Ipamorelin Injection Formulation

Oct 1, 2025

Disclaimer: For Informational Use by Qualified Professionals Only

Not Medical or Regulatory Advice
This document and the formulations, processes, and information contained herein (collectively, the “Content”) are provided solely for educational and informational purposes. Nothing in this document constitutes medical advice, legal advice, regulatory guidance, or a substitute for professional judgment by a qualified healthcare provider or licensed compounding pharmacist. The Content is not a replacement for prescriber-specific instructions, regulatory requirements, or clinical standards of care.

User Responsibility
It is the exclusive responsibility of any person or entity utilizing this information to ensure all preparations, decisions, and practices comply with federal, state, and local laws, including but not limited to USP <795>, <797>, <800>, DEA, FDA, and applicable Board of Pharmacy requirements. All compounding activities must be performed by professionals who have received proper training and operate within their licensed scope of practice.

By using this Content, you affirm that you:

  • Validate Information Independently: You will conduct independent verification and analysis to determine the suitability, accuracy, and safety of any formula, ingredient, or procedure. This includes, but is not limited to, evaluating potency, sterility, pH, stability, and compatibility with prescribed therapeutic goals and patient-specific needs.

  • Conduct Appropriate Testing: You will perform all necessary quality control measures before dispensing or administering any preparation, including analytical testing where applicable.

  • Ensure Legal and Regulatory Compliance: You will adhere strictly to all relevant compounding regulations, documentation requirements, and labeling standards.

  • Maintain Oversight and Accountability: You assume full responsibility for staff training, facilities, equipment, documentation, and procedures involved in the use of this Content.
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Suggested Master Formulation Record (MFR)

Title: Ipamorelin Injection, 2 mg/mL – Preserved Multi-Dose Vial (MDV)
Batch Size: 100 mL
Dosage Form/Route: Solution for Subcutaneous Injection, MDV
Risk Category: USP <797> Category 2 (aseptic filtration)
Environmental Controls: All manipulations in ISO 5 PEC within ISO 7 buffer room (ISO 8 ante)

Component

Quantity

Function

Notes

Ipamorelin acetate

0.200 g

API

Adjust for purity/potency

Benzyl Alcohol

0.9 mL (0.9% v/v)

Antimicrobial preservative

Contraindicated in neonates

Sodium Chloride

0.85 g

Isotonicity

≈290 mOsm/kg from NaCl alone

Disodium EDTA

0.005 g (0.005% w/v)

Chelator / preservative booster

Optional but recommended

Polysorbate 20

0.010 g (0.01% w/v)

Anti-adsorption / wetting

Optional—validate AET if used

Sodium citrate / Citric acid

q.s. to ~7 mM buffer

Buffer

Target pH 5.5–6.2 (prefer ~5.8)

HCl or NaOH (1N)

q.s.

pH adjustment

Minimal adjustments only

Sterile Water for Injection

q.s. to 100 mL

Vehicle

Equipment & Supplies
  • ISO 5 certified PEC; ISO 7 buffer; ISO 8 ante

  • Class A balance; pH meter (calibrated)

  • Sterile mixing vessels, low-shear stir bar (or orbital shaker)

  • Prefilter 0.45 µm and sterilizing filter 0.22 µm (PES) with holders/tubing

  • Sterile, depyrogenated Type I glass amber MD vials (e.g., 10 mL or 20 mL)

  • Compatible closures (e.g., bromobutyl stoppers) and aluminum seals

  • Optional nitrogen source for headspace blanket

  • Sterile syringes/needles, 0.2 µm syringe filter for samples

Procedure (Aseptic; summarize on BPR)
  1. Prep & Verification

    • Complete line clearance and cleaning; verify PEC certification.

    • Stage and verify all materials (lot/exp, CoAs), equipment, and filters.

    • Calculate API correction; record weighed amounts.

  2. Prepare Vehicle & Buffer (ISO 5 in ISO 7)

    • In sterile vessel, add ~70–80% of final SWFI volume.

    • Add sodium citrate portion; adjust pH toward 5.8 with citric acid/1N acids/bases as needed. Keep buffer ~7 mM (low capacity).

    • Add NaCl; mix gently to dissolve.

    • Add EDTA (if used) and dissolve completely.

  3. Dissolve API

    • Sprinkle Ipamorelin onto gently stirring solution; avoid vortexing/high shear. Mix until fully dissolved.

    • If using polysorbate 20, add now; mix gently.

  4. Add Preservative

    • Add Benzyl Alcohol 0.9% v/v; mix gently. Re-check pH and adjust to 5.5–6.2 (prefer ~5.8).

  5. q.s. to Volume

    • Bring to 100 mL with SWFI. Mix gently. Record appearance and pH.

  6. Sterile Filtration & Fill

    • Prefilter (0.45 µm) into a sterile receiving vessel if needed → then 0.22 µm PES sterilizing filter into sterile amber MD vials.

    • Optional: nitrogen headspace to minimize oxidation.

    • Fill volume per vial (e.g., 10 mL), stopper, crimp.

    • Perform filter integrity test (pre/post). Record results.

  7. In-Process Controls

    • Appearance (clear, colorless; no visible particulates).

