Abstract: The invention discloses a lenalidomide gastro-retentive sustained-release tablet and a preparation method thereof. The sustained-release tablet comprises 3 wt % to 14 wt % of lenalidomide, 14 wt % to 68 wt % of release enhancer with low bulk density, 23 wt % to 70 wt % of sustained-release material with low bulk density, and the balance of other pharmaceutically acceptable excipients, wherein the bulk density of the release enhancer ranges from 0.24 g/cm3 to 0.52 g/cm3; and the bulk density of the sustained-release material ranges from 0.29 g/cm3 to 0.51 g/cm3. The sustained-release tablet of the invention is in a floating state in a gastric environment, is not directly discharged from a stomach due to gastric emptying, has an effect of gastric retention, and is not easily discharged with substances contained in the stomach, and has a high drug bioavailability and small side effects.

Abstract: In the present invention, the whole preparation process of the sustained-release microparticles is at normal or low temperature, which is highly advantageous for the preparation of a polymer-based composition from a high-temperature-sensitive drug, particularly a protein, nucleic acid and peptide drug, and the bioactivity of the active substance can be maintained to the greatest extent throughout the process compared to the disclosed technology; at the same time, the prepared sustained-release microparticles have an excellent sustained-release effect close to zero order, and the drug concentration is stabilized during the release, which overcomes the defects that the microparticles obtained by the conventional S/O/W process of pre-preparing the drug microparticles have no drug release in the earlier stage and a rapid release of the drug in the later stage; and in addition, the sustained-release microparticles have higher drug loading rate and drug encapsulation rate.

Abstract: A tertiary amine pharmaceutical composition includes a drug having a tertiary amine structure, a biocompatible polymer material, and a quaternary ammonium salt impurity. The pharmaceutical composition is obtained by dissolving or dispersing the drug in a halogenated hydrocarbon or a mixed solvent mainly containing halogenated hydrocarbon or a solution containing halogenated hydrocarbon. The quaternary ammonium salt impurity is generated from reacting the drug having the tertiary amine structure with the halogenated hydrocarbon. The pharmaceutical composition comprises 40 wt % to 80 wt % of the biocompatible polymer material, and 20 wt % to 60 wt % of the drug with the tertiary amine structure. The content of the quaternary ammonium salt impurity is less than 0.05 wt %, the content of the halogenated hydrocarbon in the composition is less than 1.5 wt %, and the quaternary ammonium salt impurity does not increase or increases slowly during storage, which complies with requirements of pharmaceutical regulations.

Abstract: The whole preparation process of the sustained-release microparticles is at normal or low temperature, which is highly advantageous for the preparation of a polymer-based composition from a high-temperature-sensitive drug, particularly a protein, nucleic acid and peptide drug, and the bioactivity of the active substance can be maintained to the greatest extent throughout the process compared to the disclosed technology; at the same time, the prepared sustained-release microparticles have an excellent sustained-release effect close to zero order, and the drug concentration is stabilized during the release, which overcomes the defects that the microparticles obtained by the conventional S/O/W process of pre-preparing the drug microparticles have no drug release in the earlier stage and a rapid release of the drug in the later stage; and in addition, the sustained-release microparticles have higher drug loading rate and drug encapsulation rate.

Abstract: The present invention relates to a targeted hydrophobic anti-tumor drug nanoformulation, which comprises a hydrophobic anti-tumor drug and a carrier with a mass ratio of 1:4-32.5, wherein the carrier is composed of 37.5-95.3 wt % albumin and 4.7-62.5 wt % hyaluronic acid-albumin conjugate, and the hyaluronic acid-albumin conjugate is prepared by albumin and hyaluronic acid with a molar ratio of 1:1-20. A preparation method of the nanoformulation comprises: preparing hyaluronic acid-albumin conjugate; formulating carrier solution; formulating drug solution; and preparing nanoformulation. The nanoformulation has even particle size distribution and good dispersibility, is stable without aggregating. The particle size of the lyophilized nanoformulation after being redissolved substantially remains unchanged, the yield of the nanoformulation is high and the efficacy is good after being filtered by a millipore filter (0.22 ?m).

