Download The problem with current OTC pain relievers - Aspir-Tek

PharmStar Inc.
The problem with current OTC pain relievers
ASPIRIN, (in tablet and powdered form, including Bayer’s new “QUICK RELEASE CRYSTALS” (NSAID)
Aspirin, in tablet, powder, and Bayer’s new quick release crystal form, is acidic, non-soluble in water, and only about 40 to 45% of the
drug ever gets into the blood stream. Because of these forms, it is slow to be effective, taking as much as 30 to 40 minutes to reach
therapeutic levels and causes side effects such as stomach bleeding and gastric upset. In millions of patients this causes severe gastric
distress and sometimes even hemorrhage due to direct contact between un-dissolved aspirin particles and the stomach lining. Indeed, it
is precisely these gastro-toxic, ulcerogenic adverse-reactions that prevent many patients from taking full advantage of aspirin’s many
benefits.
ACETAMINOPHEN (TYLENOL) (Non-NSAID)
Acetaminophen, the most popular pain reliever has several problems of it’s own. It is not an anti-inflammatory drug. It is weak on
reducing pain and takes up to 1 hour to reach peak blood levels thereby a slow onset of pain relief. Side effects are liver damage.
Recently, acetaminophen products have been found to cause liver damage at lower doses & have been required to “black label” the
product packaging.
IBUPROFEN (ADVIL), (MOTRIN), (NSAID)
Ibuprofen, like aspirin tablets, has become a very popular pain reliever and basically has the same properties as aspirin. Ibuprofen is
not soluble in water and causes gastric bleeding and gastric distress in some patients. The onset of pain relief usually takes at least
25 to 35 minutes. Ibuprofen also carries having a greater risk of heart attack and reduces the effect of an aspirin regimen for
reduction of heart attack and stroke.
NAPROXEN SODIUM (ALEVE) (NSAID)
Naproxen sodium, also known as ALEVE, NUPRIN, and NAPROSYN, has been on the market for many years. It has been sold in the
past generally as an anti-inflammatory for long term use. The onset of action is very slow, (at least 30 minutes before relief begins
and a few days for inflammation reduction), and the side effects are generally the same as for aspirin and ibuprofen. This product is
mainly for long term use of inflammation reduction and arthritis pain release although, can have significant gastric side effects.
PharmStar Inc.
The Solution to the problem
The scientists at PharmStar have been developing for a period of over 20 years to effectively, rapidly, and
completely convert common aspirin, the “GOLD STANDARD” of pain relievers, into a much more effective and safer
form. What has been achieved is the most significant breakthrough in the pain reliever field in many decades. The
potassium based derivative of aspirin, “AQUAPRIN ” is the safest, most effective, and fastest acting form of aspirin,
and as a matter of fact, faster acting and safer, and therapeutically more effective than any other over the counter
pain reliever worldwide. Most likely it will be the best OTC pain reliever worldwide.
PharmStar expects to be a leader in the pain management field, and to capture a substantial segment of the
analgesic, cardio protective, anti-thrombotic and antipyretic pharmacotherapeutic market because AQUAPRIN and
other line extension products offer significant competitive advantages. AQUAPRIN is an instantly dissolving, fastacting, non-acidic, safe, potent, drinkable derivative of aspirin, which virtually eliminates irritation to the GI-tract. It
is also a more effective and efficient method of delivering salicylates into the blood stream, achieving almost peak
blood plasma levels in 5 to 7 minutes. Moreover, it contains therapeutically active levels of potassium which acts as
an antacid, neutralizing stomach acid. Potassium also lowers blood pressure and helps to dilate blood vessels
allowing for better blood circulation.
Since the aspirin-derivative salicylates in AQUAPRIN are fully dissolved into an antacid solution, they are
immediately absorbed into the blood stream. AQUAPRIN ‘s antacid characteristics help neutralize stomach acids,
thus virtually eliminating local topical and systemic gastric irritation and damage.
In addition, salicylates in conventional aspirin tablets are degraded during their passage through the GI-tract and
during metabolism. This causes them to achieve only 30 to 40% absorption efficiency. AQUAPRIN ‘s unique formula
allows it to achieve 100% absorption efficiency.
