Dutasteride soft capsule preparation and preparation process thereof

Abstract

The invention discloses a dutasteride soft capsule preparation, comprising a soft capsule and contents. A prescription for the contents comprises 0.5 g of a dutasteride raw material, 200 to 250 g of labrasol, 30 to 60 g of polyglycerol oleate, 50 to 100 g of medium-chain triglyceride and 0.02 to 0.05 g of 2,6-di-t-butyl p-cresol. The dutasteride soft capsule prepared in the invention is substantially improved in accumulated dissolution in 5 minutes of dissolving-out and enhanced in the dissolving-out efficiency of a main drug in a preceding time period and has good stability and good appearance quality.

Description

technical field

[0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a dutasteride soft capsule preparation and a preparation process thereof. Background technique

[0002] Dutasteride is a 5α-reductase inhibitor. There are two subtypes of 5α-reductase, namely type I and type II. Type I isozyme acts on the reproductive system, and type II isozyme mainly acts on the skin and Hepatic testosterone conversion. Dutasteride is 60 times more effective at inhibiting type I 5α reductase than finasteride, and it also has a strong effect on type II. Dutasteride can inhibit the conversion of testosterone into dihydrotestosterone (DHT), thereby inhibiting the production of male DHT. production, thereby inhibiting the growth of the prostate in BPH patients. Clinically, it is mainly used for the treatment of enlarged prostate, male pattern alopecia, seborrheic alopecia, and hereditary alopecia.

[0003] The dosage form of dutasteride on th...

Examples

Embodiment 1

[0057] Prescription of contents of dutasteride soft capsule preparation:

[0058] Dutasteride raw material 0.5g; caprylic capric acid macrogol glyceride 220g;

[0059] Polyglycerol oleate 45g; medium chain triglyceride 75g;

[0060] 0.035 g of 2,6-di-tert-butyl-p-cresol.

[0061] Softgel prescription:

[0062] Gelatin 160mg; Glycerin 85mg;

[0063] Yellow iron oxide 0.28mg; titanium dioxide 2mg.

[0064] Preparation:

[0065] (1) Preparation of contents: Take the prescription amount of caprylic capric acid macrogolglyceride, polyglycerol oleate and medium chain triglyceride and stir evenly, add the prescribed amount of dutasteride raw material after heating up to 40°C drug and 2,6-di-tert-butyl-p-cresol, continue to stir for 1h until uniform, and then cool down to room temperature to obtain the content;

[0066] (2) Preparation of soft capsules: Take the prescribed amount of glycerin, add water, put it in a plastic tank, stir and mix evenly, then add titanium dioxide and...

Embodiment 2

[0069] Prescription of contents of dutasteride soft capsule preparation:

[0070] Dutasteride raw material 0.5g; caprylic capric acid macrogol glyceride 225g;

[0071] Polyglycerol oleate 50g; medium chain triglyceride 72g;

[0072] 0.038g of 2,6-di-tert-butyl-p-cresol.

[0073] Softgel prescription:

[0074] Gelatin 165mg; Glycerin 83mg;

[0075] Yellow iron oxide 0.27mg; titanium dioxide 2.2mg.

[0076] Preparation:

[0077] (1) Preparation of contents: Take the prescription amount of caprylic capric acid macrogolglyceride, polyglycerol oleate and medium chain triglyceride and stir evenly, add the prescribed amount of dutasteride raw material after heating up to 40°C drug and 2,6-di-tert-butyl-p-cresol, continue to stir for 1h until uniform, and then cool down to room temperature to obtain the content;

[0078] (2) Preparation of soft capsules: Take the prescribed amount of glycerin, add water, put it in a plastic tank, stir and mix evenly, then add titanium dioxide and ...

Embodiment 3

[0081] Prescription of contents of dutasteride soft capsule preparation:

[0082] Dutasteride raw material 0.5g; caprylic capric acid macrogol glyceride 220g;

[0083] Polyglycerol oleate 45g; medium chain triglyceride 75g;

[0084] Softgel prescription:

[0085] Gelatin 160mg; Glycerin 85mg;

[0086] Yellow iron oxide 0.28mg; titanium dioxide 2mg.

