Oxytocin Dosage and Formulation

Autoimmune Chronic Pain Formulation Considerations

• Presented by Tricia Heitman, PharmD on March 27, 2025 for Personalized Medicine Certification

Oxytocin Dosage

• Available Dosage Forms Include: Nasal spray, sublingual
• Troches (melt and pour), suppositories, and oral capsules/suspensions are not appropriate dosage forms
• Heat degradation prevents use of troches and suppositories
• First-pass metabolism depletion prevents the use of oral capsules or suspensions

Oxytocin Nasal Spray

• Pros: Good absorption, easy to use, accurate dosing, good for NPO (nothing by mouth), nonsterile, noninvasive
• Cons: May cause burning at higher concentrations
• Dosing: Dosed in units and can be compounded up to 100 units per 0.1 mL
• Volume: Each metered nasal spray from PCCA delivers 0.1 mL per spray; fewer sprays are better
• Formulation: Oxytocin available from 10 Units/0.1 mL to 100 Units/0.1 mL Nasal Spray/Sublingual Suspension (MucoLox™)
• BUD Bracketed Study offers a 130-day expiration with two dosage options

Oxytocin Sublingual

• Pros: Easy to use, accurate dosing, good for NPO, nonsterile, noninvasive
• Cons: Less bioavailable than nasal spray, and requires patient education
• Sublingual lozenges requiring heat are inappropriate
• Dosing: Dosed in units and can be compounded up to 100 units per 0.1 mL
• Volume: Sublingual solution volume is best if kept low for maximum absorption, ideally 0.25 mL or less
• Tablet triturates can be an alternative to lozenges
• Formulation: Oxytocin available from 10 Units/0.1 mL to 100 Units/0.1 mL Nasal Spray/Sublingual Suspension (MucoLox™)
• BUD Bracketed Study offers a 130-day expiration with varied dosage options
• Oxytocin is found in a 12 Units Sublingual Tablet (Tablet Triturate 200 mg Mold), 24 Units Sublingual Tablet (Tablet Triturate 200 mg Mold) and 100 Units/0.1 mL Sublingual Suspension (SubMagna® SL HMW)

Oxytocin/Ketamine Unique Combination Formulations

• Nasal Spray: Ketamine 100 mg/mL and Oxytocin 24 Units/mL using MucoLox™
• Nasal Spray: Oxytocin 120 Units/mL and Hydroxocobalamin 5 mg/mL
• Sublingual Suspension: Methylene Blue 5 mg/0.25 mL and Oxytocin 25 Units/0.25 mL using Anhydrous SuspendIt®
• Sublingual Suspension: Naltrexone HCl 4.5 mg/0.2 mL, Melatonin 3 mg/0.2 mL, and Oxytocin 24 Units/0.2 mL

Ketamine Dosage

• Available Dosage Forms Options: Injectable, nasal spray, sublingual, oral, topical
• No specific dosage forms that will not work and why

Ketamine Injectable

• Pros: Most bioavailable, literature support
• Cons: Invasive, must be done in the office
• Commercially available concentrations: 10 mg/mL, 50 mg/mL, 100 mg/mL

Ketamine Nasal Spray

• Pros: Bioavailability, dosing accuracy, good for NPO, nonsterile, noninvasive
• Cons: Possible irritation, bitter taste
• Prescribing: Up to 100 mg/mL (10 mg/0.1 mL); volume limited by patient's tolerance and comfort level
• Formulations include 25 mg/mL, 50 mg/mL, and 100 mg/mL Nasal Sprays using MucoLox™ and a BUD study

Ketamine Sublingual

• Pros: Easy to use, dosing accuracy, good for NPO, nonsterile, noninvasive and multiple dosage form options
• Cons: Less bioavailable than nasal spray, patient education is a must, plus a very bitter taste
• Prescribing: Up to 150 mg/mL sublingual suspension or 300 mg per lozenge
• Dosage form considerations include the bitter taste and need for patient education
• Formulations: 150 mg/mL and 100 mg/mL Sublingual Suspension using SubMagna® SL HMW
• 30 mg and 7.5 mg Sublingual Tablet using Tablet Triturate
• 200 mg, 100 mg, and 10 mg Troche using NataTroche®

