| HS Code | 914247 |
| Productname | Guaifenesin Propafenone Hydrochloride Pharma Grade API |
| Apicomponent1 | Guaifenesin |
| Apicomponent2 | Propafenone Hydrochloride |
| Pharmaceuticalgrade | Pharma Grade |
| Dosageforms | Tablet, Capsule, Granule, Injection |
| Routesofadministration | Oral, Injectable |
| Guaifenesincasnumber | 93-14-1 |
| Propafenonehydrochloridecasnumber | 34183-22-7 |
| Guaifenesinmolecularformula | C10H14O4 |
| Propafenonehydrochloridemolecularformula | C21H28ClNO3 |
| Guaifenesinmolecularweight | 198.22 g/mol |
| Propafenonehydrochloridemolecularweight | 377.9 g/mol |
| Guaifenesinappearance | White or almost white crystalline powder |
| Propafenonehydrochlorideappearance | White to off-white crystalline powder |
| Guaifenesinsolubility | Slightly soluble in water; soluble in ethanol, chloroform, glycerol |
| Propafenonehydrochloridesolubility | Soluble in water, ethanol, chloroform; slightly soluble in acetone |
| Guaifenesinmeltingpoint | 78-82 °C |
| Propafenonehydrochloridemeltingpoint | 171-174 °C |
| Guaifenesinpharmacologicalclass | Expectorant |
| Propafenonehydrochloridepharmacologicalclass | Antiarrhythmic (Class IC) |
| Guaifenesinmechanismofaction | Increases respiratory tract fluid secretion and reduces mucus viscosity |
| Propafenonehydrochloridemechanismofaction | Sodium channel blocker; slows cardiac conduction and prolongs refractory period |
| Guaifenesintherapeuticuse | Relief of productive cough |
| Propafenonehydrochloridetherapeuticuse | Treatment of ventricular and supraventricular arrhythmias |
| Purity | ≥99.0% (HPLC) |
| Assay | 98.0-102.0% (anhydrous basis) |
| Qualitystandard | USP/EP/BP/IP |
| Packaging | 25 kg fiber drum with double polyethylene bags |
| Storageconditions | Store in a cool, dry, well-ventilated area, protected from light and moisture |
| Shelflife | 2 years |
| Lossondrying | ≤0.5% |
| Heavymetals | ≤20 ppm |
| Residueonignition | ≤0.1% |
| Identification | IR, HPLC |
| Residualsolvents | Meets USP/EP limits |
| Odor | Odorless or almost odorless |
| Particlesize | 80 mesh |
| Bulkdensity | 0.4-0.7 g/mL |
As an accredited Guaifenesin Propafenone Hydrochloride Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable factory, we enforce strict quality protocols—every batch undergoes rigorous testing to ensure consistent efficacy and safety standards.
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Direct compression of high-dose guaifenesin is replaced by wet granulation when tablet weight exceeds 800 mg and Carr index of the dry blend exceeds 28%. In a 1200 mg extended-release guaifenesin tablet, guaifenesin pharma-grade API is pre-blended with hypromellose K100M at 15–30% w/w, microcrystalline cellulose at 5–20% w/w, and colloidal silicon dioxide at 0.25–0.75% w/w; the active fraction is 60–85% w/w of the dry granulate. Purified water is added as granulating fluid at 8–15% w/w in a high-shear granulator operating with impeller tip speed 5–8 m/s and chopper speed 1500–2500 rpm. Wet mass is screened through a 1.0–1.5 mm mesh and dried in a fluidised-bed dryer at inlet air temperature 55–70 °C to loss on drying 1.0–2.0%. The dried granulate is milled through a 0.8–1.0 mm screen and lubricated with magnesium stearate at 0.5–1.5% w/w for 2–4 min; longer lubrication shifts the 1 h dissolution interval by 5–10% through hydrophobic coating of hypromellose. Tableting is performed on a rotary press with precompression 3–6 kN, main compression 15–30 kN, and turret speed 30–60 rpm, targeting hardness 180–250 N and friability below 0.8% per USP <1216>. Compliance for this dosage form is anchored to USP <711> Apparatus 2 at 50 rpm with 900 mL water, USP <905> for uniformity of dosage units with acceptance value L1 ≤ 15, ICH Q3D for elemental impurities, and 21 CFR 210/211 for current good manufacturing practice. Terminal product types include 600 mg and 1200 mg 12-hour extended-release tablets for adult expectorant therapy; subdivision of the tablet is avoided because the hydrophilic matrix is not functionally scored.
