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2 English Reference3 Chlorpheniramine maleate Pharmacopoeia Standard 3.1 Name 3.1.1 Chinese Name
Chlorpheniramine maleate
3.1.2 Chinese PinyinMalaisuan Lübennamin
3.1.3 English NameChlorDhenamine Maleate
3.1.4 Chinese PinyinChlorpheniramine maleate
3.1.5 Chinese PinyinChlorDhenamine Maleate
3.2 Structural formula 3.3 Molecular formula and molecular weight
C16H19ClN2-C4H4O4 390.87
3.4 Source (name), content (potency)The product is 2[p-chloroalpha[2(dimethylamino)ethyl]phenyl]pyridine maleate. Calculated as dry product, containing C16H19ClN2-C4H4O4 shall not be less than 98.5%.
3.5 PropertiesThis product is white crystalline powder; odorless, bitter taste.
It is soluble in water or ethanol or trichloromethane, slightly soluble in ether.
3.5.1 Melting pointThe melting point of this product (2010 version of the Pharmacopoeia, Part II, Appendix VI C) is 131.5 ~ 135 ℃.
3.5.2 Absorption coefficientTake this product, weigh it precisely, add hydrochloric acid solution (dilute hydrochloric acid 1 ml and water to 100 ml) to dissolve and quantitatively dilute it to make a solution containing about 20 μg per 1 ml, and then measure the absorbance at 264 nm according to the UV-visible spectrophotometric method (2010 Pharmacopoeia, Appendix Ⅳ A), the absorption coefficient () is 212-222. （
3.6 Identification(1) Take about 10mg of this product, add 1ml of acetic anhydride citrate test solution, and heat it on a water bath, it will show reddish purple color.
(2) take about 20mg of the product, add 1ml of dilute sulfuric acid, drop potassium permanganate test solution, the red color disappears.
(3) The infrared light absorption pattern of this product should be consistent with the pattern of the control (Infrared Spectrum Collection of Drugs, Figure 61).
3.7 Check 3.7.1 AcidityTake 0.1g of this product, add 10ml of water to dissolve, according to the law to determine (2010 version of the Pharmacopoeia, Part II, Appendix VI H), the pH value should be 4.0-5.0.
3.7.2 Related substancesTake this product, add solvent (mobile phase A acetonitrile (80:20)] to dissolve and dilute to make a 1mg per 1ml solution. As a test solution; precise amount of appropriate amount, diluted with the above solvent to make a solution containing 3μg per 1ml, as a control solution. According to the high-performance liquid chromatography (2010 version of the Pharmacopoeia II Appendix V D) test, with octadecylsilane silica gel bonded silica gel as filler; mobile phase A for phosphate buffer (take ammonium dihydrogen phosphate 11.5g, add appropriate amount of water to make soluble, add phosphoric acid 1 ml, diluted with water to 1000 ml), the mobile phase B for the acetonitrile, according to the following table for the gradient elution; flow rate of 1.2 ml per minute; the detection wavelength is 225nm. The theoretical plate number was not less than 4000 according to the peak of chlorpheniramine. 10μl of the control solution was injected into the liquid chromatograph, and the detection sensitivity was adjusted so that the peak height of the peak of chlorpheniramine chromatogram was about 25% of the full scale. Then take 10 μl of each test solution and control solution, inject them into the liquid chromatograph and record the chromatogram. If there are impurity peaks in the chromatogram of the test solution, except for the maleic acid peak, the area of individual impurity peaks shall not be greater than the area of the chlorpheniramine peak in the control solution (0.3%), and the sum of the areas of the impurity peaks shall not be greater than 3 times the area of the chlorpheniramine peak in the control solution (0.9%). Chromatogram of the test solution is smaller than the control solution chlorpheniramine peak area of 0.17 times the chromatographic peak is ignored (0.05%).