Ketamine Oral

• Pros: Better taste, easy for patients to use, less patient error, accurate dosing
• Cons: Less bioavailable, fewer studies
• Prescribing: Dosage adjusted based on bioavailability; consider for patients who cannot tolerate other forms; well-suited for chronic pain patients
• Formulations: Include immediate and modified release capsules in any appropriate strength
• 100 mg/mL and 50 mg/mL Oral Suspension using Anhydrous SuspendIt®

Ketamine Topical

• Pros: No taste issues, best for localized areas, fewer systemic adverse effects
• Cons: Can be difficult for some to apply, best for localized areas, the dose is still systemically absorbed
• Prescribing: Up to 200 mg/mL, concentration of 50 – 100 mg/mL is most common
• Volume is generally 0.25 - 1 mL per application; the 0.5 mL being most common
• Applications can be customized to fit a pump device
• Ketamine Topical Formulations: HCI 10% (Ketamine 8.7%) and HCI 11.5% (Ketamine 10%) Topical Cream using Lipoderm®

Ketamine Unique Combination Formulations

• Nasal Spray: Lidocaine HCl 4%/Ketamine 2.5% Buffered
• Nasal Spray: Ketamine 100 mg/mL/Oxytocin 24 Units/mL using MucoLox™
• Nasal Spray: Ketamine 10%/Cyanocobalamin using MucoLox™
• Topical : Ketamine HCl 0.5% to 5% (Ketamine 0.43% to 4.35%)/Amitriptyline HCl 2% using Lipoderm® and BUD Bracketed Study
• Topical: Ketamine HCl 10% (Ketamine 8.7%)/Gabapentin 6%/Diclofenac Sodium 3%/Baclofen 2%/Cyclobenzaprine HCl 2%/Bupivacaine HCl 0.5% using Lipoderm®

Magnesium

• Available Dosage Forms: Topical, oral
• For oral usage, magnesium should be chelated and a high-quality supplement
• For topical usage, sulfate or chloride salt work best

Magnesium Topical

• Pros: Easy to apply, can be used in most patient populations, plus patients with GI upset on oral magnesium can typically tolerate topical magnesium
• Cons: Localized application
• Prescribing: Up to 200 mg/mL; best concentrations are 10% and 20%, up to 1 mL is easy to apply for most patients
• Formulations: Magnesium Sulfate Heptahydrate 20% or 10% Topical using Lipoderm ActiveMax®
• Magnesium Sulfate Heptahydrate 10% Topical using Anhydrous Lipoderm®
• Magnesium Chloride at 10%Topical with Lipoderm ActiveMax® or Magnesium Chloride Hexahydrate at 10%/20% with Topical Lipoderm®

Magnesium Unique Combination Formulations

• Topical: Magnesium Chloride Hexahydrate 20%/Ketoprofen 10%/Lidocaine HCl 5%/ Menthol Topical Lipoderm®
• Topical: Magnesium Chloride Hexahydrate 10%/Baclofen 2% Topical Lipoderm®
• Topical: Magnesium Chloride Hexahydrate 20%/Melatonin 1% Topical Lipoderm ActiveMax®

Magnesium Oral

• Pros: Systemic magnesium replacement, simple to add to other pain treatments, can help with sleep and may increase GI motility
• Cons: NPO patients and may increase GI motility

Low-Dose Naltrexone (LDN)

• Available Dosage Forms: Oral, topical

LDN Oral

• Pros: Simple, literature support, makes titration simple, plus has a low GI side effect profile
• Cons: Cannot be used if the patient is on a narcotic
• Prescribing: Titration increments of 0.5 mg or 1.5 mg, typically given daily (9 pm), and adjustments can be made
• Oral dosage forms include capsule, suspension, chewable gelatin troche
• Oral Formulations: Naltrexone HCl 0.5 mg or 4.5 mg Capsules using SuspendIt® (with BUD bracketed study) and Anhydrous SuspendIt® from 0.5mg/ml to 5mg/ml along with Naltrexone HCl at 1 mg/mL and 5 mg/mL

LDN Topical

• Pros: Perfect for NPO
• Cons: Less literature, dosage may need adjustment
• Prescribing: All dosages can be accommodated; best to keep the volume low (0.25 – 0.5 mL per dosage) and can be customized to fit a pump device

Methylene Blue

• Available Dosage Forms: Oral (capsules and suspension)
• Inappropriate Dosage Forms: Transdermal and heated dosage forms (such as lozenges)

