Odor-masking coating for a pharmaceutical preparation

• US 20020132006A1
• Filed: 05/30/2001
• Published: 09/19/2002
• Est. Priority Date: 12/30/1999
• Status: Active Grant

• Current Assignee: Knobbe Martens Olson & Bear LLP
• Original Assignee: San Diego Credit Association
• Inventors: Wang, Pou-Hsiung, Smith, Lori McDonald, Sue, I-Lan T.
• Granted Patent: US 6,667,059 B2
• Time in Patent Office: Days
• US Class Current: 424/482
• CPC Class Codes: A61K 36/84 Valerianaceae (Valerian family), e.g. valerian
• CPC Class Codes: A61K 9/2886 having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer of the type active core-drug layer-inactive layer A61K9/209
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 Anxiolytics

Abstract

A coating for masking or reducing the detectable presence of certain characteristic odor or odors, taste or tastes of pharmaceutical preparations, particularly Valerian extracts, is described. The coating comprises from one to three coating compartments, in any combination or as a single-layer amalgam. The first coating compartment comprises a hydroxyalkyl cellulose and an anti-tackiness agent. The second coating compartment may comprise a sugar and at least one anti-tackiness agent. The third coating compartment may comprise a methacrylate copolymer, a hydroxyalkyl cellulose and an anti-tackiness agent.

Claims

1. A tablet comprising

a pharmaceutically effective amount of an extract of the root of Valerian;

and

a pharmaceutically-inert coating comprising one or more of the following coating compartments;

a first coating compartment comprising a hydroxyalkyl cellulose wherein the alkyl group has between 1 and 10 carbon atoms, and an anti-tackiness agent;

a second coating compartment comprising a sugar and at least one anti-tackiness agent; and

a third coating compartment comprising a methacrylate copolymer, a hydroxyalkyl cellulose and an anti-tackiness agent.

2. The tablet of claim 1, wherein the coating further comprising a coating compartment that is colored, flavored, or scented.

3. The tablet of claim 1, wherein said hydroxyalkyl cellulose is selected from the group consisting of hydroxyethyl cellulose and hydroxypropyl cellulose.

4. The tablet of claim 1, wherein said anti-tackiness agent is selected from the group consisting of talc, silicon dioxide, silica hydrogel, microcrystalline cellulose, alkali stearates, and starch.

5. The tablet of claim 1, wherein said sugar is selected from the group consisting of sucrose, dextrose, dextrin, maltose, glucose, fructose, mannose, sorbitol, lactose, mannitol, and xylose.

6. The tablet of claim 1, wherein said methacrylate copolymer is selected from the group consisting of the methacrylic acid copolymers, the aminoalkylmethacrylate copolymers, and the ammoniomethacrylate copolymers.

7. The tablet of claim 1, wherein said first coating compartment further comprises a compound which facilitates the coating process.

8. The tablet of claim 1, wherein said first coating compartment further comprises hydroxypropyl methylcellulose.

9. The tablet of claim 1, wherein first coating compartment further comprises a plasticizer.

10. The tablet of claim 9, wherein said plasticizer is selected from the group consisting of propylene glycol, glycerin, trimethylolpropane, polyethylene glycols, dibutyl sebacate, acetylated monoglycerides, diethylphthalate, triacetin, glyceryl triacetate, acetyltriethyl citrate and triethyl citrate. XXX

11. The tablet of claim 1, wherein said second coating compartment further comprises an agent which facilitates the coating process.

12. The tablet of claim 11, wherein said agent is selected from the group consisting of polyvinyl pyrrolidone, vinylpyrrolidone acetate copolymer, vinyl acetate-crotonic acid copolymer, ethyl acrylate-methacrylic acid copolymer, hydroxypropyl cellulose, gelatin, acacia, an ethylcellulose, and a methylcellulose.

13. The tablet of claim 1, wherein said second coating compartment comprises a plasticizer.

14. The tablet of claim 13, wherein said plasticizer is selected from the group consisting of propylene glycol, glycerin, trimethylolpropane, polyethylene glycols, dibutyl sebacate, acetylated monoglycerides, diethylphthalate, triacetin, glyceryl triacetate, acetyltriethyl citrate and triethyl citrate. XXX

15. The tablet of claim 1, wherein said second coating compartment comprises talc and a second anti-tackiness agent.

16. The tablet of claim 1, wherein said second coating compartment comprises silicon dioxide and a second anti-tackiness agent.

17. The tablet of claim 1, wherein said third coating compartment further comprises hydroxypropylmethyl cellulose.

18. The tablet of claim 1, wherein said third coating compartment further comprises a plasticizer.

19. The tablet of claim 18, wherein said plasticizer is selected from the group consisting of propylene glycol, glycerin, trimethylolpropane, polyethylene glycols, dibutyl sebacate, acetylated monoglycerides, diethylphthalate, triacetin, glyceryl triacetate, acetyltriethyl citrate and triethyl citrate.

20. The tablet of claim 1, wherein said third coating compartment comprises a water soluble polymer or compound.

21. The tablet of claim 20, wherein said water soluble polymer is selected from the group consisting of hydroxypropyl cellulose, hydroxypropyl methylcellulose, acacia, sodium carboxymethylcellulose, dextrin, alginic acid, ethylcellulose resin, gelatin, guar gum, liquid glucose, methylcellulose, pregelatinized starch, sodium alginate, starch, zein, polyvinylpyrrolindone, vinylpyrrolidone-vinyl acetate copolymer, vinyl acetate-crotonic acid copolymer and ethyl acrylate-methacrylic acid copolymer.

22. The tablet of claim 1, wherein the coating compartments comprise at least one of the following:

hydroxypropyl methylcellulose, triacetin/glycerol triacetate, OPADRY Clear™

, ethylcellulose, ammonium hydroxide, medium chain triglycerides, oleic acid, SureRelease™

, lactose monohydrate, hydroxypropyl methylcellulose, titanium dioxide, triacetin/glycerol triacetate, OPADRY II™

, polyvinyl alcohol, titanium dioxide, lecithin, xanthan gum, and OPADRY AMB™

.

23. The tablet of claim 1, wherein the weight of the pharmaceutically-inert coating is between approximately 4% and approximately 9% of the weight of the tablet.

26. The tablet of claim 25, wherein the hydroxyalkyl cellulose serves to control the release of the pharmaceutically effective amount of an extract of the root of Valerian.

27. The tablet of claim 25, wherein the hydroxyalkyl cellulose is hydroxypropylcellulose.

28. The tablet of claim 25, wherein the coating further comprises a colorant.

29. The tablet of claim 25, wherein the coating further comprises a scent.

30. The tablet of claim 25, wherein the coating further comprises a flavoring agent.

24. A tablet comprising

a pharmaceutically effective amount of an extract of the root of Valerian;

and

a pharmaceutically-inert coating comprising at least one of the following coating compartments;

a first coating compartment means for enhancing the viscosity of the extract;

a second coating compartment means for enhancing the palatability of the tablet; and

a third coating compartment means for effecting controlled release of the extract.

25. A tablet comprising

a pharmaceutically effective amount of an extract of the root of Valerian;

and

a pharmaceutically-inert coating comprising a hydroxyalkyl cellulose wherein the alkyl group is selected from the group consisting of methyl, ethyl and propyl groups.