? Time (min) ? Mobile phase A (%) ? Mobile phase B (%) ?0 ?90 ?10 ?25 ?75 ?25 ?40 ?60 ?40 ?45 ?90 ?10 ?50 ?90 ?10 3.7.3 Residual solventsTetrahydrofuran, dioxane, pyridine and toluene? Take this product, precision weighing, add dimethylformamide to dissolve and dilute to make a solution containing about 0.2 g per 1 ml, as a test solution; another take tetrahydrofuran, 1,4 dioxane, pyridine and toluene, precision weighing, quantitatively diluted in dimethylformamide to make a solution containing 144 μg of tetrahydrofuran, 76 μg of 1,4 dioxane, 40 μg of pyridine, toluene, 178 μg of toluene, as a solution of the control product. The solution was used as the control solution. Measure 1 ml of each of the test solution and the control solution precisely, place in a headspace bottle and seal. Determine the residual solvent according to the method of residual solvent determination (2010 version of Pharmacopoeia, Part II, Appendix VIII P, the second method), using 5% phenyl 95% methyl polysiloxane (or similar polarity) as the stationary liquid; the column temperature was maintained at 50 ℃ for 15 minutes, and then warmed up to 120 ℃ at a rate of 8 ℃ per minute, maintained for 10 minutes; the temperature of the inlet port was 200 ℃; the temperature of the detector was 250 ℃. The headspace vial equilibrium temperature was 90 ℃, equilibrium time was 30 minutes, the injection volume was 1.0 ml. Take the control solution headspace injection, the theoretical plate number according to the calculation of tetrahydrofuran peaks was not less than 5000, and the separation between the peaks of each component should meet the requirements. Then take the test solution and the control solution were headspace injection, record the chromatogram. According to the external standard method to peak area calculation, should meet the requirements.
3.7.4 Easily carbonizedTake 25mg of this product, according to the law check (2010 version of the Pharmacopoeia, Part II, Appendix VIII O), compared with the yellow No. 1 standard colorimetric solution, shall not be darker.
3.7.5 Loss of weight on dryingTake the product, dry at 105 ℃ to constant weight, weight loss should not be more than 0.5% (2010 version of the Pharmacopoeia Part II Appendix VIII L).
3.7.6 Residue from incinerationNot more than 0.1% (2010 version of the Pharmacopoeia II Appendix VIII N).
3.8 Determination of contentTake about 0.15g of this product, weigh it precisely, add 10ml of glacial acetic acid to dissolve it, add 1 drop of crystal violet indicator solution, titrate with perchloric acid titrant (0.1 mol/L) until the solution shows blue-green color, and correct the result of titration with a blank test. Each 1 ml of perchloric acid titrant (0.1 mol/L) is equivalent to 19.54 mg of C16H19ClN2-C4H4O4.
3.9 CategoryAntihistamines.
3.10 StorageShielded from light and kept sealed.
3.11 Preparation(1) Chlorpheniramine maleate tablets? (2) Chlorpheniramine maleate injection? (3) Chlorpheniramine Maleate Drops
3.12 VersionChinese People's **** and National Pharmacopoeia 2010 Edition
4 Instructions for Chlorpheniramine Maleate 4.1 Alias of Chlorpheniramine MaleateChlorpheniramine; Chlorpheniramine; Chlorpheniramine; Chlorfenamine; Chlorfenadine; Chlorfenadimeton; Malayanamine; Chlorpheniramine maleate; Chlorpheniramine Maleate: Tropinamin ,Paracetamol;Chlorfenadine; Chlorfenadimeton.
4.2 Foreign namesChlorpheniramine ,Cmeton
4.3 Indications for Chlorpheniramine maleateUsed for various allergic diseases, insect bites, allergic reactions to drugs. Used in conjunction with APC for the treatment of colds.
4.4 Dosage and Administration of Chlorpheniramine maleate1. Oral: Adults 4mg once, 3 times a day. Children 1 day 0.35mg / kg, divided into 3 ~ 4 times.
2. Intramuscular injection: 510mg/(times.d);
3. Intravenous injection: 10mg/(times.d).
4.5 Contraindications of Chlorpheniramine maleateProhibited in epilepsy patients, infants and nursing mothers, working at heights, machine operators.
4.6 Adverse effects of chlorpheniramine maleateSlight dry mouth, dizziness, nausea, drowsiness, palpitations or skin bruising, bleeding tendency, but they are rare.
4.7 Precautions1. Use with caution in patients with pyloric obstruction, prostatic hypertrophy, bladder obstruction, glaucoma, hyperthyroidism and hypertension.
2. Elderly patients are prone to dizziness, headache, hypotension, etc., so it should be used with caution.
3. Chlorpheniramine maleate can easily lead to central excitation and induce epilepsy, so epileptic patients should not use.
4.8 Drug interactionsChlorpheniramine maleate can deepen the central inhibitory effect when combined with sedatives, hypnotics and tranquilizers.
4.9 SpecificationsTablet: 4mg per tablet.