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Bupe Suboxone excipients compared to Zubsolv Inactive ingredients effect on BA

Chemist4Hire

Bluelighter
Joined
Nov 5, 2017
Messages
56
I recently found out that Zubsolv has a higher BA than Suboxone per mg of buprenorphine present inside each medication. For example: It only takes 5.7mg buprenorphine from a Zubsolv to be equal in both effectiveness and strength to Suboxone sublingual film 8mg buprenorphine. I found out through experiments, personal experience and online/medical trial research that the cause is one of the binders, excipients or inactive ingredients. I narrowed this down by finding complete active and pharmacological inactive ingredients lists for both Suboxone and Zubsolv.

First I wanted to show that both medications still carry the 4:1 Buprenorphine/Naloxone ratio:



Buprenorphine Dosage Prescriptions available in 2017: Suboxone vs Zubsolv

Suboxone Sublingual Film
Strengths by Dimensions and Drug Concentrations:

Suboxone sublingual
film unit strength (buprenorphine/naloxone)

Suboxone sublingual film unit dimensions
Buprenorphine Concentration
% (w/w)

Naloxone Concentration
% (w/w)

2 mg/0.5 mg


22.0 mm x 12.8 mm
5.4
1.53
4 mg/1 mg
(2 times the length of the 2 mg/0.5 mg unit)

22.0 mm x 25.6 mm
5.4
1.53
8 mg/2 mg



22.0 mm x 12.8 mm

17.2
4.88
12 mg/3 mg
(1.5 times the length of the 8 mg/2 mg unit)


22.0 mm X 19.2 mm
17.2
4.88

Now for Zubsolv's prescription doses available in tablet form:
Buprenorphine/Naloxone
Oval Shape
0.7mg/0.18mg
Triangle Shape
1.4mg/0.36mg
D-Shape
2.9mg/0.71mg
Round Shape
5.7mg/1.4mg
Diamond Shape
8.6mg/2.1mg
Capsule Shape
11.4mg/2.9mg


Zubsolv Inactive Ingredients list:

Inactives that are present in both medications: indicated with (*) symbol.
Mannitol *
Citric Acid *
Sodium Citrate *


Microcrystalline Cellulose (binder)
Croscarmellose Sodium (Disintegrant)
Sucralose (its Splenda)
Silicon Dioxide
Sodium Stearylfumarate (buffer)
Menthol Flavor



Microcrystalline cellulose:
(C6H10O5)n is refined wood pulp. It is a white, free-flowing powder. Chemically, it is an inert substance, is not degraded during digestion and has no appreciable absorption. In large quantities it provides dietary bulk and may lead to a laxative effect.

Microcrystalline cellulose is a commonly used excipient in the pharmaceutical industry. It has excellent compressibility properties and is used in solid dose forms, such as tablets. Tablets can be formed that are hard, but dissolve quickly. Microcrystalline cellulose is the same as cellulose, except that it meets USP standards.


Croscarmellose sodium:
or sodium CMC, is a cross-linked polymer of carboxymethylcellulose sodium. It appears as white, fibrous, free-flowing powder, and is used commonly as an FDA-approved disintegrant in pharmaceutical manufacturing. Disintegrants facilitate the breakup of a tablet in the intestinal tract after oral administration. Cross-linking allows enhanced bioavailability of the drug through superior drug dissolution. Without a disintegrant, tablets may not dissolve appropriately and may effect the amount of active ingredient absorbed, thereby decreasing effectiveness.


Suboxone Inactive Ingredients List:

Inactives that are present in both medications: Indicated with (*) symbol.

Sodium Citrate *
Mannitol *
Citric Acid *

Inactives that are only present in this medication:

Lactose Anhydrous
Corn Starch
Povidone K30 (Binder/other)
Anhydrous
Magnesium Stearate
Acesulfame K Sweetener

FD&C Yellow No.6Lemon/Lime Flavor
White Printing Ink


Povidone K30:
used in the pharmaceutical industry as a synthetic polymer vehicle for dispersing and suspending drugs. It has multiple uses, including as a binder for tablets and capsules, a film former for ophthalmic solutions, to aid in flavoring liquids and chewable tablets, and as an adhesive for transdermal systems.

Magnesium Stearate:
Exists as a salt form and is useful for it's lubricating properties for capsules and tablets in industry. It is used to help prevent pharmaceutical ingredients from adhering to industry equipment.

lactose Anhydrous:
is used to help form tablets because it has excellent compressibility properties. It is also used to form a diluent powder for dry-powder inhalations. Lactose may be listed as lactose hydrous, lactose anhydrous, lactose monohydrate, or lactose spray-dried.


The Culprit: Why Suboxone has lower Bio- availability than Zubsolv:


Corn starch
is a natural starch product that is derived from the corn kernel. It is a white to slightly yellowish fine powder commonly used in the food and pharmaceutical manufacturing industries.

In the pharmaceutical industry it is used as a disintegrant and binder. Disintegrants enable tablets and capsules to break down into smaller fragments (dissolve) so that the drug can be released for absorption.

I conclude Corn starch is the problem:
Since Corn Starch was used in Suboxone instead of:
Croscarmellose Sodium used in Zubsolv, Suboxone has lower BA than Zubsolv . 2.3 mg's of suboxone is lost via poor BA taking 8mg Suboxone instead of taking zubsolv which has the same effect with 5.7mg as 8mg of suboxone.

 
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