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SKQ1 capsule is an antioxidant product with SKQ1 (Brominated Skurachev ion) as its core component, usually in the form of capsules, aimed at clearing free radicals by targeting mitochondria, achieving anti-aging, disease prevention, and health management functions. It is a mitochondrial targeted antioxidant composed of lipophilic cations and antioxidants connected by saturated hydrocarbon chains. Its lipophilicity enables it to efficiently penetrate the cell membrane and reach the mitochondria (the "energy factory" of the cell). Mitochondria are the main production sites of free radicals such as superoxide anions and hydrogen peroxide. Excessive free radicals can attack mitochondrial DNA and proteins, leading to cellular aging and apoptosis. SKQ1 protects cellular function by neutralizing free radicals within mitochondria and blocking this process. This oral capsule is convenient for storage and administration, while also covering the taste of the medication. Some products use high permeability nano transdermal technology, which allows SKQ1 to be directly absorbed into the bloodstream and enter cell mitochondria through application.
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SKQ1 COA
SKQ1 Capsule, as a novel mitochondrial targeted antioxidant, is composed of a decaalkyltriphenylphosphine cation (TPP ⁺) and a plastid quinone group in its molecular structure. With the help of mitochondrial membrane potential difference, it can achieve concentration enrichment at a thousand fold level and exert pharmacological effects by clearing reactive oxygen species (ROS), inhibiting lipid peroxidation, and mitochondrial DNA oxidation. Preclinical studies have confirmed that SKQ1 exhibits significant therapeutic potential in various disease models such as acute kidney injury and dry eye syndrome, among which eye drops have been approved for use. Capsules, as a classic dosage form of oral preparations, have the advantages of masking adverse drug odors, improving stability, and achieving precise dose control, especially suitable for active ingredients with special physicochemical properties such as SKQ1. SKQ1 pure product is a brown solid with hygroscopicity. It needs to be stored in an inert atmosphere at -20 ℃ and has poor water solubility (only 3mg/ml at 25 ℃). After oral administration, it is easily affected by the gastrointestinal environment and its bioavailability is reduced. Therefore, the development of SKQ1 capsules requires a systematic solution to key technical issues such as drug solubilization, stability protection, and targeted delivery enhancement.
The physical and chemical properties of SKQ1 and the basis for formulation design
The use of solid dispersion technology for pretreatment is currently the most effective solution to address the low solubility issue of SKQ1. Using polyvinylpyrrolidone K30 (PVP K30) as the carrier material, a solid dispersion was prepared by solvent method with a mass ratio of drug: carrier=1:5. SKQ1 and PVP K30 were dissolved in an ethanol dichloromethane mixed solvent (volume ratio 1:1), and the solvent was removed by rotary evaporation at 60 ℃.
After vacuum drying for 12 hours, the powder was crushed and sieved through an 80 mesh sieve. Differential scanning calorimetry (DSC) analysis showed that this process can transform SKQ1 from a crystalline state to an amorphous state, increase its water solubility to 15mg/ml, and increase its in vitro dissolution rate by 3.2 times compared to the raw material.
Screening and optimization of fillers
Fillers need to have good fluidity, compatibility with drugs, and stability protection. Screen three commonly used fillers through compatibility testing (placed under accelerated conditions for one month):
Microcrystalline cellulose (MCC): After mixing with SKQ1, its content decreases by less than 2%, but it has strong hygroscopicity and needs to be used in conjunction with moisture resistant excipients;
Lactose monohydrate: Drug content decreased by 5.3%, with slight interactions present;
Mannitol: The drug content decreases by less than 1.5%, has low hygroscopicity, and can improve powder flowability.
Finally, mannitol was determined as the main filler, accounting for 40% -50% of the total prescription, and supplemented with 10% MCC to regulate the flowability of the powde
To further enhance drug stability, two stabilizers are added to the prescription:
Antioxidant: Vitamin E (0.1% content) is selected to inhibit the oxidative degradation of SKQ1, reducing the drug degradation rate by 60% in accelerated testing;
Sunscreen: Add 2% titanium dioxide to block ultraviolet radiation and reduce photodegradation reactions.
In addition, adding 5% polyethylene glycol 4000 (PEG 4000) as a plasticizer can improve the formability of solid dispersions and reduce powder delamination during capsule filling.
Selection of capsule shell
Considering the hygroscopicity and instability in acidic environments of SKQ1, hydroxypropyl methylcellulose (HPMC) capsule shells were chosen instead of traditional gelatin capsule shells. The HPMC capsule shell has the characteristics of low moisture absorption (balanced moisture absorption rate<12%) and resistance to gastric acid corrosion, which can keep the capsule intact in the stomach and release the drug after reaching the intestine, protecting the drug from gastric acid damage and reducing gastrointestinal irritation.
Preparation process and key technical control of SKQ1 capsules
Design of Preparation Process Flow
SKQ1 capsule use powder direct filling technology, and the overall process is divided into five core steps: pretreatment, mixing, filling, polishing, and packaging. The specific process is as follows:
Raw material pretreatment: SKQ1 raw material is vacuum dried (60 ℃, 8h) to remove moisture, and then crushed through a 100 mesh sieve; All auxiliary materials are sieved through an 80 mesh sieve, dried at 60 ℃ for 4 hours, and then cooled to room temperature for later use.
Preparation of solid dispersion: Mix SKQ1 and PVP K30 in proportion, prepare the solid dispersion by solvent method, and grind it through an 80 mesh sieve.
Step by step mixing: First, mix the solid dispersion with vitamin E and PEG 4000 for 10 minutes, then add mannitol and MCC for 20 minutes, and finally add titanium dioxide for 15 minutes. The mixing speed is controlled at 30 rpm.
