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Lappaconitine hydrobromide transparent patch and the preparing method thereof

A kind of technology of homogenin hydrobromide and transdermal patch, which is applied in the field of pharmacy, can solve the problems of high quality injection, high production cost, and inconvenient use, so as to improve the curative effect of the drug, reduce individual differences, and meet the needs of treatment. desired effect

Inactive Publication Date: 2011-04-13
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Injections have high quality requirements, and the preparation process requires specific conditions and equipment. The production cost is high, the price is high, the use is inconvenient, and the injection is painful.

Method used

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  • Lappaconitine hydrobromide transparent patch and the preparing method thereof
  • Lappaconitine hydrobromide transparent patch and the preparing method thereof
  • Lappaconitine hydrobromide transparent patch and the preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Weigh 29.4mg of genivirine hydrobromide, add 3ml of ethanol, and after ultrasonic dissolution, add 525mg of acrylic resin, ultrasonically dissolve and mix well. Coated on 42cm by salivation process 2 On the backing layer, evaporate the solvent naturally, dry and solidify in an oven at 80°C, and cover with a protective layer after cooling. A modified Franz diffusion cell device was used to measure its permeability to human skin in vitro, and the receiving solution was 20% polyethylene glycol 400 (PEG400) physiological saline aqueous solution. Use HPLC to measure uricine hydrobromide, using Agilent ZORBAX Eclipse×DB-C18 chromatographic column (4.6mm×150mm, 5μm), the column temperature is 35°C, and the mobile phase is 0.1mol.L -1 Sodium dihydrogen phosphate: methanol (1:1), detection wavelength 252nm, flow rate 1.0ml / min. The permeation rate is 0.09μg / cm 2 h. figure 1 It is the drug cumulative penetration-time curve (time is hours) of this embodiment.

Embodiment 2

[0043] Weighed 29.4mg of urine hydrobromide, added 3ml of ethanol, ultrasonically dissolved, then added 525mg of acrylic resin, and then added 5.6mg of propylene glycol for ultrasonically dissolved and mixed. Coated on 42cm by salivation process 2 On the backing layer, evaporate the solvent naturally, dry and solidify in an oven at 80°C, and cover with a protective layer after cooling. The following operations are the same as Example 1. The permeation rate is 0.13μg / cm 2 h. figure 2 It is the drug cumulative penetration-time curve (time is hours) of this embodiment.

Embodiment 3

[0045] Weighed 29.4 mg of urine hydrobromide, added 3 ml of ethanol, ultrasonically dissolved, then added 525 mg of acrylic resin, and then added 17.1 mg of propylene glycol for ultrasonically dissolved and mixed. Coated on 42cm by salivation process 2 On the backing layer, evaporate the solvent naturally, dry and solidify in an oven at 80°C, and cover with a protective layer after cooling. The following operations are the same as in Example 1. The permeation rate is 0.12μg / cm 2 h. image 3 It is the drug cumulative penetration-time curve (time is hours) of this embodiment.

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Abstract

The invention discloses a hydrobromic acid high babbit nail element transdermal paster, which comprises the following steps: allocating 4. 7-5. 3% hydrobromic acid high babbit nail element, 0-9. 6% transdermal absorption promoting agent and 85-95% pressure-sensitive adhesive acrylic resin; adding the hydrobromic acid high babbit nail element into alcohol; hypersonic-dissolving; adding into pressure-sensitive adhesive and accelerant; supersonic-dissolving; mixing evenly; getting solution; adopting slobbering craft; coating the solution on back lining layer; natural-drying the solution; puttinginto 80 deg. c bake oven; drying; hardening; cooling; covering on covering layer; getting the product. This product possesses convenient usage and good analgesic effect, which transdermal rate can reach 0. 34mug / cm2 . h.

Description

technical field [0001] The invention relates to the field of pharmaceutics, in particular to a transdermal patch of homogenate hydrobromide. Background technique [0002] Homoconitine hydrobromide is the hydrobromide salt of Lappaconitine, an alkaloid extracted from Aconitum sinomoutanum Nakai, a plant of the genus Ranunculaceae. The molecular weight is 683.64, the melting point is 217-221°C, soluble in methanol, slightly soluble in water and ethanol, hardly soluble in organic solvents such as chloroform, and its molecular structure formula is: [0003] [0004] Hokine hydrobromide is mainly used clinically for the treatment of moderate pain, postoperative pain and intractable pain, especially cancer pain. It is the first non-addictive analgesic in China. Its analgesic strength is equivalent to that of morphine and 7 times that of aminopyrine. It has a long acting time and is not addictive. Long-term use will not cause physical dependence. Side effects (sedation, dry mo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K31/439A61P25/04A61P23/02A61P29/00
Inventor 高建青钟韵伟吴争梁文权
Owner ZHEJIANG UNIV
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