A study of in-vitro interaction of Ketotifen Fumarate with Domperidone at different gastric and intestinal pH

Aktar, Sayeed Mohammad; Mohammed, Farhad Fuad; Tareq, Syed Mohammed; Ikram,; Nurul, Islam Md.; Alam, Siddique Saiful; Dipesh, Das

doi:10.15275/rusomj.2014.0204

Cited by 3 publications

(3 citation statements)

References 11 publications

(9 reference statements)

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“…10 patches were taken, and each one was put in 100 ml distilled water at the volumetric flask, and stirred with ultrasound to extract the drug. The content was filtered through a Whatman filter paper, and filtrate was examined for the drug content against the reference solution containing placebo patches with the ultraviolet spectrophotometer at 303 nm [16] and average was calculated.…”

Section: Content Uniformity [15]mentioning

confidence: 99%

Formulation and Evaluation in Vitro a Matrix Type of Ketotifen Fumarate Transdermal Patches for Allergic Diseases

Hamdan

Husian

2017

Asian J Pharm Clin Res

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Objective: Transdermal patches of Ketotifen fumarate (KT) were developed for prolonged effect of the drug, and to protect the patient from allergic symptoms associated with asthma and other allergic diseases.Methods: Matrix type patches were prepared by solvent casting technique using different types of polymers: Hydroxy propyl methyl cellulose (HPMC K15M) and ethyl cellulose to formed the matrix of the patch in different ratios, emulsifying agents were added as a penetration enhancers (Span 60, Tween 60, Cremophor EL) in a ratio 0.025% w/v to the matrix, 10% v/v of glycerin was added as plasticizer to 10 ml of chloroform:methanol (1:1). The drug matrix film was casted on a polyvinyl alcohol backing membrane. All patches were evaluated for physical proprieties, thickness uniformity, folding endurance, moisture uptake, moisture content, drug content, uniformity of weight, content uniformity, in vitro drug release, and kinetic models. Differential scanning calorimetry was used to characterize physical mixtures of KT and the different used excipients. Results:The results showed that the prepared patches had acceptable physical properties. The drug substance was released well. Adding the penetration enhancers delayed the release of the drug from the matrix in all the prepared formulas, formula A2 that having no enhancer, showed maximum amounts of drugs release (90.06±0.9)% for 24 hrs. However, adding penetration enhancers decreased the amount of the drug release, formula B2 having Tween 60 as a penetration enhancer, showed the maximum release of the drug (87.78±0.88)%, and formula B3 having Cremophor EL showed the minimum release of the drug (79.13±1.58) at the end of 24 hrs dissolution study. The release of the drug from all formulations was followed by Korsmeyer-Peppas pattern with n>0.45 indicating that drug release from matrix was mainly happened by swallowed and diffusion (nonFickian pattern). Conclusion:Optimized formula A2 containing the maximum amounts of HPMC K15M showed a controlled release of the drug over 12 hrs, and it identified as a successful formulation for this study.

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Section: Content Uniformity [15]mentioning

confidence: 99%

Formulation and Evaluation in Vitro a Matrix Type of Ketotifen Fumarate Transdermal Patches for Allergic Diseases

Hamdan

Husian

2017

Asian J Pharm Clin Res

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“…Ketotifen (KT) is one of antiallergic agents which belong to the long term preventive medication of asthma as it is the second generation H 1 -antihistamine drugs [1] KT recommended dose is 2 mg/day divided into two doses [2]. KT is sparingly soluble in water 15.3 mg/L at 25 °C [3], which limits its dissolution prior to its absorption and hence could limit its bioavailability upon administration.…”

Section: Introductionmentioning

confidence: 99%

Preparation and evaluation of Ketotifen suppositories

Mohamed

Mahmoud

Mohamed

2020

Journal of advanced Biomedical and Pharmaceutical Sciences

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Ketotifen KT is one of antiallergic drugs, due to its first pass effect, the bioavailability of the drug is only 50 %. The objective of this study was to formulate and evaluate suppositories containing KT a n d / o r K T s o l i d d i s p e r s i o n. The in-vitro release of KT from suppositories was done using dialysis membrane method in phosphate buffer at pH 7.4. The release of KT from water soluble suppository bases was higher than that from fatty or emulsion suppositories bases. Among all PEGs bases (F4: PEG 6000: PG (20: 80)) showed a relatively higher release of KT. Formulations prepared with glycerin bases gave more or less identical release pattern; relatively formula (F17: Gelatin: Glycerin: Propylene glycol: Water) gave the highest release pattern. Formula (F20: Suppocire AM) exhibited the highest release rate among fatty bases. Within all emulsion bases (F23: W 15 : W 75 : Tween 20: Span 60: PEG 1500: Propylene glycol) showed highest release rate. KT solid dispersion led to a higher release rate of the drug from selected bases. A histological comparison between control group of rabbits (didn`t take suppository), another group took plain suppositories and group that received suppositories containing solid dispersion of KT was carried out. The tested plain and medicated bases didn't injure the rectal mucosa of rabbits. In conclusion the incorporation of solid dispersion in formula (F4) complied with the pharmacobeial limits for hardness, dissolution time, content uniformity and weight variation. Also it showed a relatively higher invitro release of KT and considered as safe and useful formulation for clinical use.

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“…Ketotifen is a widely used antiallergy drug with a variety of biological effects, including the inhibition of the release of myotonic mediators, leukotrienes in particular; the inhibition of slow reacting substances-induced bronchoconstriction in-vivo, calcium antagonistic properties, and the prevention or reversal of decreased beta-adrenoceptor sensitivity 26 . Ketotifen belongs to the secondgeneration H1-antihistamine drugs 27 .…”

Section: Introductionmentioning

confidence: 99%

Solubility and Dissolution Enhancement of Ketotifen by Solid Dispersion Technique

Mohamed

Mahmoud

2015

Bulletin of Pharmaceutical Sciences. Assiut

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Polyethylene glycol 4000 (PEG 4000). The saturation solubility and in-vitro dissolution studies showed remarkable improvement in solubility and drug dissolution of these new solid dispersions and physical mixtures over pure ketotifen. The XRD, DSC, IR and SEM studies indicated the transformation of crystalline ketotifen (in pure drug) to amorphous ketotifen (in solid dispersions). This study concluded that the improved solubility as well as drug dissolution of these new ketotifen solid dispersions may be attributed to improved wettability and reduction in drug crystallinity, which can be modulated by appropriate level of hydrophilic carriers.

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A study of in-vitro interaction of Ketotifen Fumarate with Domperidone at different gastric and intestinal pH

Cited by 3 publications

References 11 publications

Formulation and Evaluation in Vitro a Matrix Type of Ketotifen Fumarate Transdermal Patches for Allergic Diseases

Formulation and Evaluation in Vitro a Matrix Type of Ketotifen Fumarate Transdermal Patches for Allergic Diseases

Preparation and evaluation of Ketotifen suppositories

Solubility and Dissolution Enhancement of Ketotifen by Solid Dispersion Technique

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