Propranolol hydrochloride lipidosome gel and preparation method thereof

Abstract

The invention discloses a propranolol hydrochloride lipidosome gel, which is prepared by the following bulk drugs and auxiliary materials by weight percent: 0.012-0.075% of propranolol hydrochloride, 0.037-0.150% of phosphatidyl ethanolamine, 0.012-0.075% of cholesterol, 2.5-5% of triethanolamine, 1-2% of carbopol, and the balance of water. According to the propranolol hydrochloride lipidosome gel, during the preparation, the lipidosome is uniformly dispersed in the gel, so that the stability of the lipidosome is improved; the water-soluble gel carbopol has excellent biocompatibility, can be well adhered to skin and cannot stimulate skin; drug administration time is prolonged, the toxic and side effects on the whole body are reduced, the adaptability of patients is improved, and the propranolol hydrochloride lipidosome gel has excellent application prospect.

Description

technical field

[0001] The invention relates to a propranolol hydrochloride liposome gel and a preparation method thereof. Background technique

[0002] Infantile hemangioma is the most common benign tumor in infancy. The incidence of hemangioma at birth is 1.1% to 2.6%, and the incidence can be as high as 10% to 12% within one year of age. Current clinical treatment methods include: laser therapy, drug therapy, radiation therapy, and surgery. Laser therapy includes argon ion laser, CO 2 Laser, flash lamp pump pulsed dye laser, Nd:YAG laser, etc., but laser treatment will cause certain damage to the skin. Common drug treatments include oral hormone therapy (such as prednisone), intratumoral injection of hormone or pingyangmycin, and injection of IFN-α, all of which have certain side effects on infants and young children. The cost of surgical treatment is high, the operation is difficult, and the degree of risk is high. This shows that when the above-mentioned method is ...

Examples

Embodiment 1

[0026] Weigh 30 mg of phosphatidylethanolamine and 5 mg of cholesterol, dissolve in 10 ml of organic solvent chloroform, and evaporate the mixed solution to dryness under reduced pressure until a uniform lipid film is formed. Add the lipid film to 20ml of propranolol hydrochloride solution with pH=7.4 (drug concentration is 0.75mg / ml, prepared by adding propranolol hydrochloride to PBS buffer with pH7.4), dissolve, 60 Hydrate in a water bath for 60 min to obtain propranolol hydrochloride liposomes.

[0027] Weigh 500 mg of carbomer into a beaker, add a certain amount of distilled water to make the gel concentration 2% (mass percentage), stir on a magnetic stirrer for 3 hours to make the gel swell evenly, and then place it in a refrigerator at 4°C overnight (12h) to fully expand it. The next day, the propranolol hydrochloride liposome was mixed with the gel, and then 620 mg of triethanolamine was added to adjust the pH to 7 to obtain the propranolol hydrochloride liposome gel....

Embodiment 2

[0029] Weigh 30 mg of phosphatidylethanolamine and 10 mg of cholesterol, dissolve in 10 ml of organic solvent chloroform, and evaporate the mixed solution to dryness under reduced pressure until a uniform lipid film is formed. Add the lipid film to 20ml of propranolol hydrochloride solution (drug concentration: 1.50mg / ml) at pH=7.4, dissolve, and hydrate for 60min in a water bath at 60°C to obtain propranolol hydrochloride liposomes.

[0030] Weigh 500 mg of carbomer into a beaker, add a certain amount of distilled water to make the gel concentration 2% (mass percentage), stir on a magnetic stirrer for 3 hours to make the gel swell evenly, and then place it in a refrigerator at 4°C overnight (12h) to fully expand it. The next day, the propranolol hydrochloride liposome was mixed with the gel, and then 665 mg of triethanolamine was added to adjust the pH to be 8 to obtain the propranolol hydrochloride liposome gel.

Embodiment 3

[0032] Weigh 60 mg of phosphatidylethanolamine and 5 mg of cholesterol, dissolve in 10 ml of organic solvent chloroform, and evaporate the mixed solution to dryness under reduced pressure until a uniform lipid film is formed. Add the lipid film to 20ml of propranolol hydrochloride solution (drug concentration: 1.50mg / ml) at pH=7.4, dissolve, and hydrate for 60min in a water bath at 60°C to obtain propranolol hydrochloride liposomes.

