List of Excipients in Branded Drug METHYLERGONOVINE MALEATE

Generic Drugs Containing METHYLERGONOVINE MALEATE

Company	Ingredient	NDC	Excipient
West-Ward Pharmaceuticals Corp	methylergonovine maleate	0054-0639	ACACIA
West-Ward Pharmaceuticals Corp	methylergonovine maleate	0054-0639	CELLULOSE, MICROCRYSTALLINE
West-Ward Pharmaceuticals Corp	methylergonovine maleate	0054-0639	GELATIN
West-Ward Pharmaceuticals Corp	methylergonovine maleate	0054-0639	LACTOSE MONOHYDRATE
West-Ward Pharmaceuticals Corp	methylergonovine maleate	0054-0639	METHYLPARABEN
West-Ward Pharmaceuticals Corp	methylergonovine maleate	0054-0639	POVIDONE

What are the Most Frequently-Used Excipients in METHYLERGONOVINE MALEATE?

# Of NDCs	Excipient
12	ACACIA
13	CELLULOSE, MICROCRYSTALLINE
11	GELATIN
1	GELATIN TYPE B BOVINE
13	LACTOSE MONOHYDRATE
9	MALEIC ACID

Methylergonovine Maleate Excipient Strategy, Formulation Opportunities, and Generic Market Analysis

Last updated: September 16, 2026

Methylergonovine maleate is an established ergot alkaloid used to prevent or treat postpartum uterine hemorrhage. Its commercial opportunity is primarily generic and hospital-focused. The strongest formulation opportunities are not new active-ingredient claims, but differentiated presentations that improve injection safety, oral-tablet robustness, storage, dose preparation, and supply reliability.

What is methylergonovine maleate used for?

Methylergonovine maleate is a semi-synthetic ergot alkaloid that produces sustained uterine contraction. FDA labeling identifies oral tablets and parenteral injection as dosage forms for the routine management of uterine atony and postpartum hemorrhage after delivery of the placenta.[1,2]

Attribute	Oral product	Injectable product
Typical strength	0.2 mg tablet	0.2 mg/mL
Route	Oral	Intramuscular; intravenous use is restricted and requires caution
Primary setting	Postpartum prophylaxis or treatment after delivery	Hospital, obstetric, emergency and operating-room use
Main formulation risk	Content uniformity at a low dose	Sterility, particulate control, container closure and light stability
Principal commercial buyers	Retail pharmacies, hospital pharmacies	Hospitals, group purchasing organizations and specialty distributors

The product is not used during pregnancy before delivery because it can produce powerful uterine contractions. Hypertension and toxemia are major contraindications or restrictions in labeling.[1,2]

What excipients are used in methylergonovine maleate tablets?

Commercial tablet excipients vary by manufacturer and should be confirmed against each product’s current FDA label. Legacy methylergonovine maleate tablets commonly use lactose, corn starch and stearic acid or related lubricant systems. Some manufacturers may use different fillers, disintegrants, glidants or coating materials.[1,3]

A typical low-dose tablet platform may include:

Excipient function	Candidate materials	Formulation purpose
Diluent	Lactose monohydrate, microcrystalline cellulose, mannitol	Provides tablet mass for a 0.2 mg dose
Disintegrant	Corn starch, crospovidone, croscarmellose sodium, sodium starch glycolate	Promotes tablet breakup
Binder	Povidone, pregelatinized starch, hydroxypropyl cellulose	Improves granule and tablet strength
Lubricant	Stearic acid, magnesium stearate, sodium stearyl fumarate	Reduces tooling friction
Glidant	Colloidal silicon dioxide	Improves powder flow
Moisture barrier	Hypromellose, polyvinyl alcohol, polymer film coat	Reduces moisture exposure and handling damage
Taste or swallowability aid	Film coating, colorant, polishing agent	Improves patient acceptability and product identification

The 0.2 mg strength makes content uniformity a central development issue. The active ingredient represents a very small fraction of tablet weight, so segregation, over-lubrication and poor blend homogeneity can create out-of-specification results.

How should an excipient strategy address the low-dose formulation?

The most defensible strategy is to prioritize blend uniformity, segregation control and dissolution reproducibility rather than simply minimizing excipient count.

Direct compression

Direct compression can reduce processing steps and manufacturing cost. It requires a highly flowable and uniform active-excipient blend. Microcrystalline cellulose, spray-dried lactose and co-processed excipients can support direct compression, but the approach must be validated for low-dose content uniformity.

