A new oral CBD capsule delivered more CBD into the bloodstream than the Sativex mouth spray
A gelatin matrix pellet formulation (PTL101) delivered 34% more CBD into the bloodstream than the equivalent dose of Sativex oromucosal spray, with a comparable safety profile in healthy volunteers.
Quick Facts
What This Study Found
Researchers tested a new oral CBD formulation called PTL101, which embeds highly purified CBD in seamless gelatin matrix beadlets, against Sativex oromucosal spray as a reference product. In a randomized crossover study with healthy volunteers, the 10 mg PTL101 dose produced 1.7 times higher peak blood levels and 1.3 times higher overall CBD exposure compared to the spray.
The time to reach peak blood levels was similar for both formulations at 3 to 3.5 hours, though PTL101 showed about a 1-hour lag in initial absorption. When the dose was increased from 10 mg to 100 mg, the resulting blood levels increased approximately 15-fold, slightly more than proportional to the dose increase.
Both formulations were well tolerated with no notable safety concerns, establishing PTL101 as a potentially more efficient oral delivery system for CBD.
Key Numbers
PTL101 10 mg vs Sativex: 1.7-fold higher Cmax, 1.3-fold higher AUC. Relative bioavailability of PTL101: 134% compared to Sativex. Tmax: 3-3.5 hours for both. 10-fold dose increase (10 to 100 mg) produced approximately 15-fold increase in Cmax and AUC. 1-hour absorption lag with PTL101.
How They Did This
This was a randomized, crossover, single-dose pharmacokinetic study in healthy volunteers comparing PTL101 (gelatin matrix pellet CBD formulation) at 10 mg and 100 mg doses with Sativex oromucosal spray as a reference product. Blood samples were collected at multiple time points to measure CBD pharmacokinetic parameters including Cmax, AUC, and Tmax.
Why This Research Matters
CBD bioavailability has been a persistent challenge in cannabinoid medicine. Oral CBD typically has low absorption, with much of the dose lost to first-pass metabolism. A formulation that delivers more CBD into the bloodstream from the same dose could improve therapeutic outcomes and reduce the amount of CBD patients need to take.
The Bigger Picture
Improving CBD delivery is a significant focus of pharmaceutical development. Many patients find existing formulations require high doses to achieve therapeutic effects. Technologies like gelatin matrix pellets that enhance bioavailability could make CBD-based treatments more practical and cost-effective.
What This Study Doesn't Tell Us
This was a single-dose study in healthy volunteers, not patients with conditions that CBD is used to treat. The sample size was small. Long-term safety and repeated dosing were not assessed. The enhanced bioavailability needs to be confirmed to translate to improved clinical outcomes. Food effects were not evaluated.
Questions This Raises
- ?Does the enhanced bioavailability of PTL101 translate to improved clinical outcomes in conditions like epilepsy?
- ?How does food intake affect PTL101 absorption compared to other CBD formulations?
- ?What is the optimal dose of PTL101 for specific therapeutic applications?
Trust & Context
- Key Stat:
- 134% relative bioavailability compared to Sativex spray
- Evidence Grade:
- This is a small randomized crossover pharmacokinetic study in healthy volunteers, providing preliminary evidence of improved CBD delivery.
- Study Age:
- Published in 2018. PTL101 and similar CBD delivery technologies have continued to develop.
- Original Title:
- Single-Dose Pharmacokinetics of Oral Cannabidiol Following Administration of PTL101: A New Formulation Based on Gelatin Matrix Pellets Technology.
- Published In:
- Clinical pharmacology in drug development, 7(7), 751-758 (2018)
- Authors:
- Atsmon, Jacob, Heffetz, Daphna(2), Deutsch, Lisa(2), Deutsch, Frederic, Sacks, Hagit
- Database ID:
- RTHC-01579
Evidence Hierarchy
Participants are randomly assigned to treatment or placebo groups to test cause and effect.
What do these levels mean? →Frequently Asked Questions
Does the form of CBD matter for how well it works?
Yes. This study showed that different formulations of the same CBD dose can result in substantially different blood levels. The gelatin matrix pellet formulation delivered 34% more CBD into the bloodstream than the mouth spray, which could translate to different therapeutic effects.
Why is CBD hard to absorb?
CBD is highly lipophilic (fat-loving) and undergoes extensive first-pass metabolism in the liver when taken orally. This means much of the dose is broken down before reaching the bloodstream. Formulation technologies like the gelatin matrix pellets tested here aim to improve absorption.
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Cite This Study
https://rethinkthc.com/research/RTHC-01579APA
Atsmon, Jacob; Heffetz, Daphna; Deutsch, Lisa; Deutsch, Frederic; Sacks, Hagit. (2018). Single-Dose Pharmacokinetics of Oral Cannabidiol Following Administration of PTL101: A New Formulation Based on Gelatin Matrix Pellets Technology.. Clinical pharmacology in drug development, 7(7), 751-758. https://doi.org/10.1002/cpdd.408
MLA
Atsmon, Jacob, et al. "Single-Dose Pharmacokinetics of Oral Cannabidiol Following Administration of PTL101: A New Formulation Based on Gelatin Matrix Pellets Technology.." Clinical pharmacology in drug development, 2018. https://doi.org/10.1002/cpdd.408
RethinkTHC
RethinkTHC Research Database. "Single-Dose Pharmacokinetics of Oral Cannabidiol Following A..." RTHC-01579. Retrieved from https://rethinkthc.com/research/atsmon-2018-singledose-pharmacokinetics-of-oral
Access the Original Study
Study data sourced from PubMed, a service of the U.S. National Library of Medicine, National Institutes of Health.
This study breakdown was produced by the RethinkTHC research team. We analyze and report published research findings without making health recommendations. All interpretations are based solely on the published abstract and study data.