Medicament adsorbates of decongestants with complex magnesium aluminum silicate and their preparation

• US 4,758,424 A
• Filed: 10/16/1987
• Issued: 07/19/1988
• Est. Priority Date: 03/27/1986
• Status: Expired due to Term

• Current Assignee: Warner-Lambert Company (Pfizer Inc.)
• Original Assignee: Warner-Lambert Company (Pfizer Inc.)
• Inventors: Peters, David, Denick, John Jr., Talwar, Anil K., Liao, Wei C.
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US07/109,644
• Time in Patent Office: 277 Days
• Field of Search: 424/48, 424/154, 424/155, 514/770, 514/853, 514/854, 514/948, 514/949, 514/960, 514/965, 514/974
• US Class Current: 424/48
• CPC Class Codes: A61K 9/143 with inorganic compounds

Abstract

A medicament adsorbate of decongestants and process for making same. The medicament adsorbate comprises a complex magnesium aluminum silicate having sorbed therein a decongestant. The complex magnesium aluminum silicate has the following typical chemical analysis:

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Ratio to Percent by Weight Aluminum Oxide ______________________________________ Silicon dioxide 56 to 59 14.0 to 29.5 Magnesium oxide 21 to 24 5.2 to 12.0 Aluminum oxide 2.0 to 4.0 1 Ferric oxide 0.4 to 0.6 Calcium oxide 1.1 to 1.5 Sodium oxide 2.5 to 3.5 Potassium oxide 0.5 to 1.0 Ignition Loss 5.5 to 12.6 ______________________________________

Claims

1. A medicament adsorbate which comprises:

a complex magnesium aluminum silicate having the following typical chemical analysis;

space="preserve" listing-type="tabular">______________________________________ Ratio to Percent by Weight Aluminum Oxide ______________________________________ Silicon dioxide 56 to 59 14.0 to 29.5 Magnesium oxide 21 to 24 5.2 to 12.0 Aluminum oxide 2.0 to 4.0 1 Ferric oxide 0.4 to 0.6 Calcium oxide 1.1 to 1.5 Sodium oxide 2.5 to 3.5 Potassium oxide 0.5 to 1.0 Ignition Loss 5.5 to 12.6 ______________________________________

having sorbed therein a solution of medicament drug, wherein the medicament drug is a decongestant.

2. The medicament adsorbate of claim 1 wherein the decongestant is selected from the group of decongestants consisting of phenylephrine hydrochlride, phenylpropanolamine hydrochloride, pseudoephedrine hydrochloride, ephedrine and mixtures thereof.

3. The medicament adsorbate of claim 1 wherein the medicament drug is present in an amount of about 1 to about 35% by weight and the complex magnesium aluminum silicate is present in an amount of about 65 to about 99% by weight, all percents herein are by weight percent of the medicament adsorbate.

4. The medicament adsorbate of claim 1 further comprising a solvent content up to about 20% by weight of the medicament adsorbate.

5. The medicament adsorbate of claim 1 further comprising a solvent content from about 2% to about 15% by weight of the medicament adsorbate.

6. A process for preparing a medicament adsorbate which comprises:

(A) preparing a solution by dissolving the medicament drug in a solvent,

(B) sorbing the medicament drug within a complex magnesium aluminum silicate having the following typical chemical analysis

space="preserve" listing-type="tabular">______________________________________ Ratio to Percent by Weight Aluminum Oxide ______________________________________ Silicon dioxide 56 to 59 14.0 to 29.5 Magnesium oxide 21 to 24 5.2 to 12.0 Aluminum oxide 2.0 to 4.0 1 Ferric oxide 0.4 to 0.6 Calcium oxide 1.1 to 1.5 Sodium oxide 2.5 to 3.5 Potassium oxide 0.5 to 1.0 Ignition Loss 5.5 to 12.6 ______________________________________

by admixing the solution with the complex magnesium aluminum silicate to form a homogenous mass, and

(C) recovering the medicament adsorbate, wherein the medicament drug is a decongestant.

7. The process of claim 6 wherein the decongestant is selected from the group of decongestants consisting of phenylephrine hydrochloride, phenylpropanolamine hydrochloride, pseudoephedrine hydrochloride, ephedrine and mixtures thereof.

8. The process of claim 6 which comprises employing about 10% to about 60% by weight solvent of the solution to prepare the solution.

9. The process of claim 6 wherein the mass is dried to a final solvent content of up to about 20% by weight of the medicament adsorbate.

10. The process of claim 6 wherein the mass is dried to a final solvent content of about 2% to about 15% by weight of the medicament adsorbate.

11. A medicated composition which comprises a pharmaceutically acceptable carrier and from about 1% to about 60% by weight of the final composition of a medicament adsorbate containing magnesium aluminum silicate having the following typical chemical analysis;

space="preserve" listing-type="tabular">______________________________________ Ratio to Percent by Weight Aluminum Oxide ______________________________________ Silicon dioxide 56 to 59 14.0 to 29.5 Magnesium oxide 21 to 24 5.2 to 12.0 Aluminum oxide 2.0 to 4.0 1 Ferric oxide 0.4 to 0.6 Calcium oxide 1.1 to 1.5 Sodium oxide 2.5 to 3.5 Potassium oxide 0.5 to 1.0 Ignition Loss 5.5 to 12.6 ______________________________________

and from about 1% to about 40% by weight of the adsorbate of a medicament drug, wherein the medicament drug is a decongestant.

12. The medicated composition of claim 11 wherein the pharmaceutically acceptable carrier is selected from the group consisting of a lozenge, suspension, a tablet, toffee, nougat, chewy candy and chewing gum.

13. The medicated composition of claim 11 wherein the decongestant is selected from the group of decongestants consisting of phenylephrine hydrochloride, phenylpropanolamine hydrochloride, pseudoephedine hydrochloride, ephedrine and mixtures thereof.

14. A medicated confectionery product comprising:

a bulking agent of up to about 99%;

a therapeutically effective amount of a medicament adsorbate comprising a complex magnesium aluminum silicate which has the following typical chemical analysis;

space="preserve" listing-type="tabular">______________________________________ Ratio to Percent by Weight Aluminum Oxide ______________________________________ Silicon dioxide 56 to 59 14.0 to 29.5 Magnesium oxide 21 to 24 5.2 to 12.0 Aluminum oxide 2.0 to 4.0 1 Ferric oxide 0.4 to 0.6 Calcium oxide 1.1 to 1.5 Sodium oxide 2.5 to 3.5 Potassium oxide 0.5 to 1.0 Ignition Loss 5.5 to 12.6 ______________________________________

having sorbed therein a medicament drug, said medicament adsorbate being admixed in the confectionery product, all percents herein are by weight of the medicated confectionery product, wherein the medicament drug is an decongestant.

15. The medicated confectionery product of claim 14, wherein the decongestant is selected from the group of decongestants consisting of phenylephrine hydrochloride, phenylpropanolamine hydrochloride, pseuodphendrine hydrochloride, ephedrine and mixtures thereof.

16. A medicated chewing gum product containing a therapeutically effective amount of medicament drug which comprises:

a chewing gum composition in an amount up to about 99% comprising;

a gum base,

a sweetener, and

a therapeutically effective amount of a medicament adsorbate comprising a complex magnesium aluminum silicate which has the following typical chemical analysis;

space="preserve" listing-type="tabular">______________________________________ Ratio to Percent by Weight Aluminum Oxide ______________________________________ Silicon dioxide 56 to 59 14.0 to 29.5 Magnesium oxide 21 to 24 5.2 to 12.0 Aluminum oxide 2.0 to 4.0 1 Ferric oxide 0.4 to 0.6 Calcium oxide 1.1 to 1.5 Sodium oxide 2.5 to 3.5 Potassium oxide 0.5 to 1.0 Ignition Loss 5.5 to 12.6 ______________________________________

having sorbed therein a medicament drug, said medicament adsorbate being admixed in the chewing gum composition, wherein the medicament drug is a decongestant, all percents herein are by weight of the medicated chewing gum product.

17. The medicated chewing gum product of claim 16 wherein the decongestant is selected from the group of decongestants consisting of phenylephrine hydrochloride, phenylpropanolamine hydrochloride, pseudoephedrine hydrochloride, ephedrine and mixtures thereof.