Claims for Patent: 6,214,375

Summary for Patent: 6,214,375

Title:	Phospholipid formulations
Abstract:	A liposome pharmaceutical composition is provided. The liposomes are comprised of a medicinally active agent, at least three phospholipids and at least two biodegradable polymers. The liposomes can be used for delivery of various cosmetics and drugs, and can be administered orally, topically or by injection.
Inventor(s):	Modi; Pankaj (Ancaster, CA)
Assignee:	Generex Pharmaceuticals, Inc. (Toronto, CA)
Application Number:	09/277,600
Patent Claims:	1. A liposomal formulation comprising i) at least one medicinally active ingredient, ii) at least three compounds selected from the group consisting of egg phosphatidylcholine, dilauryl phosphatidylcholine, dimyristoyl phosphatidylcholine, dipalmitoyl phosphatidylcholine, dioleoyl phosphatidylcholine, dimyristoyl phosphatidylglycerol, dipalmitoyl phosphatidic acid, dipalmitoyl phosphatidic acid, dipalmitoyl phosphatidylethanolamine, distearoyl phosphatidylcholine, brain phosphatidylserine, brain sphingomyelin, cholesterol, cardiolipin, trioctanoin, triolein, soy phosphatidylcholine, poly(adenylic acid), phosphatidylethanolamine, phosphatidyl glycerol, phosphatidyl inositol, sphingosine, cerebroside (glycolipid), and iii) at least two biodegradable polymers selected from the group consisting of copolymers of sucrose and epichlorohydrin having molecular weights of from 70 000 to 400 000, branched hydrophilic polymers of sucrose having molecular weights of from 70 000 to 400 000, polyethylene glycols having molecular weights of from 1000 to 100 000, polyvinyl alcohols having molecular weights of from 70 000 to 110 000, methoxypolyethylene glycol, ethoxypolyethylene glycol, polyethylene oxide, polyoxyethylene, polyoxypropylene, cellulose acetate, sodium alginate, N,N-diethylaminoacetate, block copolymers of polyoxyethylene and polyoxypropylene, polyvinyl pyrrolidone, polyoxyethylene X-lauryl ether wherein X is from 9 to 20, and polyoxyethylene sorbitan esters. 2. A formulation according to claim 1 wherein there are at least three biodegradable polymers in the formulation. 3. A formulation according to claim 1 wherein the compound combinations are selected from the group consisting of: i) brain phosphatidylserine, cholesterol, triolein and phosphatidylethanolamine, ii) egg phosphatidylcholine, distearoyl phosphatidylcholine, cholesterol and triolein, iii) cholesterol, cardiolipin, poly(adenylic acid) and triolein, iv) egg phosphatidylcholine, distearoyl phosphatidylcholine, cholesterol and trioctanoin, v) egg phosphatidylcholine, cholesterol, trioctanoin and phosphatidyl glycerol, vi) egg phosphatidylcholine, cholesterol, cardiolipin and triolein, vii) dioleoyl phosphatidylcholine, cholesterol, cardiolipin and triolein, viii) egg phosphatidylcholine, cholesterol, brain phosphatidylserine and triolein, ix) dioleoyl phosphatidylcholine, brain phosphatidylserine, cholesterol and triolein, x) egg phosphatidylcholine, dipalmitoyl phosphatidylglycerol, cholesterol and trioctanoin, xi) dimyristoyl phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoyl phosphatidylcholine and triolein, xii) egg phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoyl phosphatidylcholine and trioctanoin, xiii) phosphatidylcholine, cholesterol, brain phosphatidylserine and triolein, xiv) phosphatidylethanolamine, cholesterol cardiolipin and triolein, xv) phosphatidylcholine, cholesterol, trioctanoin and dipalmitoyl phosphatidylethanolamine, xvi) dimyristoyl phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoyl phosphatidylcholine and triolein, xvii) phosphatidylcholine, phosphatidylethanolamine, cholesterol, brain phosphatidylserine and triolein, xviii) phosphatidylcholine, phosphatidylthanolamine, cholesterol, cardiolipin and triolein, xix) phosphatidylcholine, dioleoyl phosphatidylcholine, cholesterol, cardiolipin and triolein, xx) phosphatidylcholine, dioleoyl phosphatidylcholine, cholesterol, brain phosphatidylserine and triolein, xxi) phosphatidylcholine, dimyristoyl phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoyl phosphatidylcholine and triolein and xxii) phosphatidylcholine, cholesterol, phosphatidylcholine ethanloamine and triolein. 