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Insoluble medicine transdemal absorption preparation and process for preparing same

A technology for transdermal absorption preparations and insoluble drugs, which is applied in the field of medicine and can solve problems such as high concentration gradients, skin irritation, and danger

Inactive Publication Date: 2003-10-22
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low solubility of vinpocetine, the drug loading of this preparation is relatively small, and it is difficult to achieve a high concentration gradient after being attached to the skin, thereby limiting the transdermal absorption rate of the drug; in addition, Because this kind of preparation uses organic solvents, it will cause residues of organic solvents in the preparation process, which may cause irritation to the skin, and if organic solvents are used in large-scale industrial production, it will inevitably cause potential danger.

Method used

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  • Insoluble medicine transdemal absorption preparation and process for preparing same
  • Insoluble medicine transdemal absorption preparation and process for preparing same
  • Insoluble medicine transdemal absorption preparation and process for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] active drug 1g

[0032] Oleic acid 4g

[0033] Cremophor RH40 15g

[0034] Transcutol P 15g

[0035] Double distilled water 65g

[0036] Full amount 100g

[0037] During the preparation process, it is necessary to heat oleic acid in a water bath, dissolve it and then add the drug, then heat and dissolve Cremophor RH40, mix it with a co-surfactant, and slowly add water to the oily mixture to obtain a microemulsion preparation.

[0038] The oleic acid in the preparation is not only used as an oil phase, but also a good transdermal absorption accelerator, which can promote the percutaneous penetration of insoluble drugs. If the active drug in the preparation is vinpocetine, the mouse skin penetration test in vitro shows that in 24h, the drug is zero-order release, and the steady-state penetration rate is 0.0417ug / cm2 / s, this microemulsion preparation coating On the skin surface of rabbits, the comprehensive irritation score index was less than 0.5, and no irritation r...

Embodiment 2

[0039] Example 2: Drug-containing microemulsion (as described in Example 1) 6g glycerin 35g aluminum hydroxide 0.2g sodium polyacrylate 5g organic acid 0.3g NMP 5g redistilled water 48.5g full amount 100g

[0040] The preparation method is according to the process described in claims 20 and 21, wherein NMP is a transdermal penetration enhancer. On the basis of Example 1, this preparation adds the drug-containing microemulsion into the water-based patch matrix, which can effectively make the insoluble drug compatible with the water-based matrix, and through the hydration of the water-based matrix to the stratum corneum, make the drug Transdermal penetration is greatly improved. In vitro, the steady-state permeation rate through mouse skin increased to 0.062ug / cm2 / s. Stimulation experiments showed that no erythema or edema was found.

Embodiment 3

[0042] Medicated microemulsion:

[0043] Active drug 3g

[0044] Maisine

[0045] 35-1 5g

[0046] Labrasol 20g

[0047] Transcutol 10g

[0048] P

[0049] Double distilled water 62g

[0050] Full amount 100g

[0051] The preparation method is as described in Example 1. Maisine 35-1 is used as the oil phase, and the stable area of ​​the prepared microemulsion preparation is larger, which can increase the drug loading capacity of the microemulsion preparation.

[0052] Water-based patch with microemulsion as carrier

[0053] Medicated Microemulsion 5g

[0054] Glycerin 40g

[0055] Aluminum hydroxide 0.3g

[0056] Polyacrylic acid

[0057] Sodium 4g

[0058] Citric acid 0.2g

[0059] peppermint oil 5g

[0060] Double distilled water 45.5g

[0061] Full amount 100g

[0062] The preparation method is the same as described above. Peppermint oil is added in the preparation, which can make the skin feel refreshed and has the effect of promoting transdermal absorpti...

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Abstract

The present invention relates to an insoluble medicine trans dermal absorption preparation and its preparation process. It raises the solubility of the insoluble medicine in the transdermal absorption preparation, and increases its permeation rate and farther raises the biological utilization rate or dermal absorption. Said preparation contains the following components: (by weight portion) medicine-containing microemulsion 2-10 portions, high-molecular polymer 4-6 portions, cross-linking agent 0.1-0.4 portion, organic acid 0.1-0.5 portion, moisture-holding agent 5-40 portions, distilling water 30-50 portions and permeation accelerator 3-5 portions. Its preparation method includes the following steps: firstly, preparing microemulsion preparation, then preparing plaster matrix, adding medicine-containing microemulsion preparation while stirring, and finally adding transdermal absorption accelerator.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to a medicine-containing microemulsion water matrix patch absorbed through human skin—a transdermal absorption preparation of insoluble medicine and a preparation process thereof. Background technique: [0002] In recent years, research on transdermal absorption preparations has become a hot topic in the field of pharmacy. This preparation has incomparable advantages over other preparations: 1. It can avoid the first-pass effect of the liver and degradation in the gastrointestinal tract, allowing the drug to directly enter the blood circulation of the human body To exert the efficacy of the drug, the absorption of the drug is not affected by gastrointestinal factors, which reduces the individual differences in drug use. 2. It can produce a constant and controllable blood drug concentration, avoid the peak and valley phenomenon of blood drug concentration caused by oral administrat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K45/00A61K47/30A61M37/00
Inventor 李华李嘉煜潘卫三
Owner SHENYANG PHARMA UNIVERSITY