Process for the production of semisolid preparations containing micronized active ingredients

• US 5,432,170 A
• Filed: 05/17/1993
• Issued: 07/11/1995
• Est. Priority Date: 07/16/1991
• Status: Expired due to Fees

• Current Assignee: Schering Ag (Merck & Co., Inc.)
• Original Assignee: Schering Ag (Merck & Co., Inc.)
• Inventors: Stindl, Wolfgang, Leitner, Erich, Dargel, Erwin, Tack, Johannes
• Primary Examiner(s): GRIFFIN, RONALD
• Application Number:
  US08/066,077
• Time in Patent Office: 785 Days
• Field of Search: 514/179, 514/180, 514/969, 514/975, 424/85.8
• US Class Current: 514/179
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00

Abstract

A process for the production of semisolid preparations containing micronized active ingredients is described which is characterized in that a mixture of one or two nonionic surfactants with an HLB of 9 to 18 with 2.3 to 100 times the amount by weight of a fatty acid ester of general formula

R.sub.1 --COO--R.sub.2

in which R₁ and R₂ each represent alkyl groups or alkenyl groups with 12 to 32 carbon atoms, or a mixture of these fatty acid esters is heated until it melts, the melt with stirring is put into 10 to 200 times the amount by weight of a semisolid preparation, which is heated approximately to the same temperature, the mixture is allowed to cool with stirring and mixed with the micronized active ingredient or active ingredient mixture as well as optionally with scents.

Claims

1. A process for the production of a micronized active ingredient-containing semi-solid preparation, comprising

heating until it melts a mixture of one or two non-ionic surfactants with an HLB of 9 to 18, with 2.3 to 100 times the amount by weight of a fatty acid ester of the formula R₁ --COO--R₂,

wherein

R₁ and R₂ each independently are a C_12-32 -alkyl or -alkenyl group, or a mixture of said fatty acid esters;

putting said melt with stirring into 10 to 100 times the amount by weight of a semi-solid preparation heated to approximately the same temperature as said melt;

cooling the resultant product with stirring; and

mixing into the cooled product a micronized active ingredient or active ingredient mixture, and optionally a scent.

2. A process of claim 1, wherein the semi-solid preparation to which the melt is added is an oil-in-water emulsion or a mixed emulsion.

3. A process of claim 1, wherein the non-ionic surfactant is an ethoxylate soluble in water and insoluble in paraffin oil.

4. A process of claim 2, wherein the non-ionic surfactant is an ethoxylate soluble in water and insoluble in paraffin oil.

5. A process of claim 1, wherein the active ingredient is an antibiotic, a non-steroidal antiphlogistic agent or a corticoid.

6. A process of claim 2, wherein the active ingredient is an antibiotic, a non-steroidal antiphlogistic agent or a corticoid.

7. A process of claim 3, wherein the active ingredient is an antibiotic, a non-steroidal antiphlogistic agent or a corticoid.

8. A process of claim 4, wherein the active ingredient is an antibiotic, a non-steroidal antiphlogistic agent or a corticoid.

9. A micronized active ingredient-containing semi-solid preparation prepared by a process of claim 1.

10. A micronized active ingredient-containing semi-solid preparation prepared by a process of claim 2.

11. A micronized active ingredient-containing semi-solid preparation prepared by a process of claim 3.

12. A micronized active ingredient-containing semi-solid preparation prepared by a process of claim 9.

13. A micronized active ingredient-containing semi-solid preparation prepared by a process of claim 10.

14. A micronized active ingredient-containing semi-solid preparation prepared by a process of claim 11.

15. A micronized active ingredient-containing semi-solid preparation prepared by a process of claim 12.

16. A micronized active ingredient-containing semi-solid preparation prepared by a process of claim 13.

17. A micronized active ingredient-containing semi-solid preparation prepared by a process of claim 1, wherein the micronized active ingredient has a grain size of at most 80 mμ

.