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PharmStar Inc.
Product Background
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Aspirin has been and is still considered the “GOLD STANDARD” of over the counter pain
relievers.
It is a superior non-steroidal, anti-inflammatory, pain reliever, anticoagulant, fever reducer,
and anti-heart attack and stroke preventative medication.
For general use, aspirin is only available in tablet and powder forms in the USA. In these
forms, it is acidic, not soluble in water or the gastric system, has low and slow absorbance
into the blood stream, and causes gastric irritation and stomach bleeding.
Calcium and sodium based water soluble forms of aspirin, available in other parts of the
world have proven to be faster acting, more efficiently absorbed into the blood stream
and produce significantly less side effects. The negative aspect of these forms is that they
take a few minutes to dissolve, leaves a lot of residue, have a gritty bad taste, high levels
of sodium or calcium carbonate and do not meet FDA regulations for sale in the USA.
AQUAPRIN, the only potassium based superior form of a water soluble aspirin is positioned
to take aspirin to the highest level of safety, efficacy, speed of relief, and taste,
outperforming all other OTC pain medications.
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PharmStar Inc.
The Product
When aspirin and potassium bicarbonate are physically combined together in the
presence of water, an instant chemical reaction takes place.
Using PharmStar’s technology, this reaction instantly and totally dissolves the aspirin
forming AQUAPRIN, which is a residue free clear drink, ready in ~15 seconds.
AQUAPRIN is the water solubilized potassium salt of aspirin, (potassium
acetylsalicylate). In this form, it is non acidic, is antacid, safest, fastest acting,
extremely more therapeutically effective derivative of aspirin. The potassium
based product provides about 350 mg of potassium with each dose.
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PharmStar Inc.
Physical Properties of AQUAPRIN
A crystalline form, packaged in a small foil “Strip Pack” which totally dissolves in less than 30
seconds in 1.5 oz or more tap water into a clear, effervescing tasty drink.
No undissolved grit or residue.
Antacid.
Solubility & taste superior to marketed sodium or calcium-based forms of aspirin in Europe.
Free-flowing crystalline form packaged in .75"x2.5" foil packets, available in several
pleasant flavors.
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PharmStar Inc
AQUAPRIN, “PAIN-AWAY”
• A special formulation of AQUAPRIN in a
crystalline form which totally dissolves in
less than 30 seconds in 1.5 oz. or more tap
water into a clear, effervescing tasty drink
leaving no undissolved grit or residue.
• Is an antacid.
A SPECIAL FORMULATION OF
AQUAPRIN , WHICH RELIEVES
HEADACHES IN 5 to 10 MINUTES
• Solubility and taste superior to marketed
sodium or calcium-based forms of aspirin in
the USA & Europe.
• Free-flowing crystalline form packaged
in .75"x2.5" foil packets.
• Available in several pleasant flavors.
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PharmStar Inc.
AQUAPRIN, “DAILY REGIMEN”
Packaged in a small foil packet (1”x 1”), and
blister strips, which contains a crystalline
formulation.
When the ingredients are added to 1 or more
ounces of water or any other drink of any
quantity, a chemical reaction takes place.
This reaction instantly solubilizes the 81 mg of
aspirin into a clear tasteless solution without any
un-dissolved particles or scum. The results are a
much safer and therapeudically more effective
delivery of aspirin.
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PharmStar Inc.
AQUAPRIN / INSTA-PRIN DELIVERY SYSTEM
DESIGNED FOR
“EMERGENCY” USE
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•
A disposable device for one-time emergency use,
which contains a crystalline formulation in one
sealed compartment and 1.5 oz. of water in an
expandable and squeezable container. Upon
activation, INSTA-PRIN is instantly solubilized in
the water compartment.
The solution can then be dispensed in seconds by
squeezing the water compartment, delivering 650
mg of solubilized aspirin.
INSTA-PRIN is intended for use where water is not
always readily available and fast effectiveness is
critical.
Ideal for first-response treatment of heart attacks
and strokes.
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PharmStar Inc.
