Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1996-06-17
1998-09-01
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
A61K 3170
Patent
active
058011617
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP94/101567 filed May 13, 1994.
The invention is related to a pharmaceutical composition for the intranasal administration of hydroxocobalamin, a substance from the Vitamin B12 family.
Vitamin B12 has been first isolated in 1948 and since that time it is widely used in therapeutically active drugs in the treatment of pernicious anemia and other vitamin B12 deficiency disorders. These diseases are mainly caused by an inadequate absorption of Vitamin B12 from the gastrointestinal tract.
Vitamin B12 occurs in the human body as methylcobalamin, adenosylcobalamin, hydroxocobalamin and cyanocobalamin. Only cyanocobalamin and hydroxocobalamin are used in the treatment of patients.
Oral, sublingual as well as nasal administration of Vitamin B12 appeared to be ineffective treatments and therefore administration by intramuscular injection is the only satisfactory and medically accepted therapy up to now. However, intramuscular injections of Vitamin B12 have many disadvantages, especially because this drug is often administered to older people. Such people may have reduced muscle mass or are atrophic, so that repeated injections are inconvenient and painful, and also require doctor's visits. Maintenance therapy with Vitamin B12 means at least monthly injections and must be continued for life.
Already in 1953 Monto et al (Am. J. Med. Sci., 1953, Vol.225, pages 113-119) published a study related to an alternative route for administering Vitamin B12, i.e. nasal inhalation aiming at deposition of therapeutically active material in the lungs. Cyanocobalamin in lactose powder and in physiological saline solutions, containing 15 to 200 .mu.g crystalline cyanocobalamin per ml, were used for nasal inhalation. The results of this investigation of Vitamin B12 administration by inhalation were reported as encouraging, but constituting only preliminary observations regarding the efficiency of inhalation crystalline cyanocobalamin treatment of pernicious anemia. The publication mentioned that intranasal B12 drops and dust, as routes of administration, were also under investigation by that time.
Israels and Shubert (The Lancet, Feb. 13, 1954, pages 341-343) stressed the disadvantage of having no alternative for the intramuscular administration of Vitamin B12 and published some experiences supporting some of the findings of Monto et al (1953), i.e. Vitamin B12 seems to be therapeutically effective when administered by inhalation as a powder.
In 1954 Monto et al published further experiences, with nasal inhalation and installation of crystalline Vitamin B12 (Arch. of Int. Med. 93, 1954, pages 219-230). They reported a good hemopoietic effect after nasal administration of cyanocobalamin in lactose powder or in a dose of 100 .mu.g per ml in a saline solution. Although the therapy was characterized as being not only effective but safe and economical, there was no follow up or any factual medical use of the therapy in the subsequent decennia. Since the urgent need for an alternative administration route continued to exist, apparently, the conclusions in the publications were too optimistic.
Other proposals for intranasal administration of Vitamin B12 are described in PCT/US 86/00665 and PCT/US 86/00793. Both proposals are based on the assumption that previous experiments failed, because of the fact that the administered cyanocobalamin, in a solution or powder, did not remain in the nasal cavity, but passes the nose to the throat or lungs. To solve this problem, both patent applications propose that the nasal formulation should stay for a much longer time in the nasal cavity. To obtain this longer residence time the formulation is administered in the form of an aerosol (PCT/US/86/00665) or the formulation should possess an enhanced viscosity, above 2500 cP (PCT/US/86/00793). This should give a consistent, continuous and uniform absorption of Vitamin B12. A concentration from 0.05% to 1% by weight based on the total weight is described as typical concentrations of Vitamin B12 in the compositions of both pat
REFERENCES:
patent: 3903253 (1975-09-01), Rolland
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