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Dutasteride soft capsule and preparation method thereof

A technology for dutasteride and soft capsules, applied in the field of improved dutasteride soft capsules and the preparation thereof, can solve the problems of slow disintegration, low dissolution of dutasteride soft capsules, unstable quality, etc. The effect of promoting disintegration, ensuring gastrointestinal safety, and avoiding safety hazards

Active Publication Date: 2019-03-01
HAINAN HUALON PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the problems of low dissolution, slow disintegration and unstable quality within the validity period of dutasteride soft capsules currently available on the market, the inventors provided a product with good dissolution, stable quality and safety through repeated prescription screening and experiments. Good dutasteride soft capsule and preparation method thereof

Method used

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  • Dutasteride soft capsule and preparation method thereof
  • Dutasteride soft capsule and preparation method thereof
  • Dutasteride soft capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～5

[0041] Embodiments 1-5 and Comparative Example: Preparation of Dutasteride Soft Capsules

[0042] 1. Preparation of Example Samples: According to the prescription of dutasteride soft capsules of Examples 1 to 5 of the present invention in Table 2, 1000 dutasteride soft capsules were prepared according to the following steps:

[0043] (1) Preparation of contents: Weigh the prescribed amount of caprylic triglyceride and heat it to 55-65°C, add the prescribed amount of raw materials dutasteride, surfactant, suspending agent and dibutyl hydroxytoluene, and stir until Dissolve completely, and control the temperature at 50°C to 60°C;

[0044] (2) Preparation of soft capsule shell: Weigh the prescribed amount of glycerin, disintegrating agent, opacifier and purified water, heat to 75-80°C in a chemical glue tank, mix evenly with gelatin under stirring condition, and vacuum remove Air, filtered for use;

[0045] (3) Pill making: the contents containing dutasteride are divided into s...

Embodiment 6

[0051] Embodiment 6: investigation on dissolution rate of dutasteride soft capsule

[0052] Sample preparation: prepare respective samples according to Examples 1-5 and comparative examples, and set aside. Commercially available dutasteride with a storage period similar to that of the prepared samples was purchased for investigation. The following other embodiments are the same.

[0053] Investigation method: according to the basket method in the "0391 Dissolution and Release Determination Method" in the 2015 edition of "Chinese Pharmacopoeia", the rotating speed is 50 revolutions / min, and the market conditions of the examples and samples, and dutasteride soft capsules are taken respectively. For commercial products, each 6 capsules were tested for dissolution rate. Measure the dissolution rate in 900ml 2.0% SDS 0.1mol / L hydrochloric acid solution (simulated gastric juice) at 37±0.5°C, take 5mL samples regularly at 5, 10, 15, 20, 30, and 45 minutes respectively, and use HPLC...

Embodiment 7

[0056] Example 7: Investigation of Dutasteride Soft Capsules Crosslinking Degree and Disintegration Time

[0057] Inspection method:

[0058] (1) Processing of the sample capsule shell: take the example sample, comparative example sample and commercially available product, cut the soft capsule sample along the middle slit, extrude the contents, wash the capsule shell 3 times with absolute ethanol, and dry to The water content is about 10%, and it is reserved.

[0059] (2) Determination of equilibrium swelling amount (Seq): different samples were placed at 40° C. and RH 75% for 3 months, and samples were taken regularly. For each sampling, take 6 pieces of sample films from different sample capsules, label them separately, weigh them precisely, place them in 500m1 distilled water at 20°C for swelling, take out the films at 1, 2, 2.5, 3, 3.5, and 4 hours and wipe off the surface with filter paper liquid, precisely weighed. In addition, 6 pieces were taken and dried at 105°C t...

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Abstract

The invention discloses a Dutasteride soft capsule which is good in dissolving out, stable in quality and good in safety. A content of the Dutasteride soft capsule comprises the ingredients by weightpercentage: 0.076%-0.230% of Dutasteride, 74.49%-91.52% of caprylic triglyceride, 7.31%-21.93% of a surfactant, 1.08%-3.32% of a suspending agent and 0.01%-0.032% of an antioxidant butylated hydroxytoluene; a shell of the Dutasteride soft capsule comprises the following ingredients by weight percentage: 31.86%-53.10% of gelatin, 9.56%-15.93% of a plasticizer glycerinum, 1.60%-5.31% of a disintegrating agent, 0.13%-0.22% of a light-screening agent and water. The invention further discloses a preparation process of the Dutasteride soft capsule, and by controlling the heating temperature of the content and controlling the drying conditions of the soft capsule, the dissolving-out situation and the quality stability of the Dutasteride soft capsule are effectively improved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an improved dutasteride soft capsule and a preparation method thereof. Background technique [0002] Benign prostatic hyperplasia (BPH) is one of the high-incidence species in middle-aged and elderly men, and dutasteride is one of the mainstream drugs for treating BPH at home and abroad. However, the water solubility of the original drug of dutasteride is extremely low (0.908mg / L), and the dissolution rate of the preparation in water is relatively poor, resulting in low oral bioavailability (<60%) of the currently commercially available dutasