US2004259952A1PendingUtilityA1
Formulations for oral administration of cromolyn sodium
Priority: Nov 29, 2001Filed: Nov 29, 2002Published: Dec 23, 2004
Est. expiryNov 29, 2021(expired)· nominal 20-yr term from priority
A61P 37/02A61P 37/08A61P 29/00A61P 11/06A61P 11/02A61K 47/183A61P 19/02A61K 9/4858A61K 31/353
46
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Claims
Abstract
An oral dosage form comprises cromolyn sodium (sodium or disodium cromoglycate), and an acylated amino acid delivery agent.
Claims
exact text as granted — not AI-modified1 - 54 . cancel.
55 . An oral dosage form comprising:
(a) cromolyn sodium; and (b) a delivery agent that upon oral administration provides a systemic absorption of the cromolyn sodium in a physiologically effective amount, wherein the physiologically effective amount is enough to inhibit the release of histamine or cytokines or histamine and cytokines from mast cells.
56 . The oral dosage form of claim 55 , wherein said delivery agent has the formula or salts thereof:
wherein
Y is carbonyl (CO) or SO 2 ;
R 1 is C 3 -C 24 alkyl, C 2 -C 20 alkenyl, C 2 -C 20 alkyne, cycloalkyl, or aromatic;
R 2 is hydrogen, C 1 -C 4 alkyl, or C 2 -C 4 alkenyl; and
R 3 is C 1 -C 7 alkyl, C 3 -C 10 cycloalkyl, aryl, thienyl, pyrrolo, or pyridyl,
where R 3 is optionally substituted by one or more C 1 -C 5 alkyl group, C 2 -C 4 alkenyl group, Br, I, F, Cl, OH, SO 2 , COOH, or SO 3 H.
57 . The oral dosage form of claim 56 , wherein R 1 is a C 3 -C 12 alkyl.
58 . The oral dosage form of claim 56 , wherein R 1 is a C 3 -C 9 alkyl.
59 . The oral dosage form of claim 56 , wherein R 1 is a C 5 -C 7 alkyl.
60 . The oral dosage form of claim 56 , wherein R 1 is a C 7 alkyl.
61 . The oral dosage form of claim 56 , wherein R 3 is a 2OH substituted phenyl.
62 . The oral dosage form of claim 56 , wherein R 3 is a 2OH substituted phenyl, further substituted with Br, I, F, or Cl.
63 . The oral dosage form of claim 56 , wherein R 3 is a 2OH substituted phenyl, further substituted with Cl.
64 . The oral dosage form of claim 56 , wherein R 1 is a C 3 -C 9 alkyl and R 3 is a 2OH substituted phenyl.
65 . The oral dosage form of claim 56 , wherein R 1 is a C 3 -C 9 alkyl and R 3 is a 2OH substituted phenyl, further substituted with Br, I, F, or Cl.
66 . The oral dosage form of claim 56 , wherein R 1 is a C 3 -C 9 alkyl and R 3 is a 2OH substituted phenyl, further substituted with Cl.
67 . The oral dosage form of claim 55 , wherein said delivery agent has the formula and pharmaceutically acceptable salts thereof:
wherein R is C 3 -C 24 alkyl, C 2 -C 20 alkenyl, C 2 -C 20 alkyne, cycloalkyl, or aromatic.
68 . The oral dosage form of claim 55 wherein said delivery agent comprises Sodium N-[8-(2-hydroxybenzoyl)amino]caprylate (SNAC)
69 . The oral dosage form of claim 68 wherein cromolyn sodium and SNAC, are in a ratio from about 1:30 to about 3:4 (weight/weight).
70 . The oral dosage form of claim 68 wherein cromolyn sodium and SNAC, are in a ratio from about 1:15 to about 3:4 (weight/weight).
71 . The oral dosage form of claim 68 wherein cromolyn sodium and SNAC, are in a ratio from about 2:15 to about 3:4 (weight/weight).
72 . The oral dosage form of claim 68 wherein cromolyn sodium and SNAC, are in a ratio from about 6:25 to about 3:4 (weight/weight).
73 . The oral dosage form of claim 55 wherein said delivery agent is an acylated amino acid delivery agent.
