Medicine comprising lysine derivatives
United States Patent Tixier Apr. 8, 1975 MEDICINE COMPRISING LYSINE 86M 1/1961 France 424/319 DERIVATIVES 4,048M 4/1966 France 424/319 4,465M 9/l966 France [76] Inventor: Georges Tixier, 37, avenue dlena, 1 Paris France [22] Filed; on. 11, 1972 Chemical Abstracts 75: 889505 (l97l abstracting French Patent No. 2,036,045, 12/24/70. [211 APPl- 296,583 Merck Manual (1972 pp. 300403.  
 [30] Foreign Application Priority Data Primary E.\&#39;aminerStanley J. Friedman 0m. 13&#39;. 1971 France 71.301104 Assismm &#39;a nerNorman A. Drezin Attorney, Agent, or Firm-Browdy and Neimark [52] US. Cl. 424/319 [51] Int. Cl. ..A61K 15/12; A6lK 27/00 57 B C [58] Field of Search 424/319. 56, 84  
  The medicme contains lysine pantothcnate 1n sultable [56] References Cited form for re-establishing a normal figure of white blood FOREIGN PATENTS OR APPLICATIONS 87M 1/1961 France 424/319 1 cells in leukopenic patients.  
 8 Claims, N0 Drawings designed for the treatment of syndromes under consideration.  
  1 2 MEDICINE COMPRISING LYSINE DERIVATIVES Low] and digestive preparations The present invention relates to a medicine based on A derivatives of lysine. and especially the pantothenate of Lysine Pammhenme g this essential amino-acid; these derivatives are utilized, Atfimmllcd exclPitfm and h i b h Distilled water Q.S.P. 5 ml accor mg to t e invention. as suita e p armaceutical 1 m 3 ampules per day preparations; they are utilized to cause stimulation of Lysine pantothenate 0.25 g different metabolic mechanisms, particularly of the Excipiem 1 com! tablet ones related to the formation of leukocytes. m 2 to 5 tablets per day This invention takes advantage for therapeutic purf h I l d y k f d Lys ne pantothenate 0.40 g poses 0 t e property, not area y noun. 0 some e- Exclplcm Suppository rivatives of lysine to stimulate the production of leukol m 3 PP F P I r 2. -,ln cctable preparations cytes According to another characteristic of the invention. t i pjulttfithenute g g the lysine salts which are utilized can be included into thmugh ml very different pharmaceutical recipes. allowing the intrtl-jmuscuktr n trati n proper utilization of the same for human therapeutic l m &#34;mpuleb use.  
  The specific physiological activity of the lysine salts, Z0 1 to 2 ampule per d claimed in the present invention, is exemplified by a Th ti product i i n f th b e f group of experimental and clinical observations. lae can be, according to therapeutic needs, reduced up A. TOXlCO-PHARMACOLOGY to 7: or increased up to 50 71 of the above men- The lysine derivatives have no acute or lingering toxtioned quantities. icity. B CLINICALLY With respect to lysine pantothenate: The administration of lysine pantothenate at suitable the LD 50 is less than 10 g/kg by oral administration, (loses to patlems &#39;l leukopeljlla 0f &#34;anous enolo&#39; and gies. causes in a relatively short time, a return to northe LD 50 is less than 8 g/kg by parenteral adminisof the leukocymry &#34;&#34;W&#39; Panamtration. CASE NO. 1 The admi istrt ti in f th i ti 1 s. th e n h l j &#39;t durmg L. JOSEPHA 68 years old v r 5 r, 9 &#34;5 l Physical and psychical asthenia with anorexia, loss of non an anatomo-pa o ogica examinations ave not a weight poor general condition. ruealcd any impairment of the main organic systems 3. Treatment. lysine pantothenate 090 g per day for (muscles. nervous tissues, digestive and endocrine teen days r glands ulld&#39;excrellfl&#34; systemslr Improvement of the general condition. psychical and The leukopenia caused by various aggressive chemih i l cal and physical agents (medical poisons and radiations) are favorably influenced experimentally by the 40 administration of lysine derivatives. Leukocytes Particularly. the administration of lysine pantothenb f after ate to a rat made leukopenic through IIIJCCIIOII of cyclotreatment treatment phosphamide (Endoxan) 40 mg/kg caused an allevia- Numcmion 3000 8000 mm of the poisonous effects. While the leukocyte nu- Polynuclears 33% 59% in rat )f the r fe ence batch remain constant dur Elsl&#39;llphils c t e r I Lymphocytes 57% 34% mg the test. i.e.. less than the initial value. the animals Monocytes 3% 4% treated by the lysine derivatives have their number of leukocytes returning to normal and even become higher than the original value. CASE No. 2 l Thelfollowing table shows an abstract of a pharmaco- HAR&#39; JUUA 85 years Old Ogle! test Sequelae of a fractured femur, surgically treated. PERCENTAGE OF VARIATION IN RELATION TO 5g Treatment: lysine pantothenate 0.60 g per day for ten THE REFERENCE LEUKOCYTE NUMERATIONS y Slight clinical improvement.  
 Batch No 4th day 6th day l lth day 13th day Batch No 1 Reference 32.35 40.5 l6.9 i 1.67 60 Leukocytes Batch No 2 before after Lysine -49.6 -26.5 +26.2 +l6.5 treatment treatment Pantothenate Numeration 3600 6600 Polynuclcai&#39;s 33% 707: Eosino hils W: Z /r Lym hocytes 63% 25% As non-restrictive examples, below are g en formula Mongcym 3% 3% CASE N 3 lowvlghat is specifically claimed in this invention is as fol- GAREL 31 years old a. the evidence ofa property of lysine and of its deriv- Disseminated sclerosis with almost a total anorexia. mi d more especially of lysine pantothenate, Treatment: lysine pantothenate 0.90 g per day for ten 5 on h f mati f hi bl d corpuscles y b. the utilization of this physiological activity for Decreased of anorexla. therapeutical purposes and more particularly in the treatment of leukopenia, and c. the utilization of the lysine derivatives in pharma- Leukocytes ceutical preparations adapted to the considered before after therapeutical uses. treatment treatment I claim: Numeration 3300 7 m 1. A method of increasing the number of leukocytes i in a patient having leukopenia which comprises admin- Lymphocytes 62&#39;); 2.362 istering to said patient, lysine pantothenate in an 3% amount effective to increase the leukocyte numeration of said patient.  
  2. The method of claim 1 wherein said lysine pantothenate is administered orally.  
  3. The method of claim 1 wherein said lysine pantothenate is administered parenterally.  
 4. The method of claim I wherein said lysine panto- CASE No. 4  
 Cation) Treatment: 1.20 g of lysine pantothenate per day for thenate l ten duys 5. The method of claim 1 wherein said lysine pantothenate is in admixture with a pharmaceutically acceptable carrier.  
  6. The method of claim 2 wherein said lysine pantothenate is administered in a daily dose of 0.5 to L8 Clinical improvement.  
  Leukocytes I g m S- hetorc alter mmmcm mmmcm 7. The method of claim 3 wherein said lysine pantothenate is administered in a daily dose of 0.2 to 0.4 Numcrauon 6100 7 I00 P olynuclears 53! 6492 bosnwphlls 0 W 8. The method of claim 4 wherein said lysine panto- Lymphocytes 41&#39;} 23&#39; 1 th t d I d f 04 t l Mum.cs r; ena e is a minis ere m a at ose o o gms.