For a low-dose propafenone hydrochloride formulation containing 150 mg active per tablet, the direct compression window is constrained by the blend’s tendency to segregate when the API mass fraction is below 20% w/w and by the low bulk density of milled propafenone hydrochloride crystals when the fraction is above 60% w/w. A pre-blend of propafenone hydrochloride with microcrystalline cellulose at 1:4 ratio is passed through a 0.5–0.8 mm screen before addition of lactose monohydrate, croscarmellose sodium 2–5% w/w, povidone K30 1–3% w/w, and magnesium stearate 0.5–1.0% w/w; total core weight is held between 300 mg and 600 mg, giving an active fraction of 25–50% w/w for the 150 mg strength. Compression is performed on a 16-station rotary tablet press with main compression 8–25 kN, precompression 2–5 kN, and turret speed 40–80 rpm; in-process controls record weight every 15 min, hardness 80–150 N, and disintegration time below 15 min per USP <701>. A film-coating step applies hypromellose-based coating at 2–4% w/w weight gain in a side-vented pan with inlet air 60–75 °C and pan speed 4–8 rpm. Dissolution testing uses USP <711> Apparatus 2 at 50 rpm in 900 mL 0.1 N HCl for immediate-release justification; additional quality bounds are provided by USP <905>, ICH Q3D, and the FDA 21 CFR 210/211 framework. Finished dosage forms include 150 mg, 225 mg, and 300 mg film-coated immediate-release tablets for ventricular and supraventricular arrhythmia management under prescription use.
Endpoint determination for a guaifenesin wet mass formulated with 70–90% w/w active, 2–5% w/w povidone K30, 3–8% w/w crospovidone, and 5–14% w/w water depends on power-consumption rise of 20–35% over dry-mix baseline at 300 rpm impeller speed in a 25 L high-shear granulator; Karl Fischer titration at the endpoint records 8–12% moisture. The endpoint is not defined by a fixed granulation time; impeller torque curves from a production-scale 10 L bowl show batch-to-batch shifts of ±3% moisture at the same water addition ratio when incoming guaifenesin particle size D50 varies from 40 µm to 90 µm. Over-wetting beyond 14% water produces dense granules with average particle size above 1200 µm and subsequent tablet hardness above 300 N, which delays drug release at the 2 h dissolution interval by 20–30% under USP <711> conditions. Drying in a fluidised-bed dryer is terminated at loss on drying 1.0–2.5%; milled granulate with particle size distribution between 75 µm and 850 µm is pressed into 600 mg guaifenesin tablets. Compliance anchors include USP <711> for dissolution, USP <905> for dosage unit uniformity, and ICH Q3D for elemental impurity risk assessment; USP <701> disintegration is applied to immediate-release granulate intermediates but not to modified-release tablets. Terminal product types include immediate-release 400 mg tablets, 600 mg extended-release tablets, and 200 mg capsulated granules.
In oral granule sachet production for single-dose guaifenesin delivery, fluidised-bed top-spray granulation with a 5% w/w povidone binder solution is preferred when the final sachet fill weight is below 2 g and the active dose is 50–200 mg per unit. The granulation substrate contains guaifenesin at 5–25% w/w, mannitol or sucrose at 50–85% w/w, sodium starch glycolate at 1–3% w/w, and a flavour/sweetener system at 0.5–2% w/w that is added after drying to avoid thermal degradation. Spraying is carried out at inlet air temperature 50–65 °C, product temperature 28–38 °C, atomising air pressure 1.5–2.5 bar, and spray rate 10–20 g/min per 1 kg charge; agglomeration is considered complete when tapped density reaches 0.55–0.75 g/mL and fines below 75 µm are below 15%. Final sachet filling is performed on a volumetric auger filler with fill weight accuracy ±5% and seal integrity verified at 30–50 kPa differential pressure. Dissolution of the reconstituted granules is assessed by USP <711> Apparatus 2 at 50 rpm in 900 mL water with a 10 mL sampling volume, while microbial limits follow USP <61> and USP <62>, and elemental impurities follow ICH Q3D. Terminal product types include single-dose oral granule sachets for adults and adolescents, and effervescent granule presentations where the base granulate is blended with anhydrous citric acid and sodium bicarbonate at a ratio of 1:2.5 before filling.
