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WO2025079861A1 - Composition pharmaceutique ayant une biodisponibilité améliorée du pranlukast, et procédé de préparation s'y rapportant - Google Patents

Composition pharmaceutique ayant une biodisponibilité améliorée du pranlukast, et procédé de préparation s'y rapportant Download PDF

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Publication number
WO2025079861A1
WO2025079861A1 PCT/KR2024/012778 KR2024012778W WO2025079861A1 WO 2025079861 A1 WO2025079861 A1 WO 2025079861A1 KR 2024012778 W KR2024012778 W KR 2024012778W WO 2025079861 A1 WO2025079861 A1 WO 2025079861A1
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Prior art keywords
pranlukast
pharmaceutical composition
weight
parts
silica
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PCT/KR2024/012778
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English (en)
Korean (ko)
Inventor
이종현
천유진
권만호
류형선
진수경
박준영
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Dasan Pharmaceutical Co ltd
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Dasan Pharmaceutical Co ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating

Definitions

  • the present invention relates to a pharmaceutical composition having improved bioavailability of pranlukast, a poorly soluble drug, and a method for producing the same.
  • Pranlukast has the problem of being practically insoluble in water and having strong adhesive properties, resulting in low bioavailability when administered orally, and thus requiring administration in larger amounts than patients require.
  • Korean Patent Registration No. 10-0389606 proposed a method of dissolving sugar, water-soluble polymer, and surfactant in purified water, suspending pranlukast, and spray drying, thereby improving the adhesion and cohesion of pranlukast, but not its solubility.
  • Korean Patent Registration No. 10-0381834 prepares a solid dispersion by dissolving pranlukast in a mixed solution of dichloromethane and methanol and spray drying.
  • it has the disadvantage of requiring a separate moisture-proof coating and moisture-proof packaging because a large amount of disintegrant is used to increase solubility and formulate it into a tablet.
  • Korean Patent Registration No. 10-1332223 discloses a method for producing a nano solid dispersion through a hot melt method and a solvent evaporation method to increase the solubility of pranlukast.
  • the hot melt method has difficulties in commercialization due to the high manufacturing cost.
  • Korean Patent Registration Nos. 10-1086254 and 10-1233235 used the hot melt method to increase the solubility of pranlukast and added an anti-caking agent with a certain HLB range to produce a pranlukast solid dispersion, which is currently sold as Pranair Capsule (pranlukast 112.5 mg/capsule, 1 capsule per dose, SK Chemical).
  • Pranair Capsule pranlukast 112.5 mg/capsule, 1 capsule per dose, SK Chemical
  • Korean Patent Registration Nos. 10-0715355 and 10-0981751 are pharmaceutical compositions in tablet form including spray-dried granules composed of a water-soluble polymer and a surfactant to improve the adhesion, cohesion, and solubility of pranlukast, which are currently commercialized as Prakanone tablets (pranlukast 75 mg/tablet, 1 tablet per dose, Yuhan-Yanghaeng).
  • spray-dried equipment has the disadvantages of being complex and bulky, requiring high one-time investment costs, and having low thermal efficiency, resulting in high energy consumption.
  • the amount of surfactant used is high, problems may occur during the manufacturing process.
  • a pharmaceutical carrier containing pranlukast manufactured using an alcohol having 1 to 6 carbon atoms by a wet granulation method has the characteristic of a single dose of pranlukast of 70 mg or less.
  • the amount of alcohol used is 1 to 1.7 times that of pranlukast, there is a possibility of environmental pollution by organic solvents.
  • the viscosity of the surfactant may differ depending on the storage temperature, which may cause problems in the manufacturing process and, as a result, may affect the density and particle size distribution of the granules.
  • the purpose of the present invention is to provide a pharmaceutical composition having improved dissolution rate and bioavailability of pranlukast and a method for producing the same.
  • the purpose of the present invention is to provide a pharmaceutical composition having improved solubility of pranlukast and a method for producing the same.