Abstract: In the present invention, the whole preparation process of the sustained-release microparticles is at normal or low temperature, which is highly advantageous for the preparation of a polymer-based composition from a high-temperature-sensitive drug, particularly a protein, nucleic acid and peptide drug, and the bioactivity of the active substance can be maintained to the greatest extent throughout the process compared to the disclosed technology; at the same time, the prepared sustained-release microparticles have an excellent sustained-release effect close to zero order, and the drug concentration is stabilized during the release, which overcomes the defects that the microparticles obtained by the conventional S/O/W process of pre-preparing the drug microparticles have no drug release in the earlier stage and a rapid release of the drug in the later stage; and in addition, the sustained-release microparticles have higher drug loading rate and drug encapsulation rate.

Abstract: The invention discloses a lenalidomide gastro-retentive sustained-release tablet and a preparation method thereof. The sustained-release tablet comprises 3 wt % to 14 wt % of lenalidomide, 14 wt % to 68 wt % of release enhancer with low bulk density, 23 wt % to 70 wt % of sustained-release material with low bulk density, and the balance of other pharmaceutically acceptable excipients, wherein the bulk density of the release enhancer ranges from 0.24 g/cm3 to 0.52 g/cm3; and the bulk density of the sustained-release material ranges from 0.29 g/cm3 to 0.51 g/cm3. The sustained-release tablet of the invention is in a floating state in a gastric environment, is not directly discharged from a stomach due to gastric emptying, has an effect of gastric retention, and is not easily discharged with substances contained in the stomach, and has a high drug bioavailability and small side effects.

Abstract: The present invention relates to a targeted hydrophobic anti-tumor drug nanoformulation, which comprises a hydrophobic anti-tumor drug and a carrier with a mass ratio of 1:4-32.5, wherein the carrier is composed of 37.5-95.3 wt % albumin and 4.7-62.5 wt % hyaluronic acid-albumin conjugate, and the hyaluronic acid-albumin conjugate is prepared by albumin and hyaluronic acid with a molar ratio of 1:1-20. A preparation method of the nanoformulation comprises: preparing hyaluronic acid-albumin conjugate; formulating carrier solution; formulating drug solution; and preparing nanoformulation. The nanoformulation has even particle size distribution and good dispersibility, is stable without aggregating. The particle size of the lyophilized nanoformulation after being redissolved substantially remains unchanged, the yield of the nanoformulation is high and the efficacy is good after being filtered by a millipore filter (0.22 ?m).

Abstract: The whole preparation process of the sustained-release microparticles is at normal or low temperature, which is highly advantageous for the preparation of a polymer-based composition from a high-temperature-sensitive drug, particularly a protein, nucleic acid and peptide drug, and the bioactivity of the active substance can be maintained to the greatest extent throughout the process compared to the disclosed technology; at the same time, the prepared sustained-release microparticles have an excellent sustained-release effect close to zero order, and the drug concentration is stabilized during the release, which overcomes the defects that the microparticles obtained by the conventional S/O/W process of pre-preparing the drug microparticles have no drug release in the earlier stage and a rapid release of the drug in the later stage; and in addition, the sustained-release microparticles have higher drug loading rate and drug encapsulation rate.

Abstract: In the present invention, the whole preparation process of the sustained-release microparticles is at normal or low temperature, which is highly advantageous for the preparation of a polymer-based composition from a high-temperature-sensitive drug, particularly a protein, nucleic acid and peptide drug, and the bioactivity of the active substance can be maintained to the greatest extent throughout the process compared to the disclosed technology; at the same time, the prepared sustained-release microparticles have an excellent sustained-release effect close to zero order, and the drug concentration is stabilized during the release, which overcomes the defects that the microparticles obtained by the conventional S/O/W process of pre-preparing the drug microparticles have no drug release in the earlier stage and a rapid release of the drug in the later stage; and in addition, the sustained-release microparticles have higher drug loading rate and drug encapsulation rate.