Product Usage

Non peptide angiotensin II receptor antagonists can selectively and irreversibly block ATI receptors without affecting other receptor systems. Used for mild to moderate hypertension. Telmisartan is a new type of antihypertensive drug, which is a specific angiotensin II receptor (AT type I) antagonist used for the treatment of primary hypertension. Substitute angiotensin II receptors bind with high affinity to AT I receptor subtypes (known angiotensin II action sites). Telmisartan has no site agonist effect at the AT I receptor site and selectively binds to the AT I receptor, with a long-lasting binding effect. There is no affinity for other receptors, including AT2 and other AT receptors with fewer characteristics. The functions of the other receptors mentioned above are not yet known, and it is also unknown whether telmisartan may cause an increase in angiotensin II levels, which may lead to receptor overstimulation effects. Telmisartan does not inhibit human plasma renin and does not block ion channels. Without inhibiting angiotensin converting enzyme II, this enzyme can also degrade adverse reactions caused by the enhanced effect of bradykinin. Administration of 80mg telmisartan in the human body can almost completely inhibit the increase in blood pressure caused by angiotensin II. The inhibitory effect lasts for 24 hours and can still be measured at 48 hours. The antihypertensive effect gradually becomes apparent within 3 hours after the first dose. The maximum antihypertensive effect can be achieved 4 weeks after the start of treatment and can be maintained over the long term. If the treatment is suddenly interrupted, the blood pressure gradually returns to the pre treatment level after a few days without the occurrence of rebound hypertension. In clinical trials that directly compared two types of hypertension drugs, the incidence of dry cough in patients in the treatment group was significantly lower than that in the angiotensin converting enzyme inhibitor treatment group.

inspect

chloride

Take 2.0g of this product, add 100mL of water, boil for 2 minutes, let cool, filter, take 25mL of the filtrate, and check according to the law. Compared with the control solution made of 5.0mL of standard sodium chloride solution, it should not be more concentrated (0.01%).

sulfate

Take 25mL of the filtrate under the chloride item and check according to the law. Compared with the control solution made from 1.0mL of standard potassium sulfate solution, it should not be more concentrated (0.02%).

Related substances

Take an appropriate amount of this product, add an appropriate amount of methanol and a 1mol/L sodium hydroxide solution of 100 μ Dissolve and dilute with methanol to produce a solution containing approximately 0.5mg per 1mL as the test sample solution; Accurately measure 1mL and place it in a 100mL volumetric flask. Dilute with methanol to the mark, shake well, and use it as the reference solution. According to the high-performance liquid chromatography method, octadecylsilane bonded silica gel is used as the filling agent; Using methanol as the mobile phase A and 0.1% potassium dihydrogen phosphate solution methanol (35:65, containing 0.2% triethylamine, adjusted to pH 5.0 with phosphoric acid) as the mobile phase B, perform linear elution according to the following table; The detection wavelength is 230nm; The flow rate is 1.0mL per minute (adjust the flow rate if necessary). Take appropriate amounts of telmisartan reference substance and 4 ‘- bromomethyl biphenyl-2-carboxylic acid methyl ester reference substance, dissolve them in methanol, and dilute them to obtain about 10% per 1mL each μ G mixed solution, take 10 μ Inject L into a liquid chromatograph to maintain the retention time of the telmisartan peak at 17-20 minutes; The tailing factor should not be greater than 2.0, and the resolution between the telmisartan peak and the 4 ‘- bromomethyl biphenyl-2-carboxylic acid methyl ester peak should meet the requirements. The number of theoretical plates should be calculated based on the telmisartan peak and not less than 5000. Take reference solution 20 μ Inject L into the liquid chromatograph, adjust the detection sensitivity to make the peak height of the main component chromatographic peak approximately 20% of the full scale, and then accurately measure 20% of the test solution and 20% of the reference solution μ Inject L into the liquid chromatograph separately and record the chromatogram. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.5 times (0.5%) of the main peak area of the reference solution, and the sum of the impurity peak areas shall not be greater than the main peak area of the reference solution (1.0%).

Residual solvents: methanol, ethyl acetate, ethanol, chlorobenzene, n-hexane, cyclohexane, tetrahydrofuran, dichloromethane, and dioxane

Take 0.2g of this product, weigh it accurately, place it in a top empty bottle, add 5mL of dimethylformamide precisely, seal it, and use it as the test solution; Take appropriate amounts of methanol, ethyl acetate, ethanol, chlorobenzene, n-hexane, cyclohexane, tetrahydrofuran, dichloromethane, and dioxane each, accurately weigh them, and dilute them quantitatively with dimethylformamide to produce a methanol content of 120% per 1mL μ g. Ethyl acetate 200 μ g. Ethanol 200 μ g. Chlorobenzene 14.4 μ g. N-hexane 11.6 μ g. Cyclohexane 155 μ g. Tetrahydrofuran 28.8 μ g. Dichloromethane 24.0 μ G and dioxane 15.2 μ Accurately measure 5mL of a mixed solution of g, place it in a top empty bottle, seal it, and use it as a reference solution. According to the residual solvent determination method (Appendix VIII, P, Second Method, Part II of the 2010 Pharmacopoeia), (5%) phenyl – (95%) methyl polysiloxane (or similar polarity) is used as the fixed solution, with an initial temperature of 50 ℃, maintained for 5 minutes, and heated at a rate of 10 ℃ per minute to 100 ℃, maintained for 5 minutes; The detector temperature is 250 ℃; The temperature of the injection port is 200 ℃. Headspace injection, the equilibrium temperature of the headspace bottle is 105 ℃, and the equilibrium time is 30 minutes. The injection volume is 1.0mL. Take the reference solution for headspace injection, record the chromatogram, and ensure that the resolution between each component peak meets the requirements. Take the test solution and the reference solution for headspace injection, record the chromatogram, and calculate the peak area using the external standard method, both of which should comply with the regulations.

Trichloromethane

Take 0.2g of this product, weigh it accurately, place it in a top empty bottle, add 5mL of dimethylformamide precisely, seal it, and use it as the test solution; Take an appropriate amount of trichloromethane and accurately weigh it. Dilute it quantitatively with dimethylformamide to make it contain 2.4 per 1mL μ Accurately measure 5mL of g solution, place it in a top empty bottle, seal it, and use it as a reference solution. According to the residual solvent determination method (Appendix VIII P, Second Method, 2010 Edition Pharmacopoeia Part II), the detector uses an electron capture detector (ECD), and other chromatographic and headspace conditions are the same as the residual solvent item. Take the test solution and the reference solution for headspace injection, record the chromatogram, and calculate the peak area using the external standard method, which should comply with regulations.

Dimethylformamide

Take 0.2g of this product, accurately weigh it, place it in a 10mL volumetric flask, add chloroform to dissolve and dilute to the mark, shake well, and use it as the test solution; Take an appropriate amount of dimethylformamide and accurately weigh it. Dilute it quantitatively with chloroform to produce approximately 17.6% per 1mL μ G solution is used as the reference solution. According to the residual solvent determination method, polyethylene glycol is used as the fixed solution, with a column temperature of 100 ℃, a detector temperature of 250 ℃, and a sample inlet temperature of 200 ℃. Accurately measure 1 sample solution and 1 reference solution respectively μ L. Inject the gas chromatograph separately and record the chromatogram. Calculated based on peak area using the external standard method, it should comply with regulations.