  • a pharmaceutical composition comprising 15 to 25 parts by weight of pranlukast; 0.1 to 10 parts by weight of a water-soluble polymer; and 0.1 to 5 parts by weight of a silica-based fluidizing agent.
  • pranlukast is a pharmaceutical composition having a particle size distribution of D(0.50) of 0.1 to 2.0 ⁇ m and D(0.90) of 1.6 to 7.0 ⁇ m.
  • silica-based fluidizing agent is at least one selected from the group consisting of silica, light anhydrous silica, colloidal silica, hydrous silica, silicate, magnesium silicate, magnesium trisilicate, and magnesium aluminum silicate.
  • a pharmaceutical composition further comprising 1 to 30 parts by weight of at least one solubilizing agent selected from the group consisting of sodium lauryl sulfate, polyethylene glycol-15 hydroxystearate, cremophor, poloxamer, polyethylene glycol, polyethylene glycol stearate, ethoxylated fatty alcohols, lecithin, and glyceryl fatty acid ester.
  • at least one solubilizing agent selected from the group consisting of sodium lauryl sulfate, polyethylene glycol-15 hydroxystearate, cremophor, poloxamer, polyethylene glycol, polyethylene glycol stearate, ethoxylated fatty alcohols, lecithin, and glyceryl fatty acid ester.
  • a pharmaceutical composition further comprising 1 to 20 parts by weight of at least one disintegrant selected from the group consisting of sodium starch glycolate, croscarmellose, croscarmellose sodium, crospovidone, low-substituted hydroxypropyl cellulose, calcium carboxymethyl cellulose, and alginic acid in the above 1.
  • at least one disintegrant selected from the group consisting of sodium starch glycolate, croscarmellose, croscarmellose sodium, crospovidone, low-substituted hydroxypropyl cellulose, calcium carboxymethyl cellulose, and alginic acid in the above 1.
  • a pharmaceutical composition further comprising 40 to 80 parts by weight of at least one diluent selected from the group consisting of microcrystalline cellulose, crystalline cellulose, mannitol, lactose monohydrate, starch, and pregelatinized starch in the above 1.
  • a pharmaceutical composition comprising pranlukast in an amount of 50 mg or less in the above 1.
  • a pharmaceutical composition formulated as a powder, granule, capsule, tablet or dry syrup according to the above 1.
  • a method for producing a pharmaceutical composition comprising the steps of mixing pranlukast, a diluent, a silica-based fluidizing agent, and a disintegrant in a mixer; performing a first association while dissolving a water-soluble polymer in water and introducing it into the mixer; and performing a second association while suspending or dissolving a solubilizing agent in ethanol and introducing it into the mixer.
  • a method for manufacturing a pharmaceutical composition further comprising the step of drying and establishing a secondary compound in the above 10.
  • a method for producing a pharmaceutical composition comprising mixing 40 to 80 parts by weight of a diluent, 0.1 to 5 parts by weight of a silica-based fluidizing agent, and 1 to 20 parts by weight of a disintegrant with respect to 15 to 25 parts by weight of pranlukast in the above 10.
  • silica-based fluidizing agent is at least one selected from the group consisting of silica, light anhydrous silica, colloidal silica, hydrous silica, silicate, magnesium silicate, magnesium trisilicate, and magnesium aluminum silicate.
  • the solubilizing agent is at least one selected from the group consisting of sodium lauryl sulfate, polyethylene glycol-15 hydroxystearate, cremophor, poloxamer, polyethylene glycol, polyethylene glycol stearate, ethoxylated fatty alcohol, lecithin, and glyceryl fatty acid ester.
  • a method for manufacturing a pharmaceutical composition comprising pranlukast in an amount of 50 mg or less in the above 10.
  • the pharmaceutical composition of the present invention shows clinical efficacy equivalent to or greater than that of a commercially available formulation, Onon Capsule, at a single dose of 225 mg (pranlukast 112.5 mg/capsule, 2 capsules at a time, 2 times a day), even when the content of pranlukast is reduced to 50 mg/tablet or less (1 tablet at a time, taken twice a day) due to improved dissolution rate and bioavailability of pranlukast.
