Pharmaceutical preparation possessing antinicotine effect and method of producing same in a gum carrier

• US 4,971,079 A
• Filed: 03/05/1987
• Issued: 11/20/1990
• Est. Priority Date: 02/22/1982
• Status: Expired due to Fees

• Current Assignee: Elena A. Rimzha, Fedor N. Kaputsky, Galina V. Ustichenko, Tatyana L. Yurkshtovich, Viktor A. Stelmakh, Vitaly I. Talapin
• Original Assignee: Elena A. Rimzha, Fedor N. Kaputsky, Galina V. Ustichenko, Tatyana L. Yurkshtovich, Viktor A. Stelmakh, Vitaly I. Talapin
• Inventors: Rimzha, Elena A., Ustichenko, Galina V., Yurkshtovich, Tatyana L., Kaputsky, Fedor N., Stelmakh, Viktor A., Talapin, Vitaly I.
• Primary Examiner(s): Millin, V.
• Application Number:
  US07/023,914
• Time in Patent Office: 1,356 Days
• Field of Search: 131/359, 131/276, 131/271, 131/270, 131/273, 428/48, 428/197, 426/3
• US Class Current: 131/359
• CPC Class Codes: A61K 47/585 Ion exchange resins, e.g. polystyrene sulfonic acid resin
• CPC Class Codes: A61K 47/61 the organic macromolecular compound being a polysaccharide or a derivative thereof
• CPC Class Codes: Y10T 428/164 Continuous two dimensionally sectional layer
• CPC Class Codes: Y10T 428/24818 Knitted, with particular or differential bond sites or intersections

Abstract

A pharmaceutical preparation, in a chewing gum carrier, possessing an antinitocine effect which comprises a biologically resorbable polymeric vehicle containing a cation-exchange group and modified thereat by an antinicotine-action action alkaloid in the following proportions thereof, percent by mass: antinitocine-action alkaloid 2.5-40.0 polymeric vehicle the balance. The method of producing the preparation comprises reacting a biologically resorbable polymeric vehicle containing a cation-exchange group with an antinicotine-action alkaloid in an aqueo-organic medium at a volume ratio of the aqueous and organic phases of 1-15:1-24 respectively and at a temperature within the range of from 8° to 22° C.

Claims

1. A pharmaceutical preparation in the form of a chewing gum effective to facilitate giving-up smoking and for the treatment of nicotinism comprising, an alkaloid in an amount of 2.5 to 40.0 percent by weight of the preparation selected from a member of the group consisting of cystisine, anabasine, lobeline and nontoxic salts thereof and a biologically absorbable polymeric vehicle containing a cation exchange group chemically combined with said alkaloid through said cation exchange group, wherein the polymeric vehicle is selected from a member of the group consisting of monocarboxycellulose, carboxymethylcellulose, phosphatecellulose, polyvinyl sulfate, polymethacrylic acid, discarboxydextran and hydroxystarch, a base, a plastifying agent, syrup, and aromatizing agent, sugar powder at the following proportions of the components, percent by mass:

polymeric vehicle modified by;

space="preserve" listing-type="tabular">______________________________________ alkaloid 0.05-4 a base 20-31 plastifying agent 1-1.5 syrup 12-19 aromatizing agent 0.4-0.6 sugar powder the balance ______________________________________

2. A method for producing a pharmaceutical preparation effective to facilitate giving-up smoking and for the treatment of nicotinism, the preparation comprising an alkaloid in an amount of 2.5 to 40.0 percent by weight of the preparation selected from a member of the group consisting of cystisine, anabasine, lobeline and nontoxic salts thereof and a biologically absorbable polymeric vehicle containing a cation exchange group chemically combined with said alkaloid through said cation exchange group, wherein the polymeric vehicle is selected from a member of the group consisting a monocarboxycellulose, carboxymethylcellulose, phosphatecellulose, polyvinylsufate, polymethacrylic acid, dicarboxydextran and hydroxystarch, the method comprising a method in which the biologically absorbable polymeric vehicle containing a cation-exchange group is reacted with said alkaloid effective to block the nicotine receptor zones of the mucous membrane of the mouth in an aqueousorganic medium at a volume ratio between the aqueous and organic phases of 1-15:

1-25 respectively at a temperature within the range of from 8°

to 22°

C.

