IL22712A - Composition for reducing the cholesterol content in the human body containing pentaerythrityl nicotinate - Google Patents
Composition for reducing the cholesterol content in the human body containing pentaerythrityl nicotinateInfo
- Publication number
- IL22712A IL22712A IL2271265A IL2271265A IL22712A IL 22712 A IL22712 A IL 22712A IL 2271265 A IL2271265 A IL 2271265A IL 2271265 A IL2271265 A IL 2271265A IL 22712 A IL22712 A IL 22712A
- Authority
- IL
- Israel
- Prior art keywords
- nicotinate
- pharmaceutical composition
- human body
- nicotinic acid
- cholesterol content
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
- C07D213/80—Acids; Esters in position 3
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Description
C O H E Z E D E S P I S B A C H PATENT ATTORNEYS 1169 I E L A V I V P A T E N T S D E S I G N S O R D I N A N C E SPECIFICATION COMPOSITION FOR REDUCING CONTENT IN THE HUMM CONTAINING PENTAERYTRITYL NICOTINATE Joint Stock of O HEREBY DECLARE the nature of this invention and in what manner the same is to be performed to be particularly described and ascertained in and by the following statement The present invention relates to a nicotinic acid compound reducing the cholesterol conten in the human It is known that pathological cholesterol tents in the blood can reduced the aid of nicotinic acid to normal use of nicotinic acid has considerable disadvantages for most patients which have been in having taken nicotinic acid in an appropriate they have a boon very strong flushing and strong in the This is an obvious which often results in that the treatment with nicotinic acid must be These disadvantages can be eliminated by producing certain esters of nicotinic although it is known that show lower such as and the same disadvantages as nicotinic acid for undergoing One ester has been meBoinosite whic does not cause flushing and prickliness of the but this ester has the disadvantage that it does not ably reduce the pathological cholesterol The problem is thus to find a compound from which nicotinic acid or nicotinic acid metabolites can be generated in the human body in such a way that said desired reduction of pathological cholesterol values can be obtained without any occurence of strong flushing or prickliness in the The invention provides a pharmaceutical composition h hl tr o n t huan bod comprising as active ingredient the compound erithritol This ingredient is included in combination with an inert pharmaceutically able diluent or nicotinate has the following Appearance4 White flaky Melting 163 trogen contenti If a patient is treated with this it been found that after a short time the logical cholesterol value is without any side effects such as flushing and prickliness in the The carrier preferably comprises a mixture of corn calcium stearate and talcum with or out and the compound and carrier may appropriately be pressed into tablet compound pentaerithritjsl nicotinate for be produced in the following 160 g of nicotinic acid chloride is charged into 100 g of carefully dried pyridine and the excess of nicotinic acid chloride are removed through repeated treatment with water at a of Through extraction with hydrochloric acid in 1000 ml of water at a pH of nicotinate is thereafter obtained from the chloroform by the hydrochloric acid salt of the The strongly acid saline solution is thereafter tracted several times with the acid saline solution is treated at room temperature for several hours with active carbon and filtered and precipitated 2 ammonia or other alkaline while The ester is then precipitated as a amorphous Recrystallization of the products in ethylalcohol gives flaky If of corn calcium stearate and talcum is used as the the tions between the pentaerithritol nicotinate and the mesoinositol can be and The tablets which are pressed therefrom can be given a weight of between g and The following description shows how a batch of tablets is g of pentaerithritol of mesoinositol and 320 g of corn are and moistened with of starch This mixture is granulated through a sieve 3 according to Pharmacopea edition and is dried at a temperature which can be up to according to Pharmacopea edition g of the granulate obtained is mixed with 210 g of talcum and 70 g of calcium Corn starch is added so that the mixture has a weight of mixture so tablets of g are the tablets having a diameter of 13 following composition can also be en aerithrityl nicotinate mesoinositbi com starch 340 starch paste 800 mixture is formed into a as g of this granulate is mixed with 120 g of 40 g of calcium and a quantity of corn tarch to the mixtu a total weight of tablets have a weigh g and a diameter of The pharmaceutical composition has been tested during several years and the following clinical observed from data have been on human peripherical disturbance as well as preparation is resorbed throug the duct the intestinal to a extent about It has been established by measuring with radioactive into being isotopes that a effect comes tha characterized in that nicotinic acid is continuously supplied to the blood circulation system and that signi increase of blood level of nicotinic acid takes In studies of muscle and an periferal blood flow is obtained in meaa and also in the skin of the out this is not so developed as the one through the forearm decrease A significant also been observed as regards the content of free fatty A significant decrease of the cholesterol has been found in patients with In many cases it has proved to to obtain reduction to a of the initial value stated before the In the treatment of peripheral circulatory has been observed that disturbances are clinically improved after treatment with the tion during some A criterion of that ef ect which for the healing of diabetic gangrene of considerable risks The beginning of the is characterized in the improvement of colour of the area of lesion with a growing healing of the edges of the Myocardial disturbances as angina pectoris have in many when the disease is due to coronal completely disappeared afte treatment with our pharmaceutical insufficientOCRQuality
Claims (8)
1. A pharmaceutical composition for reducing the cholesterol content in the human body comprising as active ingredient pentaerithrityL nicotinate.
2. A pharmaceutical composition for reduci g the cholesterol content in the human body comprising pentaerithritylnicotinate in combination with a pharmaceutically acceptable carrier.
3* A pharmaceutical composition for reducing the cholesterol content in the human body comprising pentaerithri¾& nicotinate in unit dosage form as active ingredient*
4· A pharmaceutical composition as claimed in Claim 3 comprising pentaerithritylnicotinate and meso inositol in a range of from about 3:1 to 1:1.
5* A pharmaceutical composition as claimed in Claim 3 or 4» in the form of tablets comprising per tablet from about 0.1 to 0.5 g of pentaerithrityl nicotinate. P.A. 22712 Pile 12706 17.IX.68
6. A pharmaceutical composition comprising pentaerithrite nieotinate in combination with corn starch, calcium stearate, talcum and possibly meso isonitol.
7. Method of producing a composition capable of releasing nicotinic acid in the human body in a quantity sufficient to reduce the cholestrol content in the blood without causing occurence of so-called flushing characterized in that nicotinic acid or a reactive nicotinic acid derivative is made to react with pentaerithritol or a pentaerithritol derivative, yielding pentaerithritol nicotinate with the following formulas and the compound thus obtained is mixed with a carrier substance which consists of corn starch,calcium stearate, talcum and possibly meso-inositol.
8. Procedure according to Claim £7, characterized obtained in that the mixture /is pressed into tablets. DATED THIS 29th day of December 1964 COHEN ZEDEK & SPISBACH P.O. Box 1169, Tel Aviv Attorneys for Applicants
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE1226564 | 1964-10-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL22712A true IL22712A (en) | 1969-02-27 |
Family
ID=20295449
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL2271265A IL22712A (en) | 1964-10-13 | 1965-01-01 | Composition for reducing the cholesterol content in the human body containing pentaerythrityl nicotinate |
Country Status (3)
| Country | Link |
|---|---|
| GB (1) | GB1022880A (en) |
| IL (1) | IL22712A (en) |
| NL (1) | NL6413246A (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3479364A (en) * | 1967-07-17 | 1969-11-18 | Searle & Co | Pyridinecarboxylic acid esters of benzenehexol |
-
1964
- 1964-11-13 NL NL6413246A patent/NL6413246A/xx unknown
- 1964-11-18 GB GB4701264A patent/GB1022880A/en not_active Expired
-
1965
- 1965-01-01 IL IL2271265A patent/IL22712A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| GB1022880A (en) | 1966-03-16 |
| NL6413246A (en) | 1966-04-14 |
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