Powder flowability testing: Determine the angle of repose (required to be<30 °) and bulk density (required to be 0.45-0.55g/cm ³) of the mixed powder. Only after passing the test can filling be carried out.
Capsule filling: The fully automatic capsule filling machine (model NJP-400) is used for filling, with a set filling amount of 200mg/capsule (including SKQ1 10mg).
Polishing and picking: The filled capsules are polished to remove surface powder using a polishing machine, and then manually picked to remove deformed or leaking capsules.
Aluminum plastic blister packaging: Packaging is carried out in an environment with humidity<45% and temperature 20-25 ℃.
Optimization and Control of Key Process Parameters
Optimization of solid dispersion preparation parameters
The key parameters for preparing solid dispersions by solvent method include solvent ratio, rotary evaporation temperature, and drying time. The optimal parameter combination was obtained through orthogonal experiment (L9 (3 ⁴)) optimization:
Ethanol dichloromethane volume ratio: 1:1 (solvent polarity is moderate, which can completely dissolve the raw materials and facilitate rapid evaporation);
Rotating evaporation temperature: 60 ℃ (lower than the SKQ1 degradation temperature of 75 ℃, and able to ensure complete removal of the solvent within 30 minutes);
Vacuum drying time: 12 hours (drying loss<0.5%, ensuring no solvent residue).
The dissolution rate of SKQ1 in the optimized solid dispersion (45 minutes) can reach over 85%, which is 22% higher than the unoptimized process.
Uniformity control of mixing process
The uniformity of mixing directly affects the accuracy of capsule content. Using the "equal amount recursive method" for mixing, first mix the smallest proportion of vitamin E with 10 times the amount of solid dispersion, and then gradually add other excipients. During the mixing process, the content uniformity of the mixed powder is monitored in real-time using high-performance liquid chromatography (HPLC), and the relative standard deviation (RSD) of the content at any 10 sampling points is required to be less than 3%. Research has shown that a mixing time that is too short (<30 minutes) can lead to an RSD>5%, while a mixing time that is too long (>45 minutes) can cause powder stratification. Therefore, the optimal total mixing time is 45 minutes.
Capsule filling parameter control
The key parameters of the fully automatic capsule filling machine include filling speed, pressure, and dosage adjustment. The optimized parameters are as follows:
Filling speed: 300 particles/minute (if the speed is too fast, it can cause powder flying and differences in filling amount, while if it is too slow, it can reduce production efficiency);
Filling pressure: 0.3MPa (too low pressure can cause the contents of the capsule to become loose, leading to powder leakage; If it is too high, it will cause deformation of the capsule shell;
Dose difference control: Take 20 samples every 15 minutes to test the filling amount, with an average filling amount deviation of<± 5% and a single particle deviation of<± 7.5%.
Environmental parameter control
The entire preparation process requires strict control of the temperature, humidity, and cleanliness of the production environment
Cleanliness level: The mixing and filling processes must be carried out in a D-level clean area, with a particle count of less than 200000 particles per cubic meter for air suspended particles ≥ 0.5 μ m;
Temperature and humidity control: The temperature of the pre-treatment, mixing, and filling processes should be controlled at 20-25 ℃, and the humidity should be less than 45%; The humidity in the packaging process can be relaxed to<50%.
When the environmental humidity exceeds 50%, SKQ1 capsule is prone to moisture absorption and degradation, leading to a decrease in its content; If the temperature exceeds 28 ℃, PEG 4000 will soften and affect the flowability of the powder.
SKQ1 capsules represent a promising new approach to antioxidant therapy, with the potential to protect against oxidative stress and its associated health problems. By targeting mitochondria, SKQ1 can effectively neutralize ROS and preserve cellular function, leading to a wide range of potential health benefits, including anti-aging effects, cardiovascular protection, neuroprotection, eye health, and skin health. However, more research is needed to fully establish the safety and efficacy of SKQ1 in humans, and to determine the optimal dosage and long-term use. As the research progresses, SKQ1 may emerge as a valuable tool in the prevention and treatment of various age-related diseases and conditions, offering hope for a healthier and longer life.
Frequently Asked Questions
What is SkQ1 bromide?
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SKQ1 (bromide) is a mitochondria-targeted antioxidant that decreases transmembrane potential and production of reactive oxygen species (ROS). 1. SKQ1 prevents neuronal loss and synaptic damage in a rat model of spontaneous Alzheimer's disease, as well as decreases severity of arthritic lesions in rats.
What are the different types of SK?
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Three subtypes of SK subunits, SK1 (KCa2.1), SK2 (KCa2.2) and SK3 (KCa2.3) have been cloned and are expressed differentially within the CNS (Köhler et al., 1996; Stocker and Pedarzani, 2000). These channels, which consist of homo- or heterotetramers, are exclusively gated by intracellular Ca2+.
What are the benefits of SkQ1?
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The findings suggested that SkQ1 exerts its therapeutic effects via multiple mechanisms, including the reduction of ROS accumulation, mitigation of oxidative damage, preservation of mitochondrial function, and inhibition of apoptotic pathways.
What is SkQ?
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SkQ is a class of mitochondria-targeted antioxidants, developed by Professor Vladimir Skulachev and his team. In a broad sense, SkQ is a lipophilic cation, linked via saturated hydrocarbon chain to an antioxidant. Due to its lipophilic properties, SkQ can effectively penetrate through various cell membranes.
Does CoQ10 help with sagging skin?
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In addition, CoQ10 works on the cellular level to preserve elastin and collagen. These are the proteins that keep your skin firm, supple, and rejuvenated. They help prevent loose, saggy skin. They give your skin strength and flexibility, so it can 'bounce back' more easily.
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