Compositions for nasal administration of pharmaceuticals
Compositions for nasal administration, which comprise a pharmaceutical, a physiologically active peptide, or a peptide-related compound, and as the carrier thereof, crystalline cellulose with a specific particle diameter and/or partially pregelatinized starch are provided. Such compositions improve the in vivo absorption efficiency of pharmaceuticals.
1. A method of intranasally administering a physiologically active peptide or peptide-related compound, the method comprising:
intranasally administering a powdery pharmaceutical composition comprising:
the physiologically active peptide or peptide-related compound; and
a carrier,
wherein:
the physiologically active peptide or peptide-related compound has a molecular weight of 30,000 or less, and
the carrier comprises crystalline cellulose particles, wherein 85 wt % or more of the crystalline cellulose particles are in a sieving particle diameter range of 20-60 μm, and wherein the crystalline cellulose particles have an average polymerization degree of about 20 to 250.
2. The method of claim 1 , wherein the physiologically active peptide or peptide-related compound is selected from the group consisting of insulin, human growth hormone, calcitonin, glucagon, parathyroid hormone, parathyroid hormone (1-34), glucagon-like peptide-1, interferon, interleukin, erythropoietin, luteinizing hormone-releasing hormone, somatostatin, vasopressin, oxytocin, enkephalin, adrenocorticotropic hormone, growth hormone-releasing hormone, granulocyte colony formation-stimulating factor, parathyroid hormone, thyroid-stimulating hormone-releasing hormone, angiotensin, prolactin, luteinizing hormone, gastric inhibitory polypeptide (GIP), C-peptide, cyclosporine, and FK-506.
3. The method of claim 1 , wherein the powdery pharmaceutical composition comprises insulin.
4. The method of claim 1 , wherein the powdery pharmaceutical composition comprises human growth hormone.
5. The method of claim 1 , wherein the powdery pharmaceutical composition comprises glucagon.
6. The method of claim 1 , wherein the powdery pharmaceutical composition comprises glucagon-like peptide-1.
7. The method of claim 1 , wherein the powdery pharmaceutical composition comprises calcitonin.
8. The method of claim 1 , wherein the powdery pharmaceutical composition comprises parathyroid hormone.
9. The method of claim 1 , wherein the powdery pharmaceutical composition comprises parathyroid hormone (1-34).
10. The method of claim 1 , wherein the powdery pharmaceutical composition comprises luteinizing hormone-releasing hormone.
11. The method of claim 1 , wherein the physiologically active peptide or peptide-related compound is in the form of a powder finer than the crystalline cellulose particles.
12. The method of claim 1 , wherein the crystalline cellulose particles have a sieving particle diameter distribution of:
about 10 wt % or fewer particles with a diameter smaller than 25 μm;
about 20 to 60 wt % particles with a diameter of about 25 to 38 μm;
about 20 to 60 wt % particles with a diameter greater than 38 μm and smaller than 53 μm or equal to about 53 μm; and
the remaining particles having a diameter greater than 53 μm but up to 60 μm or less.
13. The method of claim 1 , wherein the crystalline cellulose particles have an average polymerization degree of about 30 to 50.
14. The method of claim 1 , wherein the crystalline cellulose particles have a bulk density of about 0.22 to 0.65 g/cm 3 .
15. The method of claim 1 , wherein the crystalline cellulose particles have a bulk density of about 0.22 to 0.40 g/cm 3 .
16. The method of claim 1 , wherein the crystalline cellulose particles have a bulk density of about 0.22 g/cm 3 .
17. The method of claim 1 , wherein the physiologically active peptide is intranasally administered.
18. The method of claim 1 , wherein the physiologically active peptide-related compound is intranasally administered.