  • the pharmaceutical composition of the present invention can improve patient compliance with medication and reduce side effects caused by excessive administration of pranlukast.
  • Figure 1 shows comparative dissolution results of Examples 1 to 5 and Onon capsules.
  • Figure 2 shows comparative dissolution results of Examples 11 to 15 and Onon capsules.
  • Figure 3 shows the results of the in-human kinetic evaluation of Example 21 and Onon capsules (112.5 mg*2 caps).
  • the present invention provides a pharmaceutical composition having improved bioavailability of pranlukast and a method for producing the same.
  • the present invention provides a pharmaceutical composition and a method for preparing the same, which can improve patient compliance and reduce side effects caused by taking excessive pranlukast by reducing the content of pranlukast to 50 mg/tablet or less (1 tablet at a time, twice a day) by including 0.1 to 10 parts by weight of a water-soluble polymer and 0.1 to 5 parts by weight of a silica-based fluidizing agent relative to 15 to 25 parts by weight of pranlukast, thereby showing clinical efficacy equivalent to or greater than that of a commercially available formulation.
  • Pranlukast is a poorly soluble drug. Pranlukast is preferably micronized to improve solubility. In one embodiment, pranlukast can have a particle size distribution with D(0,50) of 0.1 to 2.0 ⁇ m and D(0,90) of 1.6 to 7.0 ⁇ m.
  • the use of pranlukast with a micronized particle size can help improve solubility and dissolution rate in that the particle surface area increases, but as the particle size decreases, the adhesion and cohesion between the particles becomes stronger, which may lower the dissolution rate.
  • the micronized pranlukast is uniformly mixed with a diluent, a silica-based fluidizing agent, and a disintegrant, a water-soluble polymer is dissolved in water and added to the mixture to perform the first association, and a solubilizing agent is suspended or dissolved in ethanol and added to the first association to perform the second association.
  • the present invention can improve the dissolution rate and bioavailability by granulating micronized pranlukast drug, which is a poorly soluble drug, using a water-soluble polymer, a solubilizer, and a pharmaceutically acceptable additive.
  • Water-soluble polymers are used as plasticizers or binders.
  • the water-soluble polymer may be a water-soluble polymer commonly used in the pharmaceutical field.
  • the water-soluble polymer is at least one selected from the group consisting of hydroxypropyl cellulose, hydroxypropyl methyl cellulose, polyvinyl pyrrolidone, polyethylene glycol, polyvinyl pyrrolidone vinyl acetate, and polyvinyl alcohol.
  • Polyethylene glycol is a nonionic substance with the simplest structure among water-soluble polymers and is effective in improving the solubility of pranlukast. It is preferable to use polyethylene glycol having a molecular weight in the range of 3,000 to 8,000.
  • the water-soluble polymer is included in an amount of 0.1 to 10 parts by weight based on 15 to 25 parts by weight of pranlukast.
  • the water-soluble polymer may be included in an amount of 1 to 8 parts by weight, 1 to 6 parts by weight, 1 to 4 parts by weight, or 1 to 3 parts by weight.
  • Silica-based fluidizing agents reduce the electrostatic attraction between particles of franlukast, thereby improving adhesion cohesion and fluidity.
  • the silica-based fluidizing agent is at least one selected from the group consisting of silica, light anhydrous silica, colloidal silica, hydrous silica, silicate, magnesium silicate, magnesium trisilicate, and magnesium aluminum silicate.
  • the silica-based fluidizing agent is included in an amount of 0.1 to 5 parts by weight based on 15 to 25 parts by weight of pranlukast.
  • the silica-based fluidizing agent may be included in an amount of 0.1 to 4 parts by weight, 0.1 to 3 parts by weight, or 0.1 to 2 parts by weight, and may be included in an amount of 0.5 to 5 parts by weight, 0.5 to 4 parts by weight, 0.5 to 3 parts by weight, or 0.5 to 2 parts by weight.
