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(12) Patent Application Publication (10) Pub. No.: US 2005/0181054A1 Nishibe Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2005/0181054A1 Nishibe Et Al US 2005O181054A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2005/0181054A1 Nishibe et al. (43) Pub. Date: Aug. 18, 2005 (54) PHARMACEUTICAL COMPOSITION FOR (30) Foreign Application Priority Data APPLICATION TO MUCOSA Apr. 21, 1998 (JP)................................ 10-110887(PAT) (75) Inventors: Yoshihisa Nishibe, Tokyo (JP); Wataru Apr. 21, 1998 (JP)................................ 10-110888(PAT) Kinoshita, Tokyo (JP); Hiroyuki Kawabe, Tokyo (JP) Publication Classification (51) Int. Cl." ........................... A61K 9/24; A61K 31/56; Correspondence Address: A61K 31/70; A61K 31/205 SUGHRUE MION, PLLC (52) U.S. Cl. ............................ 424/473; 514/23: 514/169; 2100 PENNSYLVANIAAVENUE, N.W. 514/554 SUTE 800 WASHINGTON, DC 20037 (US) (57) ABSTRACT (73) Assignee: TEIJIN LIMITED The present invention provides a pharmaceutical composi tion for application to the mucosa to be used in drug therapy (21) Appl. No.: 11/102,760 comprising a water-insoluble and/or water-low Soluble Sub stance, a medicament, and an aqueous medium, and having (22) Filed: Apr. 11, 2005 an osmotic pressure of less than 290 mOsm. This compo Sition is Superior over conventional pharmaceutical compo Related U.S. Application Data Sitions for application to the mucosa, due to efficient and high permeability to the blood at the mucosa. The present (63) Continuation of application No. 10/201,303, filed on invention further provides a pharmaceutical composition for Jul. 24, 2002, which is a continuation of application application to the mucosa comprising a hemostatic agent and No. 09/446,276, filed on Dec. 21, 1999, filed as 371 a medicament. This composition is Superior over conven of international application No. PCT/JP99/02126, tional pharmaceutical compositions for application to the filed on Sep. 28, 1999. mucosa, due to permeability and retentivity at the mucosa. Patent Application Publication Aug. 18, 2005 Sheet 1 of 4 US 2005/0181054A1 007 098 GT OOZ aanssaado?ous0(usou) (%) Anyaeleneog Patent Application Publication Aug. 18, 2005 Sheet 2 of 4 US 2005/0181054A1 ( %) All qeemeo.9 US 2005/0181054A1 00Z (usou)aanssaado?ouso 72 Patent Application Publication Aug. 18, 2005 Sheet 4 of 4 US 2005/0181054A1 US 2005/0181054A1 Aug. 18, 2005 PHARMACEUTICAL COMPOSITION FOR (Japanese Unexamined Patent Publication (Kokai) No. 63 APPLICATION TO MUCOSA (1988)-303931), for example, provides a method of applying to the nasal cavity a growth hormone-releasing factor at the TECHNICAL FIELD liquid form having an osmotic pressure ratio of 1 (an osmotic pressure of 290 mOsm) or lower as a method for 0001. The present invention relates to a pharmaceutical enabling quick and efficient absorption of the a growth composition for application to the mucosa to be used in drug hormone-releasing factor through the nasal mucosa to the therapy comprising a water-insoluble and/or water-low blood circulation. Furthermore, Ohwaki et al. (Japanese Soluble Substance, a medicament, and an aqueous medium, Unexamined Patent Publication (Kokai) No. 60 (1985)- and having an OSmotic pressure of less than 290 mOsm. 123426) provides a method of applying to the nasal cavity More specifically, the present invention relates to a phar a Solution of Secretin having an OSmotic preSSure ratio of 1 maceutical composition for application to the mucosa com to 5 (an osmotic pressure of 290-1450 mOsm) and a pH of prising a water-insoluble and/or water-low Soluble Sub 2 to 5 as a method for enabling quick absorption of Secretin stance, a medicament, and an aqueous medium, and having through the nasal mucosa to blood circulation. Furthermore, an osmotic pressure of less than 290 mOsm, that is Superior Awatsu et al. (Pharm. Res. Vol. 10, No. 9, 1372-1377, 1993) to conventional pharmaceutical compositions for application provides a method of applying to the nasal mucosa a to the mucosa, due to efficient and high permeability to the pharmaceutical Solution to which polyoxyethylene 9-lau blood at the mucosa. rylether was added as an absorption enhancer as a method 0002 The present invention also relates to a pharmaceu for enabling efficient absorption of a granulocyte colony tical composition for application to the mucosa comprising Stimulating factor through the nasal mucosa to blood circu a hemostatic agent and a medicament. More specifically, the lation. present invention relates to a pharmaceutical composition 0006. However, when these pharmaceutical preparations for application to the mucosa in which a medicament has are given to the mucosa, liquid-dripping can occur, or the been mixed with a hemostatic agent and that is Superior over pharmaceutical preparations are quickly excreted to the conventional pharmaceutical compositions for application to outside of the mucus tissue due to a mucociliary clearance the mucosa due to high permeability and retention at the function etc. before being adequately transported or perme COS. ated to the mucosa