Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-04-08
1999-09-28
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514974, A61K 31545
Patent
active
059589159
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to a new antibacterial composition of Cefditoren pivoxyl for use in oral administration, which has a reduced or minimized bitter taste to patients upon oral administration thereof and is quickly soluble in water and also attaining a high absorbability of the Cefditoren component at the digestive tubes, and which composition comprises a mixture of Cefditoren pivoxyl with a proportion of a pharmaceutically acceptable and water-soluble casein salt. This invention also relates to a new antibacterial composition of Cefditoren pivoxyl for use in oral administration, which has a reduced or minimized bitter taste to patients upon oral administration thereof and is quickly soluble in water and also can attain a high absorbability of the Cefditoren component at the digestive tubes and is further capable of maintaining a high rate of dissolution out of its Cefditoren pivoxyl component into water even after a storage of the composition was done at an elevated temperature, and which composition comprises a mixture of Cefditoren pivoxyl with a proportion of the water-soluble casein salt and a proportion of a pharmaceutically acceptable and water soluble polyphosphoric acid salt. This invention further embraces a method for reducing the bitter taste of Cefditoren pivoxyl and enhancing the rate of dissolution of Cefditoren pivoxyl into water, which method comprises mixing Cefditoren pivoxyl with a proportion of a pharmaceutically acceptable and water-soluble casein salt.
BACKGROUND ART
Cefditoren is a cephem compound represented by the following formula (A): ##STR1## and named as e-2-carboxylic acid. This cephem compound having the generic name "Cefditoren" is also nominated as 5-yl)vinyl!-3-cephem-4-carboxylic acid(syn-isomer, cis-isomer) in the specifications of Japanese patent No. 1698887(Japanese patent publication "Kokoku" No. Hei-3-64503 published on Oct. 7, 1991), U.S. Patent No. 4,839,350 and European patent No. 0175610. A pivaloyloxymethyl ester of Cefditoren, where the 2-carboxyl group of said cephem compound has been esterified with pivaloyloxymethyl group for the purpose of enhancing the absorbability of the cephem compound via the digestive tubes upon the oral administration thereof (the absorbability of the cephem compound in this sense is referred to simply as "oral absorbability" sometime hereinafter),is such a pro-drug which is known under a generic name "Cefditoren pivoxyl". This pro-drug compound is represented by the following formula (B): ##STR2## and has a chemical name oct-2-ene-2-carboxylic acid 2,2-dimethylpropionyloxymethyl ester".
It is generally deemed that when such a medicinal compound (called simply as a drug hereinafter) which is essentially in the form of an acid has been esterified at the acid group thereof with an ester-forming group, the resulting ester compound can gain an enhanced or improved lipophilicity through the esterification so as to increase the membrane permeability of the drug at the digestive tubes, whereby the resulting ester compound can attain an enhancement in its absorbability at the digestive tubes, namely an enhanced oral absorbability much than that of the original drug of the acid form. As be known well, however, the absorbability of a drug at the digestive tubes is closely co-related to the solubility of said drug in water. The esterified drug, owing to its enhanced lipophilicity, can have its reduced characteristics that relate to the solubilities of the drug in respect of its wettability with water, its dispersibility in water, and others. Therefore, some problems have occurred in that the esterification of a medicinal compound is not necessarily able to achieve an enhancement or improvement in the absorbability of the compound at digestive tubes to a satisfactory extent.
Cefditoren, which is the antibacterially active species, does not exhibit the bitter taste by itself upon oral administration thereof, whilst Cefditoren pivoxyl of the ester form is the pro-drug which can exhibit a strong bitter taste objectionably to
Abe Ken-ichi
Kikkoji Toshihiro
Murakami Chikako
Ota Masato
Yamaguchi Hiroyuki
Jordan Kimberly
Meiji Seika Kaisha Ltd.
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