Composition with improved dissolution property

A technology of composition and acidic polymer, which is applied in the field of medicine, can solve the problems of research, lack of dissolution test, insufficient physical stability, etc., and achieve the effect of improving dissolution rate and solubility, good stability, and favorable absorption

Active Publication Date: 2020-07-31
NEOFORM BIOPHARMACEUTICAL LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above publications (including their patent family members) have not carried out dissolution tests, nor have they carried out sufficient physical stability studies

Method used

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  • Composition with improved dissolution property
  • Composition with improved dissolution property
  • Composition with improved dissolution property

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1: Sorafenib: preparation of HPMCP salt

[0047] Sorafenib free base and HPMCP are added into a mixed solvent of methanol and ethyl acetate (1:1 volume ratio) to form a solution, and an ionic bond is formed between the basic sorafenib and the acidic polymer HPMCP.

[0048] 1.2 g of HPMCP was dissolved in a certain volume of solvent by magnetic stirring, then 0.8 g of sorafenib free base was added and allowed to dissolve. Transfer the solution to a 100mL volumetric flask, and add a certain volume of solvent to constant volume.

[0049] The obtained Sorafenib containing 40% Sorafenib (mass ratio): HPMCP salt is passed through the Büchi miniature spray dryer B290 ( Labortechnik AG, Switzerland) spray-dried separation. A high-performance cyclone separator is used for separation, and the 50mL blue cap flask can be directly mounted to the cyclone separator for product collection. The parameter settings of the spray drying process are shown in Table 1.

[0050...

Embodiment 2

[0054] Embodiment 2: Gefitinib: preparation of HPMCP salt

[0055] Add gefitinib free base and HPMCP into a mixed solvent of methanol and dichloromethane (1:1 volume ratio) to form a solution, and an ionic bond is formed between the basic gefitinib and the acidic polymer HPMCP.

[0056] 1.2 g of HPMCP was dissolved in a certain volume of solvent by magnetic stirring, then 0.8 g of gefitinib free base was added and allowed to dissolve. Transfer the solution to a 100mL volumetric flask, and add a certain volume of solvent to constant volume.

[0057] The resulting gefitinib containing 40% gefitinib (mass ratio): HPMCP salt was passed through the Büchi miniature spray dryer B290 ( Labortechnik AG, Switzerland) spray-dried separation. A high-performance cyclone separator is used for separation, and the 50mL blue cap flask can be directly mounted to the cyclone separator for product collection. The parameter settings of the spray drying process are shown in Table 2.

[0058] ...

Embodiment 3

[0061] Embodiment 3: Erlotinib: preparation of HPMCP salt

[0062] Erlotinib free base and HPMCP are added into a mixed solvent of methanol and dichloromethane (1:1 volume ratio) to form a solution, and an ionic bond is formed between the basic erlotinib and the acidic polymer HPMCP.

[0063] Dissolve 0.8 g of HPMCP in a volume of solvent by magnetic stirring, then add 1.2 g of erlotinib free base and allow to dissolve. Transfer the solution to a 100mL volumetric flask, and add a certain volume of solvent to constant volume.

[0064] The resulting Erlotinib containing 60% Erlotinib (mass ratio): HPMCP salt was passed through a Büchi miniature spray dryer B290 equipped with an inert cycle B295 ( Labortechnik AG, Switzerland) spray-dried separation. A high-performance cyclone separator is used for separation, and the 50mL blue cap flask can be directly mounted to the cyclone separator for product collection. The parameter settings of the spray drying process are shown in Ta...

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Abstract

The invention relates to a composition with an improved dissolution property. The composition comprises a salt formed by alkaline tinibs drug molecules and an acidic polymer. The composition with theimproved dissolution property comprises the salt formed by alkaline tinibs drug molecules and the acidic polymer, alkaline tinibs drugs are dispersed in the acidic polymer at a molecular level to forman amorphous solid dispersion, ionic bonds are formed between the alkaline tinibs drug molecules and the acidic polymer, the stability is good, and the dissolution property is improved. The dissolution rate and solubility of the composition are improved, so that the composition can be favorably absorbed by a patient.

Description

technical field [0001] The present invention relates to the field of medicine, and more particularly, to a composition with improved dissolution properties. Background technique [0002] Tini drugs are tyrosine kinase inhibitors, which are a change to the traditional cancer treatment plan, because they have a very high selectivity for cancer cells, so that they do not kill normal cells, and have become one of the first-line anti-tumor drugs. one. Although it has been widely used in clinical practice, solid oral drugs of tinib have the problems of poor water solubility and low bioavailability, and the clinical dosage is relatively high. [0003] The recommended dose of commercially available Sorafenib tablets is 400 mg each time, twice a day, for the treatment of advanced renal cell carcinoma and primary hepatocellular carcinoma. The absolute bioavailability of the drug is low, generally considered to be less than 50%, and only 8.43% in rats (Biomaterials 2014, 35, 4565). ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/61A61K31/44A61K31/5377A61K31/517A61P35/00
CPCA61K31/44A61K31/517A61K31/5377A61K47/61A61P35/00
Inventor 斯蒂芬·R·布林丹·史密斯帕梅拉·A·史密斯田芳安妮·齐默尔曼高明
Owner NEOFORM BIOPHARMACEUTICAL LTD
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