Claims for Patent: 5,554,378

Summary for Patent: 5,554,378

Title:	Pharmaceutical composition and its mucosal use
Abstract:	A pharmaceutical composition containing a physiologically active peptide or protein which is poorly absorbable through the gastrointestinal tract and heat-labile enterotoxin B subunit brings an increased absorbability of said peptide or protein into the mammalian body when administered through mucosa.
Inventor(s):	Uda; Yoshiaki (Hyogo, JP), Takada; Shigeyuki (Osaka, JP), Fujisawa; Yukio (Hyogo, JP)
Assignee:	Takeda Chemical Industries, Ltd. (Osaka, JP)
Application Number:	08/379,114
Patent Claims:	1. A pharmaceutical composition, comprising a physical mixture of: (a) a therapeutically effective amount of a physiologically active peptide or protein; (b) heat-labile enterotoxin B subunit present in an amount effective to promote translocation of said physiologically active peptide or protein through nasal mucosa; and (c) a pharmaceutically acceptable carrier for mucosal administration, wherein said composition is a liquid or semi-solid preparation and the weight ratio of component (a) to component (b) is in the range of from 0.004 to 4.0. 2. A pharmaceutical composition as claimed in claim 1, wherein the composition is formed into a preparation for mucosal administration. 3. A pharmaceutical composition as claimed in claim 1, wherein the peptide or protein is hydrophilic. 4. A pharmaceutical composition as claimed in claim 1, wherein the peptide or protein is a hormone, lymphokine, enzyme, analgesic, hematopoietic growth factor, neuro transmitter or growth factor. 5. A pharmaceutical composition as claimed in claim 1, wherein the molecular weight of the peptide or protein is in the range of about 200 to 60,000. 6. A pharmaceutical composition as claimed in claim 1, wherein the octanol-water partition coefficient of the peptide or protein is not more than 0.1. 7. The pharmaceutical composition as claimed in claim 1, wherein said physiologically active peptide or protein is insulin. 8. The pharmaceutical composition as claimed in claim 1, wherein said physiologically active peptide or protein is thyrotropin releasing hormone or an analog thereof. 9. The pharmaceutical composition as claimed in claim 8, wherein said analog is DN-1417. 10. The pharmaceutical composition as claimed in claim 1, wherein said physiologically active peptide or protein is .alpha.-interferon. 11. The pharmaceutical composition as claimed in claim 1, wherein said physiologically active peptide or protein is enkephalin. 12. The pharmaceutical composition as claimed in claim 1, wherein said physiologically active peptide or protein is parathyroid hormone or an active fragment thereof. 13. The pharmaceutical composition as claimed in claim 12, wherein said active fragment is the N-terminal 34-amino acid portion of parathyroid hormone. 14. The pharmaceutical composition as claimed in claim 1, wherein said composition increases the bioavailability of the physiologically active peptide or protein, wherein the physiologically active peptide or protein is one that is not substantially absorbed from the gastrointestinal tract and is selected from the group consisting of insulin, thyrotropin releasing hormone or an analog thereof, .alpha.-interferon, enkephalin, and parathyroid hormone or an active fragment thereof. 15. A composition adapted for nasal administration, comprising: the pharmaceutical composition of claim 1, wherein said composition is in the form of a gel that can be applied to the nasal cavity for intimate contact with the nasal mucosa. 16. A composition adapted for nasal administration, comprising the pharmaceutical composition of claim 1, wherein said composition is in the form of a liquid capable of being sprayed into the nasal cavity for intimate contact with the nasal mucosa. 17. A composition adapted for nasal administration, comprising the pharmaceutical composition of claim 1, wherein said composition is in the form of a powder contained in a capsule, which is capable of spraying the powder into the nasal cavity for intimate contact with the nasal mucosa. 18. A method of administering a physiologically active peptide or protein through the nasal cavity of a subject in need thereof, comprising the step of providing to the nasal mucosa of said subject a pharmaceutical composition comprising a physical mixture of: (a) a therapeutically effective amount of a physiologically active peptide or protein; (b) heat-labile enterotoxin B subunit present in an amount effective to promote translocation of said physiologically active peptide or protein through nasal mucosa; and (c) a pharmaceutically acceptable carrier for mueosal administration, wherein said pharmaceutical composition is a liquid or semi-solid preparation and the weight ratio of component (a) to component (b) is in the range of from 0.004 to 4.0. 19. A method as claimed in claim 18, wherein the pharmaceutical composition is a uniform mixture in dosage form. 20. A method as claimed in claim 18, wherein the peptide or protein is a hormone lymphokie, enzyme, analgesic, hematopoietic growth factor, neuro transmitter or growth factor. 21. The method of claim 18, wherein the molecular weight of the peptide or protein is in the range of about 200 to 60,000. 22. The method of claim 18, wherein the octanol-water partition coefficient of the peptide or protein is not more than 0.1.

Details for Patent 5,554,378

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Nps Pharmaceuticals, Inc.	NATPARA	parathyroid hormone	For Injection	125511	01/23/2015		2013-09-10