Phlojel feedback?

[natedogg]

This is a quote from Triceptor.

"on another note, i have evolved to compounding without using solvents in most cases. this does require trituration with a mortar and pestle to get the active into the finest powder posible and using concentrations of 100mg/ml to 125mg/ml. reason i mention this is that sans solvents i find the transdermal does not leave any residuals on the skin and has better cosmetic qualities. just an fyi."

With this being said I can fit (for argument sake), say 10 grams of test base in a 100 gram jar (giving me 100mg/ml) without using any solvents correct? Do you all think solvent is a must at any concentration to ease mixing or only when you exceed a certain amount as stated above? Let's say I do go with this. If I apply 2ml's a day that would give me 200mg*7= 1400mgs a week*~40%(absorbtion rate)=~560mg active hormone per week. Does this sound right?

 

[momod]

This is a quote from Triceptor.

"on another note, i have evolved to compounding without using solvents in most cases. this does require trituration with a mortar and pestle to get the active into the finest powder posible and using concentrations of 100mg/ml to 125mg/ml. reason i mention this is that sans solvents i find the transdermal does not leave any residuals on the skin and has better cosmetic qualities. just an fyi."

With this being said I can fit (for argument sake), say 10 grams of test base in a 100 gram jar (giving me 100mg/ml) without using any solvents correct? Do you all think solvent is a must at any concentration to ease mixing or only when you exceed a certain amount as stated above? Let's say I do go with this. If I apply 2ml's a day that would give me 200mg*7= 1400mgs a week*~40%(absorbtion rate)=~560mg active hormone per week. Does this sound right?

Just do this

20gm test powder crushed into oblivion
slowly add 11gm olive and oil and levigate (create paste)
before it dries add 69gms of phlojel and mix well.

this gives you 100gm of 200mg/gm cream, trust me, it works.

I discovered that my 1/8 spoon gives me about 1gm with a 10% variance or so.

The olive oil can collect at the top, so I remix it before application with the flat side of my 1/8 spoon.


Spoons rule!

bold and other compounds may be more problematic.

 

[natedogg]

Just do this

20gm test powder crushed into oblivion
slowly add 11gm olive and oil and levigate (create paste)
before it dries add 69gms of phlojel and mix well.

this gives you 100gm of 200mg/gm cream, trust me, it works.

I discovered that my 1/8 spoon gives me about 1gm with a 10% variance or so.

The olive oil can collect at the top, so I remix it before application with the flat side of my 1/8 spoon.


Spoons rule!

bold and other compounds may be more problematic.

Olive Oil huh. Why's OO and not DMSO or some other alcohol solvent? Also, you don't use the "60ml syringe method"? Just spoon it and go huh. This sounds like a good idea. How much more difficult would bold or nandro be? Is it grittier and more difficult to mix? Anyways, thanks for the reply and sorry if I'm asking too many questions. I want to do it right the first time.

 

[momod]

Olive Oil huh. Why's OO and not DMSO or some other alcohol solvent? Also, you don't use the "60ml syringe method"? Just spoon it and go huh. This sounds like a good idea. How much more difficult would bold or nandro be? Is it grittier and more difficult to mix? Anyways, thanks for the reply and sorry if I'm asking too many questions. I want to do it right the first time.

check this thread it may help.

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I'm not sure, but I believe triceptor may have originated the OO idea, it seems to have worked well and it saves some PJU. A fully flattened 1/8 spoon gave me between .9 and 1.1 gms, don't bother working in ml's as 1gm=1.05 ml's or 1ml=1.05gms (cant remember) and its hard to measure volume with a gel. Bold works the same as test, It just seems grittier with the same amount of grinding, maybe more OO or just more grinding. Possibly warming with the olive oil and bold before adding the gel. There is a thread on deca around here somewhere, try a search on phlojel and nandro. I just cant emphasize the importance of pulverizing the powder enough.

 

[natedogg]

Any old OO will do then (EVOO will work too right)? Sounds pretty simple. Some of these guys make it sound like friggin' rocket science. Time to read some more. Thanks again.

 

[momod]

Any old OO will do then (EVOO will work too right)? Sounds pretty simple. Some of these guys make it sound like friggin' rocket science. Time to read some more. Thanks again.

I used EVOO, its really simply. Make sure to figure about 10% loss, If your going to do 8 weeks, make enough for 9 weeks.

 

[natedogg]

What if I wanted to mix 30 grams of powder into a 100g of Phlogel. Is that possible even with solvent? What would you suggest?

 

[momod]

What if I wanted to mix 30 grams of powder into a 100g of Phlogel. Is that possible even with solvent? What would you suggest?

that would give you 130gm of solution at 230mg/gm.