    • pH (target 5.5–6.2).

    • Yield / fill reconciliation.

Packaging & Storage
  • Container-closure: Type I amber glass MD vials with compatible stoppers; verify CCI.

  • Storage: Refrigerate 2–8 °C, protect from light, do not freeze.

Labeling 
  • Ipamorelin 2 mg/mL — Preserved (Benzyl Alcohol 0.9%) — Multi-Dose Vial”

  • Total volume, lot #, BUD, storage, “Discard 28 days after first puncture”

  • Route: Subcutaneous use only

  • Cautions (BA warning for neonates), beyond-use after puncture, Rx only

Quality Control (release & stability panel)
  • Identity & Assay (API): Stability-indicating HPLC (report degradants).

  • pH: 5.5–6.2.

  • Osmolality: record (target ≈280–350 mOsm/kg).

  • Preservative Content: BA assay (HPLC/GC).

  • Particulate Matter: USP <788> (small-volume injections).

  • Sterility: USP <71>.

  • Bacterial Endotoxins: USP <85> (meets injectable limits).

  • Container Closure Integrity: USP <1207> (per validation/periodic verification).

  • Antimicrobial Effectiveness Test: USP <51> (final formulation) — required for MDV; if polysorbate 20 is used, include in AET.

Beyond-Use Dating (BUD)
  • Default (no extended stability program): Treat as USP <797> Category 2 CSP prepared by aseptic filtration20 days at 2–8 °C, 10 days at 20–25 °C, 45 days frozen (≤ −20 °C).

  • After first puncture (MDV): 28 days refrigerated unless otherwise supported.

  • Any longer refrigerated BUD (e.g., 60–90 days) requires full, stability-indicating studies (chemistry + microbiology) on the final formula in its container-closure.

Notes & Rationale
  • pH 5.5–6.2 (prefer ~5.8) balances peptide stability (↓ deamidation/oxidation) and injection comfort.

  • Low-capacity citrate buffer (~7 mM) minimizes site irritation and offers mild metal chelation synergy with EDTA 0.005%.

  • Benzyl Alcohol 0.9% is a standard MDV preservative; phenol 0.5% is a viable clinic-preference alternative (would require its own AET & label update).

  • Polysorbate 20 (0.01% w/v) can reduce surface adsorption/handling losses; validate in <51> and with your specific container & admin set.

References
  1. USP <797> Pharmaceutical Compounding – Sterile Preparations. United States Pharmacopeia and National Formulary (USP–NF). Latest official version.
    – Requirements for environmental controls, aseptic technique, risk categories, and default BUDs.

  2. USP <71> Sterility Tests. USP–NF.
    – Mandatory sterility testing for sterile drug products.

  3. USP <85> Bacterial Endotoxins Test. USP–NF.
    – Ensures injectable preparations meet pyrogen limits.

  4. USP <788> Particulate Matter in Injections. USP–NF.
    – Particulate testing for small-volume injections.

  5. USP <51> Antimicrobial Effectiveness Testing (AET). USP–NF.
    – Required for preserved, multi-dose vials to confirm preservative efficacy.

  6. USP <1207> Package Integrity Evaluation – Sterile Products. USP–NF.
    – Guidance on closure/container integrity for sterile drug products.

  7. FDA. Guidance for Industry: Container Closure Systems for Packaging Human Drugs and Biologics (1999).
    – Compatibility requirements for vial/stopper systems with preservatives and peptides.

  8. FDA. Guidance for Industry: Q1A(R2) Stability Testing of New Drug Substances and Products (2003).
    – Requirements for stability-indicating studies supporting extended BUDs.

  9. Allen, L.V. and Ansel, H.C. Ansel’s Pharmaceutical Dosage Forms and Drug Delivery Systems. 12th ed. Wolters Kluwer; 2020.
    – Reference for buffer systems, isotonicity, preservative systems, and excipient functions.

  10. Rowe RC, Sheskey PJ, Quinn ME (Eds.). Handbook of Pharmaceutical Excipients, 8th Edition. Pharmaceutical Press; 2017.
    – Properties and compendial status of benzyl alcohol, phenol, EDTA, polysorbate 20, sodium citrate, and phosphate buffers.

  11. Florence AT, Attwood D. Physicochemical Principles of Pharmacy: In Manufacture, Formulation and Clinical Use. 6th Edition. Pharmaceutical Press; 2016.
    – Peptide stability considerations (pH, buffer selection, oxidative degradation).

  12. Bansal G, et al. "Stability of peptide formulations: Challenges and strategies." Int J Pharm. 2019; 564: 76–94.
    – Scientific background on peptide stability, preservative effects, and excipient optimization.

  13. Martindale: The Complete Drug Reference. Pharmaceutical Press; latest online edition.
    – Clinical reference on benzyl alcohol, phenol, and multi-dose vial preservatives.

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Disclaimer

This document is provided for educational and informational purposes only. It is the responsibility of the compounding pharmacist to ensure compliance with all applicable regulatory guidelines (including USP <797> and FDA regulations). Compounded sterile preparations should only be prepared by qualified personnel in appropriate sterile environments.

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