[0033] Weigh 500 mg of carbomer into a beaker, add a certain amount of distilled water to make the gel concentration 2% (mass percentage), stir on a magnetic stirrer for 3 hours to make the gel swell evenly, and then place it in a refrigerator at 4°C overnight (12h) to fully expand it. On the next day, the propranolol hydrochloride liposome was mixed with the gel, and then 665 mg of triethanolamine was added to adjust the pH to 7 to obtain the propranolol hydrochloride liposome gel.

technical field

[0001] The invention relates to a propranolol hydrochloride liposome gel and a preparation method thereof. Background technique

[0002] Infantile hemangioma is the most common benign tumor in infancy. The incidence of hemangioma at birth is 1.1% to 2.6%, and the incidence can be as high as 10% to 12% within one year of age. Current clinical treatment methods include: laser therapy, drug therapy, radiation therapy, and surgery. Laser therapy includes argon ion laser, CO 2 Laser, flash lamp pump pulsed dye laser, Nd:YAG laser, etc., but laser treatment will cause certain damage to the skin. Common drug treatments include oral hormone therapy (such as prednisone), intratumoral injection of hormone or pingyangmycin, and injection of IFN-α, all of which have certain side effects on infants and young children. The cost of surgical treatment is high, the operation is difficult, and the degree of risk is high. This shows that when the above-mentioned method is ...

Examples

Embodiment 1

[0026] Weigh 30 mg of phosphatidylethanolamine and 5 mg of cholesterol, dissolve in 10 ml of organic solvent chloroform, and evaporate the mixed solution to dryness under reduced pressure until a uniform lipid film is formed. Add the lipid film to 20ml of propranolol hydrochloride solution with pH=7.4 (drug concentration is 0.75mg / ml, prepared by adding propranolol hydrochloride to PBS buffer with pH7.4), dissolve, 60 Hydrate in a water bath for 60 min to obtain propranolol hydrochloride liposomes.

[0027] Weigh 500 mg of carbomer into a beaker, add a certain amount of distilled water to make the gel concentration 2% (mass percentage), stir on a magnetic stirrer for 3 hours to make the gel swell evenly, and then place it in a refrigerator at 4°C overnight (12h) to fully expand it. The next day, the propranolol hydrochloride liposome was mixed with the gel, and then 620 mg of triethanolamine was added to adjust the pH to 7 to obtain the propranolol hydrochloride liposome gel....

Embodiment 2

[0029] Weigh 30 mg of phosphatidylethanolamine and 10 mg of cholesterol, dissolve in 10 ml of organic solvent chloroform, and evaporate the mixed solution to dryness under reduced pressure until a uniform lipid film is formed. Add the lipid film to 20ml of propranolol hydrochloride solution (drug concentration: 1.50mg / ml) at pH=7.4, dissolve, and hydrate for 60min in a water bath at 60°C to obtain propranolol hydrochloride liposomes.

[0030] Weigh 500 mg of carbomer into a beaker, add a certain amount of distilled water to make the gel concentration 2% (mass percentage), stir on a magnetic stirrer for 3 hours to make the gel swell evenly, and then place it in a refrigerator at 4°C overnight (12h) to fully expand it. The next day, the propranolol hydrochloride liposome was mixed with the gel, and then 665 mg of triethanolamine was added to adjust the pH to be 8 to obtain the propranolol hydrochloride liposome gel.

Embodiment 3

[0032] Weigh 60 mg of phosphatidylethanolamine and 5 mg of cholesterol, dissolve in 10 ml of organic solvent chloroform, and evaporate the mixed solution to dryness under reduced pressure until a uniform lipid film is formed. Add the lipid film to 20ml of propranolol hydrochloride solution (drug concentration: 1.50mg / ml) at pH=7.4, dissolve, and hydrate for 60min in a water bath at 60°C to obtain propranolol hydrochloride liposomes.

[0033] Weigh 500 mg of carbomer into a beaker, add a certain amount of distilled water to make the gel concentration 2% (mass percentage), stir on a magnetic stirrer for 3 hours to make the gel swell evenly, and then place it in a refrigerator at 4°C overnight (12h) to fully expand it. On the next day, the propranolol hydrochloride liposome was mixed with the gel, and then 665 mg of triethanolamine was added to adjust the pH to 7 to obtain the propranolol hydrochloride liposome gel.

Images