I would say that would be pushing it, maybe with some dmso and OO mixed in you would be good. Seems to me people are getting away from using solvents though. I would send email to Phlojel if I was you. Triceptor is good at answering questions.


Invalid Link Removed

this guy is asking the same question essentially. You may want to pipe in, Velikimajmun knows his stuff!

 

[natedogg]

that would give you 130gm of solution at 230mg/gm.

I would say that would be pushing it, maybe with some dmso and OO mixed in you would be good. Seems to me people are getting away from using solvents though. I would send email to Phlojel if I was you. Triceptor is good at answering questions.

Great idea.

 

[natedogg]

Damn, Carl is quick. Here is his reply:

Question: What if I wanted to mix 30 grams of powder into a 100g of Phlogel. Is that possible even with solvent? What would you suggest? Thanks. Nate.

Reply: My first response it that is way too much. 15g in 100g of PhloJel Ultra is
considered high and I have aided some who wanted 200mg per Ml of PhloJel
Ultra achieve that with solvent and proper levigation, but 300mg/Ml is, in
my opinion, too much. The real issue becomes the ability of the powder to
dissolve fully. My suspicion is that the final product will be grainy
feeling and will leave a residue of powder on the skins surface once dried.
What is visibly left behind on the skin is wasted powder. A proper solvent
and proper levigation with that solvent may be able to totally dissolve your
powder, but then the issue becomes how much solvent will it take to
dissolved 30G of powder. My guess is about ~30ml of solvent (totally blind
guess here so don't quote me). That would be a solvent to PhloJel Ultra
ratio of 30%. That's 20% more than recommended. The final product will be
runny and may not have the delivery rate expected, once again wasted powder.
I have aided a couple pharmacist get 200mg/ml of testosterone base into
PhloJel Ultra. That's the extent of my high concentration experience.

Sorry I couldn't be of more help. If you decide to try the 30G per 100Ml
anyway, please let me know. I'll be glad to do what I can to assist (i.e.
solvent selection, compounding procedures, etc.). You have to be prepared to
blow the whole batch and lose what you have in my opinion if you do so.

Why not just shoot for a conservative 100mg/ml. That works easily. Even
~150mg/ml will work. Is the issue convenience or $$$?
R/
Carl
PhloJel Customer Support
Invalid Link Removed

 

[momod]

Damn, Carl is quick. Here is his reply:

Question: What if I wanted to mix 30 grams of powder into a 100g of Phlogel. Is that possible even with solvent? What would you suggest? Thanks. Nate.

Reply: My first response it that is way too much. 15g in 100g of PhloJel Ultra is
considered high and I have aided some who wanted 200mg per Ml of PhloJel
Ultra achieve that with solvent and proper levigation, but 300mg/Ml is, in
my opinion, too much. The real issue becomes the ability of the powder to
dissolve fully. My suspicion is that the final product will be grainy
feeling and will leave a residue of powder on the skins surface once dried.
What is visibly left behind on the skin is wasted powder. A proper solvent
and proper levigation with that solvent may be able to totally dissolve your
powder, but then the issue becomes how much solvent will it take to
dissolved 30G of powder. My guess is about ~30ml of solvent (totally blind
guess here so don't quote me). That would be a solvent to PhloJel Ultra
ratio of 30%. That's 20% more than recommended. The final product will be
runny and may not have the delivery rate expected, once again wasted powder.
I have aided a couple pharmacist get 200mg/ml of testosterone base into
PhloJel Ultra. That's the extent of my high concentration experience.

Sorry I couldn't be of more help. If you decide to try the 30G per 100Ml
anyway, please let me know. I'll be glad to do what I can to assist (i.e.
solvent selection, compounding procedures, etc.). You have to be prepared to
blow the whole batch and lose what you have in my opinion if you do so.

Why not just shoot for a conservative 100mg/ml. That works easily. Even
~150mg/ml will work. Is the issue convenience or $$$?
R/
Carl
PhloJel Customer Support
Invalid Link Removed

Carl is great, take his advice. You can always just use it more times per day.

 

[BodyWizard]

I'm curious if anyone uses another trick of Triceptor's.

I remember him saying that he got just-as-good-as-twice-daily results with a single application of mix and a follow-up application of 'raw' PJU which would "chase thru" any unabsorbed actives.

I get the picture, and it seems reasonable, but has anyone tried it?
(open to clarification & correction)

 

[velikimajmun]

I'm curious if anyone uses another trick of Triceptor's.

I remember him saying that he got just-as-good-as-twice-daily results with a single application of mix and a follow-up application of 'raw' PJU which would "chase thru" any unabsorbed actives.

