Patient-friendly extemporaneous formulation of bisoprolol: application to stability and bioavailability studies. 2023

Soha M El-Masry, and Sally A Helmy, and Soha A M Helmy, and Eman A Mazyed
Department of Pharmaceutics, Faculty of Pharmacy, Damanhour University, Damanhour, Egypt.

Community and hospital pharmacists always face the challenge to prepare oral liquid extemporaneous formulations to fit the needs of a specific patient population when commercial forms or the required strength is unavailable. This study was performed to prepare a stable patient-friendly oral liquid extemporaneous formulation of bisoprolol. Eight different extemporaneous formulations were prepared using various suspending agent(s). The in vitro dissolution of all extemporaneous formulations was examined. A comprehensive accelerated stability study was carried out to evaluate the adequate beyond-use date of the most optimized extemporaneous formulation. A validated ultra-performance liquid chromatography method was used for the analysis and quantification of bisoprolol in the accelerated stability and bioavailability studies. A group of eight healthy volunteers was enrolled in a two-way cross-over experimental design to study the bioavailability of the most optimized extemporaneous formulation. The pharmacokinetic parameters of bisoprolol were estimated. Extemporaneous suspension containing 0.5% w/v xanthan gum was easily prepared with a simple, natural, safe, sugar-free excipients. It achieved the best dissolution behavior among other extemporaneous suspensions. It was an easily pourable viscous suspension with no sedimentation. At least 98% of the initial concentration of bisoprolol remained throughout the 6-month study period in the selected suspension regardless of the storage conditions. There was no perceptible change in color, odor, or taste, and no noticeable microbial growth was observed in any sample. The selected formulation was bioequivalent to the commercial tablet in terms of the rate and extent of absorption. This research may be of great help during development of appropriate extemporaneous formulation of bisoprolol fumarate. The simple preparation method could be utilized to draw up a standard operating procedure (SOP) easy to use by different types of pharmacy settings.

UI MeSH Term Description Entries
D004339 Drug Compounding The preparation, mixing, and assembly of a drug. (From Remington, The Science and Practice of Pharmacy, 19th ed, p1814). Drug Formulation,Drug Preparation,Drug Microencapsulation,Pharmaceutical Formulation,Compounding, Drug,Formulation, Drug,Formulation, Pharmaceutical,Microencapsulation, Drug,Preparation, Drug
D004355 Drug Stability The chemical and physical integrity of a pharmaceutical product. Drug Shelf Life,Drugs Shelf Lives,Shelf Life, Drugs,Drug Stabilities,Drugs Shelf Life,Drugs Shelf Live,Life, Drugs Shelf,Shelf Life, Drug,Shelf Live, Drugs,Shelf Lives, Drugs
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D013535 Suspensions Colloids with liquid continuous phase and solid dispersed phase; the term is used loosely also for solid-in-gas (AEROSOLS) and other colloidal systems; water-insoluble drugs may be given as suspensions. Suspension
D013607 Tablets Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed) Tablet
D013810 Therapeutic Equivalency The relative equivalency in the efficacy of different modes of treatment of a disease, most often used to compare the efficacy of different pharmaceuticals to treat a given disease. Bioequivalence,Clinical Equivalency,Equivalency, Therapeutic,Generic Equivalency,Clinical Equivalencies,Equivalencies, Clinical,Equivalencies, Therapeutic,Equivalency, Clinical,Therapeutic Equivalencies,Bioequivalences,Equivalencies, Generic,Equivalency, Generic,Generic Equivalencies
D017298 Bisoprolol A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS. Bisoprolol Fumarate,Bisoprolol Fumarate (1:1) Salt, (+-)-Isomer,Bisoprolol Fumarate (2:1) Salt, (+-)-Isomer,Bisoprolol Hydrochloride,Bisoprolol Methanesulfonate Salt,Bisoprolol, (+-)-Isomer,Bisoprolol, (-)-Isomer,Bisoprolol, Fumarate (1:1) Salt,Bisoprolol, Fumarate (2:1) Salt,CL-297939,Concor,EMD-33512,CL 297939,CL297939,EMD 33512,EMD33512,Fumarate, Bisoprolol,Hydrochloride, Bisoprolol

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