Granulate containing a pharmaceutically active substance and method for its manufacture
A technology of drug activity and emulsifier, which is applied in the direction of pharmaceutical formulation, drug combination, drug delivery, etc., can solve the problems of poor dispersion and achieve rapid absorption
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Examples
Embodiment 1
[0113] Sucrose monolaurate (HLB=15) and tetrahydrocannabinol (THC) were heated to 120°C under nitrogen flow. The ratio of THC to sucrose monolaurate was 1:15 (by weight). After mixing thoroughly, use either of the following methods to 2 To saturate (and thus soften) a putty-like melt:
[0114] • Pour the warm melt into an autoclave preheated to 120°C and pressurize to 250 bar. The autoclave was pressurized with carbon dioxide using a plunger pump (LeWa) and heated with heating oil through the jacket. By utilizing Büchi TM Magnetic stirrer in supercritical CO 2 Stir the melt for at least 30 minutes in CO 2 Saturation takes place, whereby the lump is further liquefied.
[0115] • Cool the melt to -20°C and crush to obtain maximum surface area. For this, use a mortar precooled to -20 °C in an inert dry atmosphere. The resulting powder was poured into an autoclave preheated to 60° C. and pressurized to 250 bar. The autoclave was pressurized with carbon dioxide using a plu...
Embodiment 2
[0118] THC was dissolved in a 65% (w / v) solution of sucrose monolaurate in 2-propanol to a final concentration of 7.3% (w / v). The high pressure vessel was pressurized to 200 bar with carbon dioxide by a plunger pump (Williams) and heated to 40°C with heating oil through the jacket.
[0119] The solution was sprayed into the container by a syringe pump (ISCO 260D) through a coaxial nozzle. The nozzle consists of two concentric tubes; 25 ml / min of emulsion is fed through the inner tube (inner diameter = 0.5 mm, outer diameter = 1.27 mm) and 500 g / min of carbon dioxide is fed through the outer tube (inner diameter = 1.7 mm). The carbon dioxide was heated to 60°C before nebulization. The powder formed in the container was collected on a filter at the bottom of the container. The microparticles have an average diameter measured by S.E.M. of 5-50 μm.
Embodiment 3
[0121] Dilute water with sucrose stearate (Crodesta TM F-160; HLB=15) mixed. The mixture was heated to 60 °C and the Ultraturrax TM The blender disperses the molten THC into this mixture until a stable emulsion forms. The resulting oil-in-water emulsion contained 10 wt.% THC, 30 wt.% sucrose stearate and 60 wt.% water. The autoclave was heated to 40°C with heating oil through the jacket.
[0122] Using CO 2 The autoclave was pressurized to 30 bar and the solution was sprayed into the vessel through two fluid nozzles using a syringe pump (ISCO 260D). This nozzle consists of two concentric tubes; 0.3 ml / min of emulsion is fed through the inner tube (inner diameter = 0.5 mm, outer diameter = 1.27 mm) and 500 g / min of carbon dioxide is fed through the outer tube (inner diameter = 1.7 mm). Carbon dioxide was heated to 40°C before nebulization. The powder formed in the container was collected on a filter at the bottom of the container. The microparticles have an average diam...
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Abstract
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