Preparation of sildenafil citrate microcapsules and in vitro/in vivo evaluation of taste masking efficiency

Moreover, we follow moral business policies and crystal pure transparency in all our transactions to keep healthy relations with the customers.For our accomplishment story, we are grateful to our Mr. Kirti, whose continual backing and directions have been useful to us for attaining exponential development in the current market. Exports To: United States Of America Canada Australia United Kingdom Korea United States Of America Canada Australia United Kingdom Korea We "Christ Business Hub" are the leading Wholesaler And Exporter of a wide range of Pharmaceutical Tablets, Pharmaceutical Capsules since 2023 in Nagpur, MaharashtraUnder the valuable guidance of our mentor, Mr.VIDHAN AGRAWAL, we are growing with a notable rate in the market. He has spent long years in the industry to have rich industrial experience enabling us to understand the varied requirements of our clients.

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(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. Under the valuable guidance of our mentor, Mr.VIDHAN AGRAWAL, we are growing with a notable rate in the market. 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).

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).

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

Moreover, we follow moral business policies and crystal pure transparency in all our transactions to keep healthy relations with the customers.For our accomplishment story, we are grateful to our Mr. Kirti, whose continual backing and directions have been useful to us for attaining exponential development in the current market. Exports To: United States Of America Canada Australia United Kingdom Korea United States Of America Canada Australia United Kingdom Korea We "Christ Business Hub" are the leading Wholesaler And Exporter of a wide range of Pharmaceutical Tablets, Pharmaceutical Capsules since 2023 in Nagpur, MaharashtraUnder the valuable guidance of our mentor, Mr.VIDHAN AGRAWAL, we are growing with a notable rate in the market. He has spent long years in the industry to have rich industrial experience enabling us to understand the varied requirements of our clients. Under the valuable guidance of our mentor, Mr.VIDHAN AGRAWAL, we are growing with a notable rate in the market.

Br J Clin Pharmacol

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). 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.

About the Company

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. 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).

Section snippets

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.

THERAPEUTIC INDICATIONS:

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. 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 sildenafil white 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).

Sildenafil Citrate Chewable Tablets USP 100mg Technical Specification:

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. 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 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.

Conflicts of Interest

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 sildenafil white of manufacturing small particles with sizes in the micrometer range, in which materials are coated with a solid matter or dispersed into a matrix.

Embodiment 1

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 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). 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 estimated by comparing taste-masked formulations and the unmasked pure drug. 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).

• 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.

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.

Shipping Information

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.

Sildenafil citrate, a selective phosphodiesterase type 5 inhibitor:: research and clinical implications in erectile dysfunction

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 estimated by comparing taste-masked formulations and the unmasked pure drug. Sildenafil citrate (SC) was supplied from Hanmi Pharm Co. Ltd. (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. 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.