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Continuous complexation of active pharmaceutical ingredients

A technology for active pharmaceutical ingredients and drugs, applied in the field of complexes of active pharmaceutical ingredients, can solve the problems of increasing the ratio of active pharmaceutical ingredients/cyclodextrin and the like

Active Publication Date: 2018-11-09
HOVIONE SCIENTIA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0015] It is an object of the present invention to provide an improved complexation process between cyclodextrins and active pharmaceutical ingredients, without the disadvantages of the known processes, and which allows for a shorter time, at higher complex concentrations, Lower solvent loads to obtain desired complexes, possibility to increase API / cyclodextrin ratio, and energy input to occur in a spontaneous manner

Method used

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  • Continuous complexation of active pharmaceutical ingredients
  • Continuous complexation of active pharmaceutical ingredients
  • Continuous complexation of active pharmaceutical ingredients

Examples

Experimental program
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Effect test

Embodiment 1

[0089] 60 grams of water were added to the stirred reactor. To this reactor was added 40 grams of sulfobutyl ether-β-cyclodextrin. The suspension was continuously stirred until a clear solution formed. Then, 1 gram of the active pharmaceutical ingredient (in this case using itraconazole as the model drug) was added to the solution and the timer was set immediately. The resulting suspension was stirred continuously at 25°C. 2 g of the suspension was filtered per day and analyzed by HPLC to determine the complex concentration. Figure 4 The results are shown in (dotted line).

Embodiment 2

[0091] 60 grams of water were added to the stirred reactor. To this reactor was added 40 grams of sulfobutyl ether-β-cyclodextrin. The suspension was continuously stirred until a clear solution formed. In the case of device A, 10 grams of the active pharmaceutical ingredient (itraconazole) was added to the solution and the timer was set immediately. The resulting suspension was fed to a booster pump at a pressure of 550 bar at room temperature for 1 hour. 2 g samples from the suspension were filtered every 10 minutes and analyzed by HPLC to determine the complex concentration. After 1 hour, the solution was spray-dried to obtain a powdery substance. Figure 4 The results are shown in (dotted line).

Embodiment 3

[0093] 60 grams of water were added to the stirred reactor. To this reactor was added 400 grams of sulfobutyl ether-beta-cyclodextrin. The suspension was continuously stirred until a clear solution formed. In the case of device A, 10 grams of the active pharmaceutical ingredient (itraconazole) was added to the solution and the timer was set immediately. The suspension formed was fed to a booster pump at a pressure of 550 bar at room temperature for 3 hours. 2 g samples from the suspension were filtered every 10 minutes and analyzed by HPLC to determine the complex concentration. After 3 hours, the solution was spray-dried to obtain a powdery substance. Figure 4 The results are shown in (solid line).

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Abstract

A complexation process between a cyclodextrin and active pharmaceutical ingredients is disclosed, and comprises a process for preparing a complex of at least one cyclodextrin and at least one active pharmaceutical ingredient comprising the steps of: a. preparing a first solution (solution A) comprising at least one cyclodextrin and at least one solvent; b. preparing a second solution (solution B)comprising at least one dissolved, partially dissolved or suspended API; c.Mixing said solution A and solution B by means of a microfludization system to produce a solution and / or suspension of at least one of said complex; d. isolating said solution and / or suspension and / or optionally drying it; and e. optionally collecting a powdered form of the complex. The described process has high throughputwith higher yields of complexation in less time than prior art methods. The complexes obtained by the invention are characterized by having enhanced dissolution and / or bioavailability of the activepharmaceutical ingredient in body fluids.

Description

technical field [0001] The present invention relates generally to complexes of active pharmaceutical ingredients (APIs), particularly those based on one or more cyclodextrins, and to improved methods of providing such complexes. Background technique [0002] Several active pharmaceutical ingredients have low water solubility, which reduces their bioavailability and dissolution in body fluids. Currently, several techniques can be used to solve this problem, for example, amorphous solid dispersions, co-crystals, salification or cyclodextrin complexes. [0003] Cyclodextrins are cyclic oligosaccharide compounds of 6, 7 or 8 repeating units with an increased diameter of the hydrophobic cavity. Depending on the number of repeating units, they can be designated as α, β or γ, respectively. Cyclodextrins can be prepared, for example, by enzymatic conversion of starch. Their outer groups are hydrophilic and can be chemically modified, while their inner cavity can be hydrophobic, w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/40A61K9/14A61K9/16
CPCA61K47/40A61K9/141A61K9/145A61K9/1623A61K31/496A61K31/724A61K47/6951A61K9/1694
Inventor H·利斯博阿M·特姆特姆J·文森特F·桑托斯
Owner HOVIONE SCIENTIA
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