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CN-122005510-A - Momordant mometasone furoate dry powder inhalant without carrier and preparation method thereof

CN122005510ACN 122005510 ACN122005510 ACN 122005510ACN-122005510-A

Abstract

The invention discloses a carrier-free mometasone furoate dry powder inhalant and a preparation method thereof, and relates to the technical field of pharmaceutical preparations, wherein the carrier-free mometasone furoate dry powder inhalant comprises mometasone furoate and an excipient, and the preparation method comprises the following steps of firstly mixing the mometasone furoate with the excipient according to a mass ratio of 10:90-90:10, transferring the mixture into a beaker, adding an ethanol-water mixed solution, and stirring until solids are completely dissolved to obtain spray-dried raw material liquid; and then spray drying the spray-dried raw material liquid by a spray dryer, and collecting a product after drying to obtain microspheres, namely the carrier-free mometasone furoate dry powder inhalant, wherein lactose is not required to be used as a carrier in the carrier-free mometasone furoate dry powder inhalant, so that the risk of allergy possibly caused by lactose is avoided, and a microsphere structure with surface folds is formed by a spray drying technology, so that the medicine mainly exists in an amorphous state, and the dispersibility and the solubility of mometasone furoate are obviously improved.

Inventors

  • ZHANG QIAN
  • LIU PENG
  • LI HONGYANG
  • HE GANGMIN
  • ZHENG XIN

Assignees

  • 江苏德迈药业有限公司

Dates

Publication Date
20260512
Application Date
20260318

Claims (8)

  1. 1. The carrier-free mometasone furoate dry powder inhalant is characterized by comprising mometasone furoate and an excipient, wherein the mass ratio of the mometasone furoate to the excipient is 10:90-90:10.
  2. 2. The carrier-free mometasone furoate dry powder inhalant according to claim 1 wherein the excipient is selected from at least one of polysaccharides, amino acids, phospholipids, polymers and surfactants.
  3. 3. The carrier-free mometasone furoate dry powder inhalant of claim 2 wherein the polysaccharide excipient comprises at least one of trehalose, chitosan derivatives, inulin and hyaluronic acid, the amino acid excipient comprises at least one of leucine, leucine derivatives, trileucine and glycine, the phospholipid excipient comprises at least one of dipalmitoyl phosphatidylcholine and distearoyl phosphatidylcholine, the polymer excipient comprises at least one of polylactic acid-glycolic acid copolymer, polyvinylpyrrolidone and polyvinyl alcohol, and the surfactant excipient comprises at least one of poloxamer and tween 80.
  4. 4. A method for preparing a carrier-free mometasone furoate dry powder inhalant, which is characterized by being used for preparing the carrier-free mometasone furoate dry powder inhalant according to any one of claims 1-3, and specifically comprising the following steps: s1, mixing mometasone furoate with an excipient according to a mass ratio of 10:90-90:10, transferring the mixture into a beaker, then adding an ethanol-water mixed solution, and stirring until the solid is completely dissolved to obtain spray-dried raw material liquid; S2, spray drying the spray drying raw material liquid by adopting a spray dryer, and collecting a product after drying to obtain microspheres, namely the carrier-free mometasone furoate dry powder inhalant.
  5. 5. The method for preparing a carrier-free mometasone furoate dry powder inhalant of claim 4, wherein the volume fraction of ethanol in the ethanol-water mixed solution in S1 is 10% -90%.
  6. 6. The method for preparing the carrier-free mometasone furoate dry powder inhalant of claim 4, wherein the atomizing gas sprayed and dried in the step S2 is N 2 , the gas flow rate is 10-90 m 3 /h, and the raw material sample injection flow rate is 1-30 mL/min.
  7. 7. The method for preparing a carrier-free mometasone furoate dry powder inhalant of claim 4 wherein the inlet temperature of the spray drying in S2 is 70-150 ℃.
  8. 8. Use of a carrier-free mometasone furoate dry powder inhaler according to any one of claims 1 to 3 in the manufacture of a medicament for treating acute lung injury or acute respiratory distress syndrome.

