Modified-release ointment with nitroglycerin β-cyclodextrin inclusion complex for treatment of anal fissures
| Autor: | Katarzyna Centkowska, Małgorzata Sznitowska |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
Adult
Chemistry Pharmaceutical Skin Absorption Pharmaceutical Science Absorption (skin) In Vitro Techniques Ointments Nitroglycerin Prolonged release medicine Cadaver Humans Skin Pharmacology chemistry.chemical_classification Drug Carriers Cyclodextrin business.industry beta-Cyclodextrins Hydrogels chemistry Solubility Anesthesia Delayed-Action Preparations Female Fissure in Ano business medicine.drug Nuclear chemistry |
| Zdroj: | The Journal of pharmacy and pharmacology. 65(10) |
| ISSN: | 2042-7158 |
| Popis: | Objectives The aim was to evaluate ointments for local treatment of anal fissures. Nitroglycerin (NTG) was complexed with β-cyclodextrin (β-CD) to provide prolonged NTG release, with the intention of decreasing systemic drug absorption and thus reducing side effects. Methods Gels, creams and anhydrous water-emulsifying (AWE) ointment with NTG-CD were compared with preparations containing uncomplexed NTG (diluted with crospovidone, NTG-cP). The in-vitro NTG release and ex-vivo skin absorption were studied. Key findings The prolonged-release ointment with the NTG-CD complex was formulated using AWE base or w/o cream (20% water); release of NTG from a hydrogel was very fast with both the complexed and uncomplexed forms. From the AWE ointment base, 16.4% or 4.5% of the total NTG dose was released after 6 h when NTG-cP or NTG-CD was incorporated, respectively. With the complexed form, NTG absorption to the skin after a 5-h application was 18.1 or 11.1 μg/g from AWE ointment or cream, respectively; absorption of the uncomplexed NTG was higher: 52.3 or 21.9 μg/g from AWE ointment and cream, respectively. Conclusions Complexation with β-CD results in prolonged release of NTG from AWE ointment and w/o cream, which was confirmed by the ex-vivo skin absorption results. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text