Each 10mg filmcoated montelukast sodium tablet, usp contains 10. Aug 02, 2018 montelukast sodium usp is a hygroscopic, optically active, white or almost white powder. Montelukast sodium, the active ingredient in singulair, is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene cyslt 1 receptor. Because there is no existing usp min % % monograph for this drug substance, a new monograph, based on validated methods of analysis, is being proposed. Montelukast sodium united states pharmacopeia usp reference. Mar 06, 2020 montelukast sodium pharmacokinetics absorption bioavailability. Simulation of in vitro dissolution behavior using dddplus. In vitro drug release of montelukast sodium chewable tablets was determined using usp. Sep 12, 2019 singulair montelukast sodium tablets and oral granules. 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 tablets contain montelukast sodium detector. 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. Montelukast sodium oral tablet 10mg drug medication dosage. Usp specification that not more than 2 tablets are. Medicines monographs 5 expert committee has revised the montelukast sodium tablets monograph. Computer simulations were performed using gastroplus. Montelukast sodium usp is a hygroscopic, optically active, white or almost white powder. 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 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. Published montelukast dissolution data was used for the simulations. Stability indicating assay method for montelukast sodium. Safety data sheet creation date 24apr2014 revision date 23jan2018 revision number 5 1. Triple distilled water, methanol, acetronitrile, tri ethyl amine loba chemicals used were of hplc grade. Montelukast has been shown to cross the placental barrier and is excreted in breast milk of animals. Montelukast sodium is a hygroscopic, optically active, white to offwhite powder. Draft guidance on montelukast sodium this draft guidance, once finalized, will represent the food and drug administration s fdas current thinking. No this sds was prepared in accordance with 29 cfr 1910.
Montelukast sodium pharmacokinetics absorption bioavailability. The proposed method was validated as per the ich and usp guidelines. Montelukast sodium pharmaceutical secondary standard. In two similarly designed, 12week placebocontrolled clinical studies, the only adverse experiences reported as drugrelated in. The dissolution behaviour of montelukast sodium 10 mg film coated tablets was studied using. Pdf preparation and evaluation of montelukast sodium chewable. Prapomontelukast montelukast sodium tablets usp 10 mg montelukast sodium chewable tablets usp 4 mg and 5 mg leukotriene receptor antagonist apotex inc. This material is provided for educational purposes only and is not intended for medical advice, diagnosis or treatment. 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. L6301,l6304,l6307,l6310,l6325,l6328,l6331 as a consequence, the agent can elicit. Ac456440000, ac456440010 casno 151767021 synonyms no information available recommended use laboratory chemicals. 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. L6301,l6304,l6307,l6310,l6325,l6328,l6331 as a consequence, the agent can. Nov 04, 2008 during the process development of montelukast sodium, four impurities were observed in the range of 0.
Singulair montelukast sodium tablets, chewable tablets, and oral. These secondary standards are qualified as certified reference materials. 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. The montelukast sodium chewable tablets revision bulletin supersedes the monograph becoming official in. Listing a study does not mean it has been evaluated by. Volume iii, 2017, the united states pharmacopeial convention, rockville, md, usa, pp. Montelukast sodium, the active ingredient in singulair, is a selective and orally. 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. Sample solution montelukast sodium contains nlt 98. Osmotically controlled pulsatile release capsule of. For allergic rhinitis it is a second line treatment. Biorelevant dissolution media bdm prepared using bile salts and lecithin in. Montelukast, sold under the trade name singulair among others, is a medication used in the maintenance treatment of asthma. Montelukast sodium 151767021 451446859 cymit quimica s.
Estimated delivery in united states, on tuesday 19 may 2020. 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. The esi mass spectrum of montelukast sodium was studied on 400q trap lcmsms system. 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, sold under the brand name singulair among others, is a medication used in the maintenance treatment of asthma.
In two similarly designed, 12week placebocontrolled clinical. 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. Usp is not responsible for the accuracy or completeness of the information furnished. 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. Each packet of montelukast sodium oral granules usp 4 mg contains 4. Each packet of singulair 4mg oral granules contains 4.