  • the pharmaceutical composition of the present invention may contain a solubilizer.
  • Surfactants commonly used in the pharmaceutical field can be used as solubilizers.
  • Surfactants include water-soluble and oil-soluble surfactants.
  • the solubilizer can be at least one selected from the group consisting of sodium lauryl sulfate, polyethylene glycol-15 hydroxystearate, cremophor, poloxamer, polyethylene glycol, polyethylene glycol stearate, ethoxylated fatty alcohols, lecithin, and glyceryl fatty acid esters.
  • the solubilizer may be included in an amount of 1 to 30 parts by weight based on 15 to 25 parts by weight of pranlukast.
  • the solubilizer may be included in an amount of 5 to 30 parts by weight, 5 to 20 parts by weight, 5 to 10 parts by weight, 10 to 30 parts by weight, or 10 to 20 parts by weight.
  • the pharmaceutical composition of the present invention may contain a disintegrant.
  • a disintegrant is included to ensure that the pharmaceutical composition containing pranlukast disintegrates rapidly in the body and is largely absorbed in the upper part of the small intestine.
  • the disintegrant may be a disintegrant commonly used in the pharmaceutical field.
  • the disintegrant is at least one selected from the group consisting of sodium starch glycolate, croscarmellose, croscarmellose sodium, crospovidone, low-substituted hydroxypropyl cellulose, calcium carboxymethyl cellulose, and alginic acid.
  • the disintegrant may be included in an amount of 1 to 20 parts by weight based on 15 to 25 parts by weight of pranlukast. In one embodiment, the disintegrant may be included in an amount of 1 to 20 parts by weight or 1 to 10 parts by weight.
  • the pharmaceutical composition of the present invention may contain a diluent.
  • the diluent may be a diluent commonly used in the pharmaceutical field.
  • the diluent is at least one selected from the group consisting of microcrystalline cellulose, crystalline cellulose, mannitol, lactose monohydrate, starch, and pregelatinized starch.
  • the diluent may be included in an amount of 40 to 80 parts by weight per 15 to 25 parts by weight of pranlukast. In one embodiment, the diluent may be included in an amount of 40 to 70 parts by weight or 50 to 80 parts by weight.
  • the pharmaceutical composition of the present invention is manufactured by including the steps of (i) placing pranlukast, a diluent, a silica-based fluidizing agent, and a disintegrant in a mixer and mixing them; (ii) performing a first association while dissolving a water-soluble polymer in water and slowly adding it to the mixer; and (iii) performing a second association while suspending or dissolving a solubilizing agent in ethanol and slowly adding it to the mixer.
  • the water-soluble polymer is dissolved in water, and the solubilizing agent (surfactant) is suspended or dissolved in ethanol.
  • the method for producing the pharmaceutical composition of the present invention does not use an organic solvent other than ethanol, and the amount of ethanol used is small. In one embodiment, ethanol is used in an amount of less than 25 parts by weight based on 15 to 25 parts by weight of pranlukast.
  • the solubilizer used in the pharmaceutical composition of the present invention is preferably a solid.
  • the physicochemical properties of a paste-type solubilizer may change depending on storage conditions, which may affect the physical properties (particularly, dissolution rate) of the pharmaceutical composition.
  • a liquid-type solubilizer may weaken the cohesiveness of granules during the tableting process, thereby causing tableting problems.
  • the mixer is not limited to a specific one.
  • the mixer may be a high shear granulator commonly used in the pharmaceutical industry.
  • the method for manufacturing the pharmaceutical composition of the present invention may further include (iv) a process of granulating, drying, and sizing the secondary compound.
  • the pharmaceutical composition of the present invention is in the form of a granule containing pranlukast.
  • the method for manufacturing the pharmaceutical composition of the present invention is environmentally friendly because it uses less solvent than other methods of spray drying and granulation, and is economical because it does not require equipment such as a high-speed stirrer or spray dryer.
