The Pharmacokinetic Characteristics of Sildenail Citrate Chewable Tablets Compared to Film-Coated Tablets in Healthy Male Subjects

Skip to main contentSkip to articleGraphical abstractIntroductionSection snippetsMaterialsPreparation of microcapsules containing SC and Eudragit® E100Preparation of SC microcapsulesConclusionAcknowledgementReferences (41)et al.Taste masking of diclofenac sodium using microencapsulationJournal of Microencapsulationet al.Spray drying of biopharmaceuticals: stability and process considerationsDrying TechnologyAsaka, T., Misawa, Y., Kashimura, M., Morimoto, S., Watantabe, Y., Hatayama, K., 1992.

A technology of sildenafil citrate and chewable tablets, which is applied in the directions of inactive medical preparations, pharmaceutical formulations, organic inactive ingredients, etc., can solve problems such as the way that patients are not taken, and achieve increased storage stability. , Increase shelf life, good reproducibility

2′-Modified erythromycin or…et al.Taste masking by spray-drying techniqueAAPS PharmSciTechet al.Paediatric and geriatric drug deliveryExpert Opinion on Drug DeliveryAnalytical profiles of drug substances and excipientset al.Pill swallowing by adults with dysphagiaArchives of Otolaryngology-Head & Neck Surgeryet al.Reference database of Raman spectra of pharmaceutical excipientsJournal of Raman SpectroscopyDepalmo, G.A., 1999. Composition based on ibuprofen, for oral usage. EP Patent…Orally disintegrating dosage forms and taste-masking technologies; 2010Expert Opinion on Drug DeliveryView full text Sildenafil citrate (SC) is a selective cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE-5) inhibitor that has been used extensively for treatment of erectile dysfunction (ED) in men (Ghofrani et al., 2006, Goldenberg, 1998, Moreland et al., 1999). In addition, pharmacological activity in promoting cGMP-mediated vascular smooth muscle relaxation, and it has been approved that the effectiveness of SC for treating pulmonary artery hypertension (PAH) (Galiè et al., 2005, Ghofrani et al., 2006, Michelakis et al., 2002). There is an unmet medical need for either an orally-disintegrating tablet (ODT), an orally-disintegrating film (ODF), or a chewable tablet formulation of SC for easy administration via instantaneous drug absorption for the purpose of treating ED, as well as an oral suspension appropriate for delivery of SC to neonates and elderly patients for treatment of PAH (Lee et al., 2012, Singh et al., 2009). However, the excessive bitter taste of SC is a critical hurdle for generating a palatable oral dosage form that can achieve appropriate patient compliance. The commercially-available form of SC, Viagra®, is a film-coated tablet. Tablet coating is popularly used to mask unpleasant tastes, but is not applicable to fast disintegrating formulations. For this reason, many studies have been performed to develop an efficient taste masking method suitable for orally-disintegrating systems. There have been several attempts to generate taste-masked dosage forms for SC by various means including formulation with flavorings (Singh et al., 2009, Winter and Scheiwe, 2010), coating granules with a sustained release polymer (Itoh and Niwa, 2001), and ionic bonding with acidic resins (Lee et al., 2012, Singh et al., 2009). However, the addition of flavorings and coating on granules requires a significant amount of excipient leading to a very large dosage, and thus may be improper for some drug formulations.

(2009) used ion exchange resin for direct modification of drugs, but did not perform a precise taste evaluation, relying instead on indirect methods, such as presuming from in vitro drug release test.

Enhancement of patient compliance is a primary consideration in the development of drug delivery systems. Accordingly, drugs that are administered orally are a major aspect of patient compliance compared with other routes of administration because of their non-invasiveness and convenience of self- medication. Thus, the taste of drug substances taken orally is a key factor when evaluating the organoleptic quality of drug dosage forms.

Thus, numerous studies have been conducted in an attempt to mask the unpleasant taste of pharmaceutical ingredients (Douroumis, 2011, Sohi et al., 2004).

