CA2003720A1 - Lipid emulsion for treating aids - Google Patents
Lipid emulsion for treating aidsInfo
- Publication number
- CA2003720A1 CA2003720A1 CA002003720A CA2003720A CA2003720A1 CA 2003720 A1 CA2003720 A1 CA 2003720A1 CA 002003720 A CA002003720 A CA 002003720A CA 2003720 A CA2003720 A CA 2003720A CA 2003720 A1 CA2003720 A1 CA 2003720A1
- Authority
- CA
- Canada
- Prior art keywords
- approximately
- percent
- weight
- emulsion
- composition
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
- A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
Abstract
ABSTRACT
A composition for the treatment of patients having Acquired Immune Deficiency Syndrome comprising approximatley 2 to 7 percent by weight soybean oil and approximately 1 to 2 percent by weight egg phosphatide and a method for the parenteral administration of this composition is disclosed.
4632.US.O1
A composition for the treatment of patients having Acquired Immune Deficiency Syndrome comprising approximatley 2 to 7 percent by weight soybean oil and approximately 1 to 2 percent by weight egg phosphatide and a method for the parenteral administration of this composition is disclosed.
4632.US.O1
Description
~003~
LIPID EMULSION FOR TREATING AIDS
FIELD OF THE INVENTION
The present invention relates to a composition and method for treating patients with Acquired Immune Deficiency Syndrome. More particularly, this invention relates to a composition for the parenteral administration of a non- or low carbohydrate source of calories for nutritional support and phosphatides to stimulate prostaglandin synthesis.
BACKGROUND OF THE INVENTION
The number of patients suffering from Acquired Immune Deficiency Syndrome (AIDS) has increased dramatically since the first cases were reported a few years ago. The disease has caused opportunistic infections and secondary cancers in more than 50,000 people in the United States and many more throughout the world. Patients suffering from AIDS are often nutritionally unbalanced and wasted. Weight loss and decrease in serum albumin, total iron binding capacity and retinal binding protein are often seen. Body composition analysis in AIDS patients demonstrates a depletion in total body potassium and body fat content with an increase in extracellular water. These symptoms are often seen in those suffering from chronic malnutrition.
A number of factors lead to malnutrition in AIDS patients. These include a decrease in food intake, vomiting, the side effects of therapeutic drugs and a high incidence of malabsorption syndrome with or without dlarrhea.
When malabsorption syndrome and/or diarrhea do not permit effective oral feeding, parenteral nutrition 2 ~3~ ~ O
is indica~ed. Conventional parenteral nutrition compositions and methods of therapy are unbalanced attempts at nutritional restitution. They contain too high a fat content which, if administered too rapidly, can exacerbate the formation of pro-inflammatory prostanoids and prevent the beneficial effects of low-fatty acid administration. This invention permits administration of the desired level of egg phospholipids and triglycerides over a longer period of time without exacerbating pro-inflammatory prostanoids or inducing fat overload.
It is also known that some of the manifestations of AIDS are ameliorated by non-steroidal anti-inflammatory agents. It is believed that these effects are related to a preferential suppression of certain prostaglandins by these agents. Prostaglandins are synthesized in the body from fatty acid precursors which are derived from lipids. The composition, rate of administration and concentration of neutral lipids, fatty acids and lecithins administered parenterally can determine the prostaglandin synthetic pathway and thereby the specific class of eicosanoid being preferentially synthesized.
Thus, there is a need for a low fat - high phosphatide parenteral formulation for the treatment of AIDS patients either as a component of total parenteral nutrition o as a parenteral supplement to patients receiving nutrition orally.
SUMMARY OF THE INVENTION
In accordance with the present invention, there is provided a composition and a method for the treatment of AID~ patients which comprises parenterally administering to such patients a composition comprising a soybean oil emulsion containing egg phosphatide. More 2~ %~
particularly, the compositions contain approximately 2 to 7 percent by weight soybean oil and approximately 1 to 2 percent by weight egg phosphatide. The compositions of this invention contain a higher egg phosphatide/triglyceride ratio, in comparison to commercially available fat emulsions, in the range of about 1:1 to 1:3 which makes it possible to provide a sufficient level of egg phosphatide to promote mobilization of tissue cholesterol without inducing fat overload.
DESCRIPTION OF THE PREFERRED_EMBODIMENTS
The presently preferred parenteral compositions of this invention contain approximately 2 percent by weight soybean oil and approximately 1.2 percent by weight egg phosphatide.
The most preferred parenteral composition of the present invention contains the following:
Inqredient Per mL
Soybean Oil, Wiwnterized 20 mg Egg Phosphatide 12 mg Glycerin, USP 25 mg Nitrogen, USP q.s.
Sodium Hydroxide q.s.
Water q.s.
