title: Development of amitriptyline buccoadhesive tablets for management of pain in dental procedures.
abstract: Administration of lidocaine and nonsteroidal anti-inflammatory drugs (NSAIDs) as a routine procedure for relief of dental pains by and large is restricted due to some side effects. Amitriptyline (AM) has long been known to exert analgesic activity as a result of blocking the Na⁺ channels. The objective of the present investigation was to prepare suitable buccoadhesive tablets using cellulose derivatives in order to obtain new formulations containing AM to provide local analgesic action. The tablets were evaluated in terms of physical characteristics, mucoadhesion performance, drug release, and in vivo assessment of analgesic efficiency. Tablets containing higher amounts of high-viscosity hydroxypropylmethyl cellulose (HPMC-K4M) significantly demonstrated enhanced adhesive performances. On the other hand, presence of sodium carboxymethyl cellulose (NaCMC) in formulations including HPMC of lower-viscosity grade (HPMC-E5LV) provided further adhesiveness by increase in viscosity. Rate of drug release from HPMC-E5LV tablets was significantly higher than the HPMC-K4M tablets. Kinetically, patterns of AM release from the tablets fitted best to Higuchi model. Moreover, in a randomized double-blind trial, analgesic efficiency of the prepared bioadhesive tablets was revealed to be satisfactory. It is suggested that applying the topical AM mucoadhesive tablet containing the low amount of drug is a safe and promising alternative to relief the pain in the buccal region.
authors.affiliation: Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
authors.forename: Sara
authors.initials: S
authors.lastname: Movassaghian
authors.forename: Mohammad
authors.initials: M
authors.lastname: Barzegar-Jalali
authors.forename: Mojgan
authors.initials: M
authors.lastname: Alaeddini
authors.forename: Sanaz
authors.initials: S
authors.lastname: Hamedyazdan
authors.forename: Rose
authors.initials: R
authors.lastname: Afzalifar
authors.forename: Parvin
authors.initials: P
authors.lastname: Zakeri-Milani
authors.forename: Ghobad
authors.initials: G
authors.lastname: Mohammadi
authors.forename: Khosro
authors.initials: K
authors.lastname: Adibkia
mesh_terms: D000268:Adhesiveness; D000278:Administration, Buccal; D000328:Adult; D000639:Amitriptyline / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000698:Analgesia / Q000379:methods; D018712:Analgesics, Non-Narcotic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002266:Carboxymethylcellulose Sodium / Q000008:administration & dosage; D003814:Dentistry, Operative; D004311:Double-Blind Method; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems; D005260:Female; D006244:Hardness; D006801:Humans; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000008:administration & dosage / Q000031:analogs & derivatives; D008875:Middle Aged; D010146:Pain / Q000188:drug therapy*; D010147:Pain Measurement; D013607:Tablets; D055815:Young Adult
chemical_list: D018712:Analgesics, Non-Narcotic; D013607:Tablets; D000639:Amitriptyline; D065347:Hypromellose Derivatives; D008747:Methylcellulose; D002266:Carboxymethylcellulose Sodium