Abstract
Objective: The aim of this study was to formulate and in vitro evaluate fast dissolving oral film of practically insoluble bromocriptine mesylate to enhance its solubility and to improve its oral bioavailability by avoiding first pass effect as well as to produce an immediate release action of the drug from the film for an efficient management of diabetes mellitus type II in addition to an improvement of the patient compliance to this patient-friendly dosage form.Methods: The films were prepared by the solvent casting method using hydroxypropyl methylcellulose of grades (E3, E5, E15), polyvinyl alcohol (PVA), pectin and gelatin as film-forming polymers in addition to polyethene glycol 400 (PEG400), propylene glycol (PG) and glycerin were used as a plasticizer. Poloxamer 407 was used as a surfactant, sodium saccharin as a sweetening agent, citric acid as a saliva stimulating agent, vanilla as a flavouring agent and crospovidone as a super disintegrant. The prepared films then tested for physical characterization, thickness, weight uniformity, mechanical characteristics (folding endurance, tensile strength, percent elongation and Young's modulus), surface pH, in vitro disintegration time, drug content and an in vitro drug release.Results: Films were found to be satisfactory when evaluated for physical characterization, thickness, weight uniformity, mechanical tests, in vitro disintegration time, folding endurance, drug content and an in vitro drug release. The surface pH of all the films was found to be neutral or minor change. Films in vitro drug release studies were also done using USP dissolution apparatus type II (paddle type). The in vitro drug release profile in the optimized formulation F14 was gave 86.8 % of drug released at 2 min. The optimized formulation F14 was also showed satisfactory pH (6.2±0.2), drug content (99.2±0.5%), the disintegration time of 9.2±0.1 seconds and the time needed for 80% of medication to be released (T80 %) was 1.35 minute.Conclusion: The bromocriptine mesylate fast dissolving oral film was formulated. The given film disintegrates within nine seconds which release the drug rapidly and gives an action.
Highlights
Among all routes of drug administration, the oral route is one of the most favored routes, as it is more convenient, cost-effective, and ease of administration lead to high level of patient compliance, but the problem associated with this route is the swallowing difficulty for pediatric and geriatric patients who have a fear of choking
Fast dissolving films allow the films to dissolve in the mouth, so the drug gets directly absorbed into the systemic circulation through the oral mucosa [3]
The time needed for 80 % of medication to be released (T80%) and percent medication dissolved in 2 min (% D2 min) from the formulated films (F2 and F3) are listed in the table (5). From all these results we found that the hydroxypropyl methylcellulose (HPMC) E5 had the best physical, mechanical properties and drug release profile than the other film forming polymers
Summary
Among all routes of drug administration, the oral route is one of the most favored routes, as it is more convenient, cost-effective, and ease of administration lead to high level of patient compliance, but the problem associated with this route is the swallowing difficulty for pediatric and geriatric patients who have a fear of choking. Drug delivery via the oral mucosa is a promising route when one wishes to achieve a rapid onset of action or an improved bioavailability for drugs which have a high first-pass metabolism. Fast dissolving films allow the films to dissolve in the mouth, so the drug gets directly absorbed into the systemic circulation through the oral mucosa [3]. Oral fast dissolving films (OFDFs) are the most advanced form of an oral solid dosage form. These are solid dosage forms, which disintegrate or dissolve within a minute when placed in the mouth without drinking water or chewing. OFDFs are prepared using hydrophilic polymers that rapidly dissolves in the oral cavity delivering the drug to the systemic circulation. Plasticizer helps to enhance the flexibility of the strip and reduces the brittleness of the strip [4]
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