Listing a study does not mean it has been evaluated by the u. During the process development of montelukast sodium, four impurities were observed in the range of 0. This chromatogram is provided for information only as an aid to analysts and intended as guidance for the interpretation and application of bp monographs. Method development and validation for related substances. Study of degradation behaviour of montelukast sodium and. Oxygenation of organic sulfides catalyzed by simple feiii salts. Montelukast sodium tablets type of posting revision bulletin. Coumadin crystalline warfarin sodium is an anticoagulant which acts by inhibiting vitamin kdependent coagulation factors. Montelukast sodium is a drug of choice in treatment of asthma and allergic rhinitis. Jan 04, 2020 each 10mg filmcoated montelukast sodium tablet, usp contains 10. Published montelukast sodium and glyburide dissolution data was used for the simulations. Bioequivalence study of montelukast sodium oral granules.
Combination tablet formulation containing montelukast sodium equivalent to montelukast 10 mg and fexofenadine hydrochloride 10 mg was procured from local pharmacy. Montelukast dicyclohexylamine 150 mg supporting information. Montelukast sodium, hplc and validation introduction montelukast sodium fig 1 is chemically re1. Montelukast sodium usp is soluble in ethanol, methanol, and water and practically insoluble in acetonitrile. Identification, synthesis, isolation and spectral characterization of potential impurities of montelukast sodium. Montelukast sodium api manufacturers suppliers drug. Montelukast mon te loo kast is used to prevent and treat the symptoms of asthma. The sample is introduced through hplc system by bypassing the column. Identification rs in diluent adjust with ammonium hydroxide to a ph of 5. The method was found linear over the range of 515 g per ml. Firstaid measures section 4, firstaid measures general eye contact.
Method development and validation for the simultaneous. Stability indicating assay method for montelukast sodium in. Do not prescribe singulair to treat an acute asthma attack. Dissolution testing is a performance test for many dosage forms including tablets and capsules. The revision bulletin will be incorporated in the first supplement to usp 40nf 35. 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. Other side effects not listed may also occur in some patients. The montelukast sodium oral granules revision bulletin supersedes the currently official monograph. Montelukast sodium is freely soluble in ethanol, methanol, and water and practically insoluble in acetonitrile. In the present work fast dissolving tablets of montelukast sodium were prepared using. Montelukast sodium mks was obtained as gift sample from the lupin limited pune, india.
Dynamic dissolution testing to establish in vitroin vivo. 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. Montelukast sodium tablets type of posting revision. 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. Pdf dynamic dissolution testing to establish in vitroin. Oral tablet 10mg cvs pharmacy patient statistics 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. 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. Empirical formula hill notation c 35 h 35 clno 3 sna. Singulair monograph pdf singulair montelukast as montelukast sodium. Dosing time may be individualized to patient needs. Draft guidance on montelukast sodium this draft guidance, once finalized, will represent the food and drug administration s fdas current thinking on this topic. Singulair is a leukotriene receptor antagonist indicated for.
Dynamic dissolution testing to establish in vitro in. Should you have any questions, please contact mary p. Montelukast sodium united states pharmacopeia usp reference standard. Identification product name montelukast sodium cat no. Other uses include allergic rhinitis and hives of long duration. Typical chromatogram for solution 3 in the related substances test and assay for montelukast. If the suffix psy, narc or drug precursor, or motbiotox appears, export authorizations are mandatory in. Bioequivalence study of montelukast sodium oral granules 4mg. Burning, crawling, itching, numbness, prickling, pins and needles, or tingling feelings. In vitro tests were performed in the usp apparatus ii paddle at 37 0. List of united states pharmacopoeia usp analytical reference standards of montelukast sodium and related impurities. Montelukast sodium chewable tablets type of posting. Formulation and evaluation of montelukast sodium fast dissolving. 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 has been evaluated for safety in approximately 2600 adult patients 15 years of age and older in clinical studies. Flush with water while holding eyelids open for at least 15 minutes. 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. The montelukast sodium tablets revision bulletin supersedes the monograph becoming official in usp 39nf 34. 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. Usp certificates and valid use dates for previous lots view harmonized system hs code. Dynamic dissolution testing to establish in vitro in vivo. It is generally less preferred for this use than inhaled corticosteroids. Data sources include ibm watson micromedex updated 4 may 2020, cerner multum updated 4 may. Should you haveany questions, please contact gerald hsu, ph. 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. 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.
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