Key development controls include:

• Particle-size matching between methylergonovine maleate and the principal diluent.
• Low-shear blending studies to identify segregation during transfer and hopper discharge.
• Sampling plans that test blend, tablet-core and finished-product uniformity.
• Lubrication studies because excessive magnesium stearate can slow dissolution.
• Evaluation of tablet weight variation as an indirect process-control signal.

Wet or dry granulation

Granulation is more attractive when the active ingredient has poor flow or poor blend uniformity. Dry granulation can avoid water exposure and reduce thermal stress. Wet granulation may improve content uniformity, but it introduces potential risks related to moisture, hydrolysis, drying conditions and polymorphic or salt-form changes.

For a legacy drug with modest commercial pricing, dry granulation or a simple validated direct-compression process is generally more commercially attractive than a complex multiparticulate system.

Excipient-reduced formulation

An excipient-reduced product could appeal to hospitals and patients with known sensitivities, but the commercial value is limited unless it improves a measurable product attribute. A reduced-excipient claim alone is unlikely to support a strong regulatory or patent position.

The stronger approach is a formulation that combines:

1. Demonstrated content uniformity at 0.2 mg.
2. Better mechanical strength during high-volume packaging.
3. Improved dissolution after accelerated storage.
4. A documented reduction in moisture uptake or tablet friability.

What excipients are used in methylergonovine maleate injection?

Parenteral formulations require a different strategy. The principal excipient system is typically an aqueous vehicle with tonicity adjustment and, depending on the product, pH adjustment or preservation. Current manufacturer labeling must be used to confirm the exact qualitative and quantitative composition.[2,4]

Potential components include:

Formulation need	Candidate materials	Development issue
Vehicle	Water for injection	Must meet sterile pharmaceutical-water specifications
Tonicity adjustment	Sodium chloride	Controls osmolality and injection tolerability
pH adjustment	Hydrochloric acid, sodium hydroxide or other approved agents	Controls stability and compatibility
Preservation	Product-specific preservative, where permitted	Requires preservative efficacy and safety assessment
Chelation or stabilization	Product-specific stabilizer	Must be justified by degradation and compatibility data
Container protection	Amber glass, light-protective packaging	May reduce photodegradation

A preservative-free, single-dose presentation may have the strongest hospital value. Obstetric drugs are administered in high-acuity settings, and preservative minimization can simplify neonatal and maternal safety assessments. The tradeoff is increased packaging cost, more stringent aseptic processing requirements and potentially shorter in-use flexibility.

What formulation patents could protect methylergonovine maleate?

A new methylergonovine maleate product would generally need a formulation or manufacturing distinction that produces a measurable technical effect. Broad claims covering the active ingredient itself are unlikely to be commercially useful for an old generic drug.

Potential patentable themes include:

Patent theme	Potential claim focus	Commercial value
Low-dose tablet uniformity	Defined particle-size distribution, carrier ratio or blending sequence	Moderate if linked to reproducible content uniformity
Moisture protection	Specific coating, packaging or desiccant configuration	Moderate for shelf-life extension
Injection stability	Defined pH, ionic strength, oxygen control or light protection	Moderate to high if stability is materially improved
Preservative-free injection	Sterile formulation and container-closure system	Moderate, especially for hospital procurement
Ready-to-use presentation	Prefilled syringe, unit-dose ampule or cartridge	High operational value if regulatory requirements are met
Manufacturing process	Granulation, sterilizing filtration or filling sequence	Usually narrow but useful against direct process copying
Device combination	Delivery system designed for controlled administration	Potentially valuable, but requires device-specific development

A formulation patent is more defensible when the specification documents unexpected stability, reduced particulate formation, improved assay recovery or superior content uniformity. A simple substitution of lactose with microcrystalline cellulose, without a demonstrated technical advantage, would be vulnerable to obviousness challenges under U.S. patent law.

What is the Orange Book status of methylergonovine maleate?

Methylergonovine maleate is an old, multisource drug with no meaningful period of branded market exclusivity. FDA approval is generally pursued through the abbreviated new drug application pathway when the reference product and regulatory requirements are satisfied.[5]

Regulatory issue	Commercial implication
New chemical entity exclusivity	Not available for this established active ingredient
Orphan exclusivity	Not generally applicable to the broad postpartum hemorrhage indication
Pediatric exclusivity	No routine commercial assumption should be made
GAIN or qualified infectious-disease exclusivity	Not applicable
Orange Book patents	Any current listing must be verified by product and edition
Paragraph IV exposure	Relevant only if an active listed patent exists against the selected reference product
Generic substitution	Depends on state law, product rating and institutional formulary policy

The Orange Book should be reviewed for the specific reference-listed drug and dosage form before filing. Legacy methylergonovine products may have limited or no active patent protection, making regulatory execution, manufacturing reliability and supply economics more important than patent blocking.