Sildenafil Citrate Chewable Tablets USP 25mg Technical Specification:

Thus, the taste of drug substances taken orally is a key factor when evaluating the organoleptic quality of drug dosage forms. Thus, numerous studies have been conducted in an attempt to mask the unpleasant taste of pharmaceutical ingredients (Douroumis, 2011, Sohi et al., 2004). Various taste masking technologies have been developed including addition of flavorings or sweeteners (Depalmo, 1999, Wehling et al., 1993), formation of inclusion complexes with β-CD (Motola et al., 1991), bonding with ion exchange resins (Agarwal et al., 2000, Lee et al., 2012), coating or microencapsulating with water-insoluble polymers (Al-Omran et al., 2002, Gao et al., 2006, Jańczyk et al., 2010, Wehling et al., 1993, Yajima et al., 1996, Zgoulli et al., 1999), and modifying the chemical properties of drug substances (Asaka et al., 1992, Hussain et al., 1988). With the exception of addition of flavorings and sweeteners, taste masking is achieved primarily by minimizing direct contact between taste buds on the tongue and drug substances dissolved in the buccal cavity (Sohi et al., 2004). Microencapsulation is defined as the process of manufacturing small particles with sizes in the micrometer range, in which materials are coated with a solid matter or dispersed into a matrix.

Method used

Microencapsulation is distinguished from conventional granule coating methods by modification of the primary particle (Kirk-Othmer, 2005). For this reason, microencapsulation is used for producing orodispersible systems and oral suspensions, which are highly preferred by pediatric and geriatric patients (Breitkreutz and Boos, 2007) and are necessary for individuals who 20mg sildenafil have swallowing problems (Carnaby-Mann and Crary, 2005). Thus, such formulations require more attention to adequate masking of bitterness of active pharmaceutical ingredients (Ueda et al., 1993, Zgoulli et al., 1999). Use of pH-dependent gastro-soluble polymers as carriers can be employed for taste masking through microencapsulation, because liberation of the drug in the oral cavity is retarded by a polymer that is not degraded by saliva. Conversely, microcapsule particles dissolve completely in gastric juice, and thus there is no alteration of drug absorption in the GI tract (Al-Omran et al., 2002, Bora et al., 2008, Gao et al., 2006).

Arch Dis Child Fetal Neonatal Ed

In this study, we prepared solid dispersion particles consisting of SC and Eudragit® E100, a methacrylate polymer that dissolves below pH 5.0, by a spray drying method. Spray drying is widely employed in pharmaceutical research and industry to produce small particles of desirable sizes and has the advantages of being a one-step process and having straightforward scaling-up. Furthermore, the properties of solid dispersions, including their dissolution profiles, can be thoroughly analyzed and evaluated. In order to obtain quantitative data about taste, levels of bitterness between raw materials and modified particulate systems can be measured using an electronic tongue (e-tongue). E-tongue devices have been used previously to evaluate the taste of food products and oral pharmaceutical formulations, as well as to monitor environmental samples. Various taste masking technologies have been developed including addition of flavorings or sweeteners (Depalmo, 1999, Wehling et al., 1993), formation of inclusion complexes with β-CD (Motola et al., 1991), bonding with ion exchange resins (Agarwal et al., 2000, Lee et al., 2012), coating or microencapsulating with water-insoluble polymers (Al-Omran et al., 2002, Gao et al., 2006, Jańczyk et al., 2010, Wehling et al., 1993, Yajima et al., 1996, Zgoulli et al., 1999), and modifying the chemical properties of drug substances (Asaka et al., 1992, Hussain et al., 1988). With the exception of addition of flavorings and sweeteners, taste masking is achieved primarily by minimizing direct contact between taste buds on the tongue and drug substances dissolved in the buccal cavity (Sohi et al., 2004). Microencapsulation is defined as the process of manufacturing small particles with sizes in the micrometer range, in which materials are coated with a solid matter or dispersed into a matrix. Microencapsulation is distinguished from conventional granule coating methods by modification of the primary particle (Kirk-Othmer, 2005). For this reason, microencapsulation is used for producing orodispersible systems and oral suspensions, which are highly preferred by pediatric and geriatric patients (Breitkreutz and Boos, 2007) and are necessary for individuals who 20mg sildenafil have swallowing problems (Carnaby-Mann and Crary, 2005). Thus, such formulations require more attention to adequate masking of bitterness of active pharmaceutical ingredients (Ueda et al., 1993, Zgoulli et al., 1999).

