Phlorizin 60-82-1 Blood Glucose Management Ingredient

Phlorizin (CAS No. 60-82-1) is a dihydrochalcone flavonoid compound naturally occurring in the root bark and fruit peel of apple trees (Malus domestica). It has garnered significant attention in recent years as a plant-derived active substance within research on blood glucose management and carbohydrate metabolism. As a functional ingredient with a well-defined mechanism of action, Phlorizin demonstrates considerable potential for applications in formulations targeting metabolic health and blood glucose equilibrium.

Typically supplied as a white-to-pale-yellow powder, Phlorizin exhibits excellent formulation compatibility and is suitable for capsules, tablets, granules, and composite metabolic support products. In practical applications, this ingredient is frequently incorporated into formulations targeting blood glucose management, carbohydrate absorption regulation, and metabolic equilibrium. It may also be synergistically combined with functional ingredients such as mulberry leaf extract, bitter melon extract, cinnamon extract, or alpha-lipoic acid to establish a multi-mechanism plant-based blood glucose support system.

PS: This page focuses on the product application information.

For the product Technical Data Sheet, please click 90% Phlorizin Powder HPLC Test Data.

For Sample & Supply Chain Solutions, please click Apple Extract Phlorizin Factory Sample.

Phlorizin's positioning within the field of glycaemic management may be summarised as: "The pioneering and benchmark natural SGLT inhibitor for blood glucose regulation." This positioning is grounded in a comprehensive assessment across three dimensions:

First Dimension: Pioneering Scientific Discovery

Phlorizin stands as the first natural compound historically identified to possess sodium-glucose cotransporter (SGLT) inhibitory activity. From a pharmaceutical development perspective, Phlorizin stands as the "lead compound" for the entire SGLT inhibitor drug family. The molecular designs of currently widely used SGLT2 inhibitors, such as dapagliflozin, empagliflozin, and canagliflozin, all draw inspiration from optimized modifications of Phlorizin's structure.

Second Dimension: Unique Advantages in Mechanism of Action

Phlorizin's core value in glycaemic management lies in its dual-target inhibitory properties. Research data indicate that the root bark glycoside exhibits an approximate half-maximal inhibitory concentration (IC₅₀) of 65 nM for human SGLT2 and 400 nM for SGLT1, demonstrating approximately sixfold selectivity for SGLT2 over SGLT1. This pharmacological profile enables phlorizin to simultaneously target the SGLT2 transporter in renal proximal tubules and the SGLT1 transporter in intestinal mucosa, exerting synergistic hypoglycaemic effects by inhibiting both glucose absorption and reabsorption pathways. Compared to synthetic SGLT2 inhibitors, phlorizin, as a natural plant extract, possesses the following differentiated competitive advantages:

• Firstly, multi-component synergistic effects. Plant extracts often contain multiple structurally similar active constituents, which may exhibit synergistic interactions, yielding more comprehensive biological effects than any single component alone. Phlorizin extracts typically also contain trace amounts of derivatives such as phloretin, which similarly possess certain biological activities.
• Secondly, high consumer acceptance. In an era of heightened health consciousness, "natural origin" has become a key factor influencing consumer purchasing decisions. Phlorizin, extracted from common plant sources such as apple tree bark, aligns with consumer expectations for "natural" and "plant-based" products.

Third Dimension: Market Prospects and Development Trends

The global blood glucose management market continues to expand, driven by factors including: the persistent rise in global diabetes prevalence, a substantial pre-diabetic population, and heightened health awareness fuelling demand for preventive healthcare. According to the International Diabetes Federation (IDF), approximately 537 million adults worldwide had diabetes in 2021, projected to increase to 643 million by 2030. This substantial target population creates significant market potential for dietary supplements targeting blood glucose management.