tissue. Because of this, the transport of an adequate amount of drug into the blood cannot be effected BACKGROUND ART when systemic administration through transport to the blood 0003) Application to the mucosa as a method of drug circulation is attempted. Furthermore, the method of using therapy has been recognized as a useful means of medication an absorption enhancer is yet to be realized because the for Such reasons as (1) it permits direct application to the absorption enhancer has the problem of irritating the nasal affected area for diseases of local areas Such as nasal mucosa. On the other hand, when local administration is mucosa, oral mucosa, and vaginal mucosa, (2) its immediate attempted through retention of the drug in the mucosa tissue, effects for Systemic diseases can be expected as in the case an adequate amount of the drug cannot be retained at the of a nasal Spray to the nasal mucosa and a Suppository to the tissue. In addition, even if the problem of retentivity has rectal mucosa, and (3) its application is easy compared to been Solved, permeation into the mucosa tissue is not injection, as represented by an oral drug targeted at the adequate. intestinal mucosa, and the like. For example, pharmaceutical 0007 Thus, it is strongly desired to develop a pharma preparations for application to the mucosa have already been ceutical preparation for application to the mucosa, that commercially available due to reason (1) in the case of nasal allows the transport of an adequate amount of the drug sprays for treatment of allergic rhinitis, and due to reason (2) through the mucosa to the blood circulation after the appli in the case of Suppositories to alleviate pain. cation to the mucosa. Alternatively, it is Strongly desired to 0004 AS pharmaceutical preparations for local mucus develop a pharmaceutical preparation for application to the diseases, Saunders et al., (WO 92-14473), for example, mucosa that enables the transport to and retention in the provides a Suspension preparation containing Tipredane as mucosa tissue of an adequate amount of the drug when the main drug as the pharmaceutical preparation for treat applied to the mucosa. ment of allergic rhinitis. Also, Helzner (WO 97-01337) provides a pharmaceutical preparation comprising an anti DISCLOSURE OF THE INVENTION histamic drug, a Steroid and water as the pharmaceutical 0008 Thus, the first object of the present invention is to preparation for treatment of allergic rhinitis. AS the phar provide a pharmaceutical composition for application to the maceutical preparation for local mucus diseases, further more, Kim et al., (WO 98-00178) provides a suspension mucosa, that has efficient and high permeability through the preparation having a thixotropic property as the pharmaceu mucosa to the blood when applied to the mucosa. tical preparation for application to the nasal mucosa. Suzuki 0009. The second object of the present invention is to et al. (Japanese Examined Patent Publication (Kokoku) No. provide a pharmaceutical composition for application to the 60 (1985)-34925) also provides a sustained release pharma mucosa, that has efficient and high permeability to the ceutical preparation for administration to the nasal cavity mucosa and retentivity at the mucosa when applied to the that permits the efficient Supply of the drug at a concentra COS. tion Sufficient to obtain a therapeutic effect. 0010. After intensive studies to attain the above first 0005. As the pharmaceutical preparations for systemic object, the present inventors have found that it is possible to diseases, Several methods have been provided that enhance provide a pharmaceutical preparation for application to the the absorption of drugs through the mucosa. Nagata et al. mucosa that is Superior over conventional liquid composi US 2005/0181054A1 Aug. 18, 2005 tion due to efficient and high permeability through the over conventional pharmaceutical compositions for applica mucosa to the blood, by formulating a drug that contains a tion to the mucosa, due to markedly efficient and high water-insoluble and/or water-low soluble Substance and that permeability to the blood at the mucosa. has an osmotic pressure of less than 290 mOsm, and thereby 0015. After intensive studies to attain the above second have reached the present invention. object, the present inventors have found that by formulating 0.011) An enhanced absorption of a drug through the a pharmaceutical preparation in which a hemoStatic agent mucosa by controlling the osmotic pressure of a pharma has been added to a pharmaceutical preparation containing ceutical preparation is disclosed in a patent to Ohwaki and a medicament, a pharmaceutical composition for application has been reported in a paper by AwaZu et al. (Pharm. Res. to the mucosa having efficient and high permeability to and Vol. 10, No. 9, 1372-1377, 1993). However, these phenom retentivity at the mucosa can be provided, and thereby have ena are only observed in aqueous Solution preparations that attained the present invention. do not contain a water-insoluble and/or water-low Soluble 0016.
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