IP Library Granted Patent US 8,623,416
Granted Patent B2
US 8,623,416 · App. 12/953,083 · Granted Jan 7, 2014

Formulations comprising aminosterols

Inventor: Michael Zasloff (Merion, PA)
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Quick Facts
Patent No.
US 8,623,416
App. No.
12/953,083
Granted
Jan 7, 2014
Kind
B2
Abstract

This invention relates to stable aminosterol phosphate compositions. The aminosterol phosphate compositions permit administration without associated tissue damage and achieve a sustained release effect.

Claims (52)

1. A pharmaceutical composition comprising:

(a) at least one pharmaceutical grade aminosterol, wherein the aminosterol is selected from the group consisting of squalamine, Aminosterol 1436, a pharmaceutically acceptable salt thereof, and any combination thereof; and

(b) at least one phosphate selected from the group consisting of an inorganic phosphate, an inorganic pyrophosphate, and an organic phosphate,

wherein the aminosterol is formulated as a weakly water soluble salt of the phosphate.

2. The composition of claim 1 , wherein the phosphate is an inorganic polyphosphate, and the number of phosphates can range from 3 to 400.

3. The composition of claim 1 , wherein the phosphate is an organic phosphate which comprises glycerol 2 phosphate.

4. The composition of claim 1 , wherein the aminosterol is

squalamine or a pharmaceutically acceptable salt thereof.

5. The composition of claim 1 , wherein the composition is formulated:

(a) for routes of administration selected from the group consisting of oral, pulmonary, rectal, colonic, intracisternal, intravaginal, intraperitoneal, intravenous, subcutaneous, intramuscular, nebulization, inhalation, ocular, otic, local, buccal and nasal administration;

(b) for a topical route of administration;

(c) for parenteral administration;

(d) into a dosage form selected from the group consisting of liquid dispersions, gels, aerosols, ointments, creams, lyophilized formulations, tablets, capsules; or

(e) into a dosage form selected from the group consisting of controlled release formulations, fast melt formulations, delayed release formulations, extended release formulations, pulsatile release formulations, and mixed immediate release and controlled release formulations.

6. The composition of claim 1 , wherein the composition further comprises at least one additional active agent.

7. The composition of claim 6 , wherein the additional active agent is selected from the group consisting of:

(a) an antiretroviral agent;

(b) nucleoside or nucleotide reverse transcriptase inhibitors;

(c) non-nucleoside reverse transcriptase inhibitors;

(d) nucleotide or nucleoside analogues;

(e) protease inhibitors;

(f) drugs based on “antisense” molecules;

(g) ribozyme antivirals;

(h) assembly inhibitors;

(i) release phase inhibitors;

(j) drugs which stimulate the immune system;

(k) fusion inhibitors/gp41 binders;

(l) fusion inhibitors/chemokine receptor antagonists;

(m) integrase inhibitors;

(n) hydroxyurea-like compounds;

(o) inhibitors of viral integrase;

(p) inhibitors of viral genome nuclear translocation;

(q) inhibitors of HIV entry;

(r) nucleocapsid zinc finger inhibitors;

(s) targets of HIV Tat and Rev;

(t) pharmacoenhancers;

(u) cytokines;

(v) lymphokines;

(w) an anti-inflammatory agent;

(x) antibiotic;

(y) antifungal, antiyeast, and/or antimold agent;

(z) anticancer agent;

(aa) weight loss agent; and

(bb) any combination thereof.

8. The composition of claim 1 , further comprising at least one adjuvant.

9. The composition of claim 8 , wherein the adjuvant is selected from the group consisting of cytokines, IL2, IL3, IL4, IL5, IL6, IL7, IL8, IL-9, IL10, IL-11, IL12, IL13, IL-14, IL15, IIL16, IL-17, IL-18, IL-19,IL-20, IL-21, anti-CD40, CD40L, IFN-gamma, TNF-alpha, IL-Ialpha, IL-lbeta, alum, Lipid A, monophosphoryl lipid A, bacterial products, endotoxins, cholesterol, fatty acids, aliphatic amines, paraffinic oils, vegetable oils, threonyl derivative, muramyl dipeptide, alum plus deoxycholate MTP-PE, QS21, BCG, MPL, nonviable preparations of Corynebacterium , parvum, Monophosphoryl lipid immunomodulator, QS-18, CRL1005, Aluminum salts, MF-59, and Virosomal adjuvant technology.

10. The composition of claim 1 , wherein the composition further comprises at least one antigen capable of eliciting an immune response.

11. The composition of claim 10 , wherein the antigen is selected from the group consisting of viral and prion antigens.

12. The composition of claim 1 , wherein the squalamine salt is in the form of a particulate suspension varying in particle size from between about0.1 to about 100 microns.

13. The composition of claim 1 further comprising at least one pharmaceutically acceptable excipient.

14. The composition of claim 1 formulated as an oral tablet or capsule.

15. The composition of claim 4 , wherein the aminosterol is Aminosterol 1436.

Assignments (3)
CHANGE OF NAME Recorded Oct 29, 2020
From: ENTERIN LABORATORIES, INC.
To: ENTERIN, INC.
Reel/Frame 054253/0830 →
CORRECTIVE ASSIGNMENT TO CORRECT THE COMPANY NAME PREVIOUSLY RECORDED ON REEL 038019 FRAME 0841. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT EXECUTED ON FEBRUARY 27, 2016. Recorded Mar 29, 2016
From: ZASLOFF, MICHAEL, DR.
To: ENTERIN LABORATORIES, INC.
Reel/Frame 038278/0318 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 17, 2016
From: ZASLOFF, MICHAEL, DR.
To: ENTERIN, INC.
Reel/Frame 038019/0841 →
Continuity (2)
Provisional Application 61264499 · Nov 25, 2009
Related Publication 20110123624A1 · May 26, 2011