Description

Momordant mometasone furoate dry powder inhalant without carrier and preparation method thereof Technical Field The invention relates to the technical field of pharmaceutical preparations, in particular to a carrier-free mometasone furoate dry powder inhalant and a preparation method thereof. Background Acute lung injury (Acute lung injury, ALI) is non-cardiac pulmonary edema caused by injury of pulmonary capillary endothelial cells and alveolar epithelial cells in the case of severe infection, shock, trauma, etc., and further causes progressive hypoxia and dyspnea, and acute respiratory distress syndrome (Acute respiratory distress syndrome, ARDS) may be caused when severe. ALI is used as a clinical common critical illness, the incidence is rapid, the death rate is up to 45%, and the disease course and prognosis treatment are all the time hot spots of clinical researches. Mometasone furoate (Mometasone Furoate, MF) belongs to glucocorticoid medicines and has anti-inflammatory, antiallergic and other pharmacological activities. Compared with the budesonide of the same kind, the budesonide has better solubility and quick effect, has been widely applied to the treatment of allergic rhinitis, chronic obstructive pulmonary disease, asthma and other diseases, but the budesonide has larger irritation to local tissues. The mometasone furoate has slightly poor solubility and slow onset of action, is only used for treating eczema and rhinitis at present, and is greatly limited in application in the field of treating lung diseases. Dry powder inhalants are one of the important dosage forms for pulmonary administration, and conventional dry powder inhalants often use lactose as a carrier to improve the dispersibility and pulmonary deposition properties of the drug, but lactose may cause allergic reactions in some patients, and the presence of the carrier may affect the drug release efficiency. At present, related documents and patent reports on the use of mometasone furoate carrier-free dry powder inhalants for treating lung diseases are not available. Therefore, the application aims to provide a carrier-free mometasone furoate dry powder inhalant and a preparation method thereof, so as to solve the problems of poor solubility of mometasone furoate, lactose allergy risk, poor medicine dispersibility and low release efficiency of the dry powder inhalant which relies on lactose as a carrier in the prior art. Disclosure of Invention The invention aims to provide a carrier-free mometasone furoate dry powder inhalant and a preparation method thereof, which are used for solving the problems of poor solubility of mometasone furoate, lactose allergy risk, poor medicine dispersibility and low release efficiency of the dry powder inhalant which relies on lactose as a carrier in the prior art. In order to achieve the purpose, the invention provides a carrier-free mometasone furoate dry powder inhalant which comprises mometasone furoate and an excipient, wherein the mass ratio of the mometasone furoate to the excipient is 10:90-90:10. Further, the excipient is at least one of polysaccharides, amino acids, phospholipids, polymers and surfactants. Further, the polysaccharide excipient comprises at least one of trehalose, chitosan derivatives, inulin and hyaluronic acid, the amino acid excipient comprises at least one of leucine, leucine derivatives, trileucine and glycine, the phospholipid excipient comprises at least one of dipalmitoyl phosphatidylcholine (DPPC) and distearoyl phosphatidylcholine (DSPC), the polymer excipient comprises at least one of polylactic acid-glycolic acid copolymer (PLGA), polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA), and the surfactant excipient comprises at least one of poloxamer and tween 80. The invention also discloses a preparation method of the carrier-free mometasone furoate dry powder inhalant, which is used for preparing the carrier-free mometasone furoate dry powder inhalant and specifically comprises the following steps of: s1, mixing mometasone furoate with an excipient according to a mass ratio of 10:90-90:10, transferring the mixture into a beaker, then adding an ethanol-water mixed solution, and stirring until the solid is completely dissolved to obtain spray-dried raw material liquid; S2, spray drying the spray drying raw material liquid by adopting a spray dryer, and collecting a product after drying to obtain microspheres, namely the carrier-free mometasone furoate dry powder inhalant. Further, the volume fraction of the ethanol in the ethanol-water mixed solution in the step S1 is 10% -90%. Further, the atomizing gas for spray drying in the step S2 is N 2, the gas flow rate is 10-90 m 3/h, and the raw material sample injection flow rate is 1-30 mL/min. Further, the inlet temperature of the spray drying in the step S2 is 70-150 ℃. The invention also discloses application of the carrier-free mometasone furoate dry powder inhalant in medicines for treating acute lung injury or a