METHOD OF PREPARATION
Note: It is necessary to determine the quantity of lactose, needed as a filler, using one of the methods described in the International Journal of Pharmaceutical Compounding.1-3
1. Calculate the required quantity of each ingredient for the total amount to be prepared.
2. Accurately weigh and/or measure each ingredient.
3. Confirm that the particle-size range for both powders is approximately the same. If it is not the same, reduce the particle size of the powders until it is approximately the same for both.
4. Geometrically, incorporate the triprolidine hydrochloride into the lactose and mix well.
5. Encapsulate into the required number of size no. 1 gelatin capsules.
6. Package and label.
Package in tight, light-resistant containers.
Keep out of reach of children. Use only as directed. May cause drowsiness.
A beyond-use date of 6 months can be used for this preparation.4
Triprolidine hydrochloride has been used to provide symptomatic relief of allergic symptoms caused by histamine release.5
Quality-control assessment can include weight-overall average weight, weight-individual weight variation, dissolution of capsule shell, disintegration of capsule content, active-drug assay results, physical appearance (color, uniformity, extent of fill, determination of locked status) and physical stability (discoloration, changes).6
Triprolidine hydrochloride (C^sub 19^H^sub 22^N^sub 2*^HCl^sub *^H^sub 2^O, MW 332.87) occurs as a white, crystalline powder with no more than a slight, but unpleasant, odor. It is soluble in water (approximately 476 mg/mL) and alcohol (556 mg/mL). Its solutions are alkaline to litmus, and it melts at about 115°C.4
Triprolidine hydrochloride is a propylamine-derivative, first-generation antihistamine used to provide symptomatic relief of allergic symptoms caused by histamine release. It is generally used in adults at a dose of 2.5 mg every 4 to 6 hours, not exceeding 10 mg in 24 hours. It was formerly available under the brand name of Actidil (Burroughs Wellcome Co., Research Triangle Park, North Carolina) in 2.5-mg tablets. It should be stored in tight, light-resistant containers at room temperature in a dry place. Freezing of oral solutions of triprolidine hydrochloride should be avoided. It is still commercially available in fixed combination, as Actifed Cold & Allergy, with pseudoephedrine (triprolidine hydrochloride 2.5 mg and pseudoephedrine hydrochloride 60-mg tablets). The formulation presented here can be used in patients for whom a decongestant ingredient is not required.
Lactose (milk sugar, saccharum lactis) is available either anhydrous (C^sub 12^H^sub 22^O^sub 11^, MW 342.30) or as the monohydrate (C^sub 12^H^sub 22^O^sub 11*^H^sub 2^O, MW 360.31). Commercially, it is available as anhydrous [alpha]-lactose, [alpha]-lactose monohydrate and anhydrous [beta]-lactose; it is available in different grades and different particle characteristics. It is widely used as a diluent in numerous dosage forms and in lyophilized products and infant formulas. It is soluble in water to the extent of about 1 g in 4.63 mL but is practically insoluble in ethanol. A 9.75% solution is isoosmotic with serum. If it is stored under conditions of greater than 80% humidity, mold growth may occur. Lactose will exhibit a Maillard-type reaction (a brownish discoloration) when heated with compounds containing a primary amine group. This reaction occurs more rapidly under alkaline conditions. Lactose is listed as incompatible with ainino acids, aminophylline and amphetamines (due to the amine groups present).7
1. Allen LV Jr. Compounding powder-filled capsules. IJPC 1999;3:209-215.
2. Glasnapp A, Hua YT. Making capsules using a solid oral dosage form of a different strength. IJPC 1998;2:240.
3. Allen LV Jr. Standard operating procedure: Developing a capsule formulation. IJPC 2001;5:392-393.
4. US Pharmacopeial Convention, Inc. United States Pharmacopeia 26-National Formulary 21. Rockville, MD:US Pharmacopeial Convention, Inc.; 2003:1897, 2197-2201, 2585.
5. McEvoy GK. AHFS Drug Information-2003. Bethesda, MD:American Society of Health-System Pharmacists; 2003:43.
6. Allen Jr LV. Standard operating procedure for performing physical quality assessment of powder-filled, hard-gelatin capsules. IJPC 1999;3:232-233.
7. Kibbe AH, Weller PJ. Lactose. In: Rowe RC, Sheskey PJ, Weller PJ, eds. Handbook of Pharmaceutical Excipients. 4th ed. London:Pharmaceutical Press; 2003:323-332.
Copyright International Journal of Pharmaceutical Compounding Nov/Dec 2003
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