Aseptic processing of propafenone hydrochloride injection is carried out in a Grade A zone with unidirectional airflow at 0.45 m/s ± 20% when the bulk solution cannot be subjected to terminal sterilisation at 121 °C for 15 min because published data for the thermal degradation profile of this specific API under saturated steam are limited. The bulk solution for a 70 mg/20 mL presentation is prepared by dissolving propafenone hydrochloride to a concentration of 3.5 mg/mL in water for injection, adjusting pH to 3.5–5.0 with hydrochloric acid, and adding sodium chloride to achieve osmolality of 280–320 mOsm/kg. Sterile filtration through 0.22 µm PVDF membrane filters is validated to yield a log reduction value of at least 7 for Brevundimonas diminuta per ASTM F838-20; the filtrate is filled into 20 mL type I borosilicate glass ampoules under oxygen headspace below 2%. Container closure integrity is tested by dye ingress or vacuum decay with sensitivity to defects larger than 5 µm. Particulate matter for injections must meet USP <788> subvisible particulate matter thresholds, sterility is confirmed by USP <71> membrane filtration, and bacterial endotoxin is controlled to 0.50 EU/mg or tighter per USP <85>; elemental impurities follow ICH Q3D Option 1. The terminal product is a single-dose intravenous injection for administration after dilution in 5% dextrose or 0.9% sodium chloride to a final concentration of 0.5–2.0 mg/mL under electrocardiographic monitoring.
Powder bridging in the hopper of a dosator-type capsule filler at 40,000 capsules per hour is observed when the blended guaifenesin fraction contains more than 15% fines below 75 µm and the final blend Carr index exceeds 25%. For high-dose guaifenesin capsules, the active is fluid-bed granulated or slugged at 60–90% w/w with microcrystalline cellulose 5–20% w/w, croscarmellose sodium 2–5% w/w, and colloidal silicon dioxide 0.5–1.5% w/w; magnesium stearate is added at 0.5–1.25% w/w for 3–5 min to avoid dissolution suppression at later intervals. Capsules are filled into size 00 or 0 hard gelatin or HPMC capsules at fill weight 500–700 mg for 400 mg guaifenesin; fill weight variation is maintained below ±4% and shell moisture below 14% w/w to reduce brittleness. Dissolution of the capsule product is evaluated by USP <711> Apparatus 1 at 100 rpm in 900 mL water for immediate-release expectations; disintegration time is measured by USP <701> with disks at 37 °C and should be below 15 min for uncoated shells. Quality anchors are USP <905> for uniformity, USP <61>/<62> for microbial enumeration and specified organisms, and ICH Q3D for elemental impurities. Terminal product types include 200 mg and 400 mg immediate-release guaifenesin capsules for single-agent expectorant use; clinical protocols that combine guaifenesin with pseudoephedrine or dextromethorphan require separate blend validation because the basic alkaloid components alter powder surface pH and may accelerate shell crosslinking.
| Application segment | Standard/clause | Test condition | Typical boundary |
|---|---|---|---|
| Extended-release guaifenesin tablet | USP <711> Apparatus 2 | 50 rpm, 900 mL water | Product-specific dissolution profile, ≥80% at 8–12 h |
| Immediate-release propafenone hydrochloride tablet | USP <711> Apparatus 2 | 50 rpm, 900 mL 0.1 N HCl | Immediate release, ≥80% at 30–60 min |
| Oral granule sachet | USP <61>/<62> | Microbial enumeration | Total aerobic microbial count ≤10³ CFU/g, total yeast/mold count ≤10² CFU/g |
| Injectable propafenone hydrochloride | USP <71>, USP <85>, USP <788> | Sterility, endotoxin, subvisible particles | Sterile, endotoxin ≤0.50 EU/mg, particles ≤6000 per container ≥10 µm and ≤600 per container ≥25 µm |
| All oral dosage forms | ICH Q3D, USP <905> | Elemental impurity risk assessment; dosage unit uniformity | Acceptance value L1 ≤ 15; ICH Option 1 limits |
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The designation “Guaifenesin Propafenone Hydrochloride Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable” describes a dual-monograph active pharmaceutical ingredient portfolio. It contains guaifenesin (CAS 93-14-1, C10H14O4, molecular weight 198.22 g/mol) as an expectorant for oral tablet, capsule, and granule dosage forms, and propafenone hydrochloride (CAS 34183-22-7, C21H28ClNO3, molecular weight 377.91 g/mol) as a Class Ic antiarrhythmic for oral tablet, capsule, and injectable presentations. The model designation is vendor-specific and appears in the certificate of analysis and label; no harmonized pharmacopoeial model code exists. Route-specific sub-grades are distinguished by particle-size distribution, bulk density, residual solvent profile, elemental impurities, microbiological quality, and endotoxin limits. The materials are manufactured under ICH Q7 and 21 CFR 210/211 GMP conditions and are not interchangeable with technical-grade powders because release testing for related substances, clarity of solution, loss on drying, residue on ignition, residual solvents, and elemental impurities is mandatory.
