Medicinal preparation for treating rheumatoid arthritis by transdermal administration and preparation method thereof

A technology for rheumatoid and arthritis, applied in the direction of anti-inflammatory agent, drug combination, drug delivery, etc., can solve the problems of decreased efficacy of sinomenine, unstable light and heat, short biological half-life, etc., to improve bioavailability, High long-term stability, dose-reducing effect

Pending Publication Date: 2020-09-08
ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, sinomenine hydrochloride still has many shortcomings as a clinical drug, such as its instability to light and heat, and easy decomposition, which will lead to a decline in the curative effect of sinomenine
And the biological half-life of sinomenine hydrochloride itself is relatively short, mostly taken orally, and the dosage is large; as a strong histamine release agent, sinomenine hydrochloride itself will cause clinical adverse effects such as skin rash and gastrointestinal irritation through the release of histamine. reaction

Method used

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  • Medicinal preparation for treating rheumatoid arthritis by transdermal administration and preparation method thereof
  • Medicinal preparation for treating rheumatoid arthritis by transdermal administration and preparation method thereof
  • Medicinal preparation for treating rheumatoid arthritis by transdermal administration and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The preparation of sinomenine hydrochloride cinnamaldehyde ointment:

[0046] The ratio is:

[0047] Cinnamaldehyde (0.5%, w / w, the same below).

[0048] Sinomenine hydrochloride (1%).

[0049] Oil phase ingredients: stearic acid (6.5%), white petrolatum (8%), liquid paraffin (10%), glyceryl monostearate (4%), lanolin (4%).

[0050] Aqueous Phase Components: Sodium Lauryl Sulfate (0.5%), Ethyl Paraben (0.1%), Glycerin (7.4%), Distilled Water (58%).

[0051] Precisely weigh the proportioned oil phase components in a small beaker, heat on a water bath to 70-80°C to melt, add cinnamon aldehyde, and stir well. Take the water phase ingredients in a small beaker, put them on a water bath and heat to 70-80°C to dissolve them, add sinomenine hydrochloride, stir well, add the water phase ingredients into the oil phase ingredients in a thin stream at the same temperature, and put them in the water bath Continue to heat and stir for 5 minutes, then stir at room temperature unt...

Embodiment 2

[0053] Preparation of sinomenine hydrochloride cinnamaldehyde transdermal patch:

[0054] Add 0.1g of sinomenine hydrochloride and 1g of polyacrylate pressure-sensitive adhesive (Duro-Tak 872677) into a 50mL beaker, add 10mL of absolute ethanol and 0.05g of cinnamon aldehyde and stir for 2h to completely dissolve and mix the drug, and remove air bubbles by ultrasonic , spread evenly on the anti-adhesive layer, place at room temperature for 20 minutes to evaporate the solvent, then place it in a 40°C oven to dry for 30 minutes, take it out, and press it with the backing material after cooling to obtain the sinomenine hydrochloride cinnamaldehyde transdermal patch.

Embodiment 3

[0056] Preparation of sinomenine hydrochloride cinnamaldehyde carbomer gel:

[0057] Accurately weigh 200 mg (2%, w / w) of Carbomer 940 and sprinkle evenly in a small beaker filled with an appropriate amount of distilled water (about 2.5 mL), let it stand for 12 hours, warm it in a water bath, and set aside. Precisely weigh 100 mg of sinomenine hydrochloride (1%, w / w) and add appropriate amount of distilled water to dissolve it completely, pour it into warmed carbomer, and keep stirring to dissolve it in the gel matrix. Then add cinnamaldehyde 50 mg (0.5%, w / w) dissolved in a small amount of ethanol, then add triethanolamine dropwise while stirring, so that the pH value is controlled at about 6.5 to 7.0, add distilled water to 10 g and keep stirring, cool to room temperature Obtain sinomenine hydrochloride (1%) cinnamon aldehyde (0.5%) carbomer gel, and store it in a cool place and a light-proof container for subsequent use.

[0058] As a comparison, in the above method, ①, wi...

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Abstract

The invention discloses a medicinal preparation for treating rheumatoid arthritis through transdermal delivery and a preparation method thereof, and belongs to the technical field of medicines for treating rheumatoid arthritis. A clinically acceptable external dosage form is prepared from a pharmaceutical composition consisting of sinomenine hydrochloride and cinnamaldehyde in a weight ratio of 1:(0.1-10), one or more pharmaceutically acceptable carriers and excipients, and the external dosage form comprises carbomer gel, liquid crystal gel, ointment and a transdermal patch. Combination of thesinomenine hydrochloride and the cinnamaldehyde can significantly improve the treatment effect of rheumatoid arthritis, and the cinnamaldehyde not only has an anti-inflammatory and immune effect, butalso has a transdermal absorption promoting effect on the sinomenine hydrochloride. Therefore, after drug combination, the respective administration dosage can be reduced, the treatment effect is improved, adverse reactions are reduced, and the patient compliance is improved.

Description

technical field [0001] The invention belongs to the technical field of drugs for treating rheumatoid arthritis, and in particular relates to a pharmaceutical preparation for treating rheumatoid arthritis by transdermal administration and a preparation method thereof. Background technique [0002] Rheumatoid arthritis is a common chronic, systemic autoimmune disease. The clinical manifestations are mainly erosive and symmetrical polyarthritis. The affected joints are mainly small joints, and the pathology of the main target organ is synovitis, accompanied by a variety of extra-articular manifestations. The disease erodes the joints and causes joint destruction and joint dysfunction, which is the main cause of its disability. The main measure that doctor trained in western medicine treats rheumatoid arthritis to take at present is to take non-steroidal, antibiotics, hormones, immunosuppressants or surgical treatment. Although medicine can suppress the exacerbation of the sta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61K31/11A61K9/06A61K47/06A61K47/44A61K47/32A61K47/14A61K9/70A61P19/02A61P29/00
CPCA61K31/485A61K31/11A61K9/06A61K9/0014A61K47/06A61K47/44A61K47/32A61K47/14A61K9/7061A61P19/02A61P29/00A61K2300/00
Inventor 储晓琴吴文青蔡叶桂双英
Owner ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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