Compositions that enable rapid-acting and highly absorptive intranasal administration
View Patent ↗Powdery compositions for intranasal administration, which comprise non-peptide/non-protein drugs and as a carrier, crystalline cellulose aggregates having a particular cribriform particle diameter, yield rapid action and high absorbability of the drugs.
1. A powdery composition for intranasal administration comprising:
i) a non-peptide/non-protein drug, wherein the drug is an opioid receptor agonist, or a 5-hydroxytryptaminel (5-HT 1 ) receptor agonist; and
ii) a carrier consisting essentially of crystalline cellulose aggregate, wherein 85% (w/w) or more of the crystalline cellulose aggregate has a particle size distribution of 20 to 60 μm and wherein when administered to a primate intranasally, the time to maximal blood concentration (Tmax) in said primate is achieved within 20 minutes.
2. The composition of claim 1 , wherein Tmax is achieved within 10 minutes.
3. A powdery composition for intranasal administration comprising:
i) a non-peptide/non-protein drug, wherein the drug is an opioid receptor agonist, or a 5-hydroxytryptaminel (5-HT 1 ) receptor agonist; and
ii) a carrier consisting essentially of crystalline cellulose aggregate, wherein 85% (w/w) or more of the crystalline cellulose aggregate has a particle size distribution of 20 to 60 μm and wherein when administered to a primate intranasally, the absolute bioavailability (BA) of the drug is between 64% to 99%.
4. The powdery composition of claim 1 or 3 , wherein the non-peptide/non-protein drug is sumatriptan, zolmitriptan, morphine or oxycodone.
5. The powdery composition of claim 1 or claim 3 , wherein the non-peptide/non-protein drug is morphine.
6. The powdery composition of claim 1 or claim 3 , wherein the non-peptide/non-protein drug is oxycodone.
7. The powdery composition of claim 1 or claim 3 , wherein the non-peptide/non-protein drug is sumatriptan.
8. The powdery composition of claim 1 or claim 3 , wherein the non-peptide/non-protein drug is zolmitriptan.