023 https://www.youlai.cn/yyk/article/810509.html

[9] How to scientifically use injectable somatostatin Kangdele Pharmacy, November 7, 2024 https://m.baiji.com.cn/news/yongyao_xhk/1030511202.html

[10] Somatostatin usually requires several days of treatment 39 Health Network, February 23, 2024 https://zl.39.net/a/240223/n4mx7pp.html

[11] What are the precautions for using somatostatin Popular Health Network, May 17, 2025 https://www.cndzys.com/ylcore/art_detail/1_2738197.html

[12] Li Nan and others Clinical observation on the treatment of 37 cases of refractory diarrhea with somatostatin Chinese Journal of Modern Medicine, 2004, 14 (3): 38-40

[13] Basic and Clinical Studies of Somatostatin: Diarrhea and Octreotide two thousand and eleven

[14] Chronic diarrhea and SSoma, pancreas two thousand and eighteen

[15] Application of nursing intervention in the treatment of diarrhea adverse reactions after using somatostatin to treat gastrointestinal bleeding two thousand and twenty-four

[16] E D. Efficacy of Octreotide Acetate in Treatment of Severe Postgastrectomy Dumping Syndrome [J]. Annals of Surgery, 1990.

[17] International Consensus Group on Dumping Syndrome. Diagnosis and Management of Dumping Syndrome: A Consensus Report [J]. 2020.

[18] Smith A, et al. Severe Idiopathic Secretory Diarrhoea With a Profound Sustained Response to Somatostatin Analogues: A Case Report [J]. [19] Case Reports in Gastroenterology, 2025.

 

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