Use of pH-dependent gastro-soluble polymers as carriers can be employed for taste masking through microencapsulation, because liberation of the drug in the oral cavity is retarded by a polymer that is not degraded by saliva. Conversely, microcapsule particles dissolve completely in gastric juice, and thus there is no alteration of drug absorption in the GI tract (Al-Omran et al., 2002, Bora et al., 2008, Gao et al., 2006). In this study, we prepared solid dispersion particles consisting of SC and Eudragit® E100, a methacrylate polymer that dissolves below pH 5.0, by a spray drying method. Spray drying is widely employed in pharmaceutical research and industry to produce small particles of desirable sizes and has the advantages of being a one-step process and having straightforward scaling-up. Furthermore, the properties of solid dispersions, including their dissolution profiles, can be thoroughly analyzed and evaluated. In order to obtain quantitative data about taste, levels of bitterness between raw materials and modified particulate systems can be measured using an electronic tongue (e-tongue). E-tongue devices have been used previously to evaluate the taste of food products and oral pharmaceutical formulations, as well as to monitor environmental samples. The e-tongue system is based on potentiometric measurements. Sensors interact with active ingredients that have a specific taste in aqueous media, then the chemical interaction is transformed to an electrical signal by measuring the voltage difference between a reference electrode and probe. Data obtained from e-tongue measurements are recorded and analyzed by univariate or multivariate methods as dictated by the experiment. The methods of multivariate statistical analysis include principal component analysis (PCA) and partial least square regression (PLS). Importantly, taste-masking efficiency can be sildenafil citrate tables estimated by comparing taste-masked formulations and the unmasked pure drug.

Shipping Information

The e-tongue system has the advantages of high sensitivity, readiness, and reproducibility, and avoids potential ethical issues involved with human sensory tests of certain substances (Guhmann et al., 2012, Jańczyk et al., 2010, Maniruzzaman et al., 2012, Maniruzzaman et al., 2013, Woertz et al., 2011). The objectives of this study were to design and optimize a taste masked microparticulate system by using a simple spray drying technique for the improvement of patient compliance of SC and to evaluate morphological, crystalline, and molecular properties of taste masked microcapsules. In addition, it was studied to obtain a scientific determination of the masking efficiency of taste-masked SC microcapsules using e-tongue measurements and statistical analysis. Sildenafil citrate (SC) was supplied from Hanmi Pharm Co. Ltd. (Seoul, Korea). Eudragit® E100 (E100) was obtained from Evonic-Degussa GmbH (Essen, Germany).

• Sildenafil citrate chewable tablets treat erectile dysfunction in men.
• These tablets dissolve quickly in the mouth for faster absorption.
• Generally taken 30-60 minutes before sexual activity.
• Common side effects include headache, flushing, and nasal congestion.
• Do not take with nitrate medications as it can cause severe hypotension.
• Ensure proper dosage to avoid adverse reactions or decreased effectiveness.
• Not recommended for individuals with severe heart or liver problems.
• Consult a doctor before use if you have a history of vision problems.
• Avoid alcohol while using sildenafil chewables, as it can increase side effects.
• The tablets come in various flavors for easier consumption.
• Store in a cool, dry place away from children and pets.
• Do not crush or swallow whole; dissolve well before swallowing if needed.

Methanol and acetonitrile (Honeywell Burdick & Jackson®, Muskegon, MI, USA) were of high performance liquid chromatography (HPLC) grade. Water was purified by reverse osmosis and filtered in house. All other chemicals were of reagent grade. Microencapsulation of SC with E100 was performed using a B-290 mini spray dryer (Büchi, Flawil, SE microcapsules prepared by spray drying were fine powders with a white color. The production yields, LOD values, and drug loading encapsulation efficiency of each microcapsule product are listed in Table 1. The total recovery of products after spray drying was approximately 70%, with the loss of product attributed primarily to the difficulty of manual collection and inter-particular static electricity, which could be improved by scaling up.

Sildenafil Citrate Chewable Tablets USP 50mg Technical Specification:

Microencapsulation of SC with E100 was performed using a B-290 mini spray dryer (Büchi, Flawil, SE microcapsules prepared by spray drying were fine powders with a white color. The production yields, LOD values, and drug loading encapsulation efficiency of each microcapsule product are listed in Table 1. The total recovery of products after spray drying was approximately 70%, with the loss of product attributed primarily to the difficulty of manual collection and inter-particular static electricity, which could be improved by scaling up. The taste masking microcapsules containing SC dispersed into the polymer matrix homogenously with the excellent microencapsulation efficiency were prepared by the spray drying. It was observed that the addition of the E100 increases the taste masking efficiency, and the original bitter taste of the drug may not be sensed by a human when the polymer ratios are more than twice as much as SC.

