Download Nano-E™: Nanoemulsion Drug Delivery System

Nano-E™:
Nanoemulsion Drug Delivery System For
Highly Insoluble Drugs
LATITUDE Pharmaceuticals, Inc.’s Nanoemulsion Drug Delivery System
(Nano-E™) is a versatile drug delivery platform for applications requiring a
liquid formulation for highly insoluble small molecule, peptide, and protein
drugs. Nano-E is being used in several NDA-stage and clinical-stage
products.
The Nano-E™ technology is the 505(b)(2)-enabling formulation behind two
NDA-stage compounds that LATITUDE developed for its clients
Key Advantages and Properties of Nano-E™ Technology
• Highly versatile drug delivery platform for insoluble
or soluble compounds
• Small molecule and protein friendly
• pH neutral, non-irritating, non-allergenic; clinically
proven significant safety improvement for veinirritating drugs
• For IV, IM, SC, IP, intra-thecal, intra-articular,
ophthalmic, oral routes of delivery
• IV bolus and infusion enabling
• Up to 5% drug loading by weight
• Tissue-friendly and wound compatible
• Dilutable in standard IV diluents (e.g., D5W)
• All components are GRAS listed and compendial
grade (USP, NP, EP)
• Does not contain co-solvents (e.g., Cremophor)
or detergents (e.g., polysorbate)
• PK profile bio-equivalent to solution formulations
• RT stability demonstrated for 1.5-2 years
• Filterable through 0.2 micron filters
• Lyophilizable as needed
• Simple and straightforward manufacturing
• Manufacturing feasibility demonstrated for two
NDA-stage drugs
• Patent pending
To learn how LATITUDE’s Nano-E DDS™ approach can optimize the therapeutic potential of your
drug, please contact:
Norman K. Orida, Vice President, Business Development
LATITUDE Pharmaceuticals, Inc.
6364 Ferris Square
San Diego, CA 92121
858-546-0924 ext 106
[email protected]
6364 Ferris Square
Phone: 858.546.0924
www.latitudepharma.com
San Diego, CA 92121
Fax: 858-546-0958
20121008
PG Depot™
Phospholipid Gel Depot Technology For Sustained
Release (1-7 Days)
LATITUDE Pharmaceuticals, Inc.’s Phospholipid Gel (PG) Depot™
technology is a versatile parenteral drug delivery platform for applications
requiring the sustained release of small molecules, peptides, and proteins
over 1-7 days.
Key Advantages and Properties of the PG Depot™
• Sustained release for 1-7 days
• Small molecule, peptide and protein
compatible
• Up to 20% drug loading by weight
• Protein-friendly: provides >6 month RT
stability
• Enzyme-friendly: activity, stability
uncompromised
• Tissue-friendly and wound compatible
• No collagen or other animal products
• Components all GRAS listed and compendial
grade (USP, NP, EP)
Technology
Manufacturing
Cost of
goods
Drug
Loading
PG Depot
Simple
Low
Liposomes
Complex
High
~5%
• Single phase, ready-to-use format; no premixing prior to use
• Injectable through fine needles
• Dosing paradigm shift: from once or twice
per day to once/week
• Self administration-capable
• Peakless or burst profile can be designed
into final product
• Simple and straightforward manufacturing
• Autoclavable
• ~$0.20-$2.00 vehicle cost/dose
• Patent pending
Burst
~15-20% Optional
Unavoidable
Premixing,
Resuspen
Req’d?
RT
Stable?
No
Yes
Yes
No
Collagen
Complex
High
<10%
?
No
No
SABER™
?
High
~30%
?
Yes
No
PLGA
Complex
High
~5%
Unavoidable
Yes
No
PLGA
Microspheres
Complex
High
~5%
Unavoidable
Yes
No
6364 Ferris Square
Phone: 858.546.0924
www.latitudepharma.com
San Diego, CA 92121
Fax: 858-546-0958
20121008
SC
PG DepotPK
@ 0.25
mg/kg
PGBuprenorphine
Depot™: Peakless
Profile
[Plasma] (ng/ml)
(Right) A peakless PK
profile engineered into
the PG Depot™ to
avoid Tmax issues. If
desired, a burst release
may be designed into
the application.
