Pharmaceutical preparation comprising permethylated cyclodextrin

A composition, cyclodextrin technology, applied in the directions of drug combination, active ingredients of hydroxyl compounds, drug delivery, etc., can solve the problems of incorrect dose, uncoordinated, difficult to calculate, etc. Improve, fast and reliable transmission, improve the effect of transmission speed

Active Publication Date: 2011-04-06
荣威·诺伯特 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Bioavailability for oral use is very variable and therefore difficult to calculate
Possibly incorrect dosage for anxiolytics cannot be ruled out
[0008] In addition, the distribution time of 45 to 60 minutes necessary to obtain adequate plasma concentrations when administered orally is not compatible with hospital scheduling requirements
In order to make the surgical facilities operate at a high load, the patients are usually notified 15 minutes before the operation to prepare. Taking benzodiazepines orally during such a short preparation time cannot achieve effective preoperative anxiolytics

Method used

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  • Pharmaceutical preparation comprising permethylated cyclodextrin
  • Pharmaceutical preparation comprising permethylated cyclodextrin

Examples

Experimental program
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Effect test

Embodiment 1

[0043] Midazolam compositions for transmucosal administration.

[0044] A 1% midazolam composition for transmucosal administration is formulated as follows

[0045] Midazolam 10mg

[0046] Fully methylated β-cyclodextrin (methylation degree 3) 150mg

[0047] Hypromellose 400 (hypromellose) 1mg

[0048] Concentrated phosphoric acid 2.6mg

[0049] NaOH 10%: Appropriate amount, adjust the pH value to 4.2

[0050] Potassium sorbate 1.4mg

[0051] water to 1ml

[0052] Hypromellose 400 is a hydroxypropylmethylcellulose with a molecular weight of approximately 400 that acts as a mucosal wetting agent. The pH of the prepared solution was adjusted to 4.2. The mass ratio of cyclodextrin and pharmaceutical active substance in this embodiment is 15:1, the mass ratio of cyclodextrin of the present invention and pharmaceutical active substance is preferably 50:1 to 10:1, more preferably 40:1 to 12:1 , more preferably 20:1 to 12:1.

[0053] A group of five subjects were each given ...

Embodiment 2

[0063] Intravenous propofol composition

[0064] Two 1% formulations of propofol were used. A kind of is the preparation of prior art, the fat emulsion of business name Diprivan, and emulsion matrix is ​​made up of soybean oil, glycerol, lecithin, contains 1% propofol in the emulsion matrix.

[0065] Formula of the present invention:

[0066] Propofol 10mg

[0067] Permethylated β-cyclodextrin 80.2mg

[0068] Concentrated phosphoric acid 2.mg

[0069] NaOH 10%: Appropriate amount, adjust the pH value to 6.8

[0070] water to 1ml

[0071] Hereinafter, this formula is referred to as CD-Prppofol (CD propofol).

[0072] Each of twelve Göttingen minipigs weighing between 48 and 53 kg were randomly anesthetized with Diprivan and CD-Prppofol (CD Propofol). Injection is performed through a peripheral venous catheter.

[0073] The depth of anesthesia is monitored by the depth of anesthesia monitor CSM (cerebral state monitoring) and the corresponding depth of anesthesia index C...

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Abstract

The invention relates to a pharmaceutical preparation for applying a pharmaceutical agent. According to the invention, the preparation contains: a) a pharmaceutical agent which has an aromatic group or an aromatic part and the molecule of which has a maximum diameter of = 2 nm; b) a permethylated cyclodextrin having a degree of substitution of 3 methyl groups per glucopyranose unit. The permethylated cyclodextrin and the pharmaceutical agent form a complex.

Description

technical field [0001] The present invention relates to a pharmaceutical composition, such as a composition for preoperative anxiolysis or anesthesia. Background technique [0002] After the pharmaceutically active substance is made into a preparation, it is a common problem in pharmacy to achieve the desired concentration and possible effect at the intended site of action through a certain form of administration. A proposed active substance for intravenous administration must therefore be water-soluble to some extent in order to achieve the intended systemic concentration in the blood. On the other hand, in order to reach the site of action or penetrate the cell membrane, the active substance should in principle have a certain lipophilicity. For example, a well water-soluble active substance that achieves high systemic concentrations in the blood after intravenous administration, however, exhibits poor bioavailability due to the low lipophilicity of the active substance, w...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/05A61K31/715
CPCA61K31/05A61K31/715A61K9/006A61K9/0019A61P25/00A61P25/04A61P25/22A61P29/00
Inventor 荣威·诺伯特布罗沙伊特·延斯
Owner 荣威·诺伯特
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