Biomaterial Database

Formulation and optimization of duloxetine hydrochloride buccal films: in vitro and in vivo evaluation. 2017

Amr Mostafa El Sharawy, and Marwa Hassan Shukr, and Ahmed Hassen Elshafeey

a National Organization for Drug Control and Research (NODCAR) , Cairo , Egypt.

Duloxetine hydrochloride (DH) is a serotonin-norepinephrine reuptake inhibitor (SSNRI) indicated for the treatment of depression. Duloxetine suffers from reduced oral bioavailability (≈50%) due to hepatic metabolism. This study aims to develop DH buccoadhesive films to improve its bioavailability. DH buccoadhesive films were prepared adopting the solvent casting method using hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA). The prepared films were evaluated for weight uniformity, drug content, surface pH, swelling index, mucoadhesion strength and drug release percentages. Accelerated stability and bioavailability studies in healthy human volunteers were also performed for the selected films. Results of the evaluation tests showed that the optimum physicochemical characters were obtained by the films prepared with 2% HPMC using 10% propylene glycol (F2 films). Accelerated stability studies revealed that DH showed proved stability throughout the experiment time. DH bioavailability from F2 films was determined and compared with that of the marketed oral capsules (Cymbalta® 30 mg). The pharmacokinetic results showed that Cmax for F2 was higher than the market product. In addition, ANOVA analysis showed that a Tmax of F2 film was significantly lower, while, the AUC0-72 of F2 was significantly higher than that of Cymbalta capsules. The percentage relative bioavailability of DH from F2 was found to be 296.39%. Therefore, the prepared buccal films offer an alternative route for the administration of DH with the possibility of improving its bioavailability.

UI	MeSH Term	Description	Entries
D009061	Mouth Mucosa	Lining of the ORAL CAVITY, including mucosa on the GUMS; the PALATE; the LIP; the CHEEK; floor of the mouth; and other structures. The mucosa is generally a nonkeratinized stratified squamous EPITHELIUM covering muscle, bone, or glands but can show varying degree of keratinization at specific locations.	Buccal Mucosa,Oral Mucosa,Mucosa, Mouth,Mucosa, Oral
D011142	Polyvinyl Alcohol	A polymer prepared from polyvinyl acetates by replacement of the acetate groups with hydroxyl groups. It is used as a pharmaceutic aid and ophthalmic lubricant as well as in the manufacture of surface coatings artificial sponges, cosmetics, and other products.	Liquifilm Tears,Polyviol,Alcohol, Polyvinyl,Tears, Liquifilm
D002626	Chemistry, Pharmaceutical	Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use.	Medicinal Chemistry,Chemistry, Pharmaceutic,Pharmaceutic Chemistry,Pharmaceutical Chemistry,Chemistry, Medicinal
D002645	Chickens	Common name for the species Gallus gallus, the domestic fowl, in the family Phasianidae, order GALLIFORMES. It is descended from the red jungle fowl of SOUTHEAST ASIA.	Gallus gallus,Gallus domesticus,Gallus gallus domesticus,Chicken
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000068736	Duloxetine Hydrochloride	A thiophene derivative and selective NEUROTRANSMITTER UPTAKE INHIBITOR for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC, and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA.	Cymbalta,Duloxetine,Duloxetine Ethanedioate (1:1), (+-)-isomer - T353987,Duloxetine HCl,Duloxetine, (+)-isomer,LY 227942,LY 248686,LY-227942,LY-248686,LY227942,N-methyl-3-(1-naphthalenyloxy)-2-thiophenepropanamine,N-methyl-3-(1-naphthalenyloxy)-3-(2-thiophene)propanamide,HCl, Duloxetine,Hydrochloride, Duloxetine,LY248686
D000268	Adhesiveness	A property of the surface of an object that makes it stick to another surface.	Adhesivenesses
D000278	Administration, Buccal	Administration of a soluble dosage form between the cheek and gingiva. It may involve direct application of a drug onto the buccal mucosa, as by painting or spraying.	Buccal Drug Administration,Drug Administration, Buccal,Buccal Administration,Administration, Buccal Drug,Administrations, Buccal,Administrations, Buccal Drug,Buccal Administrations,Buccal Drug Administrations,Drug Administrations, Buccal
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
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