Detailed Explanation of SGLT Inhibition Mechanism

The molecular mechanism by which phlorizin exerts its blood glucose-regulating effects primarily involves competitive inhibition of the sodium-glucose cotransporter (SGLT). SGLTs are a class of membrane-bound transporters responsible for driving glucose transport across cell membranes, utilizing the sodium ion concentration gradient. Two SGLT subtypes closely associated with glucose regulation have been identified in the human body:

• SGLT1: Primarily distributed in the brush border of the small intestinal mucosa, it is responsible for the active absorption of dietary glucose. It is also expressed in the S3 segment of the renal proximal tubule, where it participates in glucose reabsorption. SGLT1 exhibits high affinity for glucose but low transport capacity.
• SGLT2: Primarily distributed in the S1 segment of the renal proximal tubule, it accounts for approximately 90% of filtered glucose reabsorption and is a key target for maintaining blood glucose homeostasis. SGLT2 exhibits relatively low affinity for glucose but possesses substantial transport capacity.

Phlorizin competitively binds to the glucose-binding site of SGLT proteins, thereby blocking transmembrane glucose transport. Its molecular structure contains a glucose moiety that highly matches the substrate recognition pocket of SGLT, enabling highly efficient competitive inhibition.

Inhibition Activity Data

Multiple studies have quantified the inhibitory activity of Phlorizin against SGLT1 and SGLT2:

Multidimensional Mechanisms of Hypoglycaemic Effects

Phlorizin's blood glucose regulation extends beyond SGLT inhibition to involve the following synergistic mechanisms:

• Enhanced renal glucose excretion: By inhibiting tubular SGLT2, phlorizin lowers the renal glucose reabsorption threshold, facilitating the urinary excretion of filtered glucose. This action operates independently of insulin secretion, thus retaining hypoglycaemic efficacy even in insulin-resistant states characteristic of type 2 diabetes.
• Delayed intestinal glucose absorption: By inhibiting intestinal SGLT1, Phlorizin slows the absorption rate of dietary glucose, reducing postprandial blood glucose peaks and ameliorating postprandial hyperglycemia.
• Improved insulin sensitivity: Animal studies indicate phlorizin treatment corrects hyperglycemia in diabetic rats and restores peripheral tissue insulin sensitivity. This effect likely involves multiple mechanisms, including reduced glucotoxicity and improved lipid metabolism.
• β-Cell Protection: Prolonged hyperglycemia exerts toxic effects on pancreatic β-cells. By lowering blood glucose levels, Phlorizin indirectly mitigates glucose toxicity-induced β-cell damage, thereby supporting long-term pancreatic function maintenance.

Application Areas of Dietary Supplements

The application of geniposide in the dietary supplement sector primarily focuses on the following areas:

1. Blood Glucose Management Products

As a blood glucose-regulating ingredient, Phlorizin can be utilized in the following subcategories:

• Blood Glucose Balancing Formulas: Combined with other blood glucose-regulating components such as chromium, alpha-lipoic acid, and cinnamon extract to create multi-component blood glucose management products.
• Diabetes Support Products: Serving as nutritional supplements for lifestyle interventions among diagnosed diabetic populations.
• Pre-Diabetes Intervention Products: Providing preventive nutritional support for sub-healthy populations exhibiting abnormal blood glucose levels but not meeting diabetes diagnostic criteria.

2. Weight Management Products

By promoting urinary glucose excretion, phlorizin theoretically aids weight management through increased energy expenditure. Within dietary supplement formulations for weight control, Phlorizin may function as a synergistic ingredient alongside components such as green tea extract, garcinia cambogia, and conjugated linoleic acid.

3. Antioxidant and Anti-Ageing Products

As a polyphenolic compound, Phlorizin exhibits antioxidant activity. Within the cosmetics and oral beauty sectors, Phlorizin is being explored for inclusion in anti-ageing product formulations.