Each monograph is supplied with a certificate of analysis referencing current USP, Ph.Eur., or equivalent monograph methods. For oral solid dosage forms, the assay acceptance range is 98.0% to 102.0% on the dried basis for both APIs. Identification is performed by infrared absorption and HPLC retention time; for propafenone hydrochloride, a chloride identification test is also applied. Related substances are controlled by liquid chromatography; unspecified impurities are commonly limited to ≤ 0.10% and total impurities to ≤ 0.5% in monograph-based applications, but the exact thresholds follow the current pharmacopoeial monograph and the approved drug product file. Residual solvents are limited by ICH Q3C; process-relevant solvents such as methanol and ethanol are controlled to class-specific concentration limits, with methanol at 3000 ppm and ethanol at 5000 ppm under standard ICH Q3C tables. Elemental impurities are controlled by ICH Q3D with oral and parenteral limits differentiated by route. Loss on drying is specified by the monograph; typical values are ≤ 0.5% w/w for both APIs when dried at 105 °C to constant weight, but the exact drying condition and limit are monograph-specific. Microbiological quality for oral grades is assessed by Ph.Eur. 5.1.4 or equivalent; injectable propafenone hydrochloride is additionally controlled for bacterial endotoxin.
| Parameter | Guaifenesin | Propafenone hydrochloride |
|---|---|---|
| CAS registry number | 93-14-1 | 34183-22-7 |
| Molecular formula | C10H14O4 | C21H28ClNO3 |
| Molecular weight | 198.22 g/mol | 377.91 g/mol |
| Assay, dried basis | 98.0–102.0% | 98.0–102.0% |
| Identification | IR absorption, HPLC retention time | IR absorption, chloride, HPLC retention time |
| Loss on drying | USP monograph limit | USP/Ph.Eur monograph limit |
| Residual solvents | ICH Q3C class-specific limits | |
| Elemental impurities | ICH Q3D oral limits | ICH Q3D oral/parenteral limits |
| Bacterial endotoxin | Not normally specified | USP <85> product-specific limit for injection |
Physicochemical and solid-state handling characteristics differ between the two APIs. Guaifenesin is a crystalline material that is moderately soluble in water and freely soluble in ethanol; propafenone hydrochloride is more water-soluble than propafenone base but can precipitate as the free base at elevated pH. Solid-state form is controlled by X-ray powder diffraction where the monograph or stability program requires it. For solid oral dosage forms, particle-size distribution is measured by laser diffraction according to USP <429> or Ph.Eur. 2.9.31; the D10, D50, and D90 values are agreed between the API manufacturer and the dosage-form developer. Direct compression grades typically require a D90 of ≤ 150 µm, bulk density 0.35–0.55 g/mL, and Hausner ratio ≤ 1.35; however, published data for this specific grade configuration is limited, and these values are verified in the quality agreement rather than assumed from general powder-property tables. Guaifenesin granules exposed to relative humidity above 60% may require pre-drying before encapsulation; this operational boundary is stated in the API supplier’s technical data package.
Propafenone hydrochloride is a Class Ic antiarrhythmic with common adult oral doses of 150 mg to 300 mg per tablet. Direct compression is limited by the high API fraction, moderate flow, and lubricant sensitivity. When the Hausner ratio exceeds 1.35, direct compression is usually replaced by roller compaction or wet granulation. Roller compaction with roll force 8–12 kN/cm and granulator screen size 0.8–1.25 mm retains compactibility while minimizing fines. Magnesium stearate is used at 0.5–1.0% w/w; concentrations above 1.5% w/w can extend disintegration beyond 30 min in propafenone HCl tablets when tested by USP <701>. Tablet friability is evaluated by USP <1216>; a common immediate-release target is ≤ 1.0%. Content uniformity of propafenone HCl tablets is assessed by USP <905> with an acceptance value ≤ 15. The API should not be granulated with strongly alkaline binders because free base precipitation reduces dissolution. Published data for this specific grade configuration is limited; therefore, development batches should evaluate blend uniformity, hardness–dissolution relationships, and moisture sensitivity on a case-by-case basis.
