Tetracycline HCl 2.2-mg mL Topical Solution.pdf
1
224 International Journal of Pharmaceutical Compounding Vol. 7 No. 3 May/June 2003 METHOD OF PREPARATION 1. Calculate the required quantity of each ingredient for the total amount to be prepared. 2. Accurately weigh and/or measure each ingredient. 3. Dissolve the sodium bisulfite, citric acid and tetracycline hydrochloride in 50 mL purified water. 4. Add the ethyl alcohol and mix well. 5. Add a sufficient quantity of purified water to bring to a volume of 100 mL and mix well. 6. Package and label. PACKAGING Package in a tight, light-resistant glass container. LABELING Shake well. For external use only. Keep out of reach of chil- dren. Use only as directed. STABILITY When this preparation is stored at room temperature, a beyond-use date of 2 months (commercial product was 2 months) can be used. 1 USE Tetracycline topical solution is used in the treatment of mild, papular acne of puberty and early adolescence (acne vulgaris) and papular-pustular acne in adult women. The safety and effi- cacy of topical tetracycline in children younger than 11 years of age have not been established. 1 QUALITY CONTROL Quality-control assessment can include weight and/or vol- ume, pH, active-drug assay, color, physical observation, and physical stability (discoloration, foreign materials, gas forma- tion, and mold growth). 2 DISCUSSION Tetracycline hydrochloride (C 22 H 24 N 2 O 8 , MW 444.4) occurs as a yellow, crystalline, moderately hygroscopic powder. It is solu- ble in water (100 mg/mL) and in solutions of alkali hydroxides and carbonates. It is slightly soluble in alcohol (10 mg/mL). It is stable in air, but exposure to strong sunlight in moist air causes it to darken. In solution at a pH of less than about 2, it loses potency; and it is also rapidly destroyed by alkali hydrox- ide solutions. The pH of a 10-mg/mL solution is between 1.8 and 2.8. The hydrochloride salt form is more soluble than the tetracycline base and is used for parenteral and topical administration. Tetracyclines are broad-spectrum antibiotics and are active against many gram-negative, gram-positive, and other bacteria; but they are ineffective against fungi and viruses. 3 Sodium bisulfite (NaHSO 3 , MW 104.07, sodium hydrogen sul- fite) occurs as a white crystalline powder. It is soluble 1 in 3.5 parts of water and in 70 parts of 95% alcohol. 4 Alcohol (C 2 H 5 OH, MW 46.07, ethyl alcohol, ethanol, grain al- cohol) is a clear, colorless, mobile, volatile liquid with a slight characteristic odor and a burning taste. It is miscible with chloroform, with glycerin, and with water; and its solutions may be sterilized by autoclaving or filtration. 5 Citric acid (C 6 H 8 O 7 •H 2 O, citric acid monohydrate) occurs as colorless or translucent crystals or as white, crystalline, efflo- rescent powder that is odorless and has a strong, tart, acidic taste. The hydrated form of citric acid may contain up to 8.8% water, and the pH of a 1% w/v aqueous solution is about 2.2. Depending on the degree of humidity in the air, the hy- drated form of citric acid effloresces; and the anhydrous form is hygroscopic. If stored in air that is too dry, citric acid may lose its water if the temperature reaches about 40ºC. The melting point of citric acid is about 100ºC, but it softens at about 75ºC. One gram is soluble in less than 1 mL of water and in 1.5 mL of ethanol. 6 Purified water is a clear, colorless, odorless, and tasteless liquid water that is obtained by distillation, ion exchange, reverse os- mosis, or some other suitable process. Water has a specific gravity of 0.9971 at room temperature and a melting point at 0°C. It is miscible with most polar solvents and is chemically stable in all physical states (ice, liquid, and steam). 7 References 1. Ashworth LD. Medications discontinued in the United States. IJPC 2002;4:286-287. 2. Allen LV Jr. Standard operating procedure for performing physical quality assessment of oral and topical liquids. IJPC 1999;3:146-147. 3. Parfitt K, ed. MARTINDALE: The Extra Pharmacopoeia. 32nd ed. London:The Pharmaceutical Press; 1999:259-262. 4. Stewart JT. Sodium metabisulfite. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharma- ceutical Association; 2000:490-492. 5. Weller PJ. Alcohol. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharmaceutical Associa- tion; 2000:7-9. 6. Amidon GE. Citric acid monohydrate. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharma- ceutical Association; 2000:140-142. 7. Ellison A, Nash RA, Wilkin MJ. Water. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharma- ceutical Association; 2000:580-584. For 100 mL Tetracycline hydrochloride 220 mg Sodium bisulfite 100 mg Ethyl alcohol, 95% 45 mL Citric acid powder 150 mg Purified Water USP qs 100 mL Tetracycline Hydrochloride 2.2-mg/mL Topical Solution F O R M U L A T I O N S Rx
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Transcript of Tetracycline HCl 2.2-mg mL Topical Solution.pdf
224 International Journal of Pharmaceutical CompoundingVol. 7 No. 3 May/June 2003
METHOD OF PREPARATION 1. Calculate the required quantity of each ingredient for the
total amount to be prepared.2. Accurately weigh and/or measure each ingredient.3. Dissolve the sodium bisulfite, citric acid and tetracycline
hydrochloride in 50 mL purified water.4. Add the ethyl alcohol and mix well.5. Add a sufficient quantity of purified water to bring to a
volume of 100 mL and mix well.6. Package and label.
