Formulation of a Novel Tianeptine Sodium Orodispersible Film

Abstract

The present investigation was undertaken with the objective of formulating orodispersible film(s) of the antidepressant drug tianeptine sodium to enhance the convenience and compliance by the elderly and pediatric patients. The novel film former, lycoat NG73 (granular hydroxypropyl starch), along with different film-forming agents (hydroxypropyl methyl cellulose, hydroxyethyl cellulose, and polyvinyl alcohol), in addition to three film modifiers; namely, maltodextrin, polyvinyl pyrrolidone K90 and lycoat RS780 (pregelatinized hydroxypropyl starch) were evaluated. Eight formulae were prepared by the solvent-casting method; and were evaluated for their in vitro dissolution characteristics, in vitro disintegration time, and their physico-mechanical properties. The promising orodispersible film based on lycoat NG73 (F1); showing the greatest drug dissolution, satisfactory in vitro disintegration time and physico-mechanical properties that are suitable for orodispersible films, was evaluated for its bioavailability compared with a reference marketed product (Stablon® tablets) in rabbits. Statistical analysis revealed no significant difference between the bioavailability parameters (C(max) (ng/ml), t(max) (h), AUC(0-t) (ng hml(-1)), and AUC(0-∞) (ng hml(-1))] of the test film (F1) and the reference product. The mean ratio values (test/reference) of C(max) (89.74%), AUC(0-t) (110.9%), and AUC(0-∞) (109.21%) indicated that the two formulae exhibited comparable plasma level-time profiles. These findings suggest that the fast orodispersible film containing tianeptine is likely to become one of choices for acute treatment of depression.

In vitro/in vivo evaluation of an optimized fast dissolving oral film containing olanzapine co-amorphous dispersion with selected carboxylic acids

“…Before film casting, the aqueous solution was sonicated for 1 h to ensure complete removal of the entrapped air bubbles. To cast the film, the aqueous solution was poured into a dry clean Teflon plate and then kept in hot air oven at 60 C for the first 30 min and then the temperature was decreased to 40 C for the next 24 h (El-Setouhy & El-Malak, 2010). After complete drying, the films were peeled off carefully from the Teflon plates, wrapped in aluminum foil, and stored in airtight containers at room temperature until further investigations.…”

“…Owing to pregastric or oro-mucosal absorption, drugs can directly enter systemic circulation avoiding first-pass metabolism thus improving bioavailability with possibility of reduced dosing and fewer side effects (Saurabh et al, 2011). Many studies on orodispersible polymer films have been conducted for various reasons; as enhancing solubility of poorly soluble BCS class II drugs, taste masking of antihistamines, or increasing patient compliance for administration of antidepressant drugs (El-Setouhy & El-Malak, 2010;Preis et al, 2012;Sievens-Figueroa et al, 2012). Optimized formulations of orodispersible polymer films were also studied in the literature using simple methodologies such as solvent casting, hot-melt extrusion, and freeze drying (ElMeshad & El Hagrasy, 2011;Low et al, 2013;Kumria et al, 2016;Shamma & Elkasabgy, 2016).…”

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“…Glycerin, dibutyl phthalate and polyethylene glycols are most often used as plasticizers. [26][27][28] Surface-active materials which can influence the API release time are used as solubilizers, wetting or dispersing agents. Dimethyl sulfoxide, benzalkonium chloride, sodium lauryl sulfate, etc., may be used for this purpose as well.…”

Formulation and Evaluation of Fast Dissolving Oral Films of Diazepam

“…The samples were filtered immediately and analyzed for the drug concentration and calculated the percentage (%) of drug dissolved or released. The release studies were performed on 3 films and mean values were taken [10][11][12].…”