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The hot, scalding Simeaglutide that set off a national weight loss craze

Semaglutide is a blood sugar lowering drug, and some people use it to lose weight.

The mechanism of action of Semaglutide in lowering blood glucose is glucagon-like peptide 1 (GLP-1) receptor agonist. This type of drug is available only in subcutaneous injection form.

Glucagon-like peptide is a kind of “enterotrophin” secreted by the gastrointestinal mucosa of the human body, which can inhibit glucagon secretion and promote insulin secretion.

Glucagon-like peptide-1 receptor agonists enhance the secretion of insulin and inhibit the secretion of glucagon in a glucose-dependent manner to achieve the purpose of regulating blood sugar, so they are suitable for the blood sugar control of type 2 diabetes.

Simeaglutide side chains, intermediates and excipients are worth digging.

Synthesis process: intermediates → apis, + excipients = Preparations/Semaglutide (oral/injectable)

Today, let’s talk about SNAC accessories:

SNAC (SodiumN-[8-(2-hydroxybenzoyl) amino]caprylate), sodium 8-(2-hydroxybenzoyl) caprylate, is a synthetic n-acetylated amino acid derivative of amphoteric salicylic acid and is currently the most advanced intestinal osmotic enhancer (PEs). It is widely used as a delivery agent for oral pharmaceutical preparations. By the United States Emisphere company in the 1990s, a highly efficient carrier molecule screened from many penetration enhancers.

In 2014, the US Food and Drug Administration approved an oral formulation of vitamin B12, demonstrating for the first time that SNAC is feasible, even though it is a medical food, it also shows that SNAC is safe to use.

In 2017, subcutaneous injection of Semaglutide was approved, becoming the second GLP-1RA to be approved for weekly injection after Dura lutide. In 2019, oral Smeaglutide was officially approved, and it is SNAC that is added to the prescription, thereby promoting the absorption of Smeaglutide and preventing it from being degraded in the stomach.

As the most advanced intestinal osmotic enhancer (PEs), SNAC can adhere to the gastric mucosa together with peptides to promote drug penetration and absorption, and is widely used as a delivery agent for oral preparations. Using SNAC, it is possible to develop oral delivery pathways for some formulations that facilitate the oral absorption of certain poorly bioavailable macromolecules such as insulin, heparin, or small molecules without changing their chemical form, biological integrity, or pharmacological properties.

Semaglutide (a GLP-1 receptor agonist), GLP-1 is a hormone secreted by the gastrointestinal tract and released into the blood after eating, which can stimulate insulin secretion, inhibit glucagon secretion, delay gastric emptier, increase satiety, etc. [1], thereby reducing blood sugar level and playing the dual role of “on-demand” hypoglycemic and “intelligent” weight loss. Under the dual effect of hypoglycemic and weight loss, Semiglutide has become a phenomenon “new star”.

On May 4, 2023, Novo Nordisk released its first quarter earnings report, with operating income of $7.9 billion, a significant increase of 27% over the same period last year. Net profit was $2.94 billion, up 39% from a year earlier. Semaglutide became the absolute driving force of performance growth, and the sales volume of injected hypoglycemic version Semaglutide Ozempic was 2.91 billion US dollars, a substantial increase of 63%. Sales of the oral hypoglycemic version of Semaglutide Rybelsus were $650 million, a significant increase of 107%; The diet version of Smaglutide Wegovy had sales of $680 million, a significant increase of 211%. The three combined, Simeiglutide total sales of $4.24 billion, is expected to exceed $20 billion for the full year.

SNAC and Semaglutide molecules made in heaven

The combination between Semaglutide and SNAC is tailor-made and has been “unique” so far. SNAC and Semaglutide are the only oral formulations of GLP-1RA.

On the basis of the original semaglutide molecule, the absorption promoter SNAC is added to Semaglutide tablet, which can improve the local pH value in the stomach, reduce the degradation of Semaglutide molecule by pepsin, and promote the transcellular transport of semaglutide to achieve the absorption of the molecule in the stomach [2]. Semaglutide tablets can be rapidly absorbed into the blood in the transient neutral acid-base environment of the organism’s stomach, and once a day administration, the blood concentration is stable, and the bioavailability of semaglutide is greatly increased.

Tips: Unauthorized use of drugs is risky, must be used under the guidance of a doctor, do not blindly follow the trend, please choose the correct and healthy way to lose weight.

About Wisdom Drugs

Wisdom Drugs Co .,Ltd   was founded in Sep. 2011 whose headquarter located in Changzhou Creative Industry Park, having a branch in India. The company’s R&D center is engaged in not only the process development of APIs, intermediates, poly-peptide compounds and heterocyclic compounds,but also the optimization and production. We are devoted to the synthesis customization and the technology transfer, enabling compounds to be scaled from laboratory to commercial to meet the requirements of different customers.

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