Methylene Blue Oral

• Pros: Literature, ease of use, makes titration simple
• Cons: Blue staining
• Prescribing: Capsules in a range of dosages, oil filled/powder filled capsules available
• Oral suspension 10 mg/mL (used primarily for titration)
• Formulations: 5 - 50 mg Oil Capsules and 1% Oral Suspension using Anhydrous SuspendIt®
• 5 - 50 mg Capsules using LoxOral® and1% Oral Suspension using SuspendIt®

Methylene Blue Unique Combination Formulation

• Sublingual Suspension: Methylene Blue 5 mg/0.25 mL/Oxytocin 25 Units/0.25 mL with Anhydrous SuspendIt®

GLP-1s

• Compounded Dosage Form Options: Sublingual, injection?
• Compounded dosage forms that won’t work and why:
  • Oral capsules require special ingredients for bioavailability
  • Troches present watch for heat degradation
  • Injections are a problem if the chemical on patent and is NOT on the FDA shortage list

GLP-1 Sublingual

• Pros: Non-invasive, easy to use (with training), positive results with the right base
• Cons: Lack of literature support, not easy to absorb via transmucosal route, patient training is a must
• Formulations: Semaglutide (CADP) 0.75 mg/mL, 1 mg/mL, 2 mg/mL and 3 mg/mL Sublingual Suspension using SubMagna® SL HMW

Unique GLP-1 Formulations

• Sublingual: Naltrexone HCl 16 mg/mL/Semaglutide (CADP) 1 mg/mL with SubMagna® SL HMW
• Sublingual: Melatonin 10 mg/mL/Semaglutide (CADP) 2 mg/mL with SubMagna® SL HMW

PCCA Bases

• Bases mentioned include: LoxOral®, SuspendIt®, and Anhydrous SuspendIt® and SubMagna® SL HMW
• Lipoderm® , Lipoderm ActiveMax®, and Anhydrous Lipoderm®
• MucoLox™

LoxOral®

• Capsule filler that may improve the dissolution of some drugs
• Formulated without Gluten, Casein, Sodium lauryl sulfate, Lactose, Soy, Corn, Dye and Magnesium stearate

SuspendIt®

• Oral suspension base and a natural suspending agent (unique synergistic polymer complex)
• Allows for rapid redispersion of APIs with agitation and minimizes sedimentation with a pleasant taste with natural and neutral sugar-free sweetener (monk fruit)
• Formulated without Gluten, Casein, Dairy, Parabens, Soy, Propylene glycol, Carbomer, Dye and Alcohol
• Physio-chemical stability is published in studies of Clindamycin, Lansoprazole, Fluconazole, Omeprazole Phenobarbital, Spironolactone ,Trimethoprim / Sulfadiazine and Ursodiol

Anhydrous SuspendIt®

• Anhydrous oral suspending agent that is ideal for drugs unstable in water or with incompatibilities in some aqueous vehicles
• Potential for longer BUDs with thixotropic effect which allows rapid redispersion of APIs upon agitation with potentially minimal sedimentation
• Naturally sweetened with monk fruit, preservative free, offers improved palatability from traditional oil vehicles, and mixes easily with water or juice

SubMagna® SL HMW

• Accommodates a variety of drug molecular weights and provides alternative dosing delivery for commercially available semaglutide and broad range of other APIs being anhydrous to extend stability
• Clinical trials show single dose of semaglutide delivered in SubMagna showing improved bioavailability and less variability in plasma concentration compared to oral options.
• Commercial oral semaglutide has very low absorption, testing show semaglutide in SubMagna SL HMW to deliver the peptide into and through human gingival and oral tissues . The formulation has spontaneous formation of micelles which assist with delivery.

Lipoderm®

• This is the most studied proprietary permeation-enhancing vehicle used in compounding pharmacies that is supported via scientific publications

Lipoderm ActiveMax® and Lipoderm®

• Formulations are without almond, egg, fish, gluten, hazelnut, macadamia, milk, peanut, pecan and walnut

MucoLox™

• This is a unique bond with muscosal surfaces creating long lasting moisturization and adhesion that is supported with scientific publications
• Formulations are without Dye, Nuts, Gluten, Ethanol, Casein, Parabens, Dairy, Propylene glycol, Soy and Flavor