Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heavy metal containing doai
Patent
1998-01-02
1999-10-19
Jones, Dwayne C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heavy metal containing doai
514512, 424715, 534 16, A01N 5502
Patent
active
059689765
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/GB96/00575 filed on Mar. 19, 1996.
This invention concerns a novel and inventive pharmaceutical composition and method, more particularly it concerns a composition for the treatment of hyperphosphataemia.
Hyperphosphataemia is a particular problem of patients with renal failure, using dialysis equipment. Conventional dialysis fails to reduce levels of phosphate in the blood, so that the levels rise in time. It is known to control phosphate levels by the oral administration of aluminium salts, or calcium salts. With the known toxic effects of aluminium, aluminium-based therapy tends to be avoided. In the case of calcium salts, calcium is absorbed rather readily from the gut, and in turn causes hypercalcaemia.
It has been suggested (Nakagawa et al, Trans Am Soc Intern Organs, 31, (1985) 155-9) that hydrous cerium oxide could be used as a bead in an ion-exchange column, to bind phosphate during dialysis. Japanese published patent application 61 004 529 appears to cover the same idea, suggesting that the hydrous oxides of La, Ce and Y may be used in the column. However, although the rare earths are generally considered of low toxicity according to the Hodge-Sterner classification system (Am Ind Hyg Assoc Quart, 10, (1943), 93), their toxicity when given iv, which corresponds to use in a blood dialysis system, is significant and we are not aware that the suggested ion exchange system or any development thereof has met with widespread acceptance or has been tested clinically for hyperphosphataemia.
It appears that cerium oxide or oxalate was administered many years ago for different medical indications, but that this has fallen into complete disuse.
Japanese published patent application number 62-145024 (Asahi Chemical Ind KK) discloses that rare earth carbonates, bicarbonates or organic acid compounds may be used as phosphate binding agents. One example of said published application relates to the use of lanthanum carbonate, although in the tests described, cerium organic acid salts and carbonate gave better phosphate ion extraction than lanthanum carbonate. Example 11 of said published application prepares La.sub.2 (CO.sub.3).sub.3.H.sub.2 O, ie the monohydrate; all the other Examples are directed to rare earth carbonates other than lanthanum carbonate.
We have now discovered that certain forms of lanthanum carbonate exhibit improved performance in a variety of tests, over standard commercial lanthanum carbonate, which is believed to be the octahydrate form, and over La.sub.2 (CO.sub.3).sub.3.H.sub.2 O or similar compounds.
According to one aspect therefore, the present invention is the use of lanthanum carbonate of formula La.sub.2 (CO.sub.3).sub.3.xH.sub.2 O where x has a value from 3 to 6, preferably from 3.5 to 5, more especially from 3.8 to 4.5, for the preparation of a medicament for the treatment of hyperphosphataemia by administration into the gastrointestinal tract.
The invention further provides a pharmaceutical composition comprising said lanthanum carbonate, in admixture or association with a pharmaceutically acceptable diluent or carrier, in a form for administration into the gastrointestinal tract for the treatment of hyperphosphataemia.
The invention may also be expressed as a method of treatment of hyperphosphataemia in a patient with renal failure, comprising the administration of an effective dose of said lanthanum carbonate into the gastrointestinal tract.
According to another aspect, the present invention is a process for the preparation of lanthanum carbonate which comprises the steps of: lanthanum; metal carbonate to produce a wet cake of lanthanum carbonate octahydrate; and so as to obtain a lanthanum carbonate with 3 to 6 molecules of water of crystallisation.
According to yet another aspect, the present invention is lanthanum carbonate when obtained by the above-mentioned process.
According to a further aspect, the present invention is lanthanum carbonate of the formula La.sub.2 (CO.sub.3).sub.3.xH.sub.2 O where x has a value from 3 to 6.
BRIEF DESCRI
REFERENCES:
Yanagihara et al., "Synthesis of Lanthanide Carbonates", Journal of the Less-Common Metals, 167(2) pp. 223-232, 1991.
Patent Abstract of vol. 11, No. 371, (C-462), Dec. 3, 1987 & JP, A, 62 145024 (Asahi Chem Ind Co Ltd), Jun 29, 1987.
Chemical Abstracts, vol. 107, No. 26, Dec. 28, 1987, abstract No. 249009, Mineely et al., "Molten potassium pyrosulfate: reactions of lanthanum metal and six of its compunds", XP002010788, see abstract, Aust. J. Chem. 40(7), pp. 1309-1314, 1987.
Chemical Abstracts, vol. 104, No. 26, Jun. 30, 1986, abstract No. 236218, Mzareulisvili et al., "Study of interaction of lanthanum nitrate with alkali metal and ammonium carbonates", XP002010789, Soobshch. Akad. Nauk Gruz. 121(1), pp. 81-84, (1986).
Chemical Abstracts, vol. 87, No. 20, Nov. 14, 1977, abstract No. 161013, Oda et al., "Studies on the crystal water of lanthanum carbonates", XP002010790, Oita Daigaku Kyoikygakubu Kenku Kiyo, Shizen Kagaku, 4(5), pp. 1-6, 1975.
Murrer Barry A
Powell Nigel A
Anormed Inc.
Jones Dwayne C.
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