When does methylergonovine maleate lose exclusivity?

Commercial exclusivity has effectively expired for methylergonovine maleate. The active ingredient and core dosage forms have been marketed for decades, and the principal competitive barriers are regulatory approval, validated sterile manufacturing, quality systems and hospital contracting.

The practical timeline is therefore:

Event	Timing or status
Original clinical and commercial use	Historical, predating modern generic competition
Core composition-of-matter protection	Expired
New chemical entity exclusivity	Expired or unavailable
Generic tablet competition	Established market
Generic injection competition	Established but more operationally constrained
Current opportunity	Supply continuity, quality differentiation and dosage-form execution

Patent term extension is not a realistic strategy for the legacy active ingredient. A newly developed formulation or device could receive a separate patent term, but its value would depend on whether the product captures a distinct market segment.

Which companies are challenging or competing with methylergonovine maleate?

Competition is primarily among generic manufacturers and contract manufacturers rather than branded innovators. The relevant competitive set includes manufacturers of:

• Methylergonovine maleate tablets.
• Methylergonovine maleate injection.
• Oxytocin injection.
• Carboprost tromethamine injection.
• Misoprostol tablets.
• Tranexamic acid injection, which is used in postpartum hemorrhage protocols but has a different mechanism.

Methylergonovine competes most directly with oxytocin and carboprost in hospital uterotonic protocols. Oxytocin is frequently used first-line, while methylergonovine is often selected when additional uterine contraction is needed and hypertension is not present.[1,2,6]

Product	Main advantage	Main limitation
Methylergonovine	Potent, sustained uterotonic effect; oral and injectable forms	Hypertension-related restrictions
Oxytocin	Established first-line hospital use; broad obstetric familiarity	Requires controlled administration and monitoring
Carboprost	Useful in refractory uterine atony	Respiratory and other tolerability concerns
Misoprostol	Oral, sublingual or rectal administration; broad availability	Variable tolerability and administration preferences
Tranexamic acid	Antifibrinolytic benefit in postpartum hemorrhage	Does not directly contract the uterus

The commercial opportunity is strongest where the product is included in standardized postpartum hemorrhage kits, emergency carts and hospital protocol bundles.

What generic entry risks exist for methylergonovine maleate?

The main risks are operational rather than patent-based.

Sterile manufacturing risk

For injection, the applicant must manage aseptic processing, sterility assurance, endotoxin control, particulate matter, container closure integrity and stability. A manufacturing interruption can create disproportionate commercial damage because hospitals may have limited substitutes in their formularies.

Low-dose analytical risk

For tablets, the 0.2 mg strength creates content-uniformity and assay-sensitivity challenges. The analytical method must distinguish methylergonovine maleate from degradation products and excipient-related interference.

Supply-chain risk

Hospitals may prefer suppliers with dual-source API qualification, validated alternate packaging and adequate safety stock. A low-price launch without reliable supply may fail to secure durable contracts.

Labeling and medication-error risk

Methylergonovine products require clear strength, route and contraindication labeling. Injectable packaging should minimize confusion with other obstetric drugs, especially oxytocin and carboprost.

What commercial opportunities exist for methylergonovine maleate?

Hospital-ready injectable products

The strongest opportunity is a reliable, single-dose injectable product supplied in formats compatible with hospital inventory systems. Potential features include:

• Preservative-free single-dose ampules or vials.
• Bar-code-ready unit packaging.
• Light-protective packaging.
• Extended labeled shelf life.
• Ready availability through group purchasing organizations.
• Packaging designed for rapid identification in emergency carts.

A manufacturer that can demonstrate dependable supply may compete effectively despite the absence of patent exclusivity.

Robust oral tablets

A tablet with improved mechanical strength, low friability and stable dissolution can reduce pharmacy waste and improve institutional handling. Film coating may support product identification and moisture control, but it must not delay dissolution or complicate low-dose assay performance.

Contract manufacturing and private-label supply

Because the active ingredient is established, brand owners, distributors and hospital suppliers may prefer a contract-development and manufacturing organization rather than building an internal product platform. A manufacturer with both tablet and sterile capabilities can offer a broader product package.