74 . The oral dosage form of claim 55 wherein the physiologically effective amount is enough to provide an absorption of cromolyn from the gastrointestinal tract of greater than about 3.5%, by weight, of the dose of cromolyn contained in the dosage form.
75 . The oral dosage form of claim 55 wherein the physiologically effective amount is enough to provide an absorption of cromolyn from the gastrointestinal tract of greater than about 2%, by weight, of the dose of cromolyn contained in the dosage form.
76 . The oral dosage form of claims 55 wherein the oral dosage form is in the form of a tablet, capsule or oral suspension.
77 . The oral dosage form of claim 55 , wherein the oral dosage form is solid.
78 . The oral dosage form of claim 55 suitable for being administered once a day, twice a day, three times a day or four times a day.
79 . The oral dosage form of claim 55 wherein the dose of cromolyn sodium is from about 40 mg to about 1 g.
80 . The oral dosage form of claim 79 wherein the dose of cromolyn sodium is from about 40 mg to about 240 mg.
81 . The oral dosage form of claim 79 wherein the dose of cromolyn sodium is from about 50 mg to about 150 mg.
82 . The oral dosage form of claim 55 , wherein the dose of the delivery agent is from about 100 mg to about 1200 mg.
83 . The oral dosage form of claim 82 , wherein the dose of the delivery agent is from about 200 mg to about 800 mg.
84 . The oral dosage form of claim 55 , which provides a T max for cromolyn sodium at about 0.1 to about 1.5 hours after oral administration.
85 . The oral dosage form of claim 84 , which provides a T max for cromolyn sodium at less than about 1 hours after oral administration.
86 . The oral dosage form of claims 84 , which provides a T max for cromolyn sodium at about 0.2 to about 0.5 hours after administration.
87 . The oral dosage form of claim 55 , which provides an AUC for cromolyn sodium of between about 15 and about 60 ng.h/mL.
88 . The oral dosage form of claims 87 , which provides an AUC for cromolyn sodium of between about 30 and about 40 ng.h/mL.
89 . The oral dosage form of claim 55 which provides a cromolyn sodium C max from about 10 ng/ml to about 250 ng/ml.
90 . The oral dosage form of claims 89 , which provides a cromolyn sodium C max from about 20 to about 100 ng/mL.
91 . The oral dosage form of claims 89 , which provides a cromolyn sodium C max from about 40 to about 65 ng/mL.
92 . The oral dosage form of claims 89 , which provides a cromolyn sodium C max from about 20 to about 80 ng/mL within about 0.2 to about 1 hour after oral administration.
93 . A method for administering the dosage unit form of claim 55 to an animal who could benefit from Cromolyn.
94 . The method for administering of claim 93 wherein the animal is in need of Cromolyn.
95 . The method for administering of claim 93 wherein the animal is a human.
96 . The method for administering of claim 93 wherein the animal is in need of a treatment of an inflammatory disease.
97 . The method for administering of claim 93 wherein the delivery agent comprises Sodium N-[8-(2-hydroxybenzoyl)amino]caprylate (SNAC)
98 . The method for administering of claim 97 wherein the cromolyn sodium and Sodium N-[8-(2-hydroxybenzoyl)amino]caprylate (SNAC), are in a ratio from about 6:25 to about 3:4 (weight/weight).
99 . The method for administering of claim 93 wherein cromolyn sodium in an amount from about 40 mg to about 1 g together with a delivery agent in an amount from about 100 mg to about 2500 mg.
100 . The method for administering of claim 96 wherein the inflammatory disease is allergic rhinitis.
101 . The method for administering of claim 96 wherein the inflammatory disease is asthma.
102 . The method for administering of claim 96 wherein the inflammatory disease is rheumatoid arthritis.
103 . The method for administering of claim 96 wherein the inflammatory disease is an autoimmune disease.
104 . The method for administering of claim 93 wherein the composition is administered on a prophylactic basis.
105 . The method for administering of claim 93 , wherein the T max for cromolyn sodium occurs at a time less than about 1 hour after oral administration.
106 . The method for administering of claim 93 , wherein an AUC for cromolyn sodium of between about 16 and about 60 ng.h/mL is attained.
107 . The method for administering of claim 93 , wherein a cromolyn sodium C max that is from about 10 to about 250 ng/mL is attained.Cited by (0)
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