Bisoprolol Fumarate and Hydrochlorothiazide Tablets
Revised: July 2003
Rx only
DESCRIPTION
Bisoprolol fumarate and hydrochlorothiazide is indicated for the treatment of hypertension. It combines two antihypertensive agents in a once-daily dosage: a synthetic beta1-selective (cardioselective) adrenoceptor blocking agent (bisoprolol fumarate) and a benzothiadiazine diuretic (hydrochlorothiazide).
Bisoprolol fumarate is chemically described as (±)-1-[4-[[-2-(1-methylethoxy)ethoxy]methyl] phenoxy]-3-[(1-methylethyl)amino]-2-propanol (E) -2-butenedioate (2:1) (salt). It possesses an asymmetric carbon atom in its structure and is provided as a racemic mixture. The S(-) enantiomer is responsible for most of the beta-blocking activity. Its molecular formula is (C18H31NO4)2•C4H4O4 and it has a molecular weight of 766.97. Its structural formula is:
Bisoprolol fumarate is a white crystalline powder, approximately equally hydrophilic and lipophilic, and readily soluble in water, methanol, ethanol, and chloroform.
Hydrochlorothiazide USP (HCTZ) is 6-Chloro-3,4-dihydro-2 H -1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide. It is a white, or practically white, practically odorless crystalline powder. It is slightly soluble in water, sparingly soluble in dilute sodiumum hydroxide solution, freely soluble in n-butylamine and dimethylformamide, sparingly soluble in methanol, and insoluble in ether, chloroform, and dilute mineral acids. Its molecular formula is C7H8CIN3O4S2 and it has a molecular weight of 297.73. Its structural formula is:
Each tablet, for oral administration contains 2.5 mg bisoprolol fumarate and 6.25 mg hydrochlorothiazide, 5 mg bisoprolol fumarate and 6.25 mg hydrochlorothiazide, or 10 mg bisoprolol fumarate and 6.25 mg hydrochlorothiazide. In addition, each tablet contains the following inactive ingredients: colloidal silicone dioxide, dibasic calcium phosphate, magnesium stearate, microcrystalline cellulose, and pregelatinized starch. The film-coating contains the following ingredients: hypromellose, lactose monohydrate (2.5 mg/6.25 mg and 5 mg/6.25 mg only), polyethylene glycol (10 mg/6.25 mg only), polydextrose (10 mg/6.25 mg only), purified stearic acid (5 mg/6.25 mg only), synthetic red iron oxide (5 mg/6.25 mg only), synthetic yellow iron oxide (2.5 mg/6.25 mg and 5 mg/6.25 mg only), titanium dioxide, and triacetin.
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