I get the picture, and it seems reasonable, but has anyone tried it?
(open to clarification & correction)

Momod and I do it, but with chemo's home brew as the chaser.

 

[natedogg]

More from Carl.

Wow stuff sure does travel on the net. Those instructions for the 200mg/ml
using olive oil as the solvent are excerpted from my original instructions
that I've sent out to some who were interested. Yes that will work well.
It's the same instructions (less words) that I gave to a pharmacist. You
really need to use a mortar and pestle for the total process. First to
reduce the powder to the finest and then to levigate using the olive oil.
Just curious.. what board was that posted on? Also here's some other info
that I posted on a board regarding using additional penetration enhancers in
PhloJel Ultra.

If you want to increase the amount of drug penetrating the skin (the
epidermis) at a given concentration in the base then incorporating an
additional penetration enhancer in the base might accomplish this. Common
types of penetration enhancers in this context are menthol (1-3%), propylene
glycol (5-10%), DMSO (dimethylsulfoxide, 5-15%) and d-limonene (1-3%). By
their very nature they a tendency to disrupt the structure of the skin as
well as the delivery system, PHLOJEL Ultra. Hence, products containing these
are thin, more like a lotion but useable and effective. Menthol is a
crystalline substance that requires considerable particle size reduction
(levigation) in order to incorporate it and it has a strong odor and cooling
sensation on the skin. DMSO is a strong penetration enhancer but is
nonspecific with respect to what penetrates the skin (formulation
ingredients also penetrate the skin significantly). Propylene glycol simply
disrupts the water structure of skin allowing penetration through pores in
the skin. D-limonene has been widely studied in Japan and has been shown to
possess signifcant penetration power for a number of drugs applied from
simple bases. It's related to menthol but doesn't have the disadvantages of
menthol but its supply is limited and quite expensive (I don't know of a
source at the moment).
Benzyl alcohol is almost strictly used in liquid formulations as a
preservative (up to 2%) although it has been used as a solvent (5% and
above) in some situations. I don't have any information about its
incorporation in PHLOJEL Ultra but I would expect it to behave like any
other solvent and be nonspecific with regards to what penetrates the skin.
It would not be a solvent of choice in these situations. I hope this helps.

R/
Carl
PhloJel Customer Support
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[Viator]

An Excellent Solvent to mix w/ Phlogel

Is Avant Labs' Matrix-ABS. It's great at disolving fat-soluble compounds, and contains all the above-mentioned ingredients that help increase penetration. It's never let me down...

 

[velikimajmun]

Is Avant Labs' Matrix-ABS. It's great at disolving fat-soluble compounds, and contains all the above-mentioned ingredients that help increase penetration. It's never let me down...

What type of concentrations are you getting?

 

[triceptor]

Is Avant Labs' Matrix-ABS. It's great at disolving fat-soluble compounds, and contains all the above-mentioned ingredients that help increase penetration. It's never let me down...

It has DMSO in it?

 

[Viator]

It has DMSO in it?

Um... no, all but that.

you can put about 15g of "actives" in 8 oz of Matrix-ABS, about 20 if you heat it then mix in the phlojel and shake. I'm not sure what the concentration would be, but I got 6-oxo and 7-keto-DHEA

 

[BigVrunga]

Guys sorry if this has already been mentioned, but how is Phlogel better than a 'traditional' homebrew transdermal carrier? This is the recipe I used on my last transdermal cycle, and it worked really well:

40% IPA
12% IPM
12% IPP
10% OA
10% DMSO
6% D-Lim
5% PG
5% PEG400



BV

 

[titanp4]

If i get a 500g jar of phlogel how much test base can i add to it?

 

[triceptor]

If i get a 500g jar of phlogel how much test base can i add to it?

if you follow my compounding instructions - available on the phlojel.us website - you can easily add up to 150mg/ml.

Personally I feel that 100mg/ml is a perfect concentration. It's easier to administer specific doses in 100mg portions IMHO. There is compounding instructions floating around that allow incorporation of 200mg/ml however you have to triturate the powder with a solvent.

A 500G jar has 505 ML in it to if you use the 100mg/ml concentration (10% concentration) then you'll be able to incorrorate a total of 50.5 G of test base. Naturally you would not want attempt to compound this all at once - but instead in small 60ml to 100ml batches.

