What Is Miconazole Nitrate?

Miconazole nitrate is an antifungal. This product can inhibit the growth of most fungi at a concentration of 4mg / L. Bacteroides and Histoplasma are highly sensitive to it, and Cryptococcus, Candida, and Coccus sp Can interfere with the activity of cytochrome P-450, thereby inhibiting the biosynthesis of sterols, the major sterols in fungal cell membranes, damaging the fungal cell membrane and changing its permeability, leading to the leakage of important intracellular materials; it can also inhibit fungi The biosynthesis of triacylglycerol and phospholipids inhibits the activities of oxidases and peroxidases, causing the accumulation of hydrogen peroxide in cells, leading to cell sub-microstructure degeneration and cell necrosis. Candida albicans can inhibit its transformation from spores to invasive hyphae.

Miconazole nitrate

Miconazole nitrate is an antifungal. This product can inhibit the growth of most fungi at a concentration of 4mg / L, and the sporophyte and histoplasma are highly sensitive to it.

Phonetic name: Xiaosuan Mikangzuo

English name: Miconazole Nitrate

Alias: miconazole nitrate / meconazole / mycoconazole / miconazole / diclobenzimidazole / daconin

Molecular formula: C18H15CI4N3O4 Molecular weight: 479.15 CAS: 22832-87-7

The product is white or off-white crystalline or crystalline powder; odorless or almost odorless. This product is slightly soluble in methanol.

(1) The infrared absorption spectrum of this product should be consistent with the control spectrum (spectrum set 474).

(2) Take this product, add methanol-0.1mol / L hydrochloric acid solution (9: 1) to make a solution containing 0.4mg per 1ml, and measure it by spectrophotometry (Appendix IV A). Maximum absorption at wavelength.

(3) Take about 3mg of this product, add 1 drop of diphenylamine test solution, it should be dark blue.

(4) Take about 20mg of this product and perform organic destruction according to the oxygen bottle combustion method (Appendix C). Use 5ml sodium hydroxide solution 5ml as the absorption liquid. After the combustion is completed, shake it vigorously. After the absorption is complete, add water. 15ml, after adding dilute nitric acid to make it acidic, the solution showed a chloride identification reaction (Appendix III).

Take this product, add chloroform-methanol (1: 1) to make a solution containing 10mg per 1ml as the test solution; accurately measure the appropriate amount of this solution, add chloroform-methanol (1: 1) and dilute to 1ml A 25 g solution was used as a control solution. According to the thin layer chromatography (Appendix V B) test, draw 50 l of each of the above solutions, point them on the same silica gel G thin layer plate, and use n-hexane-chloroform-methanol (54:28:18) as the developing agent. Put a small beaker containing 5ml of concentrated ammonia solution in the tank, unfold it, dry it, and put color in iodine vapor. The spots of the test solution, such as spots of impurities, must not be deeper than the spots of the control solution.

Take the product after losing weight and dry it at 105 to constant weight. The weight loss should not exceed 0.5% (Appendix L).

The ignition residue shall not exceed 0.2% (Appendix N).

Take about 0.25g of this product, accurately weigh it, add 35ml of glacial acetic acid-acetic anhydride (1: 1), dissolve it, and titrate with potentiometric titration solution (0.1mol / L) according to potentiometric titration method (Appendix A) And use the results of the titration

Method name: Miconazole Nitrate-Determination of Miconazole Nitrate-Potentiometric Titration

Application range: This method uses potentiometric titration to determine the content of miconazole nitrate (C18H14Cl4N2O · HNO3).

This method is suitable for the determination of miconazole nitrate.

Principle of the method: The test sample is accurately weighed, dissolved in glacial acetic acid-acetic anhydride (1: 1), and titrated with perchloric acid according to the potentiometric titration method. The titration results were corrected by a blank test. Each 1 mL of perchloric acid titration solution (0.1 mol / L) was equivalent to 47.92 mg of C18H14Cl4N2O · HNO3.