Analytical profiles of drug substances and excipients

There might be no necessity of the excessive addition of excipients in succeeding solid dosage form This study was supported by a grant of the Korean Health Technology R&D Project, Ministry for Health, Welfare & Family Affairs (A092018) and the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIP) (No. et al.Detection of counterfeit Viagra® with Raman spectroscopyJournal of Pharmaceutical and Biomedical Analysis(2008) et al.Preparation of roxithromycin-polymeric microspheres by the emulsion solvent diffusion method for taste maskingInternational Journal of Pharmaceutics(2006) Safety and efficacy of sildenafil citrate in the treatment of male erectile dysfunctionClinical Therapeutics(1998) et al.Development of oral taste masked diclofenac formulations using a taste sensing systemInternational Journal of Pharmaceutics(2012) et al.Electronic tongue for the detection of taste-masking microencapsulation of active pharmaceutical substancesBioelectrochemistry(2010) et al.Taste masking of paracetamol by hot-melt extrusion: an in vitro and in vivo evaluationEuropean Journal of Pharmaceutics and Biopharmaceutics(2012) et al.Sildenafil citrate, a selective phosphodiesterase type 5 inhibitor:: research and clinical implications in erectile dysfunctionTrends in Endocrinology & Metabolism(1999) et al.Sustained release solid lipid matrices processed by hot-melt extrusion (HME)Colloids and Surfaces B: Biointerfaces(2013) et al.Taste sensing systems (electronic tongues) for pharmaceutical applicationsInternational Journal of Pharmaceutics(2011) et al.Studies of ion-exchange resin complex of chloroquine phosphateDrug Development and Industrial Pharmacy(2000)

Trends in Endocrinology & Metabolism

The taste masking microcapsules containing SC dispersed into the polymer matrix homogenously with the excellent microencapsulation efficiency were prepared by the spray drying.

Choosing Between the Two

Skip to main contentSkip to articleGraphical abstractIntroductionSection snippetsMaterialsPreparation of microcapsules containing SC and Eudragit® E100Preparation of SC microcapsulesConclusionAcknowledgementReferences (41)et al.Taste masking of diclofenac sodium using microencapsulationJournal of Microencapsulationet al.Spray drying of biopharmaceuticals: stability and process considerationsDrying TechnologyAsaka, T., Misawa, Y., Kashimura, M., Morimoto, S., Watantabe, Y., Hatayama, K., 1992. 2′-Modified erythromycin or…et al.Taste masking by spray-drying techniqueAAPS PharmSciTechet al.Paediatric and geriatric drug deliveryExpert Opinion on Drug DeliveryAnalytical profiles of drug substances and excipientset al.Pill swallowing by adults with dysphagiaArchives of Otolaryngology-Head & Neck Surgeryet al.Reference database of Raman spectra of pharmaceutical excipientsJournal of Raman SpectroscopyDepalmo, G.A., 1999. Composition based on ibuprofen, for oral usage. EP Patent…Orally disintegrating dosage forms and taste-masking technologies; 2010Expert Opinion on Drug DeliveryView full text Sildenafil citrate (SC) is a selective cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE-5) inhibitor that has been used extensively for treatment of erectile dysfunction (ED) in men (Ghofrani et al., 2006, Goldenberg, 1998, Moreland et al., 1999). In addition, pharmacological activity in promoting cGMP-mediated vascular smooth muscle relaxation, and it has been approved that the effectiveness of SC for treating pulmonary artery hypertension (PAH) (Galiè et al., 2005, Ghofrani et al., 2006, Michelakis et al., 2002).

Pharmacokinetic profile of sildenafil citrate in healthy Middle Eastern Males: Comparison with other ethnicities

There is an unmet medical need for either an orally-disintegrating tablet (ODT), an orally-disintegrating film (ODF), or a chewable tablet formulation of SC for easy administration via instantaneous drug absorption for the purpose of treating ED, as well as an oral suspension appropriate for delivery of SC to neonates and elderly patients for treatment of PAH (Lee et al., 2012, Singh et al., 2009). However, the excessive bitter taste of SC is a critical hurdle for generating a palatable oral dosage form that can achieve appropriate patient compliance. The commercially-available form of SC, Viagra®, is a film-coated tablet. Tablet coating is popularly used to mask unpleasant tastes, but is not applicable to fast disintegrating formulations. For this reason, many studies have been performed to develop an efficient taste masking method suitable for orally-disintegrating systems.