Advantages of AQUAPRIN
• Significantly reduces stomach distress by
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90 percent.
Five times the speed of effectiveness of aspirin
tablets & powders.
Significantly higher pain relieving therapeutic
levels for the same mg of aspirin.
Safer and faster dosing method.
Gives longer-lasting relief between doses.
Is an antacid.
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PharmStar Inc.
What is AQUAPRIN Indicated For ?
1. Normal to severe pain relief
2. Headaches, normal & migraine
3. Cox 1 & 2 inhibitor (Arthritis Sufferers)
4. Anti-pyretic (fever reducer)
5. Anti-coagulant
6. Anti-heart attack & stroke
7. Anti-inflammatory
8. Sour stomach, acid indigestion
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PharmStar Inc.
Aspirin vs. AQUAPRIN
Superiority Of AQUAPRIN Over Competition
Characteristics
% Absorbed into the Bloodstream
Time to Therapeutic Blood Levels
Time to Peak blood levels
% In Blood Stream After 5 Minutes
Time to Start Working on Pain
Efficacy of Pain Relief
Time to Relieve Headaches
Effectiveness in relieving Migraine
Gastric Irritation
Gastric Damage Score
Effect on Gastric Mucosa
Dosing Method
Aspirin Tablets & Powders
AQUAPRIN™
Improvement
40-45%
20 Minutes
45-60 Minutes
Less than 5%
20-30 Minutes
Normal
25-40 Minutes
Low
20-25% of Patients
2.0
Acid
Two 335 mg tabs + 6oz of Water
100%
2 Minutes
7-10 Minutes
70-80%
2 Minutes
More than Twice
5 to 10 Minutes
High- Proven in Studies
1-2% of Patients
.15
Antacid (soothing)
1.5 or more oz. Drink
110% More
10X Faster
6X Faster
70% More
10X Faster
More Than 2X
5X Faster
Much Higher
20X Less
90% Less
Acidic
Less Water
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PharmStar Inc.
Absorption Rate of AQUAPRIN
Aqua prin Absorption Rate Compared with Published Data for Other Asprin
Formulations
Plasma Total Salicylate, mg Per Liter
60
50
40
30
Potasium Acetylsalicylate (Aquaprin)
Sodium Acetylsalicylate (Alka-Seltzer)
Aspirin Tablet (Bayer) or equivalent
Highly Buffered Aspirin (Bufferin)
Aspirin in Hot Water (Not Available)
Effervescent Aspirin (Not Available)
20
10
0
0
5
10
15
20
25
30
35
40
45
50
55
60
Tim e, in Minutes
Plasma total salicylate concentrations follow ing the oral injestion of various preparations of aspirin. Each dose
w as equivalent to 640 milligrams of aspirin in all cases.
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PharmStar Inc.
Solubilized Aspirin (AQUAPRIN) Causes Less Gastric Irritation
Than Tablets & Powders
Mean gastric damage score for 30 volunteers taking a
solubilized aspirin vs. solid aspirin tablets at 6,12, and 24 hours.
Damage Score
2.5
Soluble Aspirin
Aspirin Tablets
2
1.5
Data shown drawn from a study by:
(Jaiswal et al IUPHAR 9th International
Congress of Pharmacology, 1984) Study
done using “Disprin” brand soluble aspirin.
1
0.5
0
This randomized, double blind, crossover
study in 30 volunteers involved visual
inspection by gastroscopy at various time
intervals after drug administration.
6 Hours
12 Hours
24 Hours
Time
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PharmStar Inc.
Status of Development
 AQUAPRIN
formulations fully developed and tested, including a sports
pain drink.
 AQUAPRIN will be available in several flavors, which have already been
developed.
 Packaging and process equipment specifications established.
 Processes and formulas are ready for full scale production.
 INSTA-PRIN device in final engineering configuration and all basic
operating principles tested.
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PharmStar Inc.
AQUAPRIN, Rapid Path to Market
 No additional FDA approvals required to market Over the counter.
 AQUAPRIN conforms to the approved Over the Counter Monographs:
• USP Official OTC Monograph: “Aspirin Effervescent Tablets for
Oral Solution”.