Reagent: 1. Water (newly boiled to room temperature)

2. Glacial acetic acid

Acetic anhydride

4. Perchloric acid titration solution (0.1mol / L)

5. Reference potassium hydrogen phthalate

6. Water glacial acetic acid

7. Crystal violet indicator liquid

equipment:

Sample preparation: 1. Chloric acid titration solution (0.1mol / L)

Preparation: Take 750mL of anhydrous glacial acetic acid (calculated with water content, add 5.22mL of acetic anhydride per 1g of water), add 8.5mL of perchloric acid (70 ~ 72%), shake well, let cool, add an appropriate amount of anhydrous glacial acetic acid 1000mL, shake well and leave for 24 hours. If the test sample is easily acetylated, the water content of the solution must be determined by the moisture measurement method, and then the water content of the solution is adjusted to 0.01% ~ 0.2% with water and acetic anhydride.

Calibration: Take about 0.16g of standard potassium hydrogen phthalate dried to constant weight at 105 , accurately weigh, add 20mL of anhydrous glacial acetic acid to dissolve, add 1 drop of crystal violet indicator solution, and slowly titrate with this solution to Blue, and the titration results are corrected with a blank test. Each 1mL of perchloric acid titration solution (0.1mol / L) is equivalent to 20.42mg of potassium hydrogen phthalate. Calculate the concentration of this solution based on the consumption of this solution and the amount of potassium hydrogen phthalate taken.

2. Crystal violet indicator liquid

Take 0.5 g of crystal violet and add 100 mL of glacial acetic acid to dissolve.

Storage: Place in a brown glass bottle and keep tightly closed.

Operation steps: Take 0.25g of this product, weigh it accurately, add 35mL of glacial acetic acid-acetic anhydride (1: 1), dissolve it, and titrate with perchloric acid titration solution (0.1mol / L) according to potentiometric titration. The titration results were corrected by a blank test. Each 1 mL of perchloric acid titration solution (0.1 mol / L) was equivalent to 47.92 mg of C18H14Cl4N2O · HNO3.

Note 1: "Precise weighing" means that the weighed weight should be accurate to one thousandth of the weighed weight. "Precision weighing" means that the accuracy of the measured volume should conform to the national standard for the volume of the pipette. Precision requirements.

Note 2: "Determination of moisture" uses the drying method, taking 2 to 5 g of the test sample, and spreading it in a flat weighing bottle that is dry to constant weight, the thickness does not exceed 5 mm, and the loose test sample does not exceed 10 mm. Open the bottle cap and dry at 100 ~ 105 ° C for 5 hours. Place the cap on the dryer, cool it for 30 minutes, and weigh it precisely. Then dry it at the above temperature for 1 hour, cool, and weigh until two times in a row. The difference in weighing does not exceed 5 mg. Calculate the moisture content (%) in the test product based on the weight lost.

References: Pharmacopoeia of the People's Republic of China, edited by the National Pharmacopoeia Committee, Chemical Industry Press, 2005 Edition Two, p.711-712.

Shaded and sealed.

(1)

1. Intravenous administration: For the treatment of deep mycosis 1, the daily dosage is 600-1800mg (10-30mg per kilogram of body weight), and it is given in 3 times. For the treatment of blastomycosis, 200 to 1200 mg per day (course of treatment 2 to 16 weeks); for the treatment of albicans, 600 to 1800 mg per day (course of treatment 1 to 20 weeks); for the treatment of cryptococcosis, 1200 to 2400 mg per day (3 to 12 weeks of treatment); for the treatment of coccidioidosis, 1800 to 3600 mg per day (3 to 20 weeks of treatment). When starting treatment, a small dose (200 mg) can be given first and then the dosage can be increased according to the patient's tolerance. Caution should be used when using large doses. One dose is diluted with isotonic saline or 5% glucose injection, and the drip time is controlled for 30 to 60 minutes.

2. Topical administration: It is often used as a supplement to systemic administration. The reference amount is as follows: Bladder perfusion: 200mg once a day, 2 to 4 times a day. The injection is diluted. Sinus perfusion: 200mg once, twice a day, directly with injection (not diluted). Tracheal instillation: 100 mg once, 4 to 8 times a day. The injection can be diluted with 3 times the amount of isotonic saline and then instilled or sprayed. Infected wounds: lavage 1 or 2 times a day, and take appropriate injection after dilution. Intrathecal injection: 20mg once (injection 2ml, not diluted), for 3 to 7 consecutive days. Vaginal insertion: 1 suppository per night, inserted deep into the vagina, usually for 10 days.