4. A formulation according to claim 2 wherein the compound combinations are selected from the group consisting of: i) brain phosphatidylserine, cholesterol, triolein and phosphatidylethanolamine, ii) egg phosphatidylcholine, distearoyl phosphatidylcholine, cholesterol and triolein, iii) cholesterol, cardiolipin, poly(adenylic acid) and triolein, iv) egg phosphatidylcholine, distearoyl phosphatidylcholine, cholesterol and trioctanoin, v) egg phosphatidylcholine, cholesterol, trioctanoin and phosphatidyl glycerol, vi) egg phosphatidylcholine, cholesterol, cardiolipin and triolein, vii) dioleoyl phosphatidylcholine, cholesterol, cardiolipin and triolein, viii) egg phosphatidylcholine, cholesterol, brain phosphatidylserine and triolein, ix) dioleoyl phosphatidylcholine, brain phosphatidylserine, cholesterol and triolein, x) egg phosphatidylcholine, dipalmitoyl phosphatidylglycerol, cholesterol and trioctanoin, xi) dimyristoyl phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoyl phosphatidylcholine and triolein, xii) egg phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoyl phosphatidylcholine and trioctanoin, xiii) phosphatidylcholine, cholesterol, brain phosphatidylserine and triolein, xiv) phosphatidylethanolamine, cholesterol cardiolipin and triolein, xv) phosphatidylcholine, cholesterol, trioctanoin and dipalmitoyl phosphatidylethanolamine, xvi) dimyristoyl phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoyl phosphatidylcholine and triolein, xvii) phosphatidylcholine, phosphatidylethanolamine, cholesterol, brain phosphatidylserine and triolein, xviii) phosphatidylcholine, phosphatidylthanolamine, cholesterol, cardiolipin and triolein, xix) phosphatidylcholine, dioleoyl phosphatidylcholine, cholesterol, cardiolipin and triolein, xx) phosphatidylcholine, dioleoyl phosphatidylcholine, cholesterol, brain phosphatidylserine and triolein, xxi) phosphatidylcholine, dimyristoyl phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoyl phosphatidylcholine and triolein and xxii) phosphatidylcholine, cholesterol, phosphatidylcholine ethanloamine and triolein. 5. A formulation according to claim 1 wherein the medicinally active ingredient is selected from the group consisting of insulin, heparin, hirugen, hirulos, hirudin, influenza virus vaccine, pneumonia vaccine, hepatitis A vaccine, hepatitis B vaccine, and hepatitis C vaccine, cholera toxin B-subunit, influenza vaccine virus, typhoid vaccine, plasmodium falciparum vaccine, diphtheria vaccine, tetanus, herpes simpex virus vaccine, tuberculosis vaccine, Bordetela vaccine, bordetela pertussis vaccine, measles vaccine, mumps vaccine and rubella vaccine (MMR), bacterial toxoids, vaccinia virus, adenovirus vaccine, canary pox vaccine, polio vaccine virus, bacillus calmette guerin (BCG), klebsiella envelope vaccine, HIV envelope glycoproteins, bovine somatropine, oestrogen, androgens, prostaglandins, somatotropins, thyroid enzyme, pituitary enzyme, digestive enzyme, .alpha.-,.beta.- and .gamma.interferons, tuftsin, interleukins, insulin and insulin like growth factors, cytokines, steroids, terpenoids, triterpenes, retinoids, anti-ulcer H.sub.2 receptor antagonists, anti-ulcer drugs, hypoglycaemic agents, moisturizers, cosmetics, drugs, tetanus toxoid, diphtheria vaccine toxoid, pseudomonas A toxoid, mycobacterium tuberculosis vaccine toxoid, HIV envelope glycoproteins. 