Currently available cannabinoid dosage forms and innovative delivery systems in clinical evaluation


Currently available cannabinoid dosage forms and innovative delivery systems in clinical evaluation

Company Name Formulation Admin route Clinical status Indication Clinical trials db/notes Dose References
Abbvie Dronabinol Marinol® capsule THC synthetic Oral, capsule Market Nausea, cachexia 2.5–10 mg/twice daily Marinol® Product Monograph
AOP Orphan Pharmaceuticals Nabilone FTD THC derivative controlled release (CD) Oral, capsule Phase II/III Parkinson’s disease EudraCT2015-004227-31 0.25 mg up to qd [95, 96]
Pain EudraCT2017-004253-16
Aphios Corporation APH-1501 CBD encapsulated in biodegradable polymer nanospheres Oral, capsule Phase II Opioid addiction NCT03813095 400–800 mg BID
APH-0802 THC in nanospheres No recent development
APH-1403 CBD encapsulated in biodegradable polymer nanospheres as a lyophilised powder Oral Multiple sclerosis
Artelo Biosciences ART12.11 Co-crystal CBD-tetramethylpyrazine Oral Preclinical PTSD, IBD, Stroke and Rare Diseases
AusCann GH THC CBD Oral Phase 1 Pain ACTRN12620000462987 2.5–10 mg/dose [130, 131]
Axim Biotech MedChew THC CBD Oral Pain 2019 no reports [132–134]
AX 1505 cannabinoids in floating capsule Oral Preclinical Crohn’s disease 2020 no reports
Bausch Health Co Nabilone Cesamet® THC derivative Oral capsule Market Antiemetic 1–2 mg/BID Cesamet® Product Monograph
Beckley Canopy Therapeutics BCT 521 THC CBD Oral capsule Phase I II Cancer pain EudraCT2019-001382-32 2,5+3,5 mg
Bionorica SE BX1 THC synthetic Oral, liquid Phase II Spasticity, PTSD NCT04448808
Phase III Chemotherapy-induced damage NCT03984214 Up to 30 mg
Phase III Pancreatic cancer NCT03756974
Botanix Pharmaceuticals BTX1204 CBD Dermal/transdrmal gel/spray Phase II Skin disorders ACTRN12618001802291 150 μL 5% or 30% per 1 cm2
Cannabics Cannabics SR Cannabicromene Oral capsule Cachexia cancer NCT02359123 5 mg daily, BID [158, 159]
Cardiol Therapeutics CardiolRx Ultrapure CBD Oral Phase II/III Cardiac and vascular inflammation Covid-19 patients NCT04615949 25–7.5 mg/kg BID
CTX01 CBD nano micellar formulation Subcutaneous Preclinical Treatment of heart failure with preserved ejection fraction
Diverse Biotech (ex Leaf) CBD-conjugate Preclinical Cancer
BRCX014 CBD Sublingual Phase I Cancer NCT03687034 Escalating dose
Echo Pharmaceuticals Arvisol CBD Oral tablet Preclinical Epilepsy, Rett syndrome, schizophrenia [110, 111]
Namisol THC Oral tablet Phase II Anorexia; multiple sclerosis; pain ACTRN12619000491167 4.5 mg TID
Emerald Health Pharmaceuticals EHP-101 CBDVH Oral liquid Phase I Safety, PK NCT03745001 Escalating dose [161, 162]
Phase IIa Diffuse cutaneous systemic sclerosis NCT04166552 Escalating dose
NB 2221 THC-prodrug
EHP-102 Cannabigerol derivative Oral liquid Preclinical Huntington’s and Parkinson’s disease [165, 166]
Ethicann Pharmaceuticals THC CBD in Zydis tablet Oral/buccal disintegrating tablet Preclinical Muscle spasticity
CAN 001 cannabinoid oil Oral oil Preclinical Chemotherapy-induced nausea and vomiting
Futura Medical/CBDerma Technology CBD 100 Dermasys technology Transdermal Preclinical Pain
Greene Street Pharma CBD-Cubed TM technology Transdermal Preclinical Pain
GW Pharmaceutics GWP42003 Epidyolex® (Epidiolex®) CBD Oral liquid Market Dravet syndrome, Lennox–Gastaut syndrome 5 mg/kg BID Epidiolex Product Monograph
Epidiolex CBD Oral liquid Phase IV Low back pain NCT03891264 5–10 mg/kg BID
Epidiolex CBD Phase III Patients with Rett syndrome NCT03848832
Epidiolex CBD Oral liquid Phase II Adjunctive therapy in participants with schizophrenia NCT04421456 5 mg/kg day
Nabiximols Sativex® THC CBD 1:1 Buccal spray Market Neuropathic pain, spasticity, cancer pain, neuroprotection in Huntington’s disease 1 spray 2.5 mg each. Max 12 spray daily [302, 303]
Sativex® Product Monograph
Nabiximols THC CBD 1:1 Buccal spray Phase I Recurrent glioblastoma NCT01812603, NCT01812616) Temozolomide plus Max 12 spray daily
CBD THC Oral Phase I Cerebral ischaemia (in neonates)
GWP-42006 Cannabidivarin Oral, IV Phase II Autistic disorder; neuropathic pain; partial epilepsies; Prader–Willi syndrome; Rett syndrome NCT02369471 10 mg/kg/day
NCT03848481 10–20 mg/kg/day
GWP-42004 Delta-9-tetrahydrocannabivarin Oral capsule Phase II Type 2 diabetes mellitus NCT02053272 EudraCT2013-001140-61 2–15 mg BID
Hoverink Biotechnologies THC synthetic IV, Oral Preclinical Pain
Kali-Extracts/PAO Group NCMB1 Cannabidiol enriched extract In vitro data Chronic obstructive pulmonary disease
Claritas Pharmaceuticals K-1052 CBD-conjugates Preclinical Sepsis-induced acute renal failure and traumatic brain injury
KAL-1816 CBD conjugated with naproxen Oral, IV Preclinical
CBD Oral Phase I GVHD NCT03840512 75–300 mg BID
Knop Laboratorios KL 16-012 THC CBD Oral liquid Phase I Fibromyalgia NCT04239469 3 + 1.3 mg to 15 + 6.5 mg day
Inmed Pharmaceutical INM-755 Cannabinol Topical cream Phase I Symptoms of epidermolysis bullosa simplex
INM-088 Cannabinol Eye drop Preclinical Glaucoma
INSYS Therapeutics/Benuvia therapeutics Syndros® oral solution THC synthetic Oral solution Market Nausea, cachexia 2.1 mg/day Syndros® Product Monograph
Intec Pharma Cannabis extracts in Accordion Pills Oral solid Phase I Pain [136, 138]
IntelGenx/Tetra Bio Pharma THC synthetic in Adversa™ film and tablet Transmucosal Phase I, II Pain, antiemetic [182, 305]
Lexaria Bioscience TurboCBD™ CBD plus other substances Oral Market (OTC) Increased circulating CBD levels NCT03295903
Nanoemulsion CBD plus other substances Oral
MannKind Corp. THC dry powder Inhalation Phase 0 Chemotherapy-induced nausea and vomiting, and anorexia
Medlab Clinical THC CBD (1:1) in Nanocelle TM Buccal spray Preclinical Pain ACTRN12617001480370 2.5+2.5 mg/dose escalating
Medexus Pharm/Vireo Health CA2476833C CBD cyclodextrins Improved solubility
CBD in sulfoalkyl ether cyclodextrin Captisol
MMJ PhytoTech PTL101 CBD in gelatin matrix pellets Oral Phase II Paediatric epilepsy NCT02987114 Up to 25 mg/kg/day [121–123]
PTL401 THC CBD SEDDS Oral Phase I Pharmacokinetics
One World Cannabis THC CBD Topical cream Phase I Psoriasis NCT02976779 Max 30+30 mg/day
Preveceutical CBD gel Intranasal stop in 2017
PureForm Global synthetic CBD (??)
PhytoPain Pharma PPP 001 THC 9.5% CBD 2.5% Inhalation Phase II Cancer pain NCT04042545 1 inh TID
Inhalation Phase I Pharmacokinetics NCT04314804, NCT0446175 280 mg/TID
RespireRx Pharmaceuticals PP01 THC low dose Oral Phase III Sleep apnoea syndrome
Stero Biotech ST 101 CBD in olive oil Oral Phase IIa Autoimmune hepatitis and Crohn’s disease NCT04056442 Up to 150 mg TID
TFF Pharmaceuticals CBD dry powder Inhalation Undisclosed [178, 179]
Tetra BioPharma HCC 011 THC synthetic Inhalation Phase I Liver cancer, pain [173, 308]
PPP001 THC CBD Inhalation Phase II Pain NCT04042545 1 inh TID
PPP001 THC CBD Inhalation Phase III Cachexia NCT04001010 1 inh TID
PPP005 THC CBD Oral capsule Phase II/III Pain NCT03763851 (terminated) 1 + 1 to 2.5 + 2.5 mg
Zynerba Pharmaceuticals Zyn002 Permeation-enhanced CBD gel Transdermal Phase I, II Fragile X syndrome and other rare neuro-psychiatrics ACTRN12618001063202 2 sachets BID [228, 229, 231]
NCT03614663 250 mg BID
Zyn001 THC d-glyceric acid ester pro-drug Transdermal Phase I Discontinued 2020


Cannabinoids, indeed, have poor oral bioavailability (estimated to be as low as 6% of a similar dose administered intravenously). Pure THC and CBD show similar plasma concentration-time profiles, with a delay of 120 min before reaching peak concentration []. Bioavailability increases when it is co-administered with food lipids. A cannabis formulation in sesame oil (a vehicle with long chain triglycerides [LCT], containing 42% oleic, 40% linoleic and 16% palmitic acids) significantly improved the bioavailability of cannabinoids [].

The contribution of intestinal lymphatic transport is also worthy of note in the case of highly lipophilic compounds []. Indeed, the fatty acids generated by the lipolysis of medium and long chain triglycerides undergo several different processes: long chain fatty acids are associated to chylomicrons that are secreted into the lymphatic system instead of the portal vein. Thus, THC and CBD, used in combination with LCT, can bypass the liver, decreasing potential pre-systemic metabolism []. By avoiding loss in pre-systemic metabolism in the liver, cannabinoids can reach 22% bioavailability [].

The role of high-fat meals on pharmacokinetic behaviour is also relevant. A formulation for CBD (administered as a single 1500 mg dose at 100 mg/mL in a sesame-oil vehicle) showed an absolute oral bioavailability of about 6% after intake in the fasting state, while co-administration with a high-fat meal would be expected to result in a bioavailability of about 25% and in reduced inter- and intra-subject variability, compared with the fasting state []. Moreover, THC showed similar bioavailability behaviour when administered with sesame oil [].

Furthermore, the potential role of cannabinoid metabolites, especially active metabolites such as 7-hydroxy-CBD, should be considered, as outlined in recent studies in subjects with renal or hepatic impairments [].

Oils that are formulated into capsule pellets and solid tablets currently allow pharmaceutical-grade compounds to be conveniently and accurately dosed.

Two important considerations to make when evaluating cannabinoid formulations are the pharmacokinetic goal and intended use. For example, if the indication is to treat acute pain, then a faster Tmax and higher Cmax may be desirable, while also potentially helping to decrease the risk of overdose via premature repeat self-administration. Alternatively, a larger AUC may be preferable for use as a chronic treatment if a user follows a regular dosing schedule.

Nevertheless, an ideal oral dosage form that has consistent delivery and high bioavailability is not yet available and is therefore warranted. Many companies have invested huge amounts of effort into improving pharmaceutical oral dosage. The different strategies taken have been detailed below, and have been marketed. The most advanced formulations have been summarised in Table Table2.2. Table Table33 summarises the ongoing clinical trials on pain treatments. Only the most recent reports on active research and the latest development phases are described. To complete the information and allow the reader to move more deeply into the composition and technology involved in the formulation procedures, the most significant data from related patents are also reported.


Continue at:

The text above is owned by the site above referred.

Here is only a small part of the article, for more please follow the link

Also see:


Manostaxx – Industrial Management Consulting






Leave a Reply

Your email address will not be published. Required fields are marked *