Hydrophilic binary systems for the administration of cyclosporine

A cyclosporine, hydrophilic phase technology, applied in the directions of antibacterial drugs, cyclic peptide components, resistance to vector-borne diseases, etc., can solve the problems of difficult production, high cost of ternary preparations, etc., and achieve the effect of easy preparation

Inactive Publication Date: 2000-04-12
ABBVIE INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, the complexity of these ternary formulations makes them expensive and difficult to produce

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 24

[0043] Composition %w / v

[0044] Cyclosporin A 13

[0045] Absolute ethanol 10

[0046] Propylene Glycol 10

[0047] CREMOPHOR  EL 37

[0048] SPAN  80 20

[0049] PEG 3350 10

Embodiment 25

[0051] The oral bioavailability of the compositions of the invention was evaluated in fasted beagle dogs as follows:

[0052] Compositions of Examples 1-24 and SANDIMMUNE containing commercial cyclosporine product  Oral solution (100mg / ml) and OPTORAL  Oral solution (100 mg / ml) of the control substance was administered to the test animals in an amount that released 50 mg of cyclosporin A to each dog. The compositions of Examples 16-24 were administered in hard gelatin capsules. Blood concentration data were normalized to a dose of 5 mg / kg per dog.

[0053] During the general test, six dogs were fasted and then given a composition at t=0. Blood samples were taken at 15, 30, 60 and 90 minutes and at 2, 4, 6, 9, 12, 15 and 24 hours post-dose and analyzed for cyclosporine blood concentrations. From these data, the maximum serum concentration (C max ), time from dosing to maximum serum concentration (T max ), the total amount absorbed (AUC) and their respective standard dev...

Embodiment 26

[0081] Additional bioavailability studies were performed on human subjects comparing the partially semisolid composition of the present invention with the commercially available cyclosporine product NEORAL  (300mg SEC) for comparison. The test compositions were administered in hard gelatin capsules and data were collected at the same regular intervals as above. The results are shown in Table 2, where the bioavailability is log-transformed C of the tested composition. max and AUC data relative to NEORAL  The comparison data are calculated. ("CI" represents the statistical confidence range for the respective bioavailability).

[0082] Table 2

[0083] The relative bioavailability of cyclosporine A Example label relative 1n (C max ) 90% CI vs 1n(AUC) 90% CI

[0084] 17 0.758 0.688-0.835 0.729 0.698-0.761

[0085] 21 0.773 0.700-0.854 0.810 0.775-0.846

[0086] 23 0.856 0.800-0.917 0.839 0.793-0.888

[0087] 24 0.884 0.819-0.955 0.898 0...

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Abstract

Binary pharmaceutical compositions comprising (i) a cyclosporine compound, (ii) a hydrophilic phase and (iii) a surfactant provide bioavailability of the active ingredient which is equivalent to that provided by ternary compositions, but without the need for a lipophilic phase.

Description

technical field [0001] The present invention relates to pharmaceutical compositions containing lipophilic pharmaceutical compounds suitable for oral, topical, topical and other routes of administration. In particular, the present invention relates to cyclosporine binary formulations comprising a hydrophilic phase and one or more surfactants, but no lipid phase. Background of the invention [0002] Highly lipophilic pharmaceutical compounds present a formulation problem. Due to their low solubility in aqueous media, including the contents of the digestive tract of mammals, these compounds often have poor or variable bioavailability when administered orally or by other routes requiring transdermal absorption Spend. Examples of such pharmaceutical compounds include the immunosuppressants cyclosporine and FK506 (tacrolimus); protease inhibitors such as ritonavir; central nervous system drugs such as tiagabine; Enzyme inhibitors. [0003] One method of formulating lipophilic ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/48A61K38/00A61K38/13A61K47/00A61K47/10A61K47/14A61K47/16A61K47/26A61K47/32A61K47/34A61K47/44A61P31/00A61P31/04A61P31/12A61P37/06
CPCA61K9/4858A61K47/44A61K38/13A61K9/1075A61K47/26A61K47/10Y10S514/975Y10S514/885A61P31/00A61P31/04A61P31/12A61P37/06Y02A50/30A61K9/00A61K47/00
Inventor L·A·阿尔-拉扎克P·P·康斯坦蒂尼德斯D·考尔J·M·利帕里L·L·麦彻斯-内-哈里斯B·Y·阿布杜拉
Owner ABBVIE INC
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