Drug – bio-affecting and body treating compositions – Lymphokine – Interferon
Reexamination Certificate
2001-01-08
2003-09-23
Russel, Jeffrey E. (Department: 1654)
Drug, bio-affecting and body treating compositions
Lymphokine
Interferon
C424S434000, C514S002600, C514S003100, C514S012200, C514S015800, C514S016700, C514S021800, C514S772000, C514S777000
Reexamination Certificate
active
06623732
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a pharmaceutical formulation of nasal administration containing a pharmaceutically active polypeptide, and particularly relates to a pharmaceutical formulation for nasal administration that comprises at least one compound selected from the group consisting of taurine, an ester thereof with C18 6 alcohol, a base metal salt of taurine, hyaluronic acid and a base metal salt of hyaluronic acid. These compounds are used as absorbefacients for the pharmaceutical formulation of the present invention. The pharmaceutical formulation of the present invention may be dosed through nasal mucosa. The present invention also relates to a method for producing the pharmaceutical formulation.
BACKGROUND ART
A powder composition for nasal administration including a physiologically active peptide with a hyaluronic acid butyrene glycol ester as a carrier is disclosed in Japanese Patent Publication (laid-open) No. 6-199681. A pharmaceutical composition for administration through nasal mucosa, with preferably a pH of about 4, containing a peptide hormone and hyaluronic acid or its salt is disclosed in Japanese Patent Publication (laid-open) No. 3-246233. A microsphere formed comprising a physiologically active peptide that is surrounded by hyaluronic acid esters or which is adsorbed on hyaluronic acid esters is disclosed in Japanese Patent Publication (laid-open) No. 7-179363. A pharmaceutical formulation with improved drug delivery comprising a physiologically active peptide, hyaluronic acid or a non-toxic salt of these compounds, and polymer substance is disclosed in Japanese Patent Publication (laid-open) No. 5-97694. A pharmaceutical formulation for administration through the lung that comprises peptide type drugs and hyaluronic acid is disclosed in Japanese Patent Publication (laid-open) No. 9-309843. A pharmaceutical formulation with sustained physiological activity comprising hyaluronic acid or its non-toxic salts is disclosed in Japanese Patent Publication (laid-open) No. 2-213. A powder pharmaceutical formulation for nasal administration that contains a granulocyte colony stimulating factor, saccharides, hyaluronic acid or its salt is disclosed in Japanese Patent Publication (laid-open) No. 8-198772. An eye drop containing insulin and hyaluronic acid or its salt as a thickening agent is disclosed in Japanese Patent Publication (laid-open) No.1-294633. An aqueous pharmaceutical composition with sustained pharmaceutical activity that contains a pharmaceutically active peptide, water soluble hyaluronic acid, and a water soluble protein which does not exhibit pharmaceutical activity is disclosed in Japanese Patent Publication (laid-open) No. 5-186362. A peptide composition having a physiologically active peptide homogenously dispersed in a carrier hyaluronic acid so that it is adhesively bound to the carrier is disclosed in Japanese Patent Publication (laid-open) No. 7-118170. A super-absorbent drug for administration through vagina that contains the absorbefacient taurine in a bioactive polypeptide is disclosed in Japanese Patent Publication (laid-open) No. 3-99021. In Chinese Patent Application No. 95119260.4, an absorbefacient for absorption of peptide containing pharmaceuticals through mucosae is disclosed. The absorbefacients disclosed in the above Chinese application include azone, saponins, glycyrrhizionic acid, and esters, salts of these compounds, glycyrrhetinic acid and a sodium salt of glycyrrhetinic acid, dihydroxymorintannic acid and its derivatives, and carboxylic acid estes of these compounds. However, the only formulation example disclosed in the above Chinese Patent Application is a sublingual tablet containing such absorbefacients. In Chinese Patent Application No. 88106763.6, a pharmaceutical formulation for administration through mucosae is disclosed. The absorbefacients contained in the formulation are monosaccarides such as D-erythrose, D-ribose, D-ribulose, D-xylose, D-arabinose, D-mannose, L-sorbose, D-sedumtheptulose, or monosacarides such as &agr;-cyclodextrin, &bgr;-cyclodextrin, &ggr;-cyclodextrin, and cyclodextrin having side chains.
Polypeptide compounds are easily degraded with enzymes in the human stomach and intestines and are easily metabolized in the human liver. Therefore, polypeptide compounds are difficult to give their intrinsic pharmaceutical effects in a patient's body. Thus, polypeptide compounds are generally administration as various injections such as hypodermic injections, intramuscular injections, and intravenous injections. However, the patient experiences pain and irritation such as, for example, injury and necrosis of his/her muscle tissue during long-term polypeptide administration of the injections and there is potential for infections caused by injection due to communicable diseases. The patient also experiences various inconveniences such as the need to receive regular outpatient treatment. For these reasons, extensive studies have recently been made to administer the polypeptide compounds through mucosae such as the nasal mucosa, no polypeptide containing pharmaceutical formulations for administration through the nasal mucosa have not yet been commercially available.
Therefore, polypeptide containing pharmaceutical formulations for administration through nasal mucosa are highly desired and their development has been waited for a long term.
An object of the present invention is to provided a pharmaceutical formulation for nasal administration containing a pharmaceutically active polypeptide and also to provide a method for producing thereof.
SUMMARY OF THE INVENTION
The inventor has found a novel pharmaceutical formulation suitable for nasal administration and succeeded in accomplishing the present invention as the result of the study to solve the above problems. The novel pharmaceutical formulation containing a pharmaceutically active polypeptide exhibits high pharmaceutical activity as high as the pharmaceutical activity obtained in the administration through injection and does not irritate patients.
According to the present invention, the pharmaceutical formulation for nasal administration comprises (1) a pharmaceutically active polypeptide, (2) at least one compound selected from the group consisting of taurine, an ester thereof with C1~6 alcohol, an base metal salt of taurine, hyaluronic acid and a base metal salt of hyaluronic acid, and (3) at least one pharmacologically acceptable additive.
Further according to the present invention, the pharmaceutical formulation for nasal administration preferably comprises (1) a pharmaceutically active polypeptide, (2) at least one compound selected from the group consisting of taurine, an ester thereof with C1~6 alcohol, a base metal salt of taurine, (3) at least one compound selected from hyaluronic acid and a base metal salt of hyaluronic acid, and (4) at least one pharmacologically acceptable additive.
Further according to the present invention, the pharmaceutical formulation for nasal administration more preferably comprises (1) a pharmaceutically active polypeptide, (2) taurine and hyaluronic acid, and (3) at least one pharmacologically acceptable additive.
Further according to the present invention, the pharmaceutical formulation may comprise at least one compound selected from the group consisting of taurine, an ester thereof with C1~6 alcohol, a base metal salt of taurine, hyaluronic acid, a base metal salt of hyaluronic acid and a mixture thereof or a carrier for the pharmaceutically active polypeptide for administration through the nasal mucosa.
In accordance with the present invention, a method for producing a pharmacological formulation is also provided. The method for producing a pharmaceutical formulation for nasal administration containing of at least one pharmaceutically active polypeptide comprises the steps of;
adding an adequate amount of distilled water to a compound selected from the group consisting of taurine, an ester thereof with C1~6 alcohol, a base metal salt of taurine, hyaluronic acid, a base metal salt of the hyalu
Greenblum & Bernstein P.L.C.
Highchem Company, Ltd.
Russel Jeffrey E.
LandOfFree
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