Guaifenesin is used in oral extended-release granules and capsules at doses from 600 mg to 1200 mg per day. Matrix-formulation work requires control of API particle size because dissolution from wax-matrix and hypromellose matrices is surface-area-dependent. Aqueous wet granulation in a fluid-bed granulator with inlet air temperature 60–75 °C and spray rate 10–30 g/min/kg is common in published development work; the exact process window depends on binder system, batch size, and humidity. Granule moisture after drying is typically controlled to 1.5–2.5% w/w, with final particle-size distribution passed through a 0.6–1.6 mm screen. Extended-release granules are encapsulated with fill weights verified by weight variation and content uniformity using USP <905>; dissolution testing follows USP <711> with the apparatus type documented in the approved product file. Guaifenesin is not directly compressible at high dose in all cases; when direct compression is used, pre-blending with a highly compressible diluent and matching excipient particle size reduce segregation. The API should be stored in a dry place because caking and flow deterioration can occur at elevated humidity; pre-drying is required when moisture exceeds the product specification.
Propafenone hydrochloride intended for injectable formulations is not supplied as a sterile API; the solution is sterile-filtered during manufacturing. The API is released with low bioburden, particulate matter, and bacterial endotoxin controls. Endotoxin limits are product-specific and are calculated from the maximum daily dose and route, with testing by USP <85> or Ph.Eur. 2.6.14. Water for injection used for dissolution must meet conductivity ≤ 1.3 µS/cm at 25 °C under USP <645>. The hydrochloride salt should not be combined with strongly alkaline buffers without pH control because propafenone free base precipitation can occur. Aseptic processing requires passage through a sterilizing-grade filter with nominal pore size 0.22 µm or smaller, with pre- and post-filtration integrity testing. Published data for this specific injectable configuration is limited; therefore, development batches should evaluate pH-dependent precipitation, filter compatibility, and oxygen sensitivity before scale-up. Oral and injectable sub-grades are not interchangeable; injectable-grade propafenone HCl requires lower bioburden and endotoxin levels than oral grade.
The product title combines two separate monographs in a single commercial listing; it does not describe a co-processed fixed-dose combination, a solid dispersion, or a co-crystal. This distinction matters for regulatory filing because a mixture of guaifenesin and propafenone hydrochloride has no pharmacopoeial monograph and no established clinical indication as a fixed-dose product. Each API is released against its own monograph; the two should be stored, sampled, and qualified independently. Blending them without a filed drug product application would create an unapproved fixed-dose combination and would require separate stability, dissolution, and bioavailability documentation. The table below summarizes differentiating attributes against technical-grade powders and single-API alternatives.
| Attribute | This pharmaceutical-grade line | Technical-grade or ungraded powder | Single-API alternative |
|---|---|---|---|
| Release testing | Pharmacopoeial monographs, ICH Q3C/Q3D, route-specific tests | Limited or absent | Monograph only |
| Route-specific controls | Oral and injectable sub-grades | No endotoxin/bioburden guarantee | May lack injectable sub-grade |
| Particle engineering | Particle size, bulk density, flow indices agreed in quality agreement | Uncontrolled | Single grade |
| Regulatory documentation | CEP/ASMF/DMF where applicable | Not available | Monograph only |
| Fixed-dose status | Two separate APIs listed together | Not applicable | Single API |
Compared with flecainide acetate, another Class Ic antiarrhythmic, propafenone hydrochloride has additional β-adrenoceptor blocking activity at therapeutic concentrations; this pharmacological difference requires separate bioequivalence and therapeutic equivalence documentation. Compared with amiodarone hydrochloride, propafenone HCl has a shorter half-life and does not require the same intensive thyroid, hepatic, or pulmonary monitoring; however, it carries proarrhythmic risk in patients with structural heart disease. Guaifenesin differs from bromhexine or acetylcysteine by acting as an expectorant through increased respiratory tract secretion volume and reduced sputum viscosity rather than by direct mucolytic disulfide bond cleavage. These differences do not imply interchangeability; substitution must follow a physician’s assessment and the relevant pharmacopoeial equivalence data.
Storage is in tightly closed containers at controlled room temperature. Stability studies for guaifenesin and propafenone hydrochloride follow ICH Q1A(R2); retest periods are justified by long-term and accelerated conditions. Propafenone hydrochloride should be protected from light and moisture; guaifenesin should be protected from high humidity to avoid caking. In-use handling for injectable grade requires immediate use after reconstitution unless formulation-specific stability data supports extended hold times. The APIs should not be blended together in a single container unless a specific drug product formulation and stability program exist.
