Development of Dissolution Test Method for Drotaverine Hydrochloride/Mefenamic Acid Combination Using Derivative Spectrophotometry

Anumolu, Panikumar Durga; Gurrala, Sunitha; Yeradesi, Venkat Raju; Puvvadi, Sathesh Babu R; Chavali, Subrahmanyam Vs

doi:10.4314/tjpr.v12i2.15

Cited by 4 publications

(5 citation statements)

References 9 publications

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“…Other alternative which is also possible to be applied is by using surfactant which can increase the solubility of the drug significantly in physiological pH range, such as cetyl-trimethylammonium-bromide (CTAB) or cetrimide. Some studies have found that the addition of cetrimide could raise the solubility and dissolution rate of mefenamic acid to a far higher extent than those resulted by other surfactants, such as Tween 80 and SLS [ 12 , 13 ]. A study showed that the use of 1% CTAB in 900 mL of phosphate buffer at pH 6.8 could result in more than 80% mefenamic acid release from the 500-mg caplet after 30 min of dissolution time [ 13 ].…”

Section: Resultsmentioning

confidence: 99%

Dissolution Profile of Mefenamic Acid Solid Dosage Forms in Two Compendial and Biorelevant (FaSSIF) Media

2016

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Mefenamic acid is a non-steroidal anti-inflammatory drug (NSAID) that is widely used for the treatment of mild-to-moderate pain. Mefenamic acid belongs to the Biopharmaceutical Classification System (BCS) class II drug which has lower water solubility but high permeability. There are two different compendial methods available for dissolution tests of mefenamic acid solid dosage forms, i.e. methods of United States Pharmacopeia 37 (USP) and Pharmacopoeia of the People’s Republic of China 2010 (PPRC). Indonesian Pharmacopeia V ed. (FI) adopted the USP method. On the other hand, many researches focused on the use of a ‘biorelevant’ medium to develop the dissolution test method. The aim of this research was to study the dissolution profile of mefenamic acid from its solid dosage forms (caplet and capsule) available in the Indonesian market with three different dissolution medium: USP, PPRC, and biorelevant fasted simulated small intestinal fluid (FaSSIF) media. The tested products consisted of the innovator’s product (available only in caplet dosage form, FN caplet) and generic products (available as caplet and capsule). The dissolution test of the drug products in all dissolution media was performed in 900 mL of medium using apparatus II (paddle) at a temperature of 37°C and rotation speed of 75 rpm, except for the capsule product and for USP medium, both of which tests were done using apparatus I (basket) with rotation speed of 100 rpm. The solubility test of mefenamic acid was carried out in all media at temperature of 37°C. The result obtained from the solubility test showed that the the highest solubility of mefenamic acid was obtained in USP medium (approximately 2 mg/mL), followed by PPRC medium (about 0.5 mg/mL), and FaSSIF medium (approximately 0.06 mg/ml). In the dissolution test, percentage of drug dissolved in in the USP and PPRC media after 45 min for all products reached more than 75%, except for the PN caplet in USP medium which reached only about 44%. Meanwhile, in the biorelevant medium, the percentage of drug dissolved for all products did not exceed 16%. In all dissolution media, the capsule dosage form achieved the highest dissolution rate.

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Section: Resultsmentioning

confidence: 99%

Dissolution Profile of Mefenamic Acid Solid Dosage Forms in Two Compendial and Biorelevant (FaSSIF) Media

2016

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“…They belong to the class of non-steroidal anti-inflammatory drugs (NSAIDs), work by inhibiting the body’s production of prostaglandin, and are competitive inhibitors of cyclooxygenase (COX1 and COX2) [ 10 ]. Drotaverine Hydrochloride 1-(3, 4-diethoxybenzylidene)-6,7-methoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride ( Figure 1 c) is an antispasmodic agent structurally related to papaverine [ 11 , 12 ], being a selective inhibitor of phosphodiesterase 4, with no anticholinergic effects. Recent studies on the action of this active substance on human cancer cell lines show that drotaverine can be used as a cytostatic agent, in addition to its normal use [ 13 ].…”

Section: Introductionmentioning

confidence: 99%

“…Among the most commonly used active pharmaceutical ingredients with analgesic action is Ibuprofen (Ibu), while Drotaverine Hydrochloride (D-HCl) is employed for the antispasmodic effect. A binary system of active pharmaceutical substances with antispasmodic and analgesic action is Drotaverine Hydrochloride and Mefenamic acid mixture that is indicated for the symptomatic treatment of spasmodic dysmenorrhea, colic pains (including ureteric), biliary and intestinal colic [ 11 , 12 ].…”

Section: Introductionmentioning

confidence: 99%

Compatibility of Drotaverine Hydrochloride with Ibuprofen and Ketoprofen Nonsteroidal Anti-Inflammatory Drugs Mixtures

et al. 2022

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Formulations with two or more active pharmaceutical ingredients (APIs) are a researched trend due to their convenient use compared with multiple medications. Moreover, drug-drug combinations may have a synergistic effect. Drotaverine hydrochloride (D-HCl) is commonly used for its antispasmodic action. The combination of a spasmolytic and an analgesic drug such as ibuprofen (Ibu) or ketoprofen (Ket) could become the answer for the treatment of localized pain. D-HCl:Ibu and D-HCl:Ket drug-drug interactions leading to the formation of eutectic compositions with increased bioavailability, obtained by mechanosynthesis, a green, solvent-free method was explored for the first time. The compatibility of Ibuprofen, Ketoprofen, and Drotaverine Hydrochloride was investigated using differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-Transform Infrared spectroscopy (FTIR). Solid-liquid equilibrium (SLE) phase diagrams for the binary systems of active pharmaceutical ingredients were developed and the Tammann diagrams were designed to determine the eutectic compositions. The excess thermodynamic functions GE for the pre-, post-, and eutectic compositions were obtained using the computed activity coefficients data. Results show that drotaverine-based pharmaceutical forms for pain treatment may be obtained at 0.9 respectively 0.8 molar fractions of ibuprofen and ketoprofen which is advantageous because the maximum allowed daily dose of Ibu is about 6 times higher than those of D-HCl and Ket. The obtained eutectics may be a viable option for the treatment of pain associated with cancer therapy.

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“…range of analytical techniques, viz UV spectrophotometry 9,10 , spectrofluorimetry 11,12 , HPLC [13][14][15] , HPTLC 16 , and electrochemistry 17 .…”

mentioning

confidence: 99%

Green fluorometric strategy for simultaneous determination of the antihypertensive drug telmisartan (A tentative therapeutic for COVID-19) with Nebivolol in human plasma

Salim

Radwan

Hadad

et al. 2023

Sci Rep

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Telmisartan (TEL) and Nebivolol (NEB) are frequently co-formulated in a single dosage form that is frequently prescribed for the treatment of hypertension, moreover, telmisartan is currently proposed to be used to treat COVID19-induced lung inflammation. Green rapid, simple, and sensitive synchronous spectrofluorimetric techniques for simultaneous estimation of TEL and NEB in their co-formulated pharmaceutical preparations and human plasma were developed and validated. Synchronous fluorescence intensity at 335 nm was used for TEL determination (Method I). For the mixture, the first derivative synchronous peak amplitudes (D1) at 296.3 and 320.5 nm were used for simultaneous estimation of NEB and TEL, respectively (Method II). The calibration plots were rectilinear over the concentration ranges of 30–550 ng/mL, and 50–800 ng/mL for NEB and TEL, respectively. The high sensitivity of the developed methods allowed for their analysis in human plasma samples. NEB`s Quantum yield was estimated by applying the single-point method. The greenness of the proposed approaches was evaluated using the Eco-scale, National Environmental Method Index (NEMI), and Green Analytical Procedure Index (GAPI) methods.

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Development of Dissolution Test Method for Drotaverine Hydrochloride/Mefenamic Acid Combination Using Derivative Spectrophotometry

Abstract: Purpose: To develop and validate a dissolution test method for tablets containing 80 mg of drotaverine hydrochloride (DRT) and 250 mg of mefenamic acid (MEF DRT and MEF combination tablets.

Cited by 4 publications

References 9 publications

Dissolution Profile of Mefenamic Acid Solid Dosage Forms in Two Compendial and Biorelevant (FaSSIF) Media

Dissolution Profile of Mefenamic Acid Solid Dosage Forms in Two Compendial and Biorelevant (FaSSIF) Media

Compatibility of Drotaverine Hydrochloride with Ibuprofen and Ketoprofen Nonsteroidal Anti-Inflammatory Drugs Mixtures

Green fluorometric strategy for simultaneous determination of the antihypertensive drug telmisartan (A tentative therapeutic for COVID-19) with Nebivolol in human plasma

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