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Aqueous compositions comprising bilastine and mometasone

A composition, water-based technology, applied in the directions of pharmaceutical combinations, non-active ingredients of polymer compounds, medical preparations containing active ingredients, etc., can solve problems such as stable compositions that are not mentioned

Pending Publication Date: 2020-08-11
FAES FARMA SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These documents do not mention a stable composition comprising bilastine and mometasone

Method used

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  • Aqueous compositions comprising bilastine and mometasone
  • Aqueous compositions comprising bilastine and mometasone
  • Aqueous compositions comprising bilastine and mometasone

Examples

Experimental program
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preparation example Construction

[0063] Methods for the preparation of these mometasone derivatives are well known in the art (eg, M.B. Smith, J. March, March's Advanced Organic Chemistry, Wiley-Interscience, 5th edition). Likewise, mometasone and mometasone derivatives may be present in the aqueous pharmaceutical composition as a free compound or as a solvate (eg, hydrate, alcoholate, etc.), and both forms are included within the scope of the present invention. Thus, for example, suitable forms of mometasone furoate in the aqueous pharmaceutical compositions of the invention include anhydrous forms or hydrated forms, such as monohydrated forms. In a preferred embodiment, the aqueous pharmaceutical composition of the present invention comprises mometasone hydrate. Solvation methods are well known in the art.

[0064] In a preferred embodiment, based on the total weight of the composition, the amount of mometasone or a pharmaceutically acceptable derivative thereof in the aqueous pharmaceutical composition of...

Embodiment 1

[0171] Example 1-visual evaluation using HPBCD as the uniformity of the solubilizer

[0172] The formulations of this example were prepared as described above. The following table shows the content of each component in the final preparation of the embodiment of the present invention:

[0173]

[0174]

[0175] *0.517 mg / mL mometasone furoate monohydrate is equivalent to 0.5 mg / mL mometasone furoate anhydrous form.

[0176] Two other aqueous pharmaceutical compositions of the present invention were prepared, which had the same composition as the above composition, but changed the content of bilastine to 2 mg / mL and 8 mg / mL.

[0177] pH measurement: 4.6

[0178] Homogeneity was assessed visually: the formulation was homogeneous.

Embodiment 2

[0179] Example 2 - Comparative. Visual Evaluation of Uniformity of Alternative Solubilizers Using Bilastine and Mometasone

[0180] Five formulations in which cyclodextrin was replaced by alternative solubilizers of bilastine and mometasone were prepared and evaluated for visual homogeneity. The formulation of this example was prepared in a similar manner to that described above, but this time with (8g.), 35 (8g.) (Fagron), 40 (8g.) (Fagron), 80 (8 g.) (Basf) or Poloxamer 188 (10 g.) (Basf) were substituted for cyclodextrins because of their surfactant properties. In the formulation of this example, Spam 80 acts as an antifoaming agent.

[0181] 2.1 Evaluation by visual method uniformity.

[0182] The following table shows the usage in this example Exact amounts of components in the final formulation as solubilizers for bilastine and mometasone:

[0183]

[0184]

[0185] Evaluation of uniformity by visual inspection: There is phase separation and thus the f...

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PUM

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Abstract

The invention relates to an aqueous pharmaceutical composition comprising: a) bilastine or a pharmaceutically acceptable salt or solvate thereof, b) mometasone, or a pharmaceutically acceptable derivative thereof, c) a suspending agent, and d) 2-hydroxypropyl-3-cyclodextrin; wherein the pH of the aqueous pharmaceutical composition is between 3.5 and 5.5, and wherein the content of 2-hydroxypropyl-beta-cyclodextrin is less than 8.5% by weight. The invention also relates to said compositions for use in the treatment and / or prevention of a disorder or disease susceptible to amelioration by antagonism of Hi histamine receptor and / or of a corticosteroid-responsive disease through nasal administration. The invention also relates to a process for preparing the aqueous pharmaceutical composition above mentioned.

Description

technical field [0001] The invention relates to an aqueous pharmaceutical composition of bilastine and steroid, and a preparation method of the aqueous pharmaceutical composition. The invention also relates to said composition for use in the treatment and / or prophylaxis by antagonizing H 1 A disorder or disease amenable to relief from histamine receptors and / or a corticosteroid-responsive disease (corticosteroid-responsive disease), wherein the aqueous pharmaceutical composition is administered intranasally. Background technique [0002] It has long been known that histamine plays a very important role in allergic diseases such as allergic rhinitis, conjunctivitis, rhinoconjunctivitis, dermatitis, urticaria and asthma. acting on H 1 - Antihistamine compounds at the level of receptor histamine can be used to treat such diseases. In this sense, documents EP 0818454A1 and EP 0580541A1 and patent application EP14382576.8 disclose 1 Benzimidazole compounds with antihistamine ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/38A61K47/40A61K31/454A61K31/58A61P11/06A61P11/02A61P37/08A61K9/08
CPCA61K9/0043A61K9/0095A61K9/08A61K31/454A61K31/58A61K47/38A61K47/40A61K2300/00A61P11/02A61P27/14A61P29/00A61K9/10
Inventor 贡萨洛·埃尔南德斯·埃雷罗安娜·贡萨洛·戈罗斯蒂萨内夫塔利·加西亚·多明格斯阿图罗·扎普·阿尔塞巴勃罗·莫兰·波拉杜拉塔尼亚·冈萨雷斯·加西亚
Owner FAES FARMA SA
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