 

[Viator]

how is Phlogel better than a 'traditional' homebrew transdermal carrier? This is the recipe I used on my last transdermal cycle, and it worked really well:

40% IPA
12% IPM
12% IPP
10% OA
10% DMSO
6% D-Lim
5% PG
5% PEG400



BV

If I'm correct, that's the homebrew listed on the old conversionboard.com, which is essentially the original formula AvantLabs used for 4-Aderm, 1, 1+, and Super 1+. Par Claimed this formulation acheives 30-40% penetration. Phlojel CLEARLY gets more. I saw someone mention 60% penetration for Phlojel and after using it, I don't doubt that for a second.

 

[JKjnr]

Hi guys - this is my first post and I think it is best posted here as this Transdermal forum is pretty unique I'd say - and what I am mostly interested in.

Thanks for all this great info - what a resource.

On reading this thread and others like it, just what is the implication with DMSO in the above original Avantlabs homebrew to the other ingredients. Meaning - what happens when DMSO draws the other ingerdients in? What are their effects?


I am 6ft and just over 200 lbs at 12-13% bf. Training about 7 years. Started out at 135 lbs. No gear use yet but it's coming soon.

JK

 

[x_muscle]

If I'm correct, that's the homebrew listed on the old conversionboard.com, which is essentially the original formula AvantLabs used for 4-Aderm, 1, 1+, and Super 1+. Par Claimed this formulation acheives 30-40% penetration. Phlojel CLEARLY gets more. I saw someone mention 60% penetration for Phlojel and after using it, I don't doubt that for a second.

60% huh thats impossible, you need to dissolve your skin to get tha high pnetration. 20% is good expectation to transdermal carriers.

 

[VitaminT]

60% huh thats impossible, you need to dissolve your skin to get tha high pnetration. 20% is good expectation to transdermal carriers.

I agree. While I think Phlojel is a good product (I did try it), I didn't notice an advantage over an oral dose assuming a 60% conversion. Thus, I think the higher the atomic weight is, the more likely the conversion rate is substantially lower. I don't know much about science so it may be completely misguided thinking. The only thing I never liked about Phlojel was how damn greasy I felt. Humid weather + greasy = :wtf:

 

[x_muscle]

i seriously think DMSO bassed dermals are much better. PLO gels and lecithen based dermal are made for local delivery of cox-inhibitory. while some active material will be delivered systematiclly, most active will be trapped in other tissues (fat, muscle, and nerve tissue). Leciten is very ampiliphilc so it will stick to different tissues.

plus PLO works with low-molecular-weight hydrophilic drugs, steroids are not hydrophilic. Because lecithin is a lipophilic substance, it is able to pass through the stratum corncum.5 When a water-soluble drug is added to a hydrophohic substance, with the aid of a surfactant, both the drug and the Hydrophobie medium can pass through the epidermis. Now PLO-ULTRA dosent contain any surfactant, so how dose it acchieve that?!

Invalid Link Removed
-------------------------------------------------
Bioavailability of transdermal methimazole in a pluronic lecithin organogel (PLO) in healthy cats.

Hoffman SB, Yoder AR, Trepanier LA.

Department of Medical Sciences, University of Wisconsin-Madison, School of Veterinary Medicine, 53706-1102, USA.

The antithyroid drug methimazole is widely used for the medical management of feline hyperthyroidism. Recently, custom veterinary pharmacies have offered methimazole in a transdermal gel containing pluronic and lecithin (PLO), with anecdotal evidence of efficacy. The purpose of this study was to determine the bioavailability, relative to i.v. and oral routes of administration, of transdermal methimazole in a PLO gel in cats. Six healthy adult cats were assigned to receive 5 mg of methimazole by the i.v., oral, or transdermal routes, in a randomized triple crossover protocol with 1 week washout between doses. Blood samples were taken for high performance liquid chromatography (HPLC) determination of serum methimazole, at 0, 5, 15, 30, 60 min, and 2, 4, 6, 12 and 24 h after dosing. Methimazole absorption following transdermal administration was poor and variable, with only two of six cats achieving detectable serum methimazole concentrations at any time point following transdermal administration. Area under the concentration-time curve (AUC), maximum concentration (Cmax), and absolute bioavailability were all significantly lower for the transdermal route (0.39 +/- 0.63 microg h/mL, 0.05 +/- 0.09 microg/mL, and 11.4 +/- 18.7%, respectively) than for either i.v. (7.96 +/- 4.38 microg h/mL, 3.34 +/- 2.00 microg/mL, 100%) or oral routes (2.94 +/- 1.24 microg h/mL, 0.51 +/- 0.15 microg/mL, 40.4 +/- 8.1%). The results of this study indicate generally low to undetectable bioavailability of methimazole in a lecithin/pluronic gel given as a single transdermal dose to healthy cats, although one individual cat did achieve nearly 100% transdermal bioavailability relative to the oral route.