Pill swallowing by adults with dysphagia

There have been several attempts to generate taste-masked dosage forms for SC by various means including formulation with flavorings (Singh et al., 2009, Winter and Scheiwe, 2010), coating granules with a sustained release polymer (Itoh and Niwa, 2001), and ionic bonding with acidic resins (Lee et al., 2012, Singh et al., 2009). However, the addition of flavorings and coating on granules requires a significant amount of excipient leading to a very large dosage, and thus may be improper for some drug formulations. (2009) used ion exchange resin for direct modification of drugs, but did not perform a precise taste evaluation, relying instead on indirect methods, such as presuming from in vitro drug release test. Enhancement of patient compliance is a primary consideration in the development of drug delivery systems. Accordingly, drugs that are administered orally are a major aspect of patient compliance compared with other routes of administration because of their non-invasiveness and convenience of self- medication. It was observed that the addition of the E100 increases the taste masking efficiency, and the original bitter taste of the drug may not be sensed by a human when the polymer ratios are more than twice as much as SC. There might be no necessity of the excessive addition of excipients in succeeding solid dosage form This study was supported by a grant of the Korean Health Technology R&D Project, Ministry for Health, Welfare & Family Affairs (A092018) and the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIP) (No.

About the Company

The e-tongue system is based on potentiometric measurements. Sensors interact with active ingredients that have a specific taste in aqueous media, then the chemical interaction is transformed to an electrical signal by measuring the voltage difference between a reference electrode and probe. Data obtained from e-tongue measurements are recorded and analyzed by univariate or multivariate methods as dictated by the experiment. The methods of multivariate statistical analysis include principal component analysis (PCA) and partial least square regression (PLS). Importantly, taste-masking efficiency can be sildenafil citrate tables estimated by comparing taste-masked formulations and the unmasked pure drug.

Embodiment 2

The e-tongue system has the advantages of high sensitivity, readiness, and reproducibility, and avoids potential ethical issues involved with human sensory tests of certain substances (Guhmann et al., 2012, Jańczyk et al., 2010, Maniruzzaman et al., 2012, Maniruzzaman et al., 2013, Woertz et al., 2011). The objectives of this study were to design and optimize a taste masked microparticulate system by using a simple spray drying technique for the improvement of patient compliance of SC and to evaluate morphological, crystalline, and molecular properties of taste masked microcapsules. In addition, it was studied to obtain a scientific determination of the masking efficiency of taste-masked SC microcapsules using e-tongue measurements and statistical analysis. Sildenafil citrate (SC) was supplied from Hanmi Pharm Co. Ltd.

Preparation of microcapsules containing SC and Eudragit® E100

(Seoul, Korea). Eudragit® E100 (E100) was obtained from Evonic-Degussa GmbH (Essen, Germany). Methanol and acetonitrile (Honeywell Burdick & Jackson®, Muskegon, MI, USA) were of high performance liquid chromatography (HPLC) grade. Water was purified by reverse osmosis and filtered in house. All other chemicals were of reagent grade. et al.Detection of counterfeit Viagra® with Raman spectroscopyJournal of Pharmaceutical and Biomedical Analysis(2008) et al.Preparation of roxithromycin-polymeric microspheres by the emulsion solvent diffusion method for taste maskingInternational Journal of Pharmaceutics(2006) Safety and efficacy of sildenafil citrate in the treatment of male erectile dysfunctionClinical Therapeutics(1998) et al.Development of oral taste masked diclofenac formulations using a taste sensing systemInternational Journal of Pharmaceutics(2012) et al.Electronic tongue for the detection of taste-masking microencapsulation of active pharmaceutical substancesBioelectrochemistry(2010) et al.Taste masking of paracetamol by hot-melt extrusion: an in vitro and in vivo evaluationEuropean Journal of Pharmaceutics and Biopharmaceutics(2012) et al.Sildenafil citrate, a selective phosphodiesterase type 5 inhibitor:: research and clinical implications in erectile dysfunctionTrends in Endocrinology & Metabolism(1999) et al.Sustained release solid lipid matrices processed by hot-melt extrusion (HME)Colloids and Surfaces B: Biointerfaces(2013) et al.Taste sensing systems (electronic tongues) for pharmaceutical applicationsInternational Journal of Pharmaceutics(2011) et al.Studies of ion-exchange resin complex of chloroquine phosphateDrug Development and Industrial Pharmacy(2000)