W/O/W-type composite nano-emulsion gel transdermal preparation containing polypeptide drugs and preparation method thereof

A technology of transdermal preparations and polypeptides, which is applied in the field of W/O/W composite nanoemulsion gel transdermal preparations and its preparation, can solve the problems of limited progress in transdermal polypeptide drugs that cannot meet the daily medication needs of ordinary patients. Poor stability of peptide molecules and other problems, to achieve the effect of easy industrial production, good compliance and strong permeability

Inactive Publication Date: 2019-03-29
JIANGSU YUANHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although polypeptide drugs have unique advantages, they also have disadvantages: the stability of polypeptide molecules is poor, and they are easily inactivated by acids and enzymes in the digestive system, so they are often administered by injection; at the same time, due to their short half-life, they need Long-term continuous administration to maintain its drug effect brings great pain and inconvenience to patients
However, these technologies often require the help of high-end equipment to produce a certain transdermal absorption effect, which still cannot meet the daily medication needs of ordinary patients.
Compared with the breakthrough of new physical transdermal technology, the progress of new dosage forms of peptide drug transdermal is still very limited, and there is no product suitable for clinical use on the market.

Method used

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  • W/O/W-type composite nano-emulsion gel transdermal preparation containing polypeptide drugs and preparation method thereof
  • W/O/W-type composite nano-emulsion gel transdermal preparation containing polypeptide drugs and preparation method thereof
  • W/O/W-type composite nano-emulsion gel transdermal preparation containing polypeptide drugs and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Dissolve leuprolide acetate (20mg) in 1mL of PBS buffer (pH7.4), add a mixed emulsifier of Span 60 (3.2g) and Tween 60 (0.8g) and stir evenly, while stirring at room temperature Add IPM (5.0g) dropwise until clear and transparent to obtain a W / O nanoemulsion containing leuprolide acetate. Use the obtained W / O nanoemulsion as the oil phase of the composite nanoemulsion, add emulsifier OP-10 (3.4g) and co-emulsifier carbitol (0.8g) and stir evenly, add PBS buffer dropwise while stirring at room temperature (25.8mL) to clear and transparent to obtain the W / O / W type composite nanoemulsion containing leuprolide acetate. Add Carbomer 940 (0.4g) into the above-mentioned W / O / W type composite nanoemulsion, wait for it to fully swell, then adjust the pH value to 6.5 with triethanolamine, and stir gently until the gel is naturally formed, that is, the leuthin acetate containing W / O / W type composite nanoemulsion gel of propylene.

Embodiment 2

[0036]Dissolve leuprolide acetate (20mg) in 1mL of PBS buffer (pH7.4), add Span 80 (3.2g) and Tween 80 (0.8g) to mix the emulsifier and stir well, drop while stirring at room temperature Add IPM (5.0g) until clear and transparent to obtain a W / O nanoemulsion containing leuprolide acetate. Use the obtained W / O nanoemulsion as the oil phase of the composite nanoemulsion, add emulsifier OP-10 (3.4g) and co-emulsifier carbitol (0.8g) and stir evenly, add PBS buffer dropwise while stirring at room temperature (25.0mL) to clear and transparent to obtain the W / O / W type composite nanoemulsion containing leuprolide acetate. The above-mentioned W / O / W type composite nanoemulsion was observed under a transmission electron microscope, and the results were as follows: figure 1 As shown, it can be seen that the prepared W / O / W type composite nanoemulsion presents a not very round spherical structure after natural drying, with an average particle size of 20-100nm. This may be due to the fact...

Embodiment 3

[0061] Dissolve leuprolide acetate (20mg) in 1mL of PBS buffer (pH7.4), add Span 80 (3.2g) and Tween 60 (0.8g) to mix the emulsifier and stir evenly, drop while stirring at room temperature Add IPM (5.0g) until clear and transparent to obtain a W / O nanoemulsion containing leuprolide acetate. The obtained W / O nanoemulsion was used as the oil phase of the composite nanoemulsion, and the emulsifier Labrasol (3.4g) and co-emulsifier ethanol (0.8g) were added and stirred evenly, and PBS buffer solution (25.0mL) was added dropwise while stirring at room temperature Until it is clear and transparent, a W / O / W type composite nanoemulsion containing leuprolide acetate is obtained. Add Carbomer 940 (0.3g) into the above-mentioned W / O / W type composite nanoemulsion, wait for it to fully swell, then add chitosan (Mw≈8000, deacetylation degree 85%) solution 0.1mL (pH5.0 , 1.0g / mL), and finally adjust the pH value to 6.5 with triethanolamine, stir gently until the gel is naturally formed, an...

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Abstract

The invention discloses a W/O/W-type composite nano-emulsion gel transdermal preparation containing polypeptide drugs and a preparation method thereof. The preparation method of the W/O/W-type composite nano-emulsion gel transdermal preparation containing the polypeptide drugs comprises the following steps: dissolving the polypeptide drugs with a PBS buffer, adding an emulsifier A, carrying out uniform stirring, and dropwise adding an oil phase while stirring at room temperature until a clear and transparent mixture is obtained so as to obtain a W/O-type nano-emulsion containing the polypeptide drugs; using the W/O-type nano-emulsion as an oil phase, adding an emulsifier B and a co-emulsifier, carrying out uniform stirring, and dropwise adding a PBS buffer while stirring at room temperature until a clear and transparent mixture is obtained so as to obtain a W/O/W-type composite nano-emulsion containing the polypeptide drugs; and then, adding a gel matrix material into the W/O/W-type composite nano-emulsion containing the polypeptide drugs, after full swelling is reached, adjusting the pH value to 6.5, and carrying out gentle stirring until gel is naturally formed so as to obtain the W/O/W-type composite nano-emulsion gel transdermal preparation containing the polypeptide drugs. The preparation method of the W/O/W-type composite nano-emulsion gel transdermal preparation containing the polypeptide drugs is simple in process, mild in conditions, beneficial for maintaining activity of polypeptide drugs and feasible for industrial production; and the prepared composite nano-emulsion is small in particle size, high in permeability and easy for drug penetration.

Description

technical field [0001] The invention relates to a transdermal preparation, in particular to a W / O / W type composite nanoemulsion gel transdermal preparation containing polypeptide drugs and a preparation method thereof. Background technique [0002] Polypeptide drugs are biological macromolecular drugs, which have the function of affecting and regulating the physiological, biochemical and pathological processes of the body. Polypeptide drugs can be produced by means of modern bioengineering technology, genetic engineering or artificial synthesis. Compared with chemical drugs, polypeptide drugs often have significant curative effect, small adverse reactions, high safety, and rarely cause serious immune reactions due to their good selectivity and biological activity. It has significant curative effect on osteoporosis, gastrointestinal diseases, central nervous system diseases, immune diseases, anti-virus and anti-bacteria. Although polypeptide drugs have unique advantages, th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/113A61K9/06A61K9/00A61K47/36
CPCA61K9/0014A61K9/06A61K9/113A61K47/36
Inventor 赵子明印晓星姜雪王联民贾瑞巧何井亮
Owner JIANGSU YUANHENG PHARMA
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