Product Dosage Forms

Common dosage forms for dietary supplements include tablets, capsules, powders, and liquids. Considering the physicochemical properties of Phlorizin, the suitability of each form is analyzed as follows:

1. Capsules

Capsules are the preferred dosage form for Phlorizin raw material, for the following reasons:

• Taste Masking: Phlorizin possesses a certain bitterness; the capsule shell effectively shields against unpleasant taste.
• Protective properties: Capsule shells shield the active ingredient from light and air exposure, enhancing stability.
• Dose precision: Facilitates standardized dosage delivery.
• High consumer acceptance: Capsules represent one of the most prevalent dosage forms in the dietary supplement market.
• Recommended specification: Each capsule containing 50-200mg of Phlorizin, with flexible adjustment based on target demographic and formulation design.

2. Tablets

Tablets are equally suitable for Phlorizin, offering lower costs and higher production efficiency.

However, note: The compression process may generate heat, requiring assessment of its impact on ingredient stability. Film coating may be considered to enhance stability and improve appearance.

3. Powder

Powder formulations facilitate flexible dosage adjustment and can be blended with other powdered ingredients to create sachets or solid beverages. However, note: Phlorizin's bitterness may affect palatability; flavouring agents or masking compounds should be added. Powders are more sensitive to humidity and light exposure, necessitating higher packaging standards.

Formulation Design Recommendations

Considering Phlorizin's mechanism of action and bioavailability characteristics, the following factors should be addressed in formulation design:

At present, the commercial application of phlorizin within the dietary supplement sector remains in its nascent stages. Market research indicates that phlorizin, as a "legitimate and sustainable ingredient", currently suffers from "underperformance in the marketplace" and "insufficient recognition". This situation reflects inadequate market promotion on the one hand, while simultaneously signifying substantial untapped market development potential on the other.

Key Competitor Comparative Analysis

1. Physicochemical Stability

As a polyphenolic glycoside compound, phlorizin's stability is influenced by multiple factors:

• Light Stability

Phlorizin exhibits sensitivity to light exposure. Prolonged exposure to ultraviolet or visible light may induce photodegradation, leading to reduced content and colour changes. Consequently, light-shielding measures must be implemented for both raw material storage and finished product packaging.

• Thermal Stability

Phlorizin exhibits relative stability at ambient temperatures but may undergo degradation or structural transformation under elevated heat conditions. Prolonged high-temperature processing should be avoided during manufacturing; it is recommended to maintain process temperatures below 60°C.

• pH Stability

Phlorizin remains relatively stable in acidic to neutral environments (pH 4–7). However, it readily undergoes hydrolysis under strongly alkaline conditions, yielding phloretin and glucose. Therefore, formulation design should avoid direct combination with strongly alkaline components.

• Oxidative Stability

Phlorizin molecules contain multiple phenolic hydroxyl groups, exhibiting reductive properties that may undergo oxidation. Storage requires airtight sealing to isolate from oxygen; consideration may be given to adding antioxidants for protection.

2. Storage Recommendations

In accordance with the technical specifications provided by the raw material supplier, the recommended storage conditions for Phlorizin are as follows:

• Temperature: Store in a cool, dry place. For long-term storage, -20°C is recommended.
• Humidity: Maintain relative humidity below 60%.
• Light Exposure: Store away from light using dark containers or opaque packaging.
• Container: Use sealed containers. Aluminum foil pouches or double-sealed bags are recommended.

3. Incompatibilities

The following potential incompatibilities require attention during formulation development:

• Alkaline components: Avoid direct combination with strongly alkaline substances such as sodium bicarbonate or sodium carbonate
• Metal ions: Polyphenolic compounds may form complexes with metal ions, potentially affecting absorption
• Enzymatic components: Phlorizin may be hydrolyzed by intestinal β-glucosidase; formulation design should account for this.

We are not only a supplier of high-quality Phloretin raw materials, but also a trusted partner on your product development journey. With years of specialisation in the field of plant extracts, we possess formidable capabilities and an outstanding reputation.

