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Lactose-free, non-hyproscopic and anhydrous pharmaceutical compositions of descarboethoxyloratadine

A technology of desethoxycarbonyl loratadine and ethoxycarbonyl loratadine, applied in the field of desethoxycarbonyl loratadine pharmaceutical composition

Inactive Publication Date: 2000-03-08
SEPACOR INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Another disadvantage of both astemizole and loratadine is that the respective drugs are associated with the growth of melanoma and fibrosarcoma

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] Compressed DCL tablets may be prepared by conventional wet granulation techniques such that individual dosage units contain 0.1 mg to 10 mg of DCL.

[0090] Per tablet Per 10,000 tablets DCL 10mg 100g Starch 60mg 600g Talc 12mg 120g Gum Arabic 12mg 120g Stearic Acid 1mg 10g

[0091] Mix gum arabic with equal weight of starch to form a paste, and use the paste for DCL granulation. The mixture is dried and sieved. Add remaining ingredients and mix thoroughly. The resulting mixture was compressed into tablets using 9 / 32 inch (7 mm) punches. Example 2

Embodiment 2

[0092] Compressed DCL tablets can be prepared using conventional dry granulation techniques, with each dosage unit containing 0.1 mg to 10 mg of DCL.

[0093] Each tablet DCL 10mg 100g starch 85mg 850g per 10,000 tablets

[0094] The starch was dried to 10% moisture and then thoroughly mixed with the DCL. The resulting mixture is compressed into chips, which are then ground into fine particles. The resulting mixture was compressed into tablets using 9 / 32 inch (7 mm) punches. Example 3

Embodiment 3

[0095] Compressed DCL tablets may be prepared using conventional direct compression techniques such that individual dosage units contain 0.1 mg to 10 mg of DCL.

[0096] Per tablet DCL 10mg 100g microcrystalline cellulose 80mg 800g stearic acid 5mg 50g colloidal silicon dioxide 1mg 10g per 10,000 tablets

[0097] All ingredients are mixed in a suitable mixer. The resulting mixture was compressed into tablets using 9 / 32 inch (7 mm) punches. Example 4

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Abstract

Stable pharmaceutical compositions of descarboethoxyloratadine (DCL), a metabolic derivative of loratadine, for the treatment of allergic rhinitis and other histamine-induced disorders are disclosed. The compositions are formulated to avoid the incompatibility between DCL and reactive excipients such as lactose and other mono- and di-saccharides. Disclosed compositions include lactose-free, non-hygroscopic and anhydrous stable pharmaceutical compositions of DCL.

Description

[0001] Cross references to related patent applications [0002] This application claims the priority of U.S. provisional patent applications 60 / 053,050 (applied on July 21, 1997), 60 / 045,184 (applied on April 30, 1997) and 60 / 037,325 (applied on February 7, 1997). Background of the invention [0003] The present invention relates to 8-chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine, known as Pharmaceutical compositions of descarboethoxyloratadine (DCL). [0004] Desethoxycarbonylloratadine [0005] DCL is a metabolic derivative of Loratadine, an H-1 histamine receptor antagonist. H-1 histamine receptor antagonists mediate the antagonistic response of conventional antihistamines. The antihistamine activity of loratadine is comparable to that of terfenadine and astemizole, and on a milligram-for-mg basis, it is four times more potent than fenadine in suppressing allergic bronchospasm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04A61KA61K9/14A61K9/20A61K31/395A61K31/445A61K31/4545A61K31/60A61P11/02A61P17/04A61P27/02A61P27/16A61P29/00A61P37/08A61P43/00
CPCA61K31/16A61K9/2013A61K9/2054A61K31/60A61K31/4545A61K9/2018A61K31/621A61K31/445A61K9/2009A61K9/2059A61K31/473A61P11/00A61P11/02A61P11/06A61P17/00A61P17/04A61P27/00A61P27/02A61P27/16A61P29/00A61P37/00A61P37/06A61P37/08A61P43/00A61K2300/00
Inventor 马丁·P·雷德蒙哈尔·T·巴特勒斯蒂芬·A·沃尔德保罗·D·鲁宾
Owner SEPACOR INC
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