• USP Official OTC Monograph: “Buffered Aspirin Tablets”
• US Federal Register designation of approved combinations with
Aspirin
http://frwebgate3.access.gpo.gov/cgi-bin/TEXTgate.cgi?WAISdocID=3060554727+1+1+0&WAISaction=retrieve
http://law.justia.com/us/cfr/title21/21-5.0.1.1.10.html#21:5.0.1.1.10.2.1.2
 CGMP-compliant manufacturing facility to be registered with the FDA.
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PharmStar Inc.
Sales Potential
 The pain reliever market in the US alone exceeds $10 billion annually and more
than $30 billion worldwide.
 AQUAPRIN will compete in the worldwide market for over the counter pain
medications having advantages over all other OTC pain relievers.
The price point of the AQUAPRIN product will be very competitive with current
OTC branded pain relievers but cost less to produce.
 COX-2 inhibitors for arthritis generate more than $4 billion annually .
 AQUAPRIN is believed to be a safe & effective COX-2 inhibitor for arthritis.
 With appropriate marketing and endorsements, the sales potential for AQUAPRIN
can exceed $1 billion in the US alone.
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PharmStar Inc.
Market & Competition
• The worldwide annual market for “soluble forms of aspirin” products alone exceeds $2 billion.
However, AQUAPRIN will be positioned to compete in the worldwide “over the counter” pain reliever
sector. The “INSTA-PRIN ” product has no competition worldwide and can command a sizeable market
alone. INSTA-PRIN will be carried by EMC, police, and anyone who needs immediate drug intervention
at the signs of stroke or heart attacks.
Major pharmaceutical firms have soluble aspirin products in Europe, the Middle East, and Asia, BUT:
•None meet the USP requirements for marketing in the USA
•All are either sodium or calcium based
•All require several minutes to dissolve and leave residue and undissolved particles in
the liquid
•Alka-Seltzer , the only soluble aspirin in the US, has a high sodium content and is
sold as an antacid/pain reliever and not a daily pain reliever and arthritus
treatment
• If PharmStar only achieves .5% market share over the next five years, it’s sales will exceed $100 million
dollars. This does not include the COX 2 arthritus market and prescription migraine market which, can
easily triple the sales. To achieve these levels of sales, additional monies will be required to succeed.
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PharmStar Inc.
Marketing & Sales Strategy
In the US, no oral competing products exist, in terms of potency, rapid onset of action, and gastric tolerance. Neither
does any competing product exists that can deliver a comparably high percentage of un-degraded salicylates per
analgesic or cardio protective dose.
1. It will, for this reason, be strategically launched in such target sectors as AARP, hospitals and nursing home
pharmacies, and by direct marketing, with detail samples and technical data, to medical professionals, as well as via
special “2-for-1” buying incentives for distributors. Internet banners, infomercials, and consumer hot-lines will likewise
be deployed after the initial 6 months, as will dedicated e-commerce, permitting direct purchase of AQUAPRIN from
The Company. A special information and product campaign will be aimed toward emergency medical service
organizations.
2. The Company recognizes the cost and difficulty for a new product to secure prominent shelf-space in drugstores.
The company will initially, during the first phase of funding, depend on vigorous sales promotion and highly visible
point-of-purchase displays at high-traffic consumer corridors. The company feels that the product is so superior to all
other OTC pain relievers, that once tried with free samples, the public will want the product. Also, local-media coupons
and direct marketing will be creatively deployed by the Company to get its products distributed. The company will
also make a strategic alliance with a major pharmaceutical distribution company. 3. The Company’s strategic marketing plan includes English/Spanish promotional, packaging and medicinal insert
formats. Overall Hispanic growth demographics show manifold increases in every quadrant of this population sector
over the past 3 decades. AQUAPRIN’s bilingual debut also translates into easier brand-recognition and penetration of
Mexican, Central and South American markets as soon as practicable, and without having to revamp or redesign
product packaging or advertising.
4. Once The Company’s brand name is established in the market, the public will express its awareness of AQUAPRIN’s
benefits by seeking out and purchasing the product on its own initiative.
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