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Oral soluble film containing sildenafil citrate

a technology of oral soluble film and sildenafil citrate, which is applied in the direction of organic active ingredients, pharmaceutical delivery mechanisms, inorganic non-active ingredients, etc., can solve the problem that individual packaged osfs are typically more difficult to tamper

Pending Publication Date: 2022-01-27
CURE PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The formulation achieves a high drug load, flexible and non-brittle film with effective taste masking, improved pharmacokinetic profile, and reduced adverse reactions, allowing for discreet, convenient, and effective administration of sildenafil citrate, suitable for ED and PAH treatment.

Problems solved by technology

Individually packaged OSFs are typically more difficult to tamper with, compared to traditional packages for tablets and capsules, such as bottles or foil blister packs.

Method used

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  • Oral soluble film containing sildenafil citrate

Examples

Experimental program
Comparison scheme
Effect test

example 1

ble Film Containing Sildenafil Citrate

[1011]

FORMULATION 1.01SLURRYORAL SOLUBLE FILMQuantityAmount inAmount inAmount inAmount in 5%Amount in 5%dispensedslurryanhydrous filmanhydrous filmhydrated film hydrated film Substance(g)(wt. %)(wt. %)(mg)(wt. %)(mg)Sildenafil Citrate1,678.616.836.0070.2434.2970.24Kollicoat ® Protect1,406.314.130.0058.5328.5758.53Microcrystalline252.12.55.4510.635.1910.63Cellulose - Avicel ®PH-101Peppermint Flavor299.93.06.4412.566.1312.56Glycerin, 99.7%558.55.612.0023.4111.4323.41pureSucralose280.02.86.0011.705.7111.70Acesulfame186.01.864.007.803.807.80Potassium (ACE-K)FD&C Blue 10.50.0050.010.020.010.02Sodium Benzoate5.00.050.100.200.100.20Water532853.3NANA5.009.76TOTAL10,000.0100100195.10100204.86FORMULATION 1.02Film weight (anhydrous): 209.6 mg; Film weight (10% hydrated): 233 mgSLURRYORAL SOLUBLE FILMAmount in QuantityAmount in Amount in Slurrydispensed 10% hydrated10% hydratedMaterial(wt. %)(g)film (wt. %)film (mg)Water47.83110010.0423.40Glycerin7.8318013....

example 2

Properties and Performance Characteristics

[1012]Physical properties and performance characteristics for the oral soluble film of Formulation 1.01 (Example 1) include:[1013]The anhydrous film weight is 195.1±5 milligrams (mg).[1014]The 5 wt. % hydrated film weight is 204.9±5 mg.[1015]The breaking strength of the film is 8-12 Newtons (N).[1016]The elongation strength of the film is 2-4 millimeters (mm).[1017]The pH of the film is 4.0-4.5.[1018]The disintegration time of the film is ˜1 minute or less.[1019]The Loss on Drying (LOD) of the film is 4±3 wt. %.[1020]The thickness of the film is 0.35±0.06 mm.[1021]The viscosity of the slurry at 20-30° Celsius is 6,000±1,000 centipoise (cP).[1022]Load of the active (sildenafil citrate) is 34.2% (in the 5% hydrated film) or 36% (in the anhydrous film).

Description of Measurement, Protocol (USPPhysical or Performance CharacteristicNo.), and EquipmentMass / weight of drug productGravimetric using calibrated scalesThickness of drug productCalipersMo...

example 3

Manufacturing Oral Dissolvable Film

[1023]The oral soluble film of Formulation 1.01 (Example 1) was manufactured as described below.

[1024]3.1 Dispensing

[1025]Dispense the following raw materials in its given amounts in separate containers.

TheoreticalIngredient% w / w(g) ThatchWater 53.30%5,327.6Sildenafil Citrate 16.79%1,678.6Kollicoat ® Protect 14.08%1,406.3Avicel ® PH-101 Microcrystalline 2.53%252.1CelluloseNatural Peppermint Flavor 3.00%299.9Glycerin 99.7% 5.59%558.5Sucralose 2.80%280.0Ace-K 1.86%186.0FD&C Blue #1 Powder0.005%0.5Sodium Benzoate Powder 0.05%5.0Total100.00%10,000.00

[1026]3.2 Blending, Method A[1027]3.2.1 Add water into a mixing container. To this container, add the glycerin and mix for approximately 10 minutes.[1028]3.2.2 Weigh and add the following powders together, in the following order:[1029]1. Kollicoat® Protect[1030]2. Sildenafil Citrate[1031]3. Sucralose[1032]4. Ace-K[1033]5. Sodium Benzoate[1034]6. Microcrystalline Cellulose[1035]7. Peppermint[1036]8. FD&C Blu...

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Abstract

The present invention relates to an oral soluble film (OSF), methods of orally administering the same, and methods of manufacturing the same. The oral soluble film includes sildenafil citrate, and can further include a binder, filler, flavoring agent, plasticizer, sweetening agent, preservative, solvent, and optionally coloring agent. The active ingredient and excipients can be provided and present in an amount effective to achieve desired physical and performance characteristics of the OSF.

Description

RELATED U.S. APPLICATION DATA[0001]The present application is a continuation of U.S. patent application Ser. No. 17 / 236,054, filed on Apr. 4, 2021, which claims the benefit of U.S. provisional patent application No. 63 / 012,988, filed on Apr. 21, 2020; each of which is incorporated by reference herein in its entirety.BACKGROUND OF THE INVENTION[0002]Sildenafil, sold under the brand name Viagra® among others, is a medication used to treat erectile dysfunction (ED) and pulmonary arterial hypertension (PAH). It is taken by mouth, or injection into a vein. Sildenafil acts by blocking phosphodiesterase 5 (PDES), an enzyme that promotes breakdown of cGMP, which regulates blood flow in the penis. It requires sexual arousal, however, to work for ED. It also results in dilation of the blood vessels in the lungs.[0003]Pfizer originally discovered the medication in 1989 while looking for a treatment for heart-related chest pain. It was approved for medical use in the United States and in the Eu...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/00A61K47/22A61K47/32A61K47/46A61K47/26A61K47/02A61K47/14A61K47/10A61K31/519A61K47/38
CPCA61K9/006A61K47/22A61K47/32A61K47/46A61K47/38A61K47/02A61K47/14A61K47/10A61K31/519A61K47/26A61K9/7007
Inventor ESPINOZA, MARIBELGIGI, VERED
Owner CURE PHARM INC
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