Process for preparation of inclusion compounds between a non-steroidal anti-inflammatory drug and betacyclodextrin by microwave treatment

一种制备药物、环糊精的技术，应用在医药配方、薄料处理、纳米药物等方向，能够解决大量、连续运转的方法不可能、耗时制备方法等问题，达到好治疗效果、有利药动学性质、减少生产次数的效果

Inactive Publication Date: 2005-07-13
CHIESI FARM SPA
View PDF4 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] Although many of these techniques have been used on an industrial scale, they usually involve time-consuming preparation methods and large amounts of solvents; in addition, continuous operation methods are not possible

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1-piroxicam: β-cyclodextrin inclusion complex

[0047] Preparation of Physical Mixtures

[0048] Accurately weigh about 10 g of piroxicam (PRX) and 92 g of β-cyclodextrin (βCD), the molar ratio of which is 1:2.5.

[0049] Combine the two powders and mix thoroughly to ensure an even distribution of particles.

[0050] After addition of water (ca. 70 ml) and 28% ammonia (1.5 ml), the physical mixture was mixed with an Ultraturrax vortex mixer at 9500 rpm for 5 minutes.

[0051] microwave treatment

[0052] Three aliquots of each approximately 25 gram portion were taken from the resulting cream paste. The sample was placed in a crystallizer, covered with a glass fiber plate to prevent it from spilling into the furnace, and microwaved according to the following protocol:

[0053] PRX:βCD

time

Power (W)

Vacuum pressure (mbar)

The first stage

5 minutes 30 seconds

450

～250

second stage

5 points

0

...

Embodiment 2

[0070] Embodiment 2-ketoprofen: β-cyclodextrin inclusion complex

[0071] Preparation of Physical Mixtures

[0072] Accurately weigh about 2 g of ketoprofen (keto) and 9.960 g of β-cyclodextrin, the molar ratio of which is 1:1.

[0073] Mix the two powders thoroughly to ensure an even dispersion.

[0074] After adding water (~8ml), the physical mixture was mixed with an Ultraturrax vortex mixer at 8000 rpm for 3 minutes.

[0075] microwave treatment

[0076] Three samples of approximately 5 grams each were taken and the samples were placed in a crystallizer and microwaved. Since the amount of material to be dried is directly proportional to the exposure time to microwaves, when reducing the amount of material per sample, the heating time can also be reduced.

[0077] The methods described below are summarized in Table 3.

[0078] Keto: βCD

time

Power (W)

Vacuum pressure (mbar)

The first stage

2 minutes 30 seconds

450

～250

...

Embodiment 3

[0081] Example 3-ketoprofen: hydroxypropyl-β-cyclodextrin inclusion complex

[0082] Preparation of Physical Mixtures

[0083] Accurately weigh about 2 g of ketoprofen (keto) and 10.5 g of cyclodextrin, the molar ratio of which is 1:1.

[0084] The two powders were mixed until uniformly dispersed; water (-5.5 ml) was added to the dispersion and the resulting mixture was mixed with an Ultraturrax vortex mixer at 8000 rpm for 3 minutes.

[0085] microwave treatment

[0086] Three samples of approximately 4 grams each were taken from the resulting mixture and the samples were microwaved as described herein.

[0087] Table 4. Parameters related to microwave treatment of three ketoprofen / hydroxypropyl-β-cyclodextrin-mixture samples

[0088] Keto / HPβCD

[0089] After this operation, the sample weight loss averaged about 30%. And the melting peak of the active ingredient disappeared again.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

A process for the preparation of inclusion complexes of a drug (piroxicam or ibuprofen) and a cyclodextrin, characterised in that: a) the drug and cyclodextrin, in the form of finely divided powders, are mixed in the presence of aqueous or hydroalcoholic solutions, ammonia solutions or acid solutions; b) the resulting mixture is treated in a microwave oven; c) the resulting product is dried under vacuum at room temperature or with heating.

Description

field of invention [0001] The invention relates to a new method for preparing inclusions of medicine and cyclodextrin. [0002] According to the invention, the powdered ingredients are mixed to form a suitable aqueous or hydroalcoholic suspension. Subjecting the suspension to microwave treatment results in a product having physical, technological and biopharmaceutical properties suitable for the preparation of solid pharmaceutical formulations, wherein said product contains the drug in predominantly or entirely amorphous form. [0003] Specifically, the method of the present invention can generate inclusion complexes of drugs and cyclodextrins, which have stronger wettability and better dissolution balance than crystalline drugs, and are soluble in aqueous media. faster. This means a more favorable pharmacokinetic profile and thus may have a better therapeutic effect. Background technique [0004] Many substances used as active ingredients (drugs) are characterized by the...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48
CPCB82Y5/00A61K47/6951Y10T428/662
Inventor F·乔尔丹诺R·贝蒂尼
Owner CHIESI FARM SPA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap