The esi mass spectrum of montelukast sodium was studied on 400q trap lcmsms system. Montelukast sodium chewable tablets type of posting. Montelukast sodium is a drug of choice in treatment of asthma and allergic rhinitis. Dosing time may be individualized to patient needs. For allergic rhinitis it is a second line treatment. Montelukast sodium pharmacokinetics absorption bioavailability. Triple distilled water, methanol, acetronitrile, tri ethyl amine loba chemicals used were of hplc grade. Montelukast sodium, hplc and validation introduction montelukast sodium fig 1 is chemically re1. The method was found linear over the range of 515 g per ml. Pdf preparation and evaluation of montelukast sodium chewable. Montelukast sodium may be used as a pharmaceutical reference standard for the determination of the analyte in bulk drug and pharmaceutical formulations by chromatography and spectrophotometric techniques. Formulation and evaluation of montelukast sodium fast dissolving.
Sep 24, 2012 bioequivalence study of montelukast sodium oral granules 4mg under fasting condition the safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Should you have any questions, please contact mary p. Other side effects not listed may also occur in some patients. Dynamic dissolution testing to establish in vitro in. Listing a study does not mean it has been evaluated by the u. Montelukast, sold under the brand name singulair among others, is a medication used in the maintenance treatment of asthma. Medicines monographs 5 expert committee has revised the montelukast sodium tablets monograph. L6301,l6304,l6307,l6310,l6325,l6328,l6331 as a consequence, the agent can elicit. Montelukast sodium united states pharmacopeia usp reference standard. Montelukast sodium is a hygroscopic, optically active, white to offwhite powder.
Montelukast sodium pharmaceutical secondary standard. Stability indicating assay method for montelukast sodium. Read the patient information leaflet if available from your pharmacist before you start taking montelukast and each time you get a refill. In the present work fast dissolving tablets of montelukast sodium were prepared using novel coprocessed superdisintegrants consisting of crospovidone and sodium starch glycolate in the different ratios 1. Identification product name montelukast sodium cat no. Each packet of montelukast sodium oral granules usp 4 mg contains 4. Dissolution testing is a performance test for many dosage forms including tablets and capsules. Flush with water while holding eyelids open for at least 15 minutes. The dissolution behaviour of montelukast sodium 10 mg film coated tablets was studied using the flowthrough cell dissolution method following a dynamic ph change protocol, as well as in the usp apparatus 2. Prapomontelukast montelukast sodium tablets usp 10 mg montelukast sodium chewable tablets usp 4 mg and 5 mg leukotriene receptor antagonist apotex inc. Listing a study does not mean it has been evaluated by. The objectives of the study was to develop a dissolution test method that can be used to predict the oral absorption of montelukast sodium, and to establish an in vitroin vivo correlation ivivc using computer simulations.
Bioequivalence study of montelukast sodium oral granules 4mg. Montelukast sodium, the active ingredient in singulair, is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene cyslt 1 receptor. Montelukast is an orally available leukotriene receptor antagonist which is widely used for the prophylaxis and chronic treatment of asthma and has been linked to rare cases of clinically apparent liver injury. This dose is equivalent to 25,000 times the recommended daily adult human dose based on an adult patient weight of 50 kg.
Montelukast sodium oral tablet 10mg drug medication dosage. Draft guidance on montelukast sodium this draft guidance, once finalized, will represent the food and drug administration s fdas current thinking on this topic. Sample solution montelukast sodium contains nlt 98. Montelukast sodium mks was obtained as gift sample from the lupin limited pune, india. Combination tablet formulation containing montelukast sodium equivalent to montelukast 10 mg and fexofenadine hydrochloride 10 mg was procured from local pharmacy. Study of degradation behaviour of montelukast sodium and. Montelukast sodium united states pharmacopeia usp reference. Do not prescribe singulair to treat an acute asthma attack.
Data sources include ibm watson micromedex updated 4 may 2020, cerner multum updated 4 may. Singulair is a leukotriene receptor antagonist indicated for. Identification rs in diluent adjust with ammonium hydroxide to a ph of 5. Other uses include allergic rhinitis and hives of long duration. Identification, synthesis, isolation and spectral characterization of potential impurities of montelukast sodium. Montelukast sodium tablets contain montelukast sodium detector.
Usp is not responsible for the accuracy or completeness of the information furnished. Stability indicating assay method for montelukast sodium in. No deaths occurred following a single oral administration of montelukast sodium at doses up to 5000 mgkg in mice and rats 15,000 mgm 2 and 30,000 mgm 2 in mice and rats, respectively the maximum dose. List of united states pharmacopoeia usp analytical reference standards of montelukast sodium and related impurities. Ac456440000, ac456440010 casno 151767021 synonyms no information available recommended use laboratory chemicals.
During the process development of montelukast sodium, three polar impurities and one nonpolar impurity with respect to montelukast sodium were detected by simple reverse phase highperformance liquid chromatography hplc. No deaths occurred following a single oral administration of montelukast sodium at doses up to 5000 mgkg in mice and rats 15,000 mgm 2 and 30,000 mgm 2 in mice and rats, respectively the maximum dose tested. If the suffix psy, narc or drug precursor, or motbiotox appears, export authorizations are mandatory in. The montelukast sodium tablets revision bulletin supersedes the monograph becoming official in usp 39nf 34. In two similarly designed, 12week placebocontrolled clinical. The authors of this trial concluded that montelukast exerts an increased action at night, either because of higher plasma concentration at the moment of the challenge test, or because of antiinflammatory effect during the first hours of the morning, or both. The objective of this study was to evaluate if computer simulations can predict the in vitro dissolution of two model drugs for which different dissolution data were available. Montelukast sodium tablets type of posting revision. Singulair monograph pdf singulair montelukast as montelukast sodium. Montelukast sodium, the active ingredient in singulair, is a selective and orally. Oral tablet 10mg cvs pharmacy patient statistics for montelukast sodium. Biorelevant dissolution media bdm prepared using bile salts and lecithin in. Montelukast mon te loo kast is used to prevent and treat the symptoms of asthma. The dissolution behaviour of montelukast sodium 10 mg film coated tablets was studied using.