The soybean oil utilized in the composition of the present invention may be obtained from any commercially available source and should have a fatty acid composition of from about 44 to about 62 weight percent linoleic acid, from about 19 to about 30 weight percent oleic acid, from about 7 to about 14 weight percent palmitic acid, from about 1 to about 6 weight percent stearic acid, and from about 4 to about 11 3~72~) weight percent linolenic acid. The egg phosphatide utilized in the composition of the present invention may also be obtained from commercially available sources and should preferably ha~e a nitrogen to phosphorous molar ratio of from about 0.97 to about 1.17.
The composition of the present invention may be prepared in accordance with known procedures in the art as illustrated by the following example.
Water for injection (approximately 1 L) is heated and protected by a nitrogen atmosphere. Egg phosphatide (12g) is added to the wa~er and dispersed by agitation at a temperature in the range of 50 to 90C.
Glycerin (25g) is filtered through an 0.8 micrometer membrane filter and added to the dispersion using a Manton-Gaulin homogenizer to finely divide the egg phosphatide and increase the degree of dispersion. The aqueous phosphatide dispersion is then filtered through a nylon or equivalent membrane of 0.45 micrometer porosity and the pH is adjusted to a range of 8.5 to 10.5 with sodium hydroxide. Soybean oil, winterized, (20g) is filtered through a 0.45 micrometer membrane, heated to a temperature in the range of 55 to 95C and added to the egg phosphatide dispersion with agitation to form a coarse emulsion concentrate which is then homogenized using a Manton-Gaulin homogenizer at a pressure of 2000 to 5000 psi. The pH is then adjusted to a rang~ of 8.5 to 9.5, if necessary, with sodium hydroxide and the emulsion is filtered through a nylon membrane of at least 0.8 micrometer porosity with sufficient surface area to provide minimum restriction of flow. The emulsion is then further homogenized in a Manton-Gaulin homogenizer, diluted to a desired concentration with sterile water and the pH adjusted to ~3~
a range of 8.5 to 9.6 with sodium hydroxide.
When used in treating patients with AIDS the emulsions of this invention should be administered parenterally in amounts su~ficient to provide approximately 50 to 30 mL/Kg day.
.
LIPID EMULSION FOR TREATING AIDS
FIELD OF THE INVENTION
The present invention relates to a composition and method for treating patients with Acquired Immune Deficiency Syndrome. More particularly, this invention relates to a composition for the parenteral administration of a non- or low carbohydrate source of calories for nutritional support and phosphatides to stimulate prostaglandin synthesis.
BACKGROUND OF THE INVENTION
The number of patients suffering from Acquired Immune Deficiency Syndrome (AIDS) has increased dramatically since the first cases were reported a few years ago. The disease has caused opportunistic infections and secondary cancers in more than 50,000 people in the United States and many more throughout the world. Patients suffering from AIDS are often nutritionally unbalanced and wasted. Weight loss and decrease in serum albumin, total iron binding capacity and retinal binding protein are often seen. Body composition analysis in AIDS patients demonstrates a depletion in total body potassium and body fat content with an increase in extracellular water. These symptoms are often seen in those suffering from chronic malnutrition.
A number of factors lead to malnutrition in AIDS patients. These include a decrease in food intake, vomiting, the side effects of therapeutic drugs and a high incidence of malabsorption syndrome with or without dlarrhea.
When malabsorption syndrome and/or diarrhea do not permit effective oral feeding, parenteral nutrition 2 ~3~ ~ O
is indica~ed. Conventional parenteral nutrition compositions and methods of therapy are unbalanced attempts at nutritional restitution. They contain too high a fat content which, if administered too rapidly, can exacerbate the formation of pro-inflammatory prostanoids and prevent the beneficial effects of low-fatty acid administration. This invention permits administration of the desired level of egg phospholipids and triglycerides over a longer period of time without exacerbating pro-inflammatory prostanoids or inducing fat overload.
It is also known that some of the manifestations of AIDS are ameliorated by non-steroidal anti-inflammatory agents. It is believed that these effects are related to a preferential suppression of certain prostaglandins by these agents. Prostaglandins are synthesized in the body from fatty acid precursors which are derived from lipids. The composition, rate of administration and concentration of neutral lipids, fatty acids and lecithins administered parenterally can determine the prostaglandin synthetic pathway and thereby the specific class of eicosanoid being preferentially synthesized.
Thus, there is a need for a low fat - high phosphatide parenteral formulation for the treatment of AIDS patients either as a component of total parenteral nutrition o as a parenteral supplement to patients receiving nutrition orally.
