Tadalafil Oral Suspension

8/11/2019 Tadalafil Oral Suspension

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Tadalafil 5 mg/mL Oral Suspension

Loyd V. Allen, Jr., PhDProfessor Emeritus

College of Pharmacy, University of OklahomaOklahoma City, Oklahoma

5/22/2012US Pharm.2012;37(5):43-44.

Method o f Preparat ion: Calculate the quantity of each ingredient for theamount to be prepared. Accurately weigh or measure each ingredient.Thoroughly pulverize the required number of tadalafil tablets to a very fine

powder. Add a small quantity of Ora-Plus and mix to obtain a smooth,uniform suspension. Geometrically, add the remainder of the Ora-Plus andmix well. Add sufficient Ora-Sweet to volume and mix well. Package andlabel.

Use:Tadalafil oral suspension may be used to treat pulmonaryhypertension (PH) in patients who are unable to swallow the solid oraldosage form.

Packaging:Package in tight, light-resistant containers.

Label ing:Shake well before taking. Keep out of the reach of children.Discard after ____ [time period].

Stabi l i ty: A beyond-use date of 91 days may be used for this preparationwhen it is stored at room temperature. In the supporting stability study, amean of at least 99% of the initial concentration of tadalafil remainedthroughout the 91-day study period in all suspensions. The stability studyfound no detectable changes in color, odor, taste, or pH, and no visiblemicrobial growth was observed.

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Qual i ty Con trol :Quality-control assessment may include weight/volume,pH, specific gravity, active drug assay, color, rheologicproperties/pourability, physical observation, and physical stability(discoloration, foreign materials, gas formation, mold growth).

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Discussion:PHis hypertension in the pulmonary circuit. It may be primaryor secondary to pulmonary or cardiac disease (e.g., fibrosis of the lung,mitral stenosis). Pulmonary circulation is somewhat unique owing to thehigh blood flow, low pressure, and low resistance. Since this system candistend the blood vessels of the lung, it can accommodate large increasesin blood flow with only modest elevations in pressure. However, PH occurswhen the pulmonary artery pressure increases to a level inappropriate for agiven cardiac output. Once PH manifests, it is self-perpetuating and canintroduce secondary structural abnormalities in pulmonary vessels.

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Diagnosis of PH can include dyspnea, fatigue, chest pain, and syncopeupon exertion. A narrow splitting of the second heart sound with a loudpulmonary component may occur, in addition to right ventricularhypertrophy and cardiac failure in advanced disease. There may also beother diagnostic parameters. PH may be idiopathic (formerlyprimary) orsecondary. Treatment of idiopathic PH includes amlodipine, diltiazem,nifedipine, oxygen, sildenafil, tadalafil, bosentan, ambrisentan,epoprostenol, iloprost, beraprost, treprostinil, and diuretics. Therapy forsecondary PH consists primarily of treating the underlying disorder. Early

recognition of PH is crucial, as the self-perpetuating cycle responsible forrapid clinical progression must be interrupted.

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Tadalafil (Cialis, C22H19N3O4, MW 389.40), a selective phosphodiesterasetype 5 inhibitor, is a vasodilating agent. It occurs as a crystalline solid thatis practically insoluble in water and slightly soluble in ethanol. Commercially,tadalafil is available as 2.5-, 5-, 10-, and 20-mg almond-shaped, film-coatedtablets. Inactive ingredients include croscarmellose, sodium, hydroxypropylcellulose, hypromellose, iron oxide lactose monohydrate, magnesium

stearate, microcrystalline cellulose, sodium lauryl sulfate, talc, titaniumdioxide, and triacetin. The tablets should be stored at 25C, with excursionspermitted to 15C to 30C (USP controlled room temperature). Tadalafil isapproved to treat erectile dysfunction, but it also is effective in thetreatment of PH in adult and pediatric patients.

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Ora-Plus is an oral suspending vehicle that accepts dilution of up to 50% ormore with water, flavoring agents, or syrups while still retaining itssuspending properties. It has a pH of approximately 4.2 and an osmolalityof about 230 mOsm/kg. Ora-Plus is a thixotropic vehicle with a viscosity of

approximately 1,000 cps at 25C. It contains purified water, microcrystallinecellulose, sodium carboxymethylcellulose, xanthan gum, carrageenan,


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sodium phosphate, and citric acid as buffering agents, simethicone as anantifoaming agent, and potassium sorbate and methylparaben aspreservatives.

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Ora-Sweet syrup vehicle is a flavoring vehicle for oral extemporaneouspreparations. It is flavored with a citrus-berry flavor blend and containsglycerin and sorbitol to prevent cap lock, a problem associated with manysyrups. Ora-Sweet is buffered to a pH of approximately 4.2 and has anosmolality of about 3,240 mOsm/kg. Ora-Sweet contains purified water,sucrose, glycerin, sorbitol (5%), flavoring, sodium phosphate, and citric acidas buffering agents, and potassium sorbate and methylparaben aspreservatives.

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Tadalafil Oral Suspension