Biodegradable periodontal intrapocket device containing metronidazole and amoxycillin: formulation and characterisation.
The purpose of the study was to formulate biodegradable intrapocket dental films, which could be easily placed into the periodontal pocket, and be capable of delivering therapeutic concentrations of amoxycillin and metronidazole for prolonged period of time with a much lower dose, hence obviating untoward side effects. A biodegradable intrapocket device containing amoxycillin and metronidazole was prepared using 69.29 mg each of amoxycillin and metronidazole, 2.0% diethyl phthalate plasticizer and 750 mg poly (L-lactide-co-glycolide). The device was optimized on the basis of evaluation parameters such as weight variation, content uniformity, surface pH, and in vitro and in vivo release studies. The films showed sustained in vitro release for a period of 16 days. In vivo release studies showed that drug concentrations were maintained above the MIC value for the entire period of the release studies. The samples from this study were capable of inhibiting the growth of most test strains. The combination of amoxycillin and metronidazole in the carrier polymer poly (L-lactide-co-glycolide) not only showed an extended spectrum of antimicrobial activity but also showed a synergistic effect against E. limosum, which had been reported the resistant to metronidazole in earlier studies. Stability studies were conducted on the optimized formulation and the degradation rate constant was found to be 4.6 x 10(-4)/day for metronidazole and 4.8 x 10-4)/day for amoxycillin. The drug was released locally and had a high benefit to low risk ratio as compared to systemic administration which is unacceptable due to, low benefit to high-risk ratio. Hence low-dose site-specific films present a better alternative.
Ahuja
A
A
Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi, India. alkaahuja@yahoo.com
Ali
J
J
Rahman
S
S
D000658:Amoxicillin / Q000008:administration & dosage* / Q000737:chemistry; D001419:Bacteria / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D004355:Drug Stability; D005881:Gingiva / Q000382:microbiology*; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D019344:Lactic Acid; D008795:Metronidazole / Q000008:administration & dosage* / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D010968:Plasticizers; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers; D012995:Solubility; D013499:Surface Properties
D010968:Plasticizers; D011108:Polymers; D008795:Metronidazole; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000658:Amoxicillin