1
0.9
0.8
0.7
0.6
0.5
0.4
0.3
0.2
0.1
0
0
12
24
36
48
60
72
84
96
108 120
132
Time (in hours)
Non-pain Response (%)
100
80
(Left) For the same API,
the PG Depot™ can be
adjusted to achieve longer
or shorter efficacy.
60
40
20
0
0
12
24
36
48
60
72
84
Time (h)
Licensing and feasibility studies
Latitude’s PG Depot™ technology is available to expand the product
possibilities and intellectual property space for your compound. Please
contact LATITUDE to discuss how the PG Depot™ technology may address
the sustained-release needs for your API. We recommend a quick
turnaround, low cost feasibility study to explore the PG Depot™ potential for
your compound.
For further information, please contact:
Norman K. Orida, Vice President, Business Development
858-546-0924 ext 106
[email protected]
6364 Ferris Square
Phone: 858.546.0924
www.latitudepharma.com
San Diego, CA 92121
Fax: 858-546-0958
20121008
RFAP™ Matrix
Powder Formulation for Extremely
Insoluble Oral Drug Candidates
Nearly half of new drug candidates in development are poorly soluble
compounds. Of these, many are extremely insoluble and lack any
appreciable water or oil solubility, making them unformulatable using
conventional approaches.
To overcome this high hurdle, LATITUDE Pharmaceuticals, Inc. is offering its
new Rapidly-dissolving, Free-flowing Amorphous Particle (RFAP) Matrix
formulation. This approach uses GRAS-listed materials to formulate
particularly challenging compounds into a rapidly-dissolving yet highly stable
matrix. In addition to its desirable pharmaceutical properties, the matrix is a
fine, freely-flowing powder that is ideal for automated tableting.
••
••
••
••
••
•
Key Features of the RFAP Matrix:
Greatly improves oral BA
Applicable for drugs that are insoluble in oil, water,
or both
Rapid dissolution
High drug loading (10-20%)
Thermodynamically stable amorphous drug form
Does not revert to crystal form (at least ~1.5 yrs)
Simple manufacturing process
Dose as a powder or in capsules
Low cost of goods
Automated tableting-capable
Patent pending
To learn how LATITUDE’s RFAP Matrix can help your drug development
program, please contact:
Norman K. Orida, Vice President, Business Development
LATITUDE Pharmaceuticals, Inc.
6364 Ferris Square
San Diego, CA 92121
858-546-0924 ext 106
[email protected]
6364 Ferris Square
Phone: 858.546.0924
www.latitudepharma.com
San Diego, CA 92121
Fax: 858-546-0958
20130502
24H™:
24 Hour Extended Release Tablet Technology
LATITUDE Pharmaceuticals, Inc.’s 24H™ technology is a versatile oral drug
delivery platform that provides the linear, sustained release of water-soluble
and water-insoluble drugs from tablets for up to 24 hours. The 24H™
formulation is being utilized in several commercially launched and clinicalstage products.
Key Advantages/Properties of the 24H™
System
• Extended release for up to 24 hours
• Compatible with many different APIs,
including highly water soluble compounds
• Up to 60-70% (w/w) drug loading
• Near zero-order release kinetics; low burst
• Simple and straightforward manufacturing
• Low cost of materials
• Components all GRAS listed and
compendial grade (USP, NP, EP)
• Patent pending (US Patent Application
20070020335 )
Case Study: 24H™-Based Glucosamine Extended Release Tablets
PRODUCT OPPORTUNITY: Glucosamine is widely used in North America as a dietary
supplement for cartilage repair and maintenance. It is highly water soluble and known to have a
short elimination half-life. A daily dose in a range of 500 mg to 1500 mg has been recommended.
Almost all currently available tablets of glucosamine are immediate release and release
glucosamine rapidly over 1-2 hours, requiring 2-6 times-a-day dosing to maintain adequate levels.
Glucosamine tablets are generally quite large, making them difficult to swallow, especially for the
geriatric population.
Solution: LATITUDE utilized the 24H™ System to develop a one dose/day tablet with typical
vitamin tablet dimensions that continually releases glucosamine and chrondroitin over a 24 hour
period with near-zero order kinetics (see graph).