International registration

Methylergonovine maleate may have opportunities in jurisdictions where postpartum hemorrhage remains a high-priority clinical problem and local sterile manufacturing capacity is limited. Geographic expansion requires country-specific review of:

• Approved indications.
• Route-of-administration restrictions.
• Preservative requirements.
• Pharmacopoeial standards.
• Stability-zone requirements.
• Serialization and packaging rules.
• Local procurement and tender systems.

How strong is the patent estate for methylergonovine maleate?

The core patent estate is weak because the active ingredient and conventional dosage forms are old. A new entrant is more likely to face regulatory and manufacturing barriers than blocking composition-of-matter patents.

Asset type	Expected strength
Active-ingredient patent	Very weak or expired
Conventional tablet formulation	Weak unless tied to a specific technical result
Conventional aqueous injection	Weak unless the formulation has a novel stability or preservation profile
Device or prefilled syringe	Moderate if structurally distinct and clinically useful
Manufacturing process	Narrow to moderate
Packaging and supply-system claims	Potentially useful but easy to design around
Trade secrets	Potentially important for sterile process controls and low-dose blending

The preferred intellectual-property strategy is a layered portfolio covering formulation, process, container closure and device presentation. Patent filings should avoid claims that merely restate routine excipient substitutions.

What patent litigation and Paragraph IV issues affect the product?

There is no established basis to treat methylergonovine maleate as a major current Paragraph IV battleground. For an ANDA applicant, the relevant analysis is product-specific: identify the reference-listed drug, review current Orange Book patent listings, determine whether any listed patent remains enforceable and assess the certification required under 21 U.S.C. §355(j).[5,7]

A new formulation product may create its own patent litigation risk if it is commercialized against an active formulation patent. Conversely, a generic tablet or injection based on conventional excipients is more likely to face ordinary ANDA review, bioequivalence or quality questions than substantive patent litigation.

Key Takeaways

• Methylergonovine maleate is a mature generic uterotonic with limited core patent protection.
• The principal opportunity is a reliable hospital injectable, not a new chemical entity strategy.
• Tablet development should focus on low-dose content uniformity, segregation control, dissolution and moisture protection.
• Injection development should focus on sterility, particulate control, container closure, light stability and preservative strategy.
• A preservative-free, single-dose injectable presentation may offer the clearest commercial differentiation.
• Orange Book and Paragraph IV exposure must be confirmed for the selected reference-listed drug and current FDA edition.
• Patent value is most likely to arise from a demonstrated formulation, process, device or packaging improvement.
• Commercial success will depend heavily on supply continuity, hospital contracting and regulatory execution.

FAQs

Can methylergonovine maleate be formulated with microcrystalline cellulose?

Yes. Microcrystalline cellulose can serve as a diluent and dry binder in a low-dose tablet, but the formulation must demonstrate acceptable blend uniformity, tablet strength, dissolution and stability.

Is methylergonovine maleate injection suitable for a prefilled syringe?

Potentially. A prefilled syringe could reduce dose-preparation steps and support emergency use, but compatibility, extractables and leachables, sterility, container closure integrity and syringe-device requirements must be established.

Does methylergonovine maleate require a preservative?

Not necessarily. The requirement depends on whether the product is single-dose or multidose, the container configuration and the approved formulation. A preservative-free single-dose product may provide a stronger hospital positioning.

Which excipient is most important for methylergonovine tablet performance?

No single excipient controls performance. The critical variables are the diluent system, particle-size distribution, disintegrant level, lubricant concentration and blending process because the active dose is very low.

Can a new methylergonovine maleate formulation receive patent protection?

Yes, if it contains a novel and non-obvious formulation, process, device or packaging configuration that produces a defensible technical result. Routine excipient substitution without unexpected performance is unlikely to support a strong patent.

References

1. U.S. Food and Drug Administration. (n.d.). Methergine (methylergonovine maleate) tablets: Prescribing information. DailyMed.

2. U.S. Food and Drug Administration. (n.d.). Methylergonovine maleate injection: Prescribing information. DailyMed.

3. U.S. Pharmacopeial Convention. (n.d.). Methylergonovine maleate monograph. United States Pharmacopeia and National Formulary.

4. U.S. Food and Drug Administration. (n.d.). Inactive ingredient database. FDA.

5. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations. Orange Book.

6. American College of Obstetricians and Gynecologists. (2017). Practice bulletin no. 183: Postpartum hemorrhage. Obstetrics & Gynecology, 130(4), e168-e186.

7. U.S. Congress. (2024). Federal Food, Drug, and Cosmetic Act, 21 U.S.C. §355(j).