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Compressed tablet containing [delta]9-tetrahydrocannabinol, method for its manufacture and use of such tablet in oral treatment

A technology of tetrahydrocannabinol and tablet, applied in the field of compressed tablet, can solve the problems of poor absorption, poor solubility and dispersibility, etc.

Active Publication Date: 2016-08-17
艾克制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Lipophilic medicinal substances such as THC are often poorly absorbed from the intestinal environment, especially due to their poor solubility and / or dispersibility in water

Method used

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  • Compressed tablet containing [delta]9-tetrahydrocannabinol, method for its manufacture and use of such tablet in oral treatment
  • Compressed tablet containing [delta]9-tetrahydrocannabinol, method for its manufacture and use of such tablet in oral treatment
  • Compressed tablet containing [delta]9-tetrahydrocannabinol, method for its manufacture and use of such tablet in oral treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0122] THC-granules were prepared by wet granulation method. Table 1 describes the composition of THC-particulates.

[0123] Table 1: Composition of THC-particulate matter

[0124]

[0125]

[0126] 1 Anhydrous, crystalline lactose (mass weighted mean particle size approx. 150 μm)

[0127] A granulation fluid comprising THC, sucrose monolaurate and ascorbic acid at a combined concentration of 0.7 g / ml was prepared as follows. Weigh out the desired amount of THC in a beaker. In another beaker, dissolve ascorbic acid (AA) in 120 ml of ethanol. The solution was heated to 60 °C and stirred to help dissolve the AA. Dissolution of AA was complete in approximately 15 minutes. When the AA had dissolved, this solution was added to the beaker containing THC. The required amount of sucrose monolaurate (SML) was also added to the beaker containing THC. The mixture was heated to 45°C and stirred to aid dissolution. The granulation fluid was stirred for 10 to 15 minutes until...

Embodiment 2

[0130] The THC-granulate obtained in Example 1 was blended with excipients and directly compressed into tablets containing 0.75 mg THC, 1.5 mg THC or 5 mg THC for oral administration. The ingredients and weights used to prepare the tablets are given in Table 2. The specifications for the compressed tablets are given in Table 3.

[0131] Table 2: Composition for the preparation of tablets containing 0.75 mg, 1.5 mg or 5 mg THC

[0132]

[0133] 1 Anhydrous, crystalline lactose, mass-weighted mean diameter approximately 150 μm

[0134] Table 3: Specifications for compressed tablets

[0135]

Embodiment 3

[0137] The dissolution rate of THC from the compressed tablets described in Example 2 was tested on oral tablets (5 mg THC) according to European Pharmacopeia (Ph. Eur. 2.9.3). For comparison, the dissolution rate of pure THC (5 mg) was determined according to the same method.

[0138] The dissolution medium consisted of 1 wt.% SDS in water. The pH of the medium was adjusted to pH 7 with diluted HCl. During the experiments, the temperature of the dissolution medium was maintained at 36°C to 41°C under stirring.

[0139] Samples were taken with disposable syringes at various time intervals after dropping the tablets into the dissolution medium. Samples were immediately syringe filtered into HPLC vials and analyzed by HPLC. The results of the solubility tests are summarized in Table 4.

[0140] Table 4: % THC Dissolved (w / w)

[0141]

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PUM

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Abstract

The present invention relates to compressed tablets for peroral deliveryof the cannabinoid [delta]9-tetrahydrocannabinol(THC).More particularly, the invention provides a compressed tablet having a tablet weight of 25-1000 mg, said tablet being composed of: compressed tablet containing delta 9-tetrahydrocannabinol, method for its manufacture and use of such tablet in oral treatment . 30-90 wt % of a granulate; . 10-70 wt % of lactose; and . 0-30wt % of other tablet excipients; wherein the granulate contains: a.2-5 wt % of [delta]9-tetrahydrocannabinol; b.2-20 wt % of sucrose fatty acid mono-ester; c.50-96 wt % of lactose; d.0.05-0.6 wt % of antioxidant; and e.0-25wt % of other granulate excipients. The compressed tablets according to the invention can conveniently be used in the treatment of spasticity and pain caused by multiple sclerosis, neurophatic pain, chronic pain, behavioral disturbance by Alzheimer's disease, stroke, spinal cord injury, peripheral neuropathy, neurogenic pain, nociceptive pain and nausea. The invention further provides a method for the manufacture of the compressed tablets.

Description

[0001] invention technical field [0002] The present invention relates to compressed tablets containing granules comprising lactose particles, Δ9-tetrahydrocannabinol and sucrose fatty acid monoesters. These compressed tablets are particularly suitable for oral administration and can be conveniently used in oral therapy, especially for the treatment of spasticity and pain due to multiple sclerosis, neuropathic pain, chronic pain, behavioral disturbances due to Alzheimer's disease , stroke, spinal cord injury, peripheral neuropathy, neuropathic pain, nociceptive pain, and nausea. The invention also provides the manufacturing method of the compressed tablet. Background of the invention [0003] It has long been known that different cannabinoids are the main active constituents of the plant Cannabis sativa (cannabis) and that they possess pharmacological activity. Well-known examples of such cannabinoids are Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD). [0004] THC is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/16A61K9/20A61K31/352
CPCA61K9/145A61K9/2018A61K9/2095A61K31/352A61K9/2009A61K9/2013A61K9/2054A61K9/2077
Inventor 让·艾伯特·德弗里斯玛丽亚·瓦内萨·费尔南德兹希德安娜·玛丽亚·埃雷迪亚洛佩斯克里斯蒂娜·玛丽亚·埃罗瓦马丁内斯
Owner 艾克制药有限公司
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