SUMMARY OF THE INVENTION
In accordance with the present invention, there is provided a composition and a method for the treatment of AID~ patients which comprises parenterally administering to such patients a composition comprising a soybean oil emulsion containing egg phosphatide. More 2~ %~
particularly, the compositions contain approximately 2 to 7 percent by weight soybean oil and approximately 1 to 2 percent by weight egg phosphatide. The compositions of this invention contain a higher egg phosphatide/triglyceride ratio, in comparison to commercially available fat emulsions, in the range of about 1:1 to 1:3 which makes it possible to provide a sufficient level of egg phosphatide to promote mobilization of tissue cholesterol without inducing fat overload.
DESCRIPTION OF THE PREFERRED_EMBODIMENTS
The presently preferred parenteral compositions of this invention contain approximately 2 percent by weight soybean oil and approximately 1.2 percent by weight egg phosphatide.
The most preferred parenteral composition of the present invention contains the following:
Inqredient Per mL
Soybean Oil, Wiwnterized 20 mg Egg Phosphatide 12 mg Glycerin, USP 25 mg Nitrogen, USP q.s.
Sodium Hydroxide q.s.
Water q.s.
The soybean oil utilized in the composition of the present invention may be obtained from any commercially available source and should have a fatty acid composition of from about 44 to about 62 weight percent linoleic acid, from about 19 to about 30 weight percent oleic acid, from about 7 to about 14 weight percent palmitic acid, from about 1 to about 6 weight percent stearic acid, and from about 4 to about 11 3~72~) weight percent linolenic acid. The egg phosphatide utilized in the composition of the present invention may also be obtained from commercially available sources and should preferably ha~e a nitrogen to phosphorous molar ratio of from about 0.97 to about 1.17.
The composition of the present invention may be prepared in accordance with known procedures in the art as illustrated by the following example.
Water for injection (approximately 1 L) is heated and protected by a nitrogen atmosphere. Egg phosphatide (12g) is added to the wa~er and dispersed by agitation at a temperature in the range of 50 to 90C.
Glycerin (25g) is filtered through an 0.8 micrometer membrane filter and added to the dispersion using a Manton-Gaulin homogenizer to finely divide the egg phosphatide and increase the degree of dispersion. The aqueous phosphatide dispersion is then filtered through a nylon or equivalent membrane of 0.45 micrometer porosity and the pH is adjusted to a range of 8.5 to 10.5 with sodium hydroxide. Soybean oil, winterized, (20g) is filtered through a 0.45 micrometer membrane, heated to a temperature in the range of 55 to 95C and added to the egg phosphatide dispersion with agitation to form a coarse emulsion concentrate which is then homogenized using a Manton-Gaulin homogenizer at a pressure of 2000 to 5000 psi. The pH is then adjusted to a rang~ of 8.5 to 9.5, if necessary, with sodium hydroxide and the emulsion is filtered through a nylon membrane of at least 0.8 micrometer porosity with sufficient surface area to provide minimum restriction of flow. The emulsion is then further homogenized in a Manton-Gaulin homogenizer, diluted to a desired concentration with sterile water and the pH adjusted to ~3~
a range of 8.5 to 9.6 with sodium hydroxide.
When used in treating patients with AIDS the emulsions of this invention should be administered parenterally in amounts su~ficient to provide approximately 50 to 30 mL/Kg day.
.
Claims (6)
1. An emulsion composition for parenteral adminis-tration comprising approximately from about 2 to about 7 percent by weight soybean oil and approximately from about 1 to about 2 percent by weight egg phosphatide.
2. An emulsion as in Claim 1, wherein the soybean oil comprises aproximately 2 percent by weight of said emul-sion and the egg phosphatide comprises approximately 1.2 percent by weight of said emulsion.
3. An emulsion as in Claim 1 having a pH in the range of approximately 8.5 to approximately 9.5.
4. An emulsion as in Claim 1 which contains glyc-erine.
5. The use of an emulsion composition according to Claim 1 against Acquired Immune Deficiency Syndrome, in host mammal, said composition comprising approximately from about 2 to 7 percent by weight soybean oil, and approximately from about 1 to about 2 percent by weight egg phosphatide.
