Sildenafil Oral Solution for Pulmonary Hypertension
Do not combine multiple ED treatments without consulting your doctor.
- Common side effects include headache, flushing, and dizziness.
- Allergic reactions are rare but require immediate medical attention.
- Effects usually last for 4 to 6 hours.
Ask your doctor about consuming grapefruit or grapefruit juice while taking this medication. If you take the oral solution, prepare it by shaking the bottle vigorously for at least 30 seconds and measuring the dose with a device intended for measuring medications. If you need emergency medical treatment for a heart problem, inform your care team that you’re taking sildenafil. They may need to know when you took your last dose. Sildenafil is a commonly prescribed treatment for ED or sexual impotence.
Supplemental data
Among the formulations, solid SNEDDS demonstrated the highest improvement in oral bioavailability (AUC; 1508.78 ± 343.95 h·ng/mL).Conclusion: Therefore, solid SNEDDS could be recommended as an oral dosage form for enhancing the oral bioavailability of sildenafil.Keywords: sildenafil, amorphous microspheres, crystalline microspheres, solid self-nanoemulsifying drug delivery system, aqueous microenvironment, oral bioavailability Sildenafil reversibly inhibits the phosphodiesterase-5 enzyme and is clinically used for the treatment of erectile dysfunction.1 Moreover, sildenafil induces pulmonary vasodilation and promotes gas exchange in the lung; and hence, it has been prescribed to patients with pulmonary arterial hypertension.2,3 Sildenafil possesses inadequate aqueous solubility. It is reported that drugs with low aqueous solubility are precipitated when in contact with gastrointestinal fluid. The precipitated drugs hardly permeate intestinal lumen, resulting in poor oral bioavailability.4,5 The citrate form has been the most common technique to enhance the solubility of sildenafil.6–8 However, salt forms lack lipophilic properties, reducing permeability through the gastrointestinal membrane, thereby decreasing oral bioavailability.9 Therefore, in the present study, various drug delivery techniques other than salt formation were studied for improving the aqueous solubility and oral bioavailability of sildenafil. Developing microspheres is one of the representative solubilising technologies.10,11 In the microspheres system, poorly water-soluble drugs are disseminated in hydrophilic excipients giving spherical shape with micrometre size.12 Microspheres are produced by utilising various methods such as spray-drying and hot melt extrusion.13,14 The former method is prepared by dissolving/suspending drugs and ingredients in proper solvent.15 Depending on the type of solvent, microspheres system can be classified into amorphous and crystalline system. In amorphous systems, drugs and carriers are completely dissolved in organic solvents and spray-dried.
12.1 Sildenafil Oral Suspension Mechanism of Action
As a result, the physicochemical properties of the drug were changed, thereby the oral bioavailability increased.16 In contrast, crystalline systems are generated using distilled water as a solvent. The use of distilled water allows free from the residual organic solvent issue. Furthermore, improved oral bioavailability of the drug was achieved without alteration of physicochemical properties.17,18 Self-nanoemulsifying drug delivery systems (SNEDDS) are composed of oil, surfactant and co-surfactant.19,20 When water penetrates drug-loaded SNEDDS, oil-in-water (o/w) nanoemulsions are naturally created. These nano-sized emulsions have a large surface area in contact with water, which increases the solubility of the drug. Likewise, o/w nanoemulsion is formed in the gastrointestinal (GI) tract, when drug-loaded SNEDDS is mixed with GI fluid.
2.3 Reconstitution of the Powder for Oral Suspension
It blocks the enzyme PDE5 and increases blood flow to the penis during sexual stimulation. Sildenafil treats PAH by relaxing and reducing the pressure in blood vessels in the lungs, allowing for increased blood flow. It takes about thirty minutes for sildenafil to work. And its action continues for a couple of hours, possibly up to a maximum of four hours.³⁴ Phosphodiesterase-5 (PDE5) Inhibitors In the Management of Erectile Dysfunction - PMC Phosphodiesterase-5 (PDE5) Inhibitors In the Management of Erectile Dysfunction - PMC Onset and duration of action of sildenafil for the treatment of erectile dysfunction - PMC Onset and duration of action of sildenafil for the treatment of erectile dysfunction - PMC Long-term safety and effectiveness of sildenafil citrate in men with erectile dysfunction - PMC Long-term safety and effectiveness of sildenafil citrate in men with erectile dysfunction - PMC Radiation-Associated Erectile Dysfunction: Viagra Demonstrat..
| Product | Dosage | Quantity + Bonus | Price | |
|---|---|---|---|---|
| Viagra Generic | 150mg | 180 + 10 Pills | 236.46€ 225.20€ | |
| Viagra Generic | 25mg | 270 + 8 Pills | 184.26€ 175.49€ | |
| Viagra Generic | 25mg | 20 Pills | 37.74€ 35.94€ | |
| Viagra Generic | 100mg | 10 Pills | 28.91€ 27.53€ | |
| Viagra Generic | 50mg | 10 Pills | 26.87€ 25.59€ | |
| Viagra Generic | 25mg | 360 + 10 Pills | 213.68€ 203.50€ | |
| Kamagra Oral Jelly | 100mg | 21 Sachets | 95.92€ 91.35€ | |
| Viagra Generic | 150mg | 30 + 2 Pills | 72.32€ 68.88€ | |
| Kamagra Polo | 100mg | 12 Pills | 60.21€ 57.34€ | |
| Kamagra Soft Tabs | 100mg | 20 Pills | 79.79€ 75.99€ | |
| Viagra Generic | 25mg | 180 + 6 Pills | 154.93€ 147.55€ | |
| Viagra Generic | 100mg | 270 + 10 Pills | 270.47€ 257.59€ | |
| Kamagra | 100mg | 84 + 6 Pills | 264.44€ 251.85€ | |
| Kamagra | 100mg | 12 Pills | 55.64€ 52.99€ |
: Oncology Times Radiation-Associated Erectile Dysfunction: Viagra Demonstrat..
Related/similar drugs
This article may not always be up to date and is not exhaustive of all of the risks and considerations relevant to this particular drug. In no circumstances should this article be relied upon without independent consideration and confirmation by a qualified medical practitioner. Your doctor will be able to explain all possible uses, dosages, precautions, interactions with other drugs, and other potential adverse effects, and you should always talk to them about any kind of medication you are taking, thinking about taking or wanting to stop taking. DescriptionDosage FormOral SuspensionIndicationPulmonary Arterial hypertensionBrand NameRevatio®TE CodeABLactoseNoGlutenNoColorOff-White to Light Yellow PowderShapeNAMarkingsNAStorage ConditionBEFORE RECONSTITUTION: Store below 30°C (86°F) in the original package in order to protect from moisture. AFTER RECONSTITUTION: Store below 30°C (86°F) or in refrigerator at 2°C to 8°C (36°F to 46°F) Do not freeze.
How is sildenafil supplied (dosage forms)?
Discard any unused portion 60 days after reconstitution.PACK SIZE: “112 mL following ReconstitutionNDC#: 27241-0175-29Click to View Package Insert Click to View Material Data Safety Sheet Revatio ® is registered trademark of Pfizer Back to Journals » International Journal of Nanomedicine » Volume 16 Comparison of Three Different Aqueous Microenvironments for Enhancing Oral Bioavailability of Sildenafil: Solid Self-Nanoemulsifying Drug Delivery System, Amorphous Microspheres and Crystalline Microspheres Authors Kim JS , Din FU , Lee SM, Kim DS, Woo MR, Cheon S, Ji SH, Kim JO, Youn YS , Oh KT , Lim SJ, Jin SG , Choi HG Editor who approved publication: Dr Yan Shen Jung Suk Kim,1,* Fakhar ud Din,2,* Sang Min Lee,1,* Dong Shik Kim,1 Mi Ran Woo,1 Seunghyun Cheon,1 Sang Hun Ji,1 Jong Oh Kim,3 Yu Seok Youn,4 Kyung Taek Oh,5 Soo-Jeong Lim,6 Sung Giu Jin,7 Han-Gon Choi1 1College of Pharmacy, Hanyang University, Ansan, South Korea; 2Department of Pharmacy, Quaid-I-Azam University, Islamabad, Pakistan; 3College of Pharmacy, Yeungnam University, Gyongsan, South Korea; 4School of Pharmacy, Sungkyunkwan University, Suwon, South Korea; 5College of Pharmacy, Chung-Ang University, Seoul, South Korea; 6Department of Bioscience and biotechnology, Sejong University, Seoul, South Korea; 7Department of Pharmaceutical Engineering, Dankook University, Cheonan, South Korea*These authors contributed equally to this workCorrespondence: Sung Giu Jin; Han-Gon Choi Tel +82 41-550-3558; +82 31-400-5802Fax +82 41-559-7945; +82 31-400-5958Email [email protected]; [email protected]Background: The purpose of this study was to screen various drug delivery systems for improving the aqueous solubility and oral bioavailability of sildenafil. Three representative techniques, solid self-nanoemulsifying drug delivery systems (SNEDDS), amorphous microspheres and crystalline microspheres, were compared.Methods: Both microspheres systems contained sildenafil:Labrasol:PVP at a weight ratio of 1:1:6. The amorphous microspheres were manufactured using ethanol, while crystalline microspheres were generated using distilled water. Liquid SNEDDS was composed of sildenafil citrate tablet sildenafil:Labrasol:Transcutol HP:Captex 300 in the ratio of 1:70:15:15 (w:w:w:w). The solidification process in SNEDDS was performed using HDK N20 Pharma as a solid carrier.Results: The amorphous microspheres appeared spherical with significantly decreased particle size compared to the drug powder.
Statistical Analysis
The crystalline microspheres exhibited a rough surface with no major particle-size difference compared with sildenafil powder, indicating that the hydrophilic excipients adhered to the sildenafil crystal. Solid SNEDDS presented a smooth surface, assuming that the oily liquid was adsorbed to the porous solid carrier. According to the physicochemical evaluation, the crystalline state maintained in crystalline microspheres, whereas the crystal state changed to amorphous state in other formulations. Amorphous microspheres, crystalline microspheres and solid SNEDDS produced about 79, 55, 82-fold increased solubility, compared to drug powder. Moreover, the prepared formulations provided a higher dissolution rate (%) and plasma concentration than did the drug powder (performance order; solid SNEDDS ≥ amorphous microspheres ≥ crystalline microspheres > drug powder). : Oncology Times Sildenafil - Drugs and Lactation Database (LactMed®) - NCBI Bookshelf Sildenafil - Drugs and Lactation Database (LactMed®) - NCBI Bookshelf Revatio, Viagra (sildenafil) dosing, indications, interactions, adverse effects, and more Revatio, Viagra (sildenafil) dosing, indications, interactions, adverse effects, and more [Interaction between sildenafil and antihypertensive drugs: what is evidence-based?] [Interaction between sildenafil and antihypertensive drugs: what is evidence-based?] We make it easy to take part. Here at HealthMatch, we’ve done our best to ensure that the information provided in this article is helpful, up to date, and, most importantly, accurate. However, we can’t replace the one-to-one advice of a qualified medical practitioner or outline all of the possible risks associated with this particular drug and your circumstances. It is therefore important for you to note that the information contained in this article does not constitute professional medical or healthcare advice, diagnosis or recommendation of treatment and is not intended to, nor should be used to, replace professional medical advice. This article may not always be up to date and is not exhaustive of all of the risks and considerations relevant to this particular drug. In no circumstances should this article be relied upon without independent consideration and confirmation by a qualified medical practitioner.
| Brand Name | Manufacturer | Available Strengths | Notes |
|---|---|---|---|
| Viagra Oral Solution | Pfizer | 10 mg/mL | Widely known; prescription only |
| Sildenafil Oral Solution | Generic or compounded brands | 10 mg/mL | Often more affordable; compounded options |
| Revatio Oral Solution | Pfizer (for PAH) | 10 mg/mL | Approved for pulmonary hypertension |
| Kamagra Oral Solution | Ajanta Pharma (generic) | 10 mg/mL | Not officially approved in many markets |
Your doctor will be able to explain all possible uses, dosages, precautions, interactions with other drugs, and other potential adverse effects, and you should always talk to them about any kind of medication you are taking, thinking about taking or wanting to stop taking. DescriptionDosage FormOral SuspensionIndicationPulmonary Arterial hypertensionBrand NameRevatio®TE CodeABLactoseNoGlutenNoColorOff-White to Light Yellow PowderShapeNAMarkingsNAStorage ConditionBEFORE RECONSTITUTION: Store below 30°C (86°F) in the original package in order to protect from moisture.
10. Overdosage
Allergy warning
AFTER RECONSTITUTION: Store below 30°C (86°F) or in refrigerator at 2°C to 8°C (36°F to 46°F) Do not freeze. Discard any unused portion 60 days after reconstitution.PACK SIZE: “112 mL following ReconstitutionNDC#: 27241-0175-29Click to View Package Insert Click to View Material Data Safety Sheet Revatio ® is registered trademark of Pfizer Back to Journals » International Journal of Nanomedicine » Volume 16 Comparison of Three Different Aqueous Microenvironments for Enhancing Oral Bioavailability of Sildenafil: Solid Self-Nanoemulsifying Drug Delivery System, Amorphous Microspheres and Crystalline Microspheres Authors Kim JS , Din FU , Lee SM, Kim DS, Woo MR, Cheon S, Ji SH, Kim JO, Youn YS , Oh KT , Lim SJ, Jin SG , Choi HG Editor who approved publication: Dr Yan Shen Jung Suk Kim,1,* Fakhar ud Din,2,* Sang Min Lee,1,* Dong Shik Kim,1 Mi Ran Woo,1 Seunghyun Cheon,1 Sang Hun Ji,1 Jong Oh Kim,3 Yu Seok Youn,4 Kyung Taek Oh,5 Soo-Jeong Lim,6 Sung Giu Jin,7 Han-Gon Choi1 1College of Pharmacy, Hanyang University, Ansan, South Korea; 2Department of Pharmacy, Quaid-I-Azam University, Islamabad, Pakistan; 3College of Pharmacy, Yeungnam University, Gyongsan, South Korea; 4School of Pharmacy, Sungkyunkwan University, Suwon, South Korea; 5College of Pharmacy, Chung-Ang University, Seoul, South Korea; 6Department of Bioscience and biotechnology, Sejong University, Seoul, South Korea; 7Department of Pharmaceutical Engineering, Dankook University, Cheonan, South Korea*These authors contributed equally to this workCorrespondence: Sung Giu Jin; Han-Gon Choi Tel +82 41-550-3558; +82 31-400-5802Fax +82 41-559-7945; +82 31-400-5958Email [email protected]; [email protected]Background: The purpose of this study was to screen various drug delivery systems for improving the aqueous solubility and oral bioavailability of sildenafil. Three representative techniques, solid self-nanoemulsifying drug delivery systems (SNEDDS), amorphous microspheres and crystalline microspheres, were compared.Methods: Both microspheres systems contained sildenafil:Labrasol:PVP at a weight ratio of 1:1:6. The amorphous microspheres were manufactured using ethanol, while crystalline microspheres were generated using distilled water. Liquid SNEDDS was composed of sildenafil citrate tablet sildenafil:Labrasol:Transcutol HP:Captex 300 in the ratio of 1:70:15:15 (w:w:w:w).
Author information
Do not combine multiple ED treatments without consulting your doctor. Ask your doctor about consuming grapefruit or grapefruit juice while taking this medication. If you take the oral solution, prepare it by shaking the bottle vigorously for at least 30 seconds and measuring the dose with a device intended for measuring medications. If you need emergency medical treatment for a heart problem, inform your care team that you’re taking sildenafil. They may need to know when you took your last dose.
Supplemental Material
Sildenafil is a commonly prescribed treatment for ED or sexual impotence. It blocks the enzyme PDE5 and increases blood flow to the penis during sexual stimulation. Sildenafil treats PAH by relaxing and reducing the pressure in blood vessels in the lungs, allowing for increased blood flow. It takes about thirty minutes for sildenafil to work. And its action continues for a couple of hours, possibly up to a maximum of four hours.³⁴ Phosphodiesterase-5 (PDE5) Inhibitors In the Management of Erectile Dysfunction - PMC Phosphodiesterase-5 (PDE5) Inhibitors In the Management of Erectile Dysfunction - PMC Onset and duration of action of sildenafil for the treatment of erectile dysfunction - PMC Onset and duration of action of sildenafil for the treatment of erectile dysfunction - PMC Long-term safety and effectiveness of sildenafil citrate in men with erectile dysfunction - PMC Long-term safety and effectiveness of sildenafil citrate in men with erectile dysfunction - PMC Radiation-Associated Erectile Dysfunction: Viagra Demonstrat..
8.7 Patients with Renal Impairment
: Oncology Times Radiation-Associated Erectile Dysfunction: Viagra Demonstrat.. : Oncology Times Sildenafil - Drugs and Lactation Database (LactMed®) - NCBI Bookshelf Sildenafil - Drugs and Lactation Database (LactMed®) - NCBI Bookshelf Revatio, Viagra (sildenafil) dosing, indications, interactions, adverse effects, and more Revatio, Viagra (sildenafil) dosing, indications, interactions, adverse effects, and more [Interaction between sildenafil and antihypertensive drugs: what is evidence-based?] [Interaction between sildenafil and antihypertensive drugs: what is evidence-based?] We make it easy to take part. Here at HealthMatch, we’ve done our best to ensure that the information provided in this article is helpful, up to date, and, most importantly, accurate. However, we can’t replace the one-to-one advice of a qualified medical practitioner or outline all of the possible risks associated with this particular drug and your circumstances. It is therefore important for you to note that the information contained in this article does not constitute professional medical or healthcare advice, diagnosis or recommendation of treatment and is not intended to, nor should be used to, replace professional medical advice. The solidification process in SNEDDS was performed using HDK N20 Pharma as a solid carrier.Results: The amorphous microspheres appeared spherical with significantly decreased particle size compared to the drug powder. The crystalline microspheres exhibited a rough surface with no major particle-size difference compared with sildenafil powder, indicating that the hydrophilic excipients adhered to the sildenafil crystal. Solid SNEDDS presented a smooth surface, assuming that the oily liquid was adsorbed to the porous solid carrier. According to the physicochemical evaluation, the crystalline state maintained in crystalline microspheres, whereas the crystal state changed to amorphous state in other formulations. Amorphous microspheres, crystalline microspheres and solid SNEDDS produced about 79, 55, 82-fold increased solubility, compared to drug powder. Moreover, the prepared formulations provided a higher dissolution rate (%) and plasma concentration than did the drug powder (performance order; solid SNEDDS ≥ amorphous microspheres ≥ crystalline microspheres > drug powder).
| Patient Group | Recommended Dose | Administration Tips | Notes |
|---|---|---|---|
| Adult males with ED | 50 mg, 1 hour before activity | Take on an empty stomach if possible | Max 100 mg/day |
| Patients with PAH | 2.5 mg to 10 mg, 3 times daily | With or without food | Adjust based on response |
| Pediatric use (off-label) | Not recommended | Under strict medical supervision | Safety not established |
Among the formulations, solid SNEDDS demonstrated the highest improvement in oral bioavailability (AUC; 1508.78 ± 343.95 h·ng/mL).Conclusion: Therefore, solid SNEDDS could be recommended as an oral dosage form for enhancing the oral bioavailability of sildenafil.Keywords: sildenafil, amorphous microspheres, crystalline microspheres, solid self-nanoemulsifying drug delivery system, aqueous microenvironment, oral bioavailability Sildenafil reversibly inhibits the phosphodiesterase-5 enzyme and is clinically used for the treatment of erectile dysfunction.1 Moreover, sildenafil induces pulmonary vasodilation and promotes gas exchange in the lung; and hence, it has been prescribed to patients with pulmonary arterial hypertension.2,3 Sildenafil possesses inadequate aqueous solubility. It is reported that drugs with low aqueous solubility are precipitated when in contact with gastrointestinal fluid. The precipitated drugs hardly permeate intestinal lumen, resulting in poor oral bioavailability.4,5 The citrate form has been the most common technique to enhance the solubility of sildenafil.6–8 However, salt forms lack lipophilic properties, reducing permeability through the gastrointestinal membrane, thereby decreasing oral bioavailability.9 Therefore, in the present study, various drug delivery techniques other than salt formation were studied for improving the aqueous solubility and oral bioavailability of sildenafil. Developing microspheres is one of the representative solubilising technologies.10,11 In the microspheres system, poorly water-soluble drugs are disseminated in hydrophilic excipients giving spherical shape with micrometre size.12 Microspheres are produced by utilising various methods such as spray-drying and hot melt extrusion.13,14 The former method is prepared by dissolving/suspending drugs and ingredients in proper solvent.15 Depending on the type of solvent, microspheres system can be classified into amorphous and crystalline system. In amorphous systems, drugs and carriers are completely dissolved in organic solvents and spray-dried.
- The solution is stored at room temperature, away from light.
- Alcohol consumption may increase side effects.
- Do not mix with hot beverages, which can affect stability.
As a result, the physicochemical properties of the drug were changed, thereby the oral bioavailability increased.16 In contrast, crystalline systems are generated using distilled water as a solvent. The use of distilled water allows free from the residual organic solvent issue.
- Sildenafil oral solution is prescribed by a healthcare provider.
- It should be taken on an empty stomach for faster effects.
- The liquid form provides flexibility in dosing.
Furthermore, improved oral bioavailability of the drug was achieved without alteration of physicochemical properties.17,18 Self-nanoemulsifying drug delivery systems (SNEDDS) are composed of oil, surfactant and co-surfactant.19,20 When water penetrates drug-loaded SNEDDS, oil-in-water (o/w) nanoemulsions are naturally created. These nano-sized emulsions have a large surface area in contact with water, which increases the solubility of the drug. Likewise, o/w nanoemulsion is formed in the gastrointestinal (GI) tract, when drug-loaded SNEDDS is mixed with GI fluid.
| Ingredient | Concentration | Function | Notes |
|---|---|---|---|
| Sildenafil citrate | 10 mg/mL | Active pharmaceutical ingredient | Main therapeutic agent |
| Purified water | - | Solvent | Ensures proper dissolution |
| Preservative (e.g., parabens) | 0.1% | Prevent microbial growth | Preserves solution stability |
| Flavouring agents | - | Improve palatability | Fruit or mint flavors |
| Sweeteners | - | Mask bitterness | Aspartame or sucralose |