Oxygenation of organic sulfides catalyzed by simple feiii salts. Usp certificates and valid use dates for previous lots view harmonized system hs code. Usp specification that not more than 2 tablets are. Bioequivalence study of montelukast sodium oral granules 4mg under fasting condition the safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Jun 17, 2008 the objectives of the study was to develop a dissolution test method that can be used to predict the oral absorption of montelukast sodium, and to establish an in vitroin vivo correlation ivivc using computer simulations. Each 10mg filmcoated montelukast sodium tablet, usp contains 10.
Montelukast sodium tablets type of posting revision bulletin. Method development and validation for the simultaneous. Computer simulations were performed using gastroplus. Transfer one tablet equivalent to 10 mg of montelukast to a suitable volumetric flask, add 25% of the flask volume of water, and let stand for 510 min until the tablet has disintegrated. In the present work fast dissolving tablets of montelukast sodium were prepared using. Montelukast sodium usp is soluble in ethanol, methanol, and water and practically insoluble in acetonitrile.
No this sds was prepared in accordance with 29 cfr 1910. Published montelukast sodium and glyburide dissolution data was used for the simulations. Because there is no existing usp min % % monograph for this drug substance, a new monograph, based on validated methods of analysis, is being proposed. Published montelukast dissolution data was used for the simulations. In vitro tests were performed in the usp apparatus ii paddle at 37 0. Singulair montelukast sodium tablets, chewable tablets, and oral. Dynamic dissolution testing to establish in vitroin vivo. Information for the user montelukast 5 mg chewable tablets for children from 6 to 14 years read all of this leaflet carefully before you start giving this medicine to your child because it.
Montelukast sodium is freely soluble in ethanol, methanol, and water and practically insoluble in acetonitrile. The revision bulletin will be incorporated in the first supplement to usp 40nf 35. Mar 06, 2020 montelukast sodium pharmacokinetics absorption bioavailability. Montelukast, sold under the trade name singulair among others, is a medication used in the maintenance treatment of asthma. Jan 04, 2020 each 10mg filmcoated montelukast sodium tablet, usp contains 10. Montelukast sodium api manufacturers suppliers drug. Firstaid measures section 4, firstaid measures general eye contact. Montelukast dicyclohexylamine 150 mg supporting information. Uses advised against food, drug, pesticide or biocidal product use. Empirical formula hill notation c 35 h 35 clno 3 sna. Method development and validation for related substances.
In vitro drug release of montelukast sodium chewable tablets was determined using usp. Pdf dynamic dissolution testing to establish in vitroin. Montelukast has been shown to cross the placental barrier and is excreted in breast milk of animals. Dynamic dissolution testing to establish in vitro in vivo. It is generally less preferred for this use than inhaled corticosteroids. W is the weight, in mg, of clopidogrel in the portion of tablets used to prepare the test solution based on the labeled quantity of clopidogrel per tablet, tablet weight, and the weight of the portion of tablets used. Montelukast sodium has been evaluated for safety in approximately 2600 adult patients 15 years of age and older in clinical studies. During the process development of montelukast sodium, four impurities were observed in the range of 0. Should you haveany questions, please contact gerald hsu, ph.
Clinical trial adverse drug reactions adults 15 years of age and older with asthma montelukast sodium has been evaluated for safety in approximately 2600 adult patients 15 years of age and older in clinical studies. Montelukast sodium 151767021 451446859 cymit quimica s. Simulation of in vitro dissolution behavior using dddplus. Montelukast is a leukotriene receptor antagonist that demonstrates a marked affinity and selectivity to the cysteinyl leukotriene receptor type1 in preference to many other crucial airway receptors like the prostanoid, cholinergic, or betaadrenergic receptors. Osmotically controlled pulsatile release capsule of. Nov 04, 2008 during the process development of montelukast sodium, four impurities were observed in the range of 0. Method development and validation for related substances of. As per the general guidelines recommended by ich 4 to qualify the drug substance, the amount of acceptable level for a known and unknown related compound impurity.
Draft guidance on montelukast sodium this draft guidance, once finalized, will represent the food and drug administration s fdas current thinking. Estimated delivery in united states, on tuesday 19 may 2020. Montelukast sodium usp is a hygroscopic, optically active, white or almost white powder. The proposed method was validated as per the ich and usp guidelines. This chromatogram is provided for information only as an aid to analysts and intended as guidance for the interpretation and application of bp monographs. The montelukast sodium chewable tablets revision bulletin supersedes the monograph becoming official in. Cellulose acetate, sodium chloride and talc were obtained from loba chemie ltd. Bioequivalence study of montelukast sodium oral granules. Singulair montelukast dosing, indications, interactions. Burning, crawling, itching, numbness, prickling, pins and needles, or tingling feelings. Each packet of singulair 4mg oral granules contains 4. Volume iii, 2017, the united states pharmacopeial convention, rockville, md, usa, pp. This material is provided for educational purposes only and is not intended for medical advice, diagnosis or treatment. The montelukast sodium oral granules revision bulletin supersedes the currently official monograph.83 230 958 1261 920 1375 1386 720 160 199 623 949 258 387 68 335 1042 217 1572 262 1528 1484 27 530 336 868 1274 572 567 1499 257 187 1180 888 568 1092 1365 1175 1240 266 548 1201 1219 447 924 307 163 998