6. The use of an emulsion composition according to Claim 5, wherein the effective amount used is in the range of approximately 5 to 30 mL/Kg.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US27618188A | 1988-11-23 | 1988-11-23 | |
US276,181 | 1988-11-23 |
Publications (1)
Publication Number | Publication Date |
---|---|
CA2003720A1 true CA2003720A1 (en) | 1990-05-23 |
Family
ID=23055541
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA002003720A Abandoned CA2003720A1 (en) | 1988-11-23 | 1989-11-23 | Lipid emulsion for treating aids |
Country Status (8)
Country | Link |
---|---|
US (1) | US5134130A (en) |
EP (1) | EP0370457B1 (en) |
JP (1) | JPH02184633A (en) |
AU (1) | AU641369B2 (en) |
CA (1) | CA2003720A1 (en) |
DE (1) | DE68903930T2 (en) |
ES (1) | ES2053925T3 (en) |
GR (1) | GR3006646T3 (en) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5817646A (en) * | 1991-11-15 | 1998-10-06 | Laboratoires Inocosm | Polar lipid composition of plant origin |
US6784326B1 (en) * | 1998-06-17 | 2004-08-31 | Cognis Corporation | Process for improving stability of glycerin |
US20080187562A1 (en) * | 2007-02-02 | 2008-08-07 | Aixing Fan | Antiperspirant/Deodorant Compositions |
US9789038B2 (en) | 2007-02-02 | 2017-10-17 | Colgate-Palmolive Company | Antiperspirant/deodorant compositions |
US7976828B2 (en) * | 2007-02-02 | 2011-07-12 | Colgate-Palmolive Company | Antiperspirant/deodorant composition |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA725596A (en) * | 1960-08-26 | 1966-01-11 | J. Wretlind Arvid | Method of preparing intravenously injectable fat emulsions free from side reactions or complications |
DE1249454B (en) * | 1960-08-26 | 1967-09-07 | Vitrum Apoteksvar | Process for the preparation of intravenously administrable fat emulsions |
DE2533612A1 (en) * | 1974-08-19 | 1976-03-04 | Pharmacia Ab | PARENTERALLY ADMINISTRATIVE OIL AND PROCESS FOR ITS MANUFACTURING |
US4073943A (en) * | 1974-09-11 | 1978-02-14 | Apoteksvarucentralen Vitrum Ab | Method of enhancing the administration of pharmalogically active agents |
US4157404A (en) * | 1978-07-28 | 1979-06-05 | Asahi Kasei Kogyo Kabushiki Kaisha | Process for obtaining yolk lecithin from raw egg yolk |
JPS5810365B2 (en) * | 1978-09-08 | 1983-02-25 | 田辺製薬株式会社 | fat emulsion |
GB2046092B (en) * | 1979-03-05 | 1983-11-02 | Toyama Chemical Co Ltd | Pharmaceutical composition containing a lysophospholid and a phospholipid |
DE2948607A1 (en) * | 1979-12-03 | 1981-06-11 | Chemische Fabrik Dr. Meyer-Castens & Co Nfg., 2000 Hamburg | METHOD FOR PRODUCING A LECITHIN-BASED EMULSIFIER |
US4677099A (en) * | 1981-09-04 | 1987-06-30 | Yeda Research And Development Co., Ltd. | Medical processes employing a novel lipid fraction |
IL63734A (en) * | 1981-09-04 | 1985-07-31 | Yeda Res & Dev | Lipid fraction,its preparation and pharmaceutical compositions containing same |
DE3339236A1 (en) * | 1983-10-28 | 1985-05-09 | Bayer Ag | PREPARATION OF MEDICINAL PRODUCTS |
EP0145873B1 (en) * | 1983-12-16 | 1989-01-04 | TERUMO KABUSHIKI KAISHA trading as TERUMO CORPORATION | Transfusion emulsion |
NO862999L (en) * | 1985-07-26 | 1987-01-27 | Yeda Res & Dev | LIPID MIXTURE FOR MEMBRANE FLUIDIZATION. |
IL78930A0 (en) * | 1985-07-29 | 1986-09-30 | Abbott Lab | Lyophilized emulsion compositions for parenteral administration |
US4857514A (en) * | 1985-09-17 | 1989-08-15 | Yeda Research And Development Company, Ltd. | Virus inactivation |
-
1989
- 1989-11-21 JP JP1303055A patent/JPH02184633A/en active Pending
- 1989-11-21 ES ES89121512T patent/ES2053925T3/en not_active Expired - Lifetime
- 1989-11-21 DE DE8989121512T patent/DE68903930T2/en not_active Expired - Fee Related
- 1989-11-21 EP EP89121512A patent/EP0370457B1/en not_active Expired - Lifetime
- 1989-11-22 AU AU45451/89A patent/AU641369B2/en not_active Expired - Fee Related
- 1989-11-23 CA CA002003720A patent/CA2003720A1/en not_active Abandoned
-
1991
- 1991-08-21 US US07/751,597 patent/US5134130A/en not_active Expired - Fee Related
-
1992
- 1992-12-23 GR GR920403094T patent/GR3006646T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
EP0370457A1 (en) | 1990-05-30 |
JPH02184633A (en) | 1990-07-19 |
DE68903930T2 (en) | 1993-05-19 |
GR3006646T3 (en) | 1993-06-30 |
DE68903930D1 (en) | 1993-01-28 |
ES2053925T3 (en) | 1994-08-01 |
AU641369B2 (en) | 1993-09-23 |
US5134130A (en) | 1992-07-28 |
EP0370457B1 (en) | 1992-12-16 |
AU4545189A (en) | 1990-05-31 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FZDE | Discontinued |