I belive that PLO has less or similar absorption rate as DMSO.

 

[jcam222]

hmmmm my brain feels like a tennis ball as I drift back and forth on which carrier to use. Triceptor can you comment on Xmuscles analysis of the efficacy of phlogel with steroid powders.

 

[velikimajmun]

plus PLO works with low-molecular-weight hydrophilic drugs,

This is false. Plogels are amphipathic containing both hydrophilic and lipophilic fractions which are held together in an emulsion. They are suitable for delivery of both hydrophilic and lipophilic compounds.

Now PLO-ULTRA dosent contain any surfactant, so how dose it acchieve that?!

Lecithin is a surfactant.

 

[x_muscle]

Lecithin is a surfactant.

Yes Lecithen is a surfactant, but its a week one. Plus the surfactant used in PLO gel (Pluronic) has special properties: Pluronic (poloxamcrs) are bifunctional block copolymer surfactants consisting of ethylene oxide and propylene oxide terminating in a primary hydroxyl group. Pluronic gels are believed to be formed by hydrogen bonding in aqueous Pluronic systems, caused by attraction of the surfactant ether oxygen atoms with water protons, making a high level of oxyethylation coupled with a high molecular weight, so it it carries lecithen visscles and adhere it to water molecules within the cell, and that act to penetrate deep giving systematic delivery.Lecithen alone is amphiphilic making systematic delivery less likely, and local delivery much highier.

 

[x_muscle]

his comes directly from the pharmacutical company that make PHLO Ultra:

The absolute bioavailability of a compound delivered transdermally is generally less than
that delivered orally unless the compound is highly metabolized in the liver (which is not a major concern for NSAIDs). Preliminary studies have indicated that the bioavailability of diclofenac from PHLOJEL® Ultra applied topically is approximately 5-10% of an equivalent oral dose, meaning that 90% less drug entered the circulation.


So according to this penetration is 5-10% only.

 

[VitaminT]

his comes directly from the pharmacutical company that make PHLO Ultra:

The absolute bioavailability of a compound delivered transdermally is generally less than
that delivered orally unless the compound is highly metabolized in the liver (which is not a major concern for NSAIDs). Preliminary studies have indicated that the bioavailability of diclofenac from PHLOJEL® Ultra applied topically is approximately 5-10% of an equivalent oral dose, meaning that 90% less drug entered the circulation.


So according to this penetration is 5-10% only.

AHA!!! :study:

 

[jonny21]

his comes directly from the pharmacutical company that make PHLO Ultra:

The absolute bioavailability of a compound delivered transdermally is generally less than
that delivered orally unless the compound is highly metabolized in the liver (which is not a major concern for NSAIDs). Preliminary studies have indicated that the bioavailability of diclofenac from PHLOJEL® Ultra applied topically is approximately 5-10% of an equivalent oral dose, meaning that 90% less drug entered the circulation.


So according to this penetration is 5-10% only.

Where did you get this from? Not on their site. The studies provided do not have anything mentioning this. Was any ad-libbing done? Could you provide a link to this?

It would not make any sense for them to state that there is ~40-60% absorption rate and then provide studies that contradict.

 

[x_muscle]

Where did you get this from? Not on their site. The studies provided do not have anything mentioning this. Was any ad-libbing done? Could you provide a link to this?

It would not make any sense for them to state that there is ~40-60% absorption rate and then provide studies that contradict.

Invalid Link Removed

 

[jonny21]

Why thank you very much.

 

[triceptor]

First of all this assumption that ANY transdermal delivery vehicle has the ability to LOCALIZE the drugs compounded into it is flawed. Once the vehicle delivers the drug through the stratum corneum and into the dermis, the drug makes its way to the fatty layer where the small blood vesels pick it up and once in the blood supply it WILL be delivered systemically. To waht degree is more the issue. These small vesles have no way of keeping a drug localized. Now.. it is true that the drug will initially be taken up in the local tissue where it's actions will be seen first, however, it will not simply stay there. There is no way to restrict it or limit it to this one area. So this idea that one vehicle is good for a local delivery -vs- one which is good for systemic delivery is a bit flawed.

Yes, if you have a vehicel that has a poor absorption/delivery quality, it may have a "more" local effect.. but this is simply due to the fact that LESS of the drug is getting through the skin.

The same can be achieve with a vehicle that has a higher delievry rate by using a lower concentration of the drug (0.25% to 1% concentration).

If you have an agent that you want to act on a local area.. say for instance a spot fat reduction product.. if you have a vehicle that has a high delivery rate.. you simply use less of the drug compounded into it and the end result is less evidendce of systemic delivery since the drug is utilized by the local tissue first and its actions are exhausted before any trace of it can make it upstream.

