Formulation of a drug delivery system based on a mixture of monoglycerides and triglycerides for use in the treatment of periodontal disease.
This paper describes the development of a stable, controlled-release formulation of metronidazole for use in the treatment of periodontal disease. It is formulated as a suspension, which undergoes transformation to a release-controlling, semi-solid on contact with gingival fluid. The system is based on the ability of mixtures of monoglycerides and triglycerides to form liquid crystals, i.e., reversed hexagonals, in contact with water. The reversed hexagonal form was found to have the most favourable sustained release properties, compared with those from the cubic form. The source of metronidazole is the prodrug, metronidazole benzoate, which further helps to slow down the release rate. Product characteristics are assessed by differential scanning calorimetry and viscometry. The release data derive from the results of in vitro dissolution tests. X-ray diffraction, phase diagrams, and polarized light microscopy were used to elucidate the structure of the liquid crystalline phases.
Norling
T
T
A/S Dumex, Copenhagen, Denmark.
Lading
P
P
Engström
S
S
Larsson
K
K
Krog
N
N
Nissen
S S
SS
D001673:Biodegradation, Environmental; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D003692:Delayed-Action Preparations; D004058:Diffusion; D015195:Drug Design; D004343:Drug Implants; D005782:Gels; D005989:Glycerides / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D008795:Metronidazole / Q000008:administration & dosage* / Q000737:chemistry; D010510:Periodontal Diseases / Q000188:drug therapy; D012715:Sesame Oil / Q000138:chemical synthesis / Q000737:chemistry*; D012995:Solubility; D013594:Syringes; D013696:Temperature; D014783:Viscosity; D014961:X-Ray Diffraction
D003692:Delayed-Action Preparations; D004343:Drug Implants; D005782:Gels; D005989:Glycerides; D008795:Metronidazole; D012715:Sesame Oil; C005953:monoolein