6364 Ferris Square
Phone: 858.546.0924
www.latitudepharma.com
San Diego, CA 92121
Fax: 858-546-0958
20121008
Near-zero order kinetics in vitro release profile of 24H™
glucosamine/chondritin (LPI Extra Strength G750mg/C600mg)
compared to other extended release glucosamine products.
Licensing and feasibility studies
Latitude’s 24H™ technology is available to expand the product possibilities
and intellectual property space for your compound. Please contact
LATITUDE to discuss how the 24H™ technology may address the extendedrelease needs for your API. We recommend a quick turnaround, low cost
feasibility study to explore the 24H™ potential for your compound.
For further information, please contact:
Norman K. Orida, Vice President, Business Development
LATITUDE Pharmaceuticals, Inc.
6364 Ferris Square
San Diego, CA 92121
858-546-0924 ext 106
6364 Ferris Square
Phone: 858.546.0924
www.latitudepharma.com
San Diego, CA 92121
Fax: 858-546-0958
20121008
MiniSpheres™
Oral Drug Delivery Platform for High &
Bulky Dose Drugs
MiniSpheres™ are LATITUDE Pharmaceuticals Inc.’s new oral drug delivery
technology especially suited for high/bulky dose and/or sustained release
applications. MiniSpheres™ are tiny spherical pellets (~0.5 to 1.5 mm diameter)
that can be dispensed in a packet or a bottle. Unlike bulky tablets, MiniSpheres™
are very easy to swallow – even in large quantities – because of their small,
spherical, smooth shape. For oral dosing, the pellets may be sprinkled on food or
mixed with water or flavored liquids to form a drinkable oral suspension, which may
be ideal for pediatric applications and for patients with swallowing difficulties. Multigram dosing is possible with this approach. For low-dose drugs, the MiniSpheres™
may be dispensed in capsules.
Despite their small size, MiniSpheres™ can provide a sustained release profile –
up to 24 hours in vitro – even for highly water-soluble drugs. The release profile is
adjustable to meet most any dosing requirements. If needed, the taste-masking
agents may be incorporated during their production.
Key Features of MiniSpheres™:
Ideal for high dose (>1-2 grams) drugs
Applicable for insoluble and highly water soluble
drugs, nutraceuticals, and vitamins
Converts multiple dosing/day to complianceenhancing once/day format
Simple manufacturing process
Manufacturable using conventional equipment
Low cost of goods
Patent pending
To learn how LATITUDE’s MiniSpheres™ can optimize the therapeutic
potential of your drug, please contact:
Norman K. Orida, Vice President, Business Development
858-546-0924 ext 106
[email protected]
6364 Ferris Square
Phone: 858.546.0924
www.latitudepharma.com
San Diego, CA 92121
Fax: 858-546-0958
20121008
RTT
Rapid Tox Template Formulations
LATITUDE Pharmaceuticals, Inc. is now offering a Rapid Tox Template
(RTT) Formulation Service to help drug developers maximize oral drug
exposure and identify potential toxicity of poorly soluble drug candidates in
animal studies.
Key Advantages/Properties of RTTs:
•
•
•
•
•
•
•
•
•
Proven track records for significantly improving oral bioavailability
(up to 16-fold enhancement) for a large number and variety of
insoluble compounds.
Extremely well tolerated vehicle (MTD >7.5g/kg in dogs).
Composed of naturally occurring oils and lipids; do not contain
large amounts of organic co-solvents or toxic detergents.
May be dosed by oral gavage or filled into capsules.
Up to 10% drug load, as permitted by drug solubility.
The RTT-formulated compounds are provided with strength (in
mg/g or % wt) information. An optional HPLC assay to confirm
strength and purity or stability test is available.
Each RTT-formulated compound is individually packaged and
labeled. Instructions for use/storage are also provided.
Minimal API requirements (~200 mg).
HPLC method development and in vivo tox evaluation services
are also available.
For further information, please contact:
Norman K. Orida, Vice President, Business Development
LATITUDE Pharmaceuticals, Inc.
6364 Ferris Square
San Diego, CA 92121
858-546-0924 ext 106
[email protected]
6364 Ferris Square
Phone: 858.546.0924
www.latitudepharma.com
San Diego, CA 92121
Fax: 858.546.0958
20090924