Abstract

Objective: Saxagliptin is an orally anti-diabetic drug. It has an oral bioavailability of 50% due to first pass hepatic metabolism. To achieve sustained action of drug, reduce dosing frequency, bypass the hepatic first pass effect and improve bioavailability, buccal films formulation was planned.
 Methods: Compatibility of the drug with the excipients was studied with the help of FTIR. 23 factorial design was planned using concentration of Sodium alginate, concentration of Chitosan and PEG 400. Solvent casting method was used for the fabrication of films. Weight, thickness, surface pH, mucoadhesive strength, in vitro residence time, % swelling and % drug release were evaluated for the prepared film formulations.
 Results: All the films were found have surface pH close to neutral pH and were found to have content uniformity. Mucoadhesive strength was found to increase with increase in concentration of Chitosan. Drug release is more controlled by the high swelling film formers than sodium alginate. Among the film formers, though swelling is more, % drug release is also more from sodium alginate and Chitosan films because of its ionic nature and more solubility.
 Conclusion: Because of high mucoadhesive strength and more % drug release, combination of Sodium alginate with Chitosan film formulations was selected.
  Key Words: Saxagliptin, Buccal films

Highlights

  • Introduction of drug and excipient interactions. (Drug) Delivery System1.1.1 Introduction of Buccal Drug delivery system [1, 2]Bioadhesive medication conveyance details were presented in 1947 when gum tragacanth was blended with dental glue powder to apply penicillin to the oral mucosa

  • New formulation of buccal films containing rizatriptan benzoate (RB) was prepared by solvent casting method using various concentrations of hydroxypropyl methylcellulose (HPMC K4M), polyvinyl alcohol (PVA), polyethylene oxide (PEO), glycerol, stevia, and goat buccal mucosa used as a model membrane

  • In vivo studies of optimum buccal tablet formulation carried out on human healthy volunteers showed that the relative bioavailability of PX was 67.52 ± 21.47%. These results demonstrate that buccal tablet formulation of PX seems to be an alternative drug delivery for patients especially suffering from GI disturbances

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Summary

Introduction of Drug Delivery System

Bioadhesive medication conveyance details were presented in 1947 when gum tragacanth was blended with dental glue powder to apply penicillin to the oral mucosa. Double and multilayered tablets are already formulated using bioadhesive polymers and excipients These tablets are solid dosage forms that ate prepared by the direct compression of powder and can be placed into contact with the oral mucosa and allowed to dissolve or adhere depending on the type of excipients incorporated into the dosage form. They can deliver drug multi- directionally into the oral cavity or to the mucosal surface. Acesulfame potassium is used as an intense sweetening agent in cosmetics, foods, beverage products, table-top sweeteners, vitamin and pharmaceutical preparations, including powder mixes, tablets, and liquid products It is widely used as a sugar substitute in compounded formulations

Review of Literature on Drug Delivery System
Summary of PSAR Report
EXPERIMENTAL WORK
THEORETICAL DRUG RELEASE PROFILE
Surface pH
Drug Content Uniformity
Percent Swelling Index
In-vitro drug release
5.6.11 Residence Time
5.6.12 Stability Study
PRE FORMULATION STUDIES
EVALUATION OF SAXAGLIPTIN BUCCAL FILMS
F2 F3 F4
FACTORIAL DESIGN FOR FORMULA OPTIMIZATION
ANALYSIS OF FACTORIAL BATCHES F5-F12
40 Dissolution in 1 hour
CONCLUSION
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