[0087] Preparation:

[0088] (1) Preparation of contents: Take the prescription amount of caprylic capric acid macrogolglyceride, polyglycerol oleate and medium chain triglyceride and stir evenly, add the prescribed amount of dutasteride raw material after heating up to 40°C Continue to stir the medicine for 1 hour until it is uniform and then cool down to room temperature to obtain the content;

[0089] (2) Preparation of soft capsules: Take the prescribed amount of glycerin, add water, put it in a plastic tank, stir and mix evenly, then add titanium dioxide and yellow iron oxide passed through an 80-mesh sieve and mix evenl...

technical field

[0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a dutasteride soft capsule preparation and a preparation process thereof. Background technique

[0002] Dutasteride is a 5α-reductase inhibitor. There are two subtypes of 5α-reductase, namely type I and type II. Type I isozyme acts on the reproductive system, and type II isozyme mainly acts on the skin and Hepatic testosterone conversion. Dutasteride is 60 times more effective at inhibiting type I 5α reductase than finasteride, and it also has a strong effect on type II. Dutasteride can inhibit the conversion of testosterone into dihydrotestosterone (DHT), thereby inhibiting the production of male DHT. production, thereby inhibiting the growth of the prostate in BPH patients. Clinically, it is mainly used for the treatment of enlarged prostate, male pattern alopecia, seborrheic alopecia, and hereditary alopecia.

[0003] The dosage form of dutasteride on th...

Examples

Embodiment 1

[0057] Prescription of contents of dutasteride soft capsule preparation:

[0058] Dutasteride raw material 0.5g; caprylic capric acid macrogol glyceride 220g;

[0059] Polyglycerol oleate 45g; medium chain triglyceride 75g;

[0060] 0.035 g of 2,6-di-tert-butyl-p-cresol.

[0061] Softgel prescription:

[0062] Gelatin 160mg; Glycerin 85mg;

[0063] Yellow iron oxide 0.28mg; titanium dioxide 2mg.

[0064] Preparation:

[0065] (1) Preparation of contents: Take the prescription amount of caprylic capric acid macrogolglyceride, polyglycerol oleate and medium chain triglyceride and stir evenly, add the prescribed amount of dutasteride raw material after heating up to 40°C drug and 2,6-di-tert-butyl-p-cresol, continue to stir for 1h until uniform, and then cool down to room temperature to obtain the content;

[0066] (2) Preparation of soft capsules: Take the prescribed amount of glycerin, add water, put it in a plastic tank, stir and mix evenly, then add titanium dioxide and...

Embodiment 2

[0069] Prescription of contents of dutasteride soft capsule preparation:

[0070] Dutasteride raw material 0.5g; caprylic capric acid macrogol glyceride 225g;

[0071] Polyglycerol oleate 50g; medium chain triglyceride 72g;

[0072] 0.038g of 2,6-di-tert-butyl-p-cresol.

[0073] Softgel prescription:

[0074] Gelatin 165mg; Glycerin 83mg;

[0075] Yellow iron oxide 0.27mg; titanium dioxide 2.2mg.

[0076] Preparation:

[0077] (1) Preparation of contents: Take the prescription amount of caprylic capric acid macrogolglyceride, polyglycerol oleate and medium chain triglyceride and stir evenly, add the prescribed amount of dutasteride raw material after heating up to 40°C drug and 2,6-di-tert-butyl-p-cresol, continue to stir for 1h until uniform, and then cool down to room temperature to obtain the content;

[0078] (2) Preparation of soft capsules: Take the prescribed amount of glycerin, add water, put it in a plastic tank, stir and mix evenly, then add titanium dioxide and ...

Embodiment 3

[0081] Prescription of contents of dutasteride soft capsule preparation:

[0082] Dutasteride raw material 0.5g; caprylic capric acid macrogol glyceride 220g;

[0083] Polyglycerol oleate 45g; medium chain triglyceride 75g;

[0084] Softgel prescription:

[0085] Gelatin 160mg; Glycerin 85mg;

[0086] Yellow iron oxide 0.28mg; titanium dioxide 2mg.

[0087] Preparation:

[0088] (1) Preparation of contents: Take the prescription amount of caprylic capric acid macrogolglyceride, polyglycerol oleate and medium chain triglyceride and stir evenly, add the prescribed amount of dutasteride raw material after heating up to 40°C Continue to stir the medicine for 1 hour until it is uniform and then cool down to room temperature to obtain the content;

[0089] (2) Preparation of soft capsules: Take the prescribed amount of glycerin, add water, put it in a plastic tank, stir and mix evenly, then add titanium dioxide and yellow iron oxide passed through an 80-mesh sieve and mix evenl...

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