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Preparation for treating allergic rhinitis and asthma

A technology for allergic rhinitis and preparations, applied in the biological field, can solve the problems of difficult extraction and separation, difficulty in drug quality control, and inability to meet market demands, and achieve stable and reliable products.

Inactive Publication Date: 2005-05-18
KUNMING ZIJIAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the only preparation that has been developed is the compound preparation—Coleus oral solution, which is far from meeting the market demand.
In addition, because the content of isofaskolin in medicinal materials is extremely low (0.05%), and the extraction and separation are difficult, coupled with factors such as high activity and small dose, it is difficult to control the quality of medicines.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Prepare 10% isofaskolin according to the following process steps:

[0033] 1. Make the dried root of Coleus forskohlii into a coarse powder, and use 95% ethanol to carry out heat reflux extraction in order of 9 times, 7 times, 7 times, and 7 times, each extraction for 1 hour, and combined extraction Liquid, concentrated to 50% volume;

[0034] 2. Add active carbon to decolorize by 0.1% (mass ratio) of the solution amount, remove impurities once with a short silica gel column, and concentrate to dryness to obtain an extract containing 10% isofaskolin.

Embodiment 2

[0036] Prepare 80% isofaskolin according to the following process steps:

[0037] 1. Make the dry product of Coleus forskohlii into a coarse powder, and use 95% ethanol to carry out heat reflux extraction in order of 9 times, 7 times, 7 times, and 7 times, each extraction for 1 hour, and combine the extracts , concentrated to 50% of the amount:

[0038] 2. Add activated carbon to decolorize according to 0.1% (mass ratio) of the solution amount, remove impurities once with a short silica gel column, and concentrate to 5% amount:

[0039] 3. Add 8 times the amount of chloroform or dichloromethane under stirring, and place it overnight at 5-10 ° C. After separating the chloroform or dichloromethane layer, filter it, concentrate it in a vacuum until dry, and obtain 80% isofeskoline the extract;

[0040] 4. Separation on a silica gel column, eluting fractions with the following solvents: petroleum ether (boiling point 60-80°C), petroleum ether-benzene mixture, benzene, benzene-et...

Embodiment 3

[0043] According to the physical and chemical properties of isoferskolin, supercritical (SC-CO 2 ) extraction method to extract isoflurane, that is, the solvent selects CO 2 , CO 2 entrained ethanol, CO 2 Entrained methanol, etc., the extraction temperature is 45-65°C, the extraction pressure is 30-50Mpa, the analysis pressure is 8-14Mpa, and the analysis temperature is 42-67°C. The advantage is that the method belongs to clean production, and there are few residual solvents in the extract. Strict control of the conditions and the amount of entrained solvent can yield isofeskoline.

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Abstract

The present invention provides a kind of preparation for treating allergic rhinitis and asthma, and features that each ml of the preparation contains isoforskolin 0.005-0.4 mg except medicine supplementary material and is prepared into acceptable inhalant. The preparation has high stability, no irritation to skin including damaged skin and relatively high antiphlogistic effect. It has curative effect on allergic rhinitis and bronchial asthma, and is practical.

Description

technical field [0001] The invention relates to a preparation for treating allergic rhinitis and asthma, belonging to the field of biotechnology. Background technique [0002] In the 1970s, German and Indian scholars collected Coleus Forskohlii from Mumbai, India, and isolated from it the highly active Laudanane diterpene compound - Forskolin (forkolin) and its analogous compounds. Pharmacological studies have confirmed that forskolin is the strongest adenylyl cyclase activator known so far. It does not inhibit phosphodiesterase, but directly increases the concentration of cAMP in cells to produce physiological activity. 10 -9 g / ml is active. Since this type of compound exhibits obvious antihypertensive and cardiotonic activities, it has remarkable curative effects in the treatment of cardiovascular diseases, congestive heart failure, tumor metastasis, bronchial asthma, skin diseases, etc., and has a good development prospect. The Coleus plant in Huize, Yunnan Province i...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K9/14A61K9/50A61K9/70A61K31/352A61P11/02A61P11/06A61P37/08
Inventor 于军
Owner KUNMING ZIJIAN BIOTECH
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