Company Milestones

Established in 2006, our company specialises in the research, development, and production of natural active ingredients. In 2007, we invested in establishing a modern, independent factory spanning over 6,900 square metres, integrating R&D, production, and quality control under one roof. In 2008, we achieved our first ISO 9001 Quality Management System certification, signifying a new level of management excellence. Today, we hold the designation of "National High-Tech Enterprise", possess multiple invention patents, and serve hundreds of renowned global cosmetic brands.

[To learn more about our journey, please click here to visit our "Development History" page]

 

 

 

 

Cutting-Edge R&D and Production Facilities

Research Centre: Our Xi'an-based technical centre houses specialised laboratories equipped with advanced analytical and R&D instruments, including High-Performance Liquid Chromatography (HPLC), Gas Chromatography (GC), Liquid Chromatography-Mass Spectrometry (LC-MS), and Fourier Transform Infrared Spectroscopy (FTIR).

Production Environment: Our manufacturing facilities are designed and managed in strict compliance with GMP standards, featuring four independent production lines to ensure clean, controlled, and efficient processes.

[To explore our innovation capabilities, please click here to visit our 'R&D and Innovation' page]

Stringent Quality Control System

We guarantee that every batch of Phloretin undergoes rigorous, comprehensive testing.

Purity: Determined via HPLC analysis, ensuring content ≥90%.

Residual Solvents: Strictly adhering to guidelines, solvent residues are maintained well below safety thresholds.

Heavy Metals: Lead, arsenic, mercury, cadmium, and other heavy metals comply with the most stringent international standards (≤10ppm). Microorganisms: Total plate count ≤1000cfu/g, yeast and mould ≤100cfu/g.

Authoritative Certification

We hold ISO 9001 Quality Management System certification, ensuring standardised processes and customer satisfaction. We hold ISO 22000, SC, Kosher, and Halal certifications, demonstrating our production environment and operational standards meet international benchmarks.

[To view our full certification portfolio, click here to visit our 'Certification' page]

Reference
[1]W. Blaschek. "Natural Products as Lead Compounds for Sodium Glucose Cotransporter (SGLT) Inhibitors." Planta Médica (2017).
[2]Luclano Rossetti, Douglas Smith et al. "Correction of hyperglycemia with phlorizin normalizes tissue sensitivity to insulin in diabetic rats." The Journal of Clinical Investigation (1987).
[3]A. Oku, K., Ueta et al. "T-1095, an inhibitor of renal Na+-glucose cotransporters, may provide a novel approach to treating diabetes." Diabetes (1999).
[4]E. M. Wright, D. Loo et al. "Biology of human sodium glucose transporters." Physiological reviews (2011).
[5]E. Makarova, P. Górnaś et al. "Acute anti-hyperglycaemic effects of an unripe apple preparation containing phlorizin in healthy volunteers: a preliminary study." Journal of the science of food and agriculture (2015).
[6]P. Hilt, A. Schieber et al. "Detection of phloridzin in strawberries (Fragaria x ananassa Duch.) by HPLC-PDA-MS/MS and NMR spectroscopy." Journal of agricultural and food chemistry (2003).
[7]C. Gosch, H. Halbwirth et al. "Phloridzin: biosynthesis, distribution and physiological relevance in plants." Phytochemistry (2010).
[8]M. Najafian, M. Z. Jahromi et al. "Phloridzin reduces blood glucose levels and improves lipid metabolism in streptozotocin-induced diabetic rats." Molecular Biology Reports (2011).
[9]M. Anastassiadou, Alba Brancato et al. "Pesticide Residue Intake Model‐ EFSA PRIMo revision 3.1." EFSA Supporting Publications (2019).
[10]Alba Brancato, D. Brocca et al. "Use of the EFSA Pesticide Residue Intake Model (EFSA PRIMo, revision 3)." EFSA Journal (2018).