3. A method according to claim 2, in which the interaction between said components is effected at a pH of the medium ranging from 6.5 to 8.5.

4. A method according to claim 2, in which aqueous ethanol or an aqueous-isopropanol medium is used.

5. A pharmaceutical preparation effective to facilitate giving-up smoking and for the treatment of nicotinism comprising an active component comprised of an alkaloid in an amount of 2.5 to 40.0% by weight of the active component selected from a member of the group consisting of cystisine, anabasine, lobeline and nontoxic salts thereof and a biologically absorbable polymeric vehicle containing a cation exchange group chemically combined with said alkaloid through said cation exchange group, wherein the polymeric vehicle is selected from a member of the group consisting of monocarboxycellulose, carboxymethylcellulose, phosphatecellulose, polyvinylsulfate, polymethacrylic acid, dicarboxydextran and hydroxystarch in an amount effective for the treatment of nicotinism, in combination with phosphate cellulose modified by pyrroxane in an amount of 5 to 10% of the preparation and a pharmaceutically acceptable vehicle.

6. The pharmaceutical preparation according to claim 5 in which the active component is anabasine hydrochloride chemically combined with carboxymethylcellulose.

7. The pharmaceutical preparation according to claim 6 in which the pharmaceutically acceptable vehicle is chewing gum.

8. A pharmaceutical preparation effective to facilitate giving-up smoking and for the treatment of nicotinism comprising an active component comprised of an alkaloid in an amount of 2.5 to 40% by weight of the active component selected from a member of the group consisting of cystisine, anabasine, lobeline and nontoxic salts thereof and a biologically absorbable polymeric vehicle containing a cation exchange group chemically combined with said alkaloid through said cation exchange group, wherein the polymeric vehicle is selected from a member of the group consisting of monocarboxycellulose, carboxymethylcellulose, phosphatecellulose, polyvinylsulfate, polymethacrylic acid, dicarboxydextran and hydroxystarch in an amount effective for the treatment of nicotinism, in combination with aminocarboxycellulose modified with ascorbic acid in an amount of 5 to 15% of the preparation and a pharmaceutically acceptable vehicle.

9. The pharmaceutical preparation according to claim 8, in which the active component is anabasine hydrochloride chemically combined with carboxymethylcellulose.

10. The pharmaceutical preparation according to claim 9 in which the pharmaceutically acceptable vehicle is chewing gum.

11. A pharmaceutical preparation in the form of chewing gum effective to facilitate giving-up smoking and for the treatment of nicotinism comprising in percent by mass:

space="preserve" listing-type="tabular">______________________________________ an active component comprised of anabasine 0.05-4 hydrochloride in an amount of 2.5 to 40 wt. % of the active component and a biologically absorbable polymeric vehicle containing a cation exchange group comprised of carboxymethylcellulose chemi- cally combined with the anabasine hydrochloride through the cation exchange group phosphate cellulose modified by pyrroxane 5-10 a base 20-31 plastifying agent 1-1.5 syrup 12-19 aromatizing agent 0.4-0.6 sugar powder the balance. ______________________________________

12. A pharmaceutical preparation in the form of chewing gum effective to facilitate giving-up smoking and for the treatment of nicotinism comprising in percent by mass:

space="preserve" listing-type="tabular">______________________________________ an active component comprised of anaba- 0.05-4 sine hydrochloride in an amount of 2.5 to 40 wt. % of the active component and a biologically absorbable polymeric vehicle containing a cation exchange group comprised of carboxymethylcellulose chemically combined with the anabasine hydrochlo- ride through the cation exchange group amino-carboxycellulose modified by ascorbic acid 5-15 a base 20-31 plastifying agent 1-1.5 syrup 12-19 aromatizing agent 0.4-0.6 sugar powder the balance ______________________________________