6. A formulation according to claim 2 wherein the medicinally active ingredient is selected from the group consisting of insulin, heparin, hirugen, hirulos, hirudin, influenza virus vaccine, pneumonia vaccine, hepatitis A vaccine, hepatitis B vaccine, and hepatitis C vaccine, cholera toxin B-subunit, influenza vaccine virus, typhoid vaccine, plasmodium falciparum vaccine, diphtheria vaccine, tetanus, herpes simpex virus vaccine, tuberculosis vaccine, Bordetela vaccine, bordetela pertussis vaccine, measles vaccine, mumps vaccine and rubella vaccine (MMR), bacterial toxoids, vaccinia virus, adenovirus vaccine, canary pox vaccine, polio vaccine virus, bacillus calmette guerin (BCG), klebsiella envelope vaccine, HIV envelope glycoproteins, bovine somatropine, oestrogen, androgens, prostaglandins, somatotropins, thyroid enzyme, pituitary enzyme, digestive enzyme, .alpha.-, .beta.- and .gamma.interferons, tuftsin, interleukins, insulin and insulin like growth factors, cytokines, steroids, terpenoids, triterpenes, retinoids, anti-ulcer H.sub.2 receptor antagonists, anti-ulcer drugs, hypoglycaemic agents, moisturizers, cosmetics, drugs, tetanus toxoid, diphtheria vaccine toxoid, pseudomonas A toxoid, mycobacterium tuberculosis vaccine toxoid, HIV envelope glycoproteins. 7. A formulation according to claim 3 wherein the medicinally active ingredient is selected from the group consisting of insulin, heparin, hirugen, hirulos, hirudin, influenza virus vaccine, pneumonia vaccine, hepatitis A vaccine, hepatitis B vaccine, and hepatitis C vaccine, cholera toxin B-subunit, influenza vaccine virus, typhoid vaccine, plasmodium falciparum vaccine, diphtheria vaccine, tetanus, herpes simpex virus vaccine, tuberculosis vaccine, Bordetela vaccine, bordetela pertussis vaccine, measles vaccine, mumps vaccine and rubella vaccine (MMR), bacterial toxoids, vaccinia virus, adenovirus vaccine, canary pox vaccine, polio vaccine virus, bacillus calmette guerin (BCG), klebsiella envelope vaccine, HIV envelope glycoproteins, bovine somatropine, oestrogen, androgens, prostaglandins, somatotropins, thyroid enzyme, pituitary enzyme, digestive enzyme, .alpha.-, .beta.- and .gamma.interferons, tuftsin, interleukins, insulin and insulin like growth factors, cytokines, steroids, terpenoids, triterpenes, retinoids, anti-ulcer H.sub.2 receptor antagonists, anti-ulcer drugs, hypoglycaemic agents, moisturizers, cosmetics, drugs, tetanus toxoid, diphtheria vaccine toxoid, pseudomonas A toxoid, mycobacterium tuberculosis vaccine toxoid, HIV envelope glycoproteins.

Details for Patent 6,214,375

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Glaxosmithkline Biologicals	HAVRIX	hepatitis a vaccine inactivated	Injection	103475	02/22/1995		2016-07-16
Seqirus Vaccines Limited	FLUVIRIN	influenza virus vaccine	Injection	103837	11/03/1998		2016-07-16
Sanofi Pasteur Inc.	FLUZONE, FLUZONE HD QUADRIVALENT, FLUZONE HIGH DOSE, FLUZONE INTRADERMAL, FLUZONE QUADRIVALENT	influenza virus vaccine	Injection	103914	12/09/1999		2016-07-16
Sanofi Pasteur Inc.	FLUZONE, FLUZONE HD QUADRIVALENT, FLUZONE HIGH DOSE, FLUZONE INTRADERMAL, FLUZONE QUADRIVALENT	influenza virus vaccine	Injection	103914	12/23/1909		2016-07-16
Sanofi Pasteur Inc.	FLUZONE, FLUZONE HD QUADRIVALENT, FLUZONE HIGH DOSE, FLUZONE INTRADERMAL, FLUZONE QUADRIVALENT	influenza virus vaccine	Injection	103914	05/09/2011		2016-07-16
Sanofi Pasteur Inc.	FLUZONE, FLUZONE HD QUADRIVALENT, FLUZONE HIGH DOSE, FLUZONE INTRADERMAL, FLUZONE QUADRIVALENT	influenza virus vaccine	Injection	103914	06/07/2013		2016-07-16