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Last Updated: March 29, 2024

Claims for Patent: 4,670,419


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Summary for Patent: 4,670,419
Title: Pharmaceutical composition and its rectal use
Abstract:A pharmaceutical composition containing a hydrophilic drug which is poorly absorbable through the gastrointestinal tract, and cyclodextrin, increases the absorbability of the drug into the mammalian body when administered by a non-oral or non-injection route.
Inventor(s): Uda; Yoshiaki (Takarazuka, JP), Hirai; Shin-ichiro (Kyoto, JP), Yashiki; Takatsuka (Takarazuka, JP)
Assignee: Takeda Chemical Industries, Ltd. (Osaka, JP)
Application Number:06/753,816
Patent Claims:1. A method for administering a pharmaceutical composition, which comprises administering a pharmaceutical composition containing a physical mixture of a hydrophilic, physiologically active polypeptide, which is poorly adsorbable through the gastrointestinal tract, and cyclodextrin through the rectum.

2. A method as claimed in claim 1, wherein the cyclodextrin is .alpha.-cyclodextrin.

3. A method as claimed in claim 1, wherein the pharmaceutical composition is a uniform mixture in dosage form.

4. A method as claimed in claim 1, wherein the physiologically active polypeptide is selected from the group consisting of L-pyroglutamyl-L-histidyl-L-prolinamide, its salts, a polypeptide represent by the formula: ##STR4## wherein A stands for hydrogen, alkyl, aralkyl, alkoxyalkyl, hydroxyalkyl or alkoxy, R stands for ##STR5## X stands for --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --S--, R and each of the other constituent amino acid residues may have an L- or D-configuration or be racemic, and its salts.

5. A method as claimed in claim 1, wherein the physiologically active polypeptide is selected from the group consisting of luteinizing hormone-releasing hormone (LH-RH) and a peptide which has LH-RH activity and has the formula:

wherein R.sub.1 stands for His, Tyr, Trp or p-NH.sub.2 -Phe; R.sub.2 stands for Tyr or Phe; R.sub.3 stands for Gly or a D-amino acid residue; R.sub.4 stands for Leu, Ile or Nle; R.sub.5 stands for Gly-NH-R.sub.6 (R.sub.6 stands for H or a lower alkyl group which may optionally have a hydroxyl group) or NH-R.sub.6 (R.sub.6 is as defined above).

6. A method as claimed in claim 1, wherein the physiologically active polypeptide is selected from the group consisting of insulin, somatostatin, somatostatin derivatives, growth hormone, prolactin, adrenocorticotrophic hormone, melanocyte stimulating hormone, thyrotropin releasing hormone, its salts or its derivatives, thyroid stimulating hormone, luteinizing hormone, follicle stimulating hormone, vasopressin, vasopressin derivatives, oxytocin, carcitonin, parathyroid hormone, glucagon, gastrin, secretin, pancreozymin, cholecystokinin, angiotensin, human placental lactogen, human chorionic gonadotropin, enkephalin, enkephalin derivatives, endorphin, interferon (.alpha., .beta., .gamma.), urokinase, kallikrein, thymopoietin, thymosin, motilin, dynorphin, bombesin, neutotensin, caerulein, bradykinin, substance P, kyotorophin, nerve growth factor, polymyxin B, colistin, gramicidin, bacitracin, bleomycin and neocarzinostatin.

Details for Patent 4,670,419

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Ferring Pharmaceuticals Inc. NOVAREL chorionic gonadotropin For Injection 017016 01/15/1974 ⤷  Try a Trial 2004-06-02
Ferring Pharmaceuticals Inc. NOVAREL chorionic gonadotropin For Injection 017016 12/27/1984 ⤷  Try a Trial 2004-06-02
Ferring Pharmaceuticals Inc. NOVAREL chorionic gonadotropin For Injection 017016 02/15/1985 ⤷  Try a Trial 2004-06-02
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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