Research On The Preparation Of Cyclodextrin Supramolecular Inclusions Of Triamcinolone Acetonide And Its Nasal Spray

Allergic Rhinitis(AR)is a kind of systemic inflammatory response caused by a variety of allergic sources and mediated by immunoglobulin Ig E.It's major clinical manifestations including nasal congestion,itchy,runny nose,sneezing and so on.It affects the patient's normal life seriously.Using the nasal spray is the main way to treat allergic rhinitis,and relieve symptoms.Cyclodextrins are an important part of supramolecular chemistry and it can form supramolecular inclusions with hydrophobic drugs through non-covalent bonds.Supramolecular drugs have the advantages of good solubility,high bioavailability and low toxicity.Triamcinolone acetonide is a potent corticosteroids.As the first choice for treatment of allergic rhinitis medicine,it has the very good treatment effect and less adverse reactions.Due to the poor solubility of triamcinolone acetonide,triamcinolone acetonide nasal sprays listed at home and abroad are suspension agent.Drugs mix unevenly after vibration wave and its evenness is poorer.Furthermore,there isn't solve the poor solubility of triamcinolone acetonide.Therefore,cyclodextrins were selected as binding material to form the supramolecular inclusions with triamcinolone acetonide.This method can increase the solubility of triamcinolone acetonide.Solution-type triamcinolone acetonide nasal spray has a better spread in the nasal cavity and it can promote the absorption of triamcinolone acetonide in the nasal cavity.Thereby,the bioavailability of drugs were enhanced.The physical and chemical properties of triamcinolone acetonide were studied and hydroxypropyl-beta-cyclodextrin and sulfonated butyl-beta-cyclodextrin were selected as binding material to form cyclodextrin supramolecular inclusions which are two types of beta of cyclodextrin derivatives.Inclusion rate was used as index to determine the molecular weight ratio between subject and object and the best preparation technology.HP-?-cyclodextrins supramolecular inclusions of triamcinolone acetonide was prepared by the method of freeze drying.In addition the validation of inclusion was verified by characterization and spectral form.On the basis of the preparation technology of aqueous solution of cyclodextrin supramolecular inclusions of triamcinolone acetonide,the types of complementary makings was determined using sanofi products(Nasacort AQ)as a reference.It wasdetermined that the amount of the biological adhesion agent HPMC and osmotic pressure regulator anhydrous glucose according to the viscosity and millimoles osmotic pressure.Then the prescription of nasal spray of cyclodextrin supramolecular inclusions of triamcinolone acetonide was determined.The nasal spray triamcinolone acetonide of cyclodextrin supramolecular inclusions is better than that of thixotropy triamcinolone acetonide nasal spray determined by comparative study on the characteristic.In order to examine the effects of the nasal spray of triamcinolone acetonide-cyclodextrin supramolecular inclusions on acute inflammation,the auricle swelling model was induced by xylene on mice and the paw swelling model induced by carrageen glue on rats test.The results showed that the nasal spray of triamcinolone acetonide-cyclodextrin supramolecular inclusions have excellent therapeutic effect on acute inflammation.The modeling allergic rhinitis on guinea pig was used to determine the effects of the nasal spray of triamcinolone acetonide-cyclodextrin supramolecular inclusions on allergic rhinitis.The experimental results showed that the nasal spray of triamcinolone acetonide-cyclodextrin supramolecular inclusions have obvious effect on allergic rhinitis and the effect of middle dose group and high dose group are better than positive control group.