PACKAGING Package in a tight, light-resistant glass container.
LABELING Shake well. For external use only. Keep out of reach of chil-
dren. Use only as directed.
STABILITY When this preparation is stored at room temperature, a
beyond-use date of 2 months (commercial product was 2months) can be used.1
USE Tetracycline topical solution is used in the treatment of mild,
papular acne of puberty and early adolescence (acne vulgaris)and papular-pustular acne in adult women. The safety and effi-cacy of topical tetracycline in children younger than 11 yearsof age have not been established.1
QUALITY CONTROL Quality-control assessment can include weight and/or vol-
ume, pH, active-drug assay, color, physical observation, andphysical stability (discoloration, foreign materials, gas forma-tion, and mold growth).2
DISCUSSION Tetracycline hydrochloride (C22H24N2O8, MW 444.4) occurs as ayellow, crystalline, moderately hygroscopic powder. It is solu-ble in water (100 mg/mL) and in solutions of alkali hydroxidesand carbonates. It is slightly soluble in alcohol (10 mg/mL). Itis stable in air, but exposure to strong sunlight in moist aircauses it to darken. In solution at a pH of less than about 2, itloses potency; and it is also rapidly destroyed by alkali hydrox-ide solutions. The pH of a 10-mg/mL solution is between 1.8and 2.8. The hydrochloride salt form is more soluble than the tetracycline base and is used for parenteral and topical
administration. Tetracyclines are broad-spectrum antibioticsand are active against many gram-negative, gram-positive, and other bacteria; but they are ineffective against fungi and viruses.3
Sodium bisulfite (NaHSO3, MW 104.07, sodium hydrogen sul-fite) occurs as a white crystalline powder. It is soluble 1 in 3.5parts of water and in 70 parts of 95% alcohol.4
Alcohol (C2H5OH, MW 46.07, ethyl alcohol, ethanol, grain al-cohol) is a clear, colorless, mobile, volatile liquid with a slightcharacteristic odor and a burning taste. It is miscible withchloroform, with glycerin, and with water; and its solutionsmay be sterilized by autoclaving or filtration.5
Citric acid (C6H8O7•H2O, citric acid monohydrate) occurs ascolorless or translucent crystals or as white, crystalline, efflo-rescent powder that is odorless and has a strong, tart, acidictaste. The hydrated form of citric acid may contain up to 8.8% water, and the pH of a 1% w/v aqueous solution is about2.2. Depending on the degree of humidity in the air, the hy-drated form of citric acid effloresces; and the anhydrous formis hygroscopic. If stored in air that is too dry, citric acid maylose its water if the temperature reaches about 40ºC. Themelting point of citric acid is about 100ºC, but it softens atabout 75ºC. One gram is soluble in less than 1 mL of waterand in 1.5 mL of ethanol.6
Purified water is a clear, colorless, odorless, and tasteless liquidwater that is obtained by distillation, ion exchange, reverse os-mosis, or some other suitable process. Water has a specificgravity of 0.9971 at room temperature and a melting point at0°C. It is miscible with most polar solvents and is chemicallystable in all physical states (ice, liquid, and steam).7
References1. Ashworth LD. Medications discontinued in the United States. IJPC
2002;4:286-287.2. Allen LV Jr. Standard operating procedure for performing physical
quality assessment of oral and topical liquids. IJPC 1999;3:146-147.3. Parfitt K, ed. MARTINDALE: The Extra Pharmacopoeia. 32nd ed.
London:The Pharmaceutical Press; 1999:259-262.4. Stewart JT. Sodium metabisulfite. In: Kibbe AH, ed. Handbook of
Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharma-ceutical Association; 2000:490-492.
5. Weller PJ. Alcohol. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharmaceutical Associa-tion; 2000:7-9.
6. Amidon GE. Citric acid monohydrate. In: Kibbe AH, ed. Handbook ofPharmaceutical Excipients. 3rd ed. Washington, DC:American Pharma-ceutical Association; 2000:140-142.
7. Ellison A, Nash RA, Wilkin MJ. Water. In: Kibbe AH, ed. Handbook ofPharmaceutical Excipients. 3rd ed. Washington, DC:American Pharma-ceutical Association; 2000:580-584.
For 100 mLTetracycline hydrochloride 220 mgSodium bisulfite 100 mgEthyl alcohol, 95% 45 mLCitric acid powder 150 mgPurified Water USP qs 100 mL
Tetracycline Hydrochloride 2.2-mg/mL Topical Solution
F O R M U L A T I O N S
Rx