  • a method of manufacturing a suspension (spray) by adding pranlukast while vigorously stirring a solution composed of a water-soluble polymer or a surfactant (e.g., a propeller-equipped stirrer or a homomixer), or of manufacturing a spray using a high-pressure homogenizer, and then spraying the solution in a fluidized bed granulator or spray dryer of the spray drying method has the disadvantages of using a large amount of solvent and requiring additional equipment compared to the method for manufacturing the pharmaceutical composition of the present invention.
  • a pharmaceutical composition comprising pranlukast, a diluent, a silica-based fluidizing agent, and a disintegrant is uniformly mixed in a high-shear mixer to reduce the interparticle attractive force of pranlukast and improve the cohesion, and polyethylene glycol, a water-soluble polymer, is dissolved in purified water and slowly introduced into the high-shear mixer to perform primary coalescence.
  • the purified water reduces the interparticle attractive force of pranlukast and at the same time increases the solubility of pranlukast by attaching the water-soluble polymer to the surface of the pranlukast particles.
  • a solubilizing agent (surfactant) having a low critical micelle concentration (CMC) is suspended or dissolved in ethanol and slowly introduced into the first coalescence to perform secondary coalescence. This is a process for attaching the solubilizing agent to the first coalescence.
  • the coalescence is granulated as needed, dried in a fluidized bed dryer, and the dried material is granulated to manufacture pharmaceutical granules containing pranlukast.
  • the pharmaceutical composition of the present invention may be a granule containing pranlukast, and the method for producing the pharmaceutical composition of the present invention may be a wet granulation method.
  • the pharmaceutical composition of the present invention can be formulated as a powder, granule, granule, capsule, tablet, dry syrup, etc.
  • the pharmaceutical composition of the present invention can be formulated by including a granule containing pranlukast and an acceptable pharmaceutical additive.
  • Acceptable pharmaceutical excipients may include excipients, disintegrants, glidants, coating agents, etc.
  • Excipients include mannitol, sorbitol, refined sugar, lactose, lactose monohydrate, microcrystalline cellulose, starch, pregelatinized starch, silicified microcrystalline cellulose, corn starch, crystalline cellulose, etc.; disintegrants include sodium starch glycolate, croscarmellose sodium, crospovidone, low-substituted hydroxypropyl cellulose, etc.; and lubricants include magnesium stearate, stearic acid, sodium stearyl fumarate, colloidal silicon dioxide, silicon dioxide, etc.
  • a process of film coating using a coating agent may be included.
  • Opadry series may be used as the coating agent.
  • the type and content of pharmaceutical additives can be selected according to the properties of the composition and can be appropriately selected according to the formulation.
  • the excipients may be included in an amount of 1 to 80 parts by weight, the disintegrant in an amount of 1 to 20 parts by weight, the lubricant in an amount of 0.1 to 10 parts by weight, and the coating agent in an amount of 1 to 5 parts by weight, based on 15 to 25 parts by weight of pranlukast.
  • Pranlukast, diluent, fluidizing agent, and disintegrant which were micronized to D(0.50) of 0.1 to 2.0 ⁇ m and D(0.90) of 1.6 to 7.0 ⁇ m, were placed in a high-shear mixer and mixed.
  • a water-soluble polymer (hydroxypropyl cellulose) was dissolved in water and slowly introduced into the high-shear mixer to perform the first association, and each solubilizing agent was suspended or dissolved in ethanol to perform the second association. Thereafter, granulation was performed, and the solvent was evaporated using a fluidized bed dryer. The dried product was granulated to obtain a granule containing pranlukast.
  • Table 1 The compositions of each example are as shown in the following Table 1.
  • Granules containing pranlukast were obtained in the same manner as in Examples 1 to 5.
  • the compositions of each example are as shown in Table 2 below.
  • Granules containing pranlukast were obtained in the same manner as in Examples 1 to 5.
  • the compositions of each example are as shown in Table 3 below.
  • Tablets were manufactured from the granules manufactured in Examples 2, 6, 7, 8, 10, and 15 with the ingredients and contents of Table 4.