This is also the main point of the Diclofenac study execuretd by JAR Pharma. Less NSAID in a vehilce allows you to experience the benefits of localize effcts to the specified joint without the high degree of systemic delivery it would take using an oral. If you compounded a 10% batch of diclofenac and dosed out 2ML (200Mg) much more of it will spill over into systemic delivery.

When using PJU to deliver a drug systemically, concentration and dose make the difference. If you mix a batch of 10% test base and rub 2 Ml on your upper abdomen for instance.. you should expect a systemic delivery of ~40% over a 12 hour period.

Also.. where you apply a transdermal has profound effect on how it will be delivered. the knee is no at vascular as the upper chest/clavicle area and thus the not a good application site for a drug you WANT to be delivered systemically.

 

[triceptor]

Where did you get this from? Not on their site. The studies provided do not have anything mentioning this. Was any ad-libbing done? Could you provide a link to this?

It would not make any sense for them to state that there is ~40-60% absorption rate and then provide studies that contradict.

OK.. the Diclofenac study is not being read properly and does not contradict the previously stated delivery estimates of 40% to 60% delivery.. Whne the study refers to the "90% less drug is delivered systemically" they are referring to a comparison to an oral dose. the goal of this study was to show that a far lower concentration could be sued as an effective dose to reduce joint pain. ..you only NEED 5% to 10% of an equivelent ORAL dose to see the same effectiveness on a SPECIFIED joint where the transdermal was DIRECTLY applied.

You woul dhave to know how much of an oral dose of diclofenac is bioavailable, and then how much of it is delivered to that specific joint/area since an oral is delivered non-specifically to the whole body.. for you to be able to make any assumptions.

This simply shows that far less drug need be used to have an efefct.. which also points to the efficiency of PJU.

I have always used 40% to 50% as the target delivery rate when using PJU in a concentration and dosing regimen (including the appropriate application area) for s systemically delivere active.

 

[x_muscle]

First of all this assumption that ANY transdermal delivery vehicle has the ability to LOCALIZE the drugs compounded into it is flawed. Once the vehicle delivers the drug through the stratum corneum and into the dermis, the drug makes its way to the fatty layer where the small blood vesels pick it up and once in the blood supply it WILL be delivered systemically. To waht degree is more the issue. These small vesles have no way of keeping a drug localized. Now.. it is true that the drug will initially be taken up in the local tissue where it's actions will be seen first, however, it will not simply stay there. There is no way to restrict it or limit it to this one area. So this idea that one vehicle is good for a local delivery -vs- one which is good for systemic delivery is a bit flawed.

Yes, if you have a vehicel that has a poor absorption/delivery quality, it may have a "more" local effect.. but this is simply due to the fact that LESS of the drug is getting through the skin.

The same can be achieve with a vehicle that has a higher delievry rate by using a lower concentration of the drug (0.25% to 1% concentration).

If you have an agent that you want to act on a local area.. say for instance a spot fat reduction product.. if you have a vehicle that has a high delivery rate.. you simply use less of the drug compounded into it and the end result is less evidendce of systemic delivery since the drug is utilized by the local tissue first and its actions are exhausted before any trace of it can make it upstream.

This is also the main point of the Diclofenac study execuretd by JAR Pharma. Less NSAID in a vehilce allows you to experience the benefits of localize effcts to the specified joint without the high degree of systemic delivery it would take using an oral. If you compounded a 10% batch of diclofenac and dosed out 2ML (200Mg) much more of it will spill over into systemic delivery.

When using PJU to deliver a drug systemically, concentration and dose make the difference. If you mix a batch of 10% test base and rub 2 Ml on your upper abdomen for instance.. you should expect a systemic delivery of ~40% over a 12 hour period.

Also.. where you apply a transdermal has profound effect on how it will be delivered. the knee is no at vascular as the upper chest/clavicle area and thus the not a good application site for a drug you WANT to be delivered systemically.

Only Handful of systematic studies have been conducted by clinicians and veterinarians to probe the efficacy of PLO as a transdermal delivery vehicle.

In man: the in vivo studies in man where PLO was applied repeatedly, suggest PLO may be beneficial as delivery vehicle for local action. In these studies, diclofenac in PLO was applied over number of weeks for the treatment of osteoarthritis of the knee for lateral epiconylitis. Following application of PLO, patients experienced less pain, and increased wrist extension strength. However, drug levels in the blood were not measured and drug absorption into the systematic circulation can not be assured.


