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Application of (-)doxazosin in preparing medicine for treating lower urinary tract symptom and bladder excessive activities diseases

A technology of overactive bladder and doxazosin, which is applied in the direction of urinary system diseases, drug combinations, and pharmaceutical formulas, and can solve problems such as side effects

Inactive Publication Date: 2007-03-07
任雷鸣
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Although (±) doxazosin as selective alpha 1 Receptor blockers can relieve the symptoms of BPH urinary tract obstruction, but they are found to have significant cardiovascular and central side effects, such as hypotension, dizziness, headache, dry mouth, restlessness, tension, sweating, tachycardia Speed ​​and skin flushing, etc. (Lepor H, Knapp-Maloney G, Sunshine H.A dose titration study evaluating terazosin, a selective, once-a-day α 1 -blocker for the treatment of symptomatic benign prostatic hyperplasia, J Urol., 1990, 144(6): 1393~7; Fulton B, Wagstaff AJ, Sorkin EM.Doxazosin: An update of its clinici pharmacology and therapeutic applications in hypertension and benign prostatic hyperplasia , Drugs, 1995, 49(2): 295-320.)

Method used

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  • Application of (-)doxazosin in preparing medicine for treating lower urinary tract symptom and bladder excessive activities diseases
  • Application of (-)doxazosin in preparing medicine for treating lower urinary tract symptom and bladder excessive activities diseases
  • Application of (-)doxazosin in preparing medicine for treating lower urinary tract symptom and bladder excessive activities diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0230] Embodiment 1: Preparation 1 of (-) doxazosin (methanesulfonic acid or hydrochloride) salt tablet

[0231] (-) Doxazosin (methanesulfonic acid or hydrochloric acid) salt 3%

[0232] Lactose 40%

[0233] Starch 33%

[0234] Microcrystalline Cellulose 20%

[0235] Croscarmellose Sodium 3%

[0236] 5% PVP ethanol solution appropriate amount

[0237] Magnesium Stearate 1%

Embodiment 2

[0238] Embodiment 2: Preparation 2 of (-) doxazosin (methanesulfonic acid or hydrochloride) salt tablet

[0239] (-) doxazosin (methanesulfonic acid or hydrochloride) salt 1%

[0240] Lactose 42%

[0241] Starch 33%

[0242] Microcrystalline Cellulose 20%

[0243] Croscarmellose Sodium 3%

[0244] 5% PVP ethanol solution appropriate amount

[0245] Magnesium Stearate 1%

[0246] Preparation steps of Examples 1 and 2: (-) doxazosin (methanesulfonic acid or hydrochloride) salt, lactose, microcrystalline cellulose and 1% croscarmellose sodium were sieved and mixed, and mixed with 5 The % PVP ethanol solution is used as a binder to make a soft material, which is granulated, dried, and granulated, and then 2% croscarmellose sodium and magnesium stearate are added, mixed evenly, and compressed into tablets.

Embodiment 3

[0247] Embodiment 3: Preparation 1 of (-) doxazosin (methanesulfonic acid or hydrochloride) salt capsule

[0248] (-) Doxazosin (methanesulfonic acid or hydrochloric acid) salt 3%

[0249] Starch 54%

[0250] Lactose 42%

[0251] 5% PVP ethanol solution appropriate amount

[0252] Magnesium Stearate 1%

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Abstract

The invention relates to a method for using (-) apholate to prepare the drug that treats urinary tract infection and bladder disease. Wherein, the (-)apholate (methanesulfonic acid or alcaine) can treat blood pressure and heart weaker than (+-) apholate (methanesulfonic acid or alcaine) and (+)apholate (methanesulfonic acid or alcaine). Therefore, its side effect is less than them. The invention can strengthen the eccentric heart muscle contract force, and the (+-) apholate (methanesulfonic acid or alcaine) and (+)apholate (methanesulfonic acid or alcaine) will restrain said force.

Description

technical field [0001] The present invention relates to the specific treatment of lower urinary tract symptoms (lower urinary tract symptoms, LUTS) or bladder overactivity (over active bladder, OAB) using optically active (-) doxazosin (methanesulfonic acid or hydrochloride) salts ), which can specifically block the smooth muscle alpha of the lower urinary tract (bladder, ureter, prostate) 1 receptors and alpha in the central and lower urinary tract nerves 1 At the same time, it can avoid or significantly reduce (±) doxazosin (the English name is called doxazosin mesylate, the Chinese name is called doxazosin mesylate or quinazosin, and the slow-release product name is Kedu Hua) Adverse reactions to the cardiovascular system and central nervous system. More specifically, the present invention relates to the use of optically active (-) (Levorotatory) doxazosin (methanesulfonic acid or hydrochloride) salts (including type I, type II, type III, type IV, type V of mesylate) (-)...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/517A61P13/02A61P13/10A61P13/08A61P13/00
Inventor 任雷鸣
Owner 任雷鸣
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