Quality standards and purity indicators
Content (calculated as anhydrous): 98.5% -101.5% (titrated with perchloric acid)
Related substances (HPLC): Single maximum impurity ≤ 0.2%, total impurity ≤ 0.5%
Moisture content: ≤ 2.5%
Burning residue: ≤ 0.1%
Heavy metal: ≤ 10ppm
Residual solvents: Methanol, dichloromethane, DMF, etc. meet the pharmacopoeia limit for residual solvents
Identification: HPLC retention time consistent, infrared spectrum matched with reference substance
2. Research experimental level
HPLC purity ≥ 98.0%, providing COA detection report, impurity indicators can be adjusted as needed, suitable for formulation trials, pharmacological in vitro cell experiments, and animal model experiments.
Pharmacology and pharmacokinetics
mechanism of action
Belonging to type 5 phosphodiesterase (PDE-5) selective inhibitors.
During sexual stimulation, the corpus cavernosum releases nitric oxide (NO), activates guanylate cyclase, and enhances intracellular cGMP; Sildenafil inhibits PDE-5, reduces cGMP hydrolysis, promotes smooth muscle relaxation and vasodilation of the corpus cavernosum, and increases local blood flow. There will be no physiological effects under conditions of no sexual stimulation.
At the same time, it can relax the smooth muscle of pulmonary blood vessels, enhance cGMP in lung tissue, and be used for pharmacological research in the direction of pulmonary arterial hypertension; Inhibition of PDE6 in the retina can lead to visual abnormalities and side effects at high doses.
In vitro, the selectivity for PDE5 is significantly higher than that for PDE1-PE4, but there is still cross inhibitory activity against PDE6.
Pharmacokinetic parameters (human literature data)
Absorption: Oral administration on an empty stomach for 30-120 minutes to reach peak blood drug levels, with an absolute bioavailability of approximately 41%; A high-fat diet delays peak time and reduces peak concentration.
The protein binding rate is about 96%, and it is widely distributed in tissues.
Metabolism: CYP3A4 is the main metabolic pathway in the liver, generating N-demethylated active metabolites; The half-life of the prototype and active metabolite is about 4 hours.
Excretion: Mainly excreted through feces, with a small amount excreted through urine.
Pharmacological research direction
Research experiments on animal models of erectile dysfunction, pharmacology of pulmonary arterial hypertension, vasodilation, antiplatelet therapy, transdermal formulations, and nanoformulation development.
Detection Methods
1. High performance liquid chromatography (HPLC)
Reverse phase C18 chromatographic column, UV detection wavelength 290nm; used for content determination and separation of related substance impurities; The conventional testing methods for raw material storage and finished product release can separate main components, oxidative degradation impurities, and process impurities.
2. Potentiometric titration method (pharmacopoeia arbitration content determination)
Ice acetic acid acetic anhydride system, titrated with perchloric acid titrant, suitable for the determination of total content of sildenafil citrate raw material, not affected by chromatographic impurities.
3 LC‑MS / UPLC‑MS
High sensitivity, used for measuring drug concentration in biological samples such as plasma and tissues; Screening for illegal addition of health food and samples can detect trace amounts of sildenafil and its metabolites.
4. Infrared spectroscopy (IR)
Qualitative identification, comparison of sample infrared spectra with reference spectra.
5. Thin layer chromatography (TLC)
Quick qualitative identification, suitable for initial screening of large quantities of samples.
Product specifications, packaging, and logistics distribution
Research trial specifications: 10g, 50g, 100g, sealed in aluminum foil vacuum bag packaging.
Specification of pilot raw materials: 1kg aluminum foil vacuum bag; 25kg cardboard drum, inner double-layer PE bag.
Supporting materials: COA quality inspection report and MSDS safety technical manual can be provided for each batch.
6, Logistics transportation
Domestic transportation: Belonging to ordinary chemical research raw materials, non flammable and non explosive hazardous chemicals; Transport away from light and moisture, and avoid high temperatures and direct sunlight.
Overseas export: declared as ordinary scientific research chemicals; Essential MSDS and COA documents; Different countries require corresponding import filing documents; Prohibited from being declared as raw materials for food and health products.
This product is only for drug development and scientific experiments,
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