Invalid Link Removed

 

[x_muscle]

OK.. the Diclofenac study is not being read properly and does not contradict the previously stated delivery estimates of 40% to 60% delivery.. Whne the study refers to the "90% less drug is delivered systemically" they are referring to a comparison to an oral dose. the goal of this study was to show that a far lower concentration could be sued as an effective dose to reduce joint pain. ..you only NEED 5% to 10% of an equivelent ORAL dose to see the same effectiveness on a SPECIFIED joint where the transdermal was DIRECTLY applied.

You woul dhave to know how much of an oral dose of diclofenac is bioavailable, and then how much of it is delivered to that specific joint/area since an oral is delivered non-specifically to the whole body.. for you to be able to make any assumptions.

This simply shows that far less drug need be used to have an efefct.. which also points to the efficiency of PJU.

I have always used 40% to 50% as the target delivery rate when using PJU in a concentration and dosing regimen (including the appropriate application area) for s systemically delivere active.

I never saw study claims 60-40% penetration rate. can you post a link please.

 

[jcam222]

This is indeed some confusing stuff to wade through. The pdf file from Phlogel Ultra has a couple comments that confuse / concern me.

1) It states that generally topical is ineffetive for systemic effects.

2) It does state that 90% less diclofenac entered circulation. While we dont know the absorbtion rate of the oral dose it cant be higher than 100%. Assuming 100% this would still only give 10% absorbition via the phlogel wouldnt it??

 

[triceptor]

Only Handful of systematic studies have been conducted by clinicians and veterinarians to probe the efficacy of PLO as a transdermal delivery vehicle.

In man: the in vivo studies in man where PLO was applied repeatedly, suggest PLO may be beneficial as delivery vehicle for local action. In these studies, diclofenac in PLO was applied over number of weeks for the treatment of osteoarthritis of the knee for lateral epiconylitis. Following application of PLO, patients experienced less pain, and increased wrist extension strength. However, drug levels in the blood were not measured and drug absorption into the systematic circulation can not be assured.


Invalid Link Removed

PhloJel Ultra is NOT a PLO.... there is absolutely evidence of systemic deliver with hormones and transdermal lecithin organogels. You can look at one study on T at

 

[triceptor]

This is indeed some confusing stuff to wade through. The pdf file from Phlogel Ultra has a couple comments that confuse / concern me.

1) It states that generally topical is ineffetive for systemic effects.

2) It does state that 90% less diclofenac entered circulation. While we dont know the absorbtion rate of the oral dose it cant be higher than 100%. Assuming 100% this would still only give 10% absorbition via the phlogel wouldnt it??

again.. you are not reading this right. 90% less systeminc delivery than the ORAL dose. this study was not doen to show delivery rates. Onlyt to show that less diclofenac would be delivered systemically than oral yet have beneficial effect controling pain at the target joint.

 

[jcam222]

again.. you are not reading this right. 90% less systeminc delivery than the ORAL dose. this study was not doen to show delivery rates. Onlyt to show that less diclofenac would be delivered systemically than oral yet have beneficial effect controling pain at the target joint.

I am kinda dense on this I think so bear with me. I do understand they are saying it delivered 90% less systemically than the oral dose. The maximum percent the oral dose could have delivered is 100% thus isnt the best systemic delivery phlogel could have gotten 10%?

 

[jonny21]

In this case they wanted to show that with a low dose transdermal a lower amount of NSAID would be delivered systemically while achieving a higher concentration in the target area. This due to the fact that NSAIDs can cause other negative issues when taken orally. At least that is what I am now getting out of it.

I would imagine entry into the bloodstream would have to depend on the chemical. If the chemical is not taken up by the tissue enroute to capillaries more will enter the system. For our use I do not believe there is use of AAS in peripheral tissues.

Someone please correct me if I am off on this. Please provide info. I love to learn.

 

[x_muscle]

In this case they wanted to show that with a low dose transdermal a lower amount of NSAID would be delivered systemically while achieving a higher concentration in the target area. This due to the fact that NSAIDs can cause other negative issues when taken orally. At least that is what I am now getting out of it.

I would imagine entry into the bloodstream would have to depend on the chemical. If the chemical is not taken up by the tissue enroute to capillaries more will enter the system. For our use I do not believe there is use of AAS in peripheral tissues.

Someone please correct me if I am off on this. Please provide info. I love to learn.

I think systematic absorption depend on the area the gel is applied to. I have been reading alot obout PLO gel. if you apply to area close to blood capillairies then systematic deliver may be achived . But if you apply on you abs for example then systematic delivery will be very minimum and more active ingredient will be retained in tissues creating some type of local deliver. Seems like common sense.

