POLYPRENYL ALCOHOL-CONTAINING INJECTIONS AND USE THEREOF

Abstract: Polyprenyl alcohol-containing injections comprising polyprenyl alcohols shown by formula: wherein n is an integer of 5 to 7, and lecithin as essential ingredients. The subject injections can enhance utilization of the polyprenyl alcohols contained therein in vivo, thereby in­ fectious diseases in human or animals are effectively preven­ ted or treated. The above polyprenyl alcohols and lecithin may be used in the preparation of an injection for the preven­ tion and treatment of diseases caused by human or animal immunodeficiency and infectious diseases in humans or ani­ mals.

Description: FIELD OF THE INVENTION The present invention relates to polyprenyl alcohol-containing injections. More particularly, the present invention relates to polyprenyl alcohol-containing injections which aim at enhancing utilization of polyprenyl alcohol in vivo. BACKGROUND OF THE INVENTION BRIEF DESCRIPTION OF THE PRIOR ART Polyprenyl alcohols shown by formula: wherein n is an integer of 5 to 7, act to prevent and treat diseases caused by human or animal immunodeficiency and are particularly effective against infectious diseases of human or animals. The polyprenyl alcohols are already known in Japanese Laid-open Patent Application (KOKAI) No. 58206517. The polyprenyl alcohols are generally administered in the form of injections. The present inventors have made investigations for purposes of enhancing utilization of the polyprenyl alcohols in vivo when they are administered in the form of injections. As a result, the inventors have found that the aimed object has been achieved when the alcohols were administered together with lecithin and thus accomplished the present invention. SUMMARY OF THE INVENTION That is, an object of the present invention is to enhance utilization of the polyprenyl alcohols in accordance with the present invention in vivo . For achieving the purpose, the present invention provides polyprenyl alcohol-containing injections comprising polyprenyl alcohols shown by formula: wherein n is an integer of 5 to 7, and lecithin as essential ingredients. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS In the field of medical preparations, a technique in which lecithin is incorporated to effectively exhibit actions of drugs has been hitherto known, as shown in, for example, Japanese Laid-open Patent Application (KOKAI) Nos. 135,416/81, 150,508/83, 47,608/80 and 75,916/82. However, it is unknown that utilization of the polyprenyl alcohols in vivo could be markedly improved by incorporating lecithin in the polyprenyl alcohol. Hereafter the present invention will be described in detail. In the present invention, the polyprenyl alcohols are shown by formula: wherein n is an integer of 5 to 7. Specific examples of the polyprenyl alcohols include Compounds A, B and C described below. Compound A: 3,7,11,15,19,23-Hexamethyl-6,10,14,18,22-tetracosapentaen-1-ol Compound B: 3,7,11,15,19,23,27-Heptamethyl-6,10,14,18,22,26-octacosahexaen-1-ol Compound C: 3,7,11,15,19,23,27,31-Octamethyl-6,10,14,18,22,26,30-dotriacontaheptaen-1-ol Lecithin in accordance with the present invention is extracted from yolk and soyebean; if necessary, further purified phospholipid-containing materials or hydrogenated products thereof or synthetic glycerophosphates, can also be used. The injection of the present invention can be administered in any form of subcutaneous, intramuscular and intravenous injections. The injection of the present invention can be prepared in a conventional manner of producing injection. While there is no particular limitation of contents of the polyprenyl alcohol and lecithin in accordance with the present invention in the injection of the present invention, it is preferrred that the polyprenyl alcohol content and the lecithin content be in ranges of 0.01 to 10% (w/w) and 0.01 to 10% (w/w), respectively. The present invention will be concretely described with reference to the examples described below. Example 1 3,7,11,15,19,23-Hexamethyl-6,10,14,18,22-tetracosapentaen-1-ol (Compound A, 1.0 g), 1.5 g of soybean lecithin, 0.7 g of sesame oil, 5.0 g of D-sorbitol and 5.0 g of propylene glycol were mixed with heating and distilled water was added to the mixture to make the volume 100 ml. The mixture was treated ultrasonically and filtered, and the filtrate was filled in an ampoule. The air in the ampoule was replaced by N₂ gas. The ampoule was sealed and sterilized by heating to make an injection. Example 2 An injection was prepared in a manner similar to Example 1 except that 3,7,11,15,19,23,27-pentamethyl-6,10,14,18,22,26-octacosahexaen-1-ol (Compound B) was used in lieu of Compound A in Example 1. Example 3 An injection was prepared in a manner similar to Example 1 except that 3,7,11,15,19,23,27,31-octamethyl-6,10,14,18,22,26,30-dotriacontaheptaen-1-ol (Compound C) was used in lieu of Compound A in Example 1. The effect of the present invention is explained with reference to the following experiments. Experiment 1 Sample and Method: Injections obtained in Examples 1 to 3 were used as samples. Each injection was intramuscularly administered to ICR male mice (6 to 7 week age, weighing 22 to 30 g) at a dose described in Table 1, column of "Dose". After 24 hours, 2.8 × 10⁸ CFU/mouse of clinically derived Escherichia coli was subcutaneously inoculated. A survival rate was determined from the number of living mice 7 days after infection. Separately, injections were prepared as in Examples 1 to 3 except that HCO-60 (Polyoxyethylene (60 mol.)-Hydrogenated Castor Oil) was used instead of soybean lecithin in Examples 1 to 3. The injections were used as comparison samples. With respect to the comparison samples, survival rates were determined in a manner similar to the above samples. Results: The results are shown in Table 1, in which numerical values within parenthesis show the number of living mice/the number of mice tested. From the results of Table 1, it is noted that the injection of the present invention enhances utilization of polyprenyl alcohol in accordance with the present invention in vivo . Experiment 2 Sample and Method: The sample and the comparison sample obtained using Compound B were chosen from the samples used in Experiment 1 an intravenously injected to ICR mice (6 week age, weighing 20 to 30 g), respectively. After 24 hours 1.2 × 10⁷ CFU/mouse of Escherichia coli was subcutaneously inoculated. Each survival rate was determined from the number of living mice 7 days after infection. Results: The results are shown in Table 2, in which numerical values within parenthesis shows the number of living mice/the number of mice tested. From the results, the fact similar to Experiment 1 is noted. Experiment 3 Sample and Method: An injection was prepared in a manner similar to Example 2 except that yolk lecithin was used instead of soybean lecithin in Example 2. The injection was used as a sample. The injection was intramuscularly administered to ICR mice (6 week age, weighing 30 g). After 24 hours, 6.9 × 10⁷ CFU/mouse of clinically derived Escherichia coli was subcutaneously inoculated. A survival rate was determined from the number of living mice 7 days after infection. Results: The results are shown in Table 3, in which numerical values within parenthesis show the number of living mice/the number of mice tested. From the results, the fact similar to Experiment 1 is noted. The polyprenyl alcohols of the present invention and lecithin may be used in the preparation of an injection for the prevention and treatment of diseases caused by human or animal immunodeficiency. The polyprenyl alcohols of the present invention and lecithin may also be used in the preparation of an injection effective against infectious diseases in humans or animals.

Claims: Claims for the Contracting States BE CH DE FR GB IT LI LU NL SE: 1. A polyprenyl alcohol-containing injection comprising a polyprenyl alcohol shown by formula: wherein n is an integer of 5 to 7, and lecithin as essential ingredients. 2. A polyprenyl alcohol-containing injection as claimed in claim 1 wherein said polyprenyl alcohol is contained in an amount of 0.01 to 10% (w/w) and lecithin is contained in an amount of 0.01 to 10% (w/w). 3. Use of a polyprenyl alcohol of formula: wherein n is an integer of 5 to 7, and lecithin in the preparation of an injection for the prevention and treatment of diseases caused by human or animal immunodeficiency and infectious diseases of humans or animals. Claims for the Contracting States AT ES GR: 1. A process for preparing a polyprenyl alcohol-containing injection characterized by mixing a polyprenyl alcohol shown by formula: wherein n is an integer of 5 to 7, and lecithin as essential ingredients. 2. A process for preparing a polyprenyl alcohol-containing injection as claimed in claim 1 characterized in that said polyprenyl alcohol and lecithin are mixed in an amount such that each comprises 0.01 to 10% by weight of the final product. 3. A process for preparing a polyprenyl alcohol-containing injection according to claim 1 or 2 characterized in that said lecithin is soya bean lecithin. 4. Use of a polyprenyl alcohol of formula: wherein n is an integer of 5 to 7, and lecithin in the preparation of an injecticn for treating and preventing diseases caused by human or animal immunodeficiency and infectious diseases in humans or animals.

Inventors: ARAKI, SEIICHI, IDA, KATSUMI, IKEUCHI, TAKAYUKI, KITOH, KYOSUKE, KOYAMA, NORITOSHI
Applicants: EISAI CO., LTD.
Application year: 1987
Main classification: A61K31
IPC codes: A61K47, A61P37, A61K31, A61K9