  • the granules containing pranlukast and excipients, disintegrants, lubricants, and coating agents were placed in a mixer, and mixing and lubricating were performed, and tableting and coating processes were performed to manufacture Examples 16 to 21.
  • a comparative dissolution test was conducted on one coated tablet obtained by pressing the granules manufactured in Examples 1 to 5 and two Onon capsules (pranlukast 112.5 mg/capsule, 2 capsules taken at a time, Dong-A ST) according to the paddle method of the second dissolution test method of the Korean Pharmacopoeia.
  • the test method is as follows.
  • Test Example 2 Comparative dissolution test by water-soluble polymer and solubilizing agent content
  • Example 21 manufactured as coated tablets of Example 15, and commercially available Onon capsules (112.5 mg*2 caps) were used to evaluate the kinetics in the human body.
  • the tablets manufactured in Example 21 (Example 21, pranlukast 50 mg/tablet, 1 tablet) (Group 1) and the commercially available preparation (Onon capsule 112.5 mg/cap., 2 capsules, total pranlukast 225 mg) (Group 2) were administered cross-wise with 200 mL of water on an empty stomach. The washout period was set to 2 weeks. Approximately 5.0 mL of blood was collected immediately before administration and at 0.25, 0.50, 0.75, 1.00, 1.50, 2.00, 2.50, 3.00, 3.50, 4.00, 5.00, 6.00, 7.00, 8.00, 10.00, 12.00, and 24.00 hours after administration.
  • the collected blood was placed in a vacuum polyethylene tube containing K3EDTA and centrifuged at 1538 ⁇ 10g for 15 minutes.
  • the plasma was collected, transferred to a polyethylene tube, and stored frozen at 120°C ⁇ 5°C until analysis.
  • the concentration of pranlukast in the plasma was analyzed using UPLC-MS/MS. The results of the analysis are presented in Table 5 and Fig. 3.
  • Example 21 tablet manufactured by the manufacturing method according to the present invention showed the same level of T/R Ratio of AUC 0-t and C max even when administered at a much lower dose (50 mg) than the existing commercially available formulation, Onon Capsule 2 capsules (pranlukast 225 mg), confirming that it can show the same level of efficacy as the commercially available formulation.
  • T max appears faster than the existing commercially available formulation, patients with bronchial asthma and allergic rhinitis, which are indications for pranlukast, can expect a faster onset of efficacy when taking it, and it was found to be an improvement in therapeutic terms compared to the existing commercially available formulation.

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Abstract

La présente invention concerne une composition pharmaceutique ayant une biodisponibilité améliorée du pranlukast, et un procédé de préparation s'y rapportant, et, plus spécifiquement, une composition pharmaceutique et un procédé de préparation s'y rapportant, la composition comprenant, sur la base de 15 à 25 parties en poids de pranlukast, de 0,1 à 10 parties en poids d'un polymère hydrosoluble et de 0,1 à 5 parties en poids d'un superplastifiant à base de silice, présentant ainsi une efficacité médicamenteuse qui est au moins cliniquement égale à celle des formulations disponibles dans le commerce même si la quantité de pranlukast est réduite à 50 mg/comprimé ou moins (1 comprimé pris deux fois par jour), et améliore ainsi l'observance médicamenteuse du patient et réduit les effets secondaires provoqués par la prise d'une quantité excessive de pranlukast.
PCT/KR2024/012778 2023-10-12 2024-08-27 Composition pharmaceutique ayant une biodisponibilité améliorée du pranlukast, et procédé de préparation s'y rapportant Pending WO2025079861A1 (fr)

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KR1020230136112A KR20250052834A (ko) 2023-10-12 2023-10-12 프란루카스트의 생체이용률이 개선된 약제학적 조성물 및 그 제조방법
KR10-2023-0136112 2023-10-12

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20080071557A (ko) * 2005-11-24 2008-08-04 오노 야꾸힝 고교 가부시키가이샤 고형 제제 및 제제 조성물
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