 

[x_muscle]

PhloJel Ultra is NOT a PLO.... there is absolutely evidence of systemic deliver with hormones and transdermal lecithin organogels. You can look at one study on T at Invalid Link Removed

PhloJel is PLO minus the surfactant, but they both se same primary method of delivering drugs. You will notice the Jar Pharma uses studies done on PLO to provide support to their product claims, so abviously what applies to PLO applies also to PhloJel.

 

[triceptor]

PhloJel is PLO minus the surfactant, but they both se same primary method of delivering drugs. You will notice the Jar Pharma uses studies done on PLO to provide support to their product claims, so abviously what applies to PLO applies also to PhloJel.

To a degree. Pluronic adds some diferent qualities to the cosmetic effects of the gel. These cosmetic attributes have an effect on through the skin delievry over time of use. PhloJel Ultra is superior to PLO gels. It has several other penetration enhancers and has excelent cosmetic qualities that will not dry or irritate the skin over time of use. The later can create obstacles to drug delivery. skin hydration plays an important and.. and often overlooked role in how much of the drug gets delivered. The water in the dermis is important to a drugs progression through an onto the fatty layer. if a delivery vehicle dries the skin over time.. less and less of teh drug will be delivered when applying to the same area.

Also, becuse of the way a transdermal drug gets delivered over hours (much longer in fact than most 12 hour studies) you can get ~15% more drug in your system if you rotate the application area. Once an area is saturated with a drug and no more can get into the dermis, it lasy on the stratum corneum waiting for entry. By rotating the application areas (i.e. AM inner upper arm, PM clavicle) you create two fully saturated site that are delivering simultaneously. Think of it as a hose whose diameter can only sustain 1 gal per minute flow throug and you want to deliver 2 gallons of liquid. You can wait two minutes or add a second hose and get it done in one minute.... if that makes any sence...

Oh and its worth stating as often as possible.. avoid transdermal T application to the scrotum. the scrotum has a very high degreee of 5AR and is just a couple CM away fromt he prostate... get the picture?

 

[triceptor]

In this case they wanted to show that with a low dose transdermal a lower amount of NSAID would be delivered systemically while achieving a higher concentration in the target area. This due to the fact that NSAIDs can cause other negative issues when taken orally. At least that is what I am now getting out of it.

I would imagine entry into the bloodstream would have to depend on the chemical. If the chemical is not taken up by the tissue enroute to capillaries more will enter the system. For our use I do not believe there is use of AAS in peripheral tissues.

Someone please correct me if I am off on this. Please provide info. I love to learn.

the goal of the diclofenac study was to show that joint pain could be managed with a very small amount of the drug when delivered directly to the joint as to have no or very little systemic deliver.. since many NSAIDS are tough on the liver the benefits are clrea as to not having much of the drug circulating in the blood stream. so the goal was to show little or no systemic delivery. This was achieved by way of very low drug concentrations and the area of applicatioon being a poor candidate for systemic delivery.

this does not prove the lack of efficacy of any transdermal vehicle delivering the drug compounded into it systemically. transdermal progesterone, testosterone, estrogen, etc. have all been proven to work. As stated in one of teh other posts by X muscle.. systemic delievry depends a great deal on the area of application... high vascular density and lack of large amounts of subcutaneous fat make an area a good candidate for systemic delivery.....

 

[x_muscle]

Triceptor, do you know any way that i can test penetration rate through blood testing. Im thinking about doing a cycle with PhloJel with DMSO, and i want to do a before and after blood test to measure penetration rate.

but im thinking a simple blood test wont help me determine that , right?!

 

[triceptor]

Triceptor, do you know any way that i can test penetration rate through blood testing. Im thinking about doing a cycle with PhloJel with DMSO, and i want to do a before and after blood test to measure penetration rate.

but im thinking a simple blood test wont help me determine that , right?!

if you are trying t guage delivery of a given drug that has a systemic effect you may have to first do a cycle using injections and sample your blood. Then do a cycle using transdermal and sample your blood.

Compare the results of circulating values with injections. Keep in mind that you would have to use base active in both cases. If you use an esterfied active you have to take into account the actual amount of active versus the ester....

I have asked Dr. Rogers about doing a study on PJU delivery through the skin using acdavor skin. It may happen in the future. Its a bit complicsated and expensive.

 

[jcam222]

Triceptor, do you know any way that i can test penetration rate through blood testing. Im thinking about doing a cycle with PhloJel with DMSO, and i want to do a before and after blood test to measure penetration rate.

but im thinking a simple blood test wont help me determine that , right?!

How are you going to incorporate the DMSO x?