Medicinal composition

A composition and compound technology, applied in the field of medicine, can solve the problems of unsuitable preparation of injections, low water solubility, insoluble in various mineral oils, etc.

Inactive Publication Date: 2013-10-23
SHANGHAI HUATUO MEDICAL SCI CO LTD
View PDF5 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, as we all know, most of the camptothecin drugs have low water solubility, such as 9-nitrocamptothecin, camptothecin, 9-aminocamptothecin, etc. are insoluble in water, and difficult to dissolve in various mineral oils, with poor stability , not suitable for preparation into injection
Yan Jingchao and others studied the pharmacokinetics of 9-nitrocamptothecin in dogs, and found that the absolute bioavailability of 9-nitrocamptothecin was very low (less than 6%) after oral administration [Yan Jingchao et al. Pharmacology and Therapeutics (2005), 10(11)]

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
  • Medicinal composition
  • Medicinal composition
  • Medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] The preparation of embodiment 1 medicinal composition

[0022] 1) Formulation:

[0023] Compound of formula I

1g

Hydroxypropyl-β-cyclodextrin

800g

Add water to

2000ml

[0024] 2) Preparation:

[0025] Take 800g of hydroxypropyl-β-cyclodextrin (MS4.1 ~ 4.8), add water for injection and stir to dissolve to 80% of the total volume; add hydrochloric acid, adjust pH = 3.5 ~ 4.5; add the compound of formula I and stir to dissolve; add Activated carbon for medicine, stirring and adsorption, decarbonization; add water to the full amount, sterilize and filter, spray dry or freeze-dry after sub-packaging, or directly sub-package.

Embodiment 2

[0026] The preparation of embodiment 2 pharmaceutical compositions

[0027] 1) Formulation:

[0028] Compound of formula I

1g

Sodium sulfobutyl ether β-cyclodextrin

800g

Add water to

2000ml

[0029] 2) Preparation:

[0030] Take 800 g of sodium sulfobutyl ether β-cyclodextrin (MS4.1-4.8), add water for injection and stir to dissolve to make the total volume 80%; add hydrochloric acid to adjust pH=3.5-4.5; add the compound of formula I and stir to dissolve; Add medicinal activated carbon, stir for adsorption, and decarbonize; add water to the full amount, sterilize and filter, spray dry or freeze-dry after sub-packaging, or directly sub-package.

Embodiment 3

[0031] The preparation of embodiment 3 medicinal compositions

[0032] 1) Formulation:

[0033] Compound of formula I

1g

Sodium sulfobutyl ether β-cyclodextrin

400g

Hydroxypropyl-β-cyclodextrin

400g

Add water to

2000ml

[0034] 2) Preparation:

[0035] Take 400g of sulfobutyl ether β-cyclodextrin sodium (MS4.1~4.8) and 400g of hydroxypropyl-β-cyclodextrin (MS4.1~4.8), add water for injection and stir to dissolve to 80% of the total volume Add hydrochloric acid to adjust pH=3.5-4.5; add compound I and stir to dissolve; add medicinal activated carbon, stir for adsorption, decarbonize; add water to the full amount, sterilize and filter, spray dry or freeze-dry after subpackaging, or directly divide Pack.

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

Disclosed in the present invention is a pharmaceutical composition, comprising a weight ratio of 1 : 120 to 1 : 1000 of Camptothecin compounds of formula I and beta-cyclodextrin or derivatives thereof, and an acidic buffer to adjust the pH = 3.5-6.0. The composition can be used to treat solid tumours, such as melanoma, pancreatic cancer, liver cancer, etc. The pharmaceutical composition of the present invention is miscible with a water-miscible co-solvent system in any proportion, and can be used as an intravenous infusion solvent, and has no obvious hemolysis or vascular stimulation; the pharmaceutical composition has a better tumour inhibiting rate than solubilization of surfactants.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a camptothecin pharmaceutical composition, in particular to a camptothecin compound containing the structure of formula I, water-soluble β-cyclodextrin and its derivatives for treating solid tumors. Pharmaceutical compositions of substances. Background technique [0002] Chinese invention patent CN1897942A discloses the following content: the water solubility of medicine plays an important role in the preparation of pharmaceutical dosage forms. For the oral route of administration, much experience has shown that potential absorption problems may arise if the water solubility of the substance is not greater than 10 mg / ml in the pH range 1-7. Solubility less than 1 mg / ml may result in dissolution rate limited absorption due to the correlation between solubility and dissolution rate. [0003] Camptothecin anticancer compounds are mainly given intravenous injection, and there are al...

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): A61K31/4745A61K47/40A61K9/19A61P35/00
CPCA61K47/40A61K9/20A61K9/19A61K9/08A61K31/4745A61P35/00
Inventor 唐开勇潘俊芳朱勤方通牛成成李万亥吕伟卿晨范国荣
Owner SHANGHAI HUATUO MEDICAL SCI CO LTD
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