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Modified release pharmaceutical compositions of huperzine and methods of using the same

a technology of huperzine and pharmaceutical compositions, which is applied in the direction of drug compositions, microcapsules, capsule delivery, etc., can solve the problems of higher dose levels of transient dose related nausea and no published data on the efficacy of huperzine, and achieve the effect of better side effect profile and better side effect profil

Inactive Publication Date: 2018-11-22
BISCAYNE NEUROTHERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a new pharmaceutical composition of huperzine that can be used to treat various neurological disorders such as pain, Alzheimer's disease, and seizure disorders. This modified release pharmaceutical composition has the advantage of reducing the risk of serious adverse events associated with previous immediate release pharmaceutical compositions, which may have either dose limiting or prevent continued use. Additionally, the modified release pharmaceutical compositions provide optimal efficacy with reduced duration, severity, and risk of adverse events. This allows for continuous use of huperzine for longer periods of time.

Problems solved by technology

While these studies showed a favorable safety profile, in some studies, transient dose related nausea occurred at the higher dose levels.
There are no available published data on the efficacy of huperzine A in patients with epilepsy in the medical or patent literature.

Method used

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  • Modified release pharmaceutical compositions of huperzine and methods of using the same
  • Modified release pharmaceutical compositions of huperzine and methods of using the same
  • Modified release pharmaceutical compositions of huperzine and methods of using the same

Examples

Experimental program
Comparison scheme
Effect test

example 1

Dissolution Testing

[0188]The compositions were tested according to USP 1 type apparatus at 50 revolutions per minute in 50 mM phosphate (pH 6.8) at 37° C. Results are shown in FIG. 4.

example 2

inetic Study in Dogs

[0189]A Study Objective

[0190]The objective of this study was to determine the plasma pharmacokinetics of modified release huperzine Composition 4A in male beagle dogs. The huperzine A was monitored in plasma for up to 24 hours.

[0191]Vehicle and Pharmaceutical Composition Preparation

[0192]Animals were dosed at a nominal dose of 5.45 mg / kg modified release huperzine A (composition 4A, equivalent to 0.049 mg / kg huperzine A)

[0193]Animal Specifications

[0194]Three, non-naïve, male, beagle dogs (Marshall Bioresources, Beijing, China) weighing ≥6 kg were used in the study. Animals underwent a physical examination for general health by a staff veterinarian prior to assignment to the study. The animals were acclimated to the testing facility prior to the study.

[0195]Environmental Conditions

[0196]Animals were housed in room(s) that were controlled and monitored for relative humidity (targeted mean range 40% to 70%) and temperature (targeted mean range 18° to 26° C.) with 10...

example 3

n of the Bioavailability, Safety and Tolerability of Modified Release Huperzine a Following Multiple Dose Administrations in Healthy Subjects

[0217]A single center, on-site / outpatient, dose escalation study was conducted with oral pharmaceutical composition 4D. The subjects were dosed twice daily (BID) in 4 cohorts of 2 subjects each (Pharmaceutical composition 4D) and 2 cohorts of 3 subjects total (Pharmaceutical composition 4E) to assess plasma levels, safety, and allow necessary dosing alterations to occur prior to dosing any subsequent subjects. The study was conducted in an on-site setting at dose initiation and at times of dose escalation to evaluate safety, and for specimen collection for routine laboratory and pharmacokinetic analysis. Subjects were discharged and compliance of BID dosing was monitored via twice daily phone calls by site staff. The initial dose was 0.5 mg BID with a dose escalation every 2-3 days until a maximum tolerated dose was observed or a maximum of 2.5...

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Abstract

The present application discloses pharmaceutical compositions for modified release of huperzine. The pharmaceutical compositions and methods described herein, allow for dosing of huperzine at higher therapeutic thresholds, while avoiding rapid serum peak plasma levels, thereby avoiding the adverse nausea and vomiting associated with the immediate release pharmaceutical compositions. Methods of treating neurological disorders and / or seizure disorders with the modified release compositions is also described.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]The present application claims benefit of and priority to U.S. Provisional No. 62 / 508,554 entitled “EXTENDED RELEASE FORMULATIONS OF HUPERZINE AND METHODS OF USING THE SAME,” filed May 19, 2017, the contents of which is hereby incorporated by reference in its entirety.SUMMARY OF THE INVENTION[0002]Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the firmoss Huperzia serrata. It is a potent inhibitor of acetylcholinesterase. In several countries, Huperzine A is sold as a dietary supplement for memory support. In China, huperzine A is State Food and Drug Administration (SFDA) approved for the treatment of dementia.[0003]Huperzine A has been administered to healthy volunteers and patients in numerous trials, many in China, demonstrating acceptable safety and tolerability as well as efficacy in Alzheimer's disease, benign senescent forgetfulness, vascular dementia, myasthenia gravis, schizophrenia, and cocaine dep...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/50A61K31/435A61K47/32A61K47/38
CPCA61K9/5078A61K9/5042A61K31/435A61K47/32A61K47/38A61P25/08A61K31/4748A61K9/5047A61K9/4866A61K9/48
Inventor COLLINS, STEPHEN D.GOLDSTEIN, PETERJOHNSTONE, JOSHUA T.
Owner BISCAYNE NEUROTHERAPEUTICS INC
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