Medicament for treating inflammatory bowel disease

A technology for inflammatory bowel disease and medicine, which is applied in the field of colon-targeted pellets and preparation thereof, and can solve the problem that the active metabolite of ciclesonide that does not function as a system can be used, the bioavailability is small, the undisclosed avoidance or Alleviate problems such as side effects

Inactive Publication Date: 2009-01-21
TIANJIN PHARMA GROUP CORP
View PDF3 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Chinese patent application (application number CN 98119007.3 publication date 1999-02-24) discloses a pharmaceutical composition containing dexamethasone, and discloses that the pharmaceutical composition can be used for the treatment of UC and CD, but in this application, Only discloses the curative effect of the short-term treatment of the pharmaceutical composition, and does not disclose how to avoid or reduce the side effects of long-term use
[0008] At present, there is no report that oral ciclesonide can metabolize the active metabolite des-CIC (des-CIC) in the human colon. On the contrary, Clin Pharmacokinet 2004; 43 (7) 479-486 reported that the Pharmacokinetic studies of ciclesonide after oral administration to healthy subjects demonstrated that any orally administered ciclesonide has no effect on systemically available ciclesonide or its active metabolites
At the same time, the literature also reported that the systemic bioavailability of des-CIC, the active metabolite of CIC, was less than 1% after injection.

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

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Medicament for treating inflammatory bowel disease
  • Medicament for treating inflammatory bowel disease
  • Medicament for treating inflammatory bowel disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Weigh 1 gram of ciclesonide, 9 grams of β-cyclodextrin, 6 grams of polyethylene glycol 6000, and 1 gram of talcum powder, and disperse the above materials in 45 grams of water under stirring; Slowly disperse in 10 grams FS30D (based on solid content) polymer suspension, passed through a 120-mesh sieve to prepare a medicinal water dispersion suspension (referred to as liquid); in addition, weigh 3 grams of talcum powder, 4.5 grams of triethyl citrate gram, add 20 grams of water and mix well to make a water-dispersed suspension, which is slowly added to the weighed 25 grams of A water-dispersed suspension was formed in FS30D, and the mixed solution was passed through a 120-mesh sieve to prepare a colon coating solution (referred to as solution). The colon-targeted pellets were prepared by spraying and solution on the sugar core pellets by fluidized bed coating method. The prepared micropills were assayed, and the results were: the peak time of the bulk drug (refer...

Embodiment 2

[0073] Weigh 40g ciclesonide, 120g beta-cyclodextrin, 105g polyethylene glycol 6000, 100g polyethylene glycol 4000, 20g talcum powder, and disperse the above materials in 600g water under stirring; Slowly disperse in 150g of FS30D (based on solid content) polymer suspension, pass through a 120-mesh sieve to prepare a medicinal water dispersion suspension (abbreviated as liquid); in addition, take 20g of talcum powder and 5g of triethyl citrate, Add 30g of water and mix well to make a water dispersion suspension, and slowly add the suspension to the weighed coating material under stirring 220g of FS30D (based on solid content) was used to form a water-dispersed suspension, and the mixture was passed through a 120-mesh sieve to prepare a colon coating solution (abbreviated as solution). The colon-targeted pellets were prepared by spraying and solution on the sugar core pellets by fluidized bed coating method. The measured release see figure 2 .

Embodiment 3

[0075] Weigh 35g ciclesonide, 70gβ-cyclodextrin, 20g polyethylene glycol 6000, 50g polyethylene glycol 4000, 20g talcum powder, and disperse the above materials in 350g water under stirring; Slowly disperse in 50g of FS30D (based on solid content) polymer suspension, passed through a 120 mesh sieve to prepare a medicinal water dispersion suspension (abbreviated as liquid); in addition, weigh 6g of talcum powder and 15g of triethyl citrate, Add 70g of water and mix well to make a water dispersion suspension, and slowly add the suspension to the weighed coating material under stirring FS30D170g forms a water-dispersed suspension, and passes the mixed solution through a 120-mesh sieve to prepare a colon coating solution (referred to as solution). Using the fluidized bed coating method, the solutions and were sprayed on the blank core to prepare colon-targeted pellets. For the results of the determination of the release rate, see figure 2 .

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

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
Login to view more

Abstract

The invention relates to a colon-targeted pellet and a preparation method thereof, in particular to a colon-targeted pellet with ciclesonide and a preparation method thereof. The invention also discloses a pharmaceutical composition for treating inflammatory bowel diseases in mammals, especially in human; and the pharmaceutical composition consists of an active component and a pharmaceutically acceptable adjuvant for oral administration, which is characterized in that the active component contains the ciclesonide.

Description

technical field [0001] The invention relates to a colon targeting pellet and a preparation method thereof. In particular, colon-targeted pellets containing ciclesonide and methods for their preparation. Background technique [0002] Inflammatory bowel disease (IBD) is a chronic non-specific intestinal inflammatory disease of unknown etiology, including ulcerative colitis (ulcerative colitis, UC) and Crohn's disease (Crohn's disease, CD). Clinically, non-steroidal anti-inflammatory drugs and glucocorticoids are often used for treatment. However, non-steroidal anti-inflammatory drugs have large gastrointestinal reactions, and can induce clinical recessive enteropathy such as intestinal perforation and inflammatory lesions... Long-term use of glucocorticoids can cause immunosuppression and adrenal cortex suppression due to systemic absorption. series of side effects. Therefore, reducing or avoiding the side effects of drugs for the treatment of UC and CD has become one of th...

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): A61K31/58A61K9/16A61K47/32A61K47/40A61P1/12
Inventor 卢彦昌李静张乐陈松
Owner TIANJIN PHARMA GROUP CORP
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