Pharmaceutical preparation for oral cavity administration

• US 4,059,686 A
• Filed: 09/22/1975
• Issued: 11/22/1977
• Est. Priority Date: 09/24/1974
• Status: Expired due to Term

• Current Assignee: Nippon Kayaku Company Limited
• Original Assignee: Nippon Kayaku Company Limited
• Inventors: Akito, Eiichiro, Tanaka, Wataru, Yoshida, Koichi, Ninomiya, Hiroshi, Terada, Takashi
• Primary Examiner(s): Jiles, Henry R.
• Assistant Examiner(s): Owens, Cary
• Application Number:
  US05/615,301
• Time in Patent Office: 792 Days
• Field of Search: 424/19, 424/81, 424/83, 424/22, 426/19, 426/549, 426/601
• US Class Current: 424/435
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates

Abstract

A pharmaceutical preparation of oral cavity administration, characterized by being a mixture of a pharmacologically active agent, a pharmaceutical carrier, and sodium polyacrylate, in conventional dosage form. It has advantages in that it adheres strongly to local site and dissolves gradually over a prolonged period of time while releasing appropriate amounts of the active agent.

Claims

1. A pharmaceutical preparation for oral cavity administration comprising 10 to 60% by weight of sodium polyacrylate, 90 to 10% by weight of a pharmaceutical carrier selected from the group consisting of an excipient and ointment, and 50 to 0.05% by weight of a pharmacologically active agent.

2. A pharmaceutical preparation for oral cavity administration according to claim 1, wherein the sodium polyacrylate has an average molecular weight of 185,000 to 8,500,000.

3. A pharmaceutical preparation for oral cavity administration according to claim 1, wherein the excipient is microcrystalline cellulose, mannitol, crystalline lactose, spray-dried lactose, sorbitol, anhydrous calcium phosphate, amylose, powdered lactose, or powdered sucrose.

4. A pharmaceutical preparation for oral cavity administration according to claim 1, wherein the ointment base is white petrolatum, polyethylene glycol, a compatible mixture of peanut oil or purified sesame oil with beeswax, or a compatible mixture of polyethylene and liquid paraffin.

5. A pharmaceutical preparation for oral cavity administration according to claim 1, wherein the pharmacologically active agent is selected from the group consisting of a steroid hormone, an antiinflammatory steroid, an antiinflammatory enzyme, callicrein, a peptide, a nitrate ester, isoproterenol, methacholine, an antibiotic, a lysozyme, dextrinase, and a local anesthetic.

6. A pharmaceutical preparation for oral cavity administration according to claim 1, wherein the said pharmaceutical is selected from the group consisting of a buccal tablet, a sublingual tablet, and an ointment.

7. A pharmaceutical preparation for oral cavity administration according to claim 1, wherein the pharmaceutical preparation comprising 10 to 60% by weight of sodium polyacrylate, 80 to 10% by weight of an excipient and 50 to 0.05% by weight of a pharmacologically active agent is a tablet selected from the group consisting of a buccal tablet and a sublingual tablet.

8. A pharmaceutical preparation for oral cavity administration according to claim 1, wherein the pharmaceutical preparation comprising 10 to 50% by weight of sodium polyacrylate, 90 to 40% by weight of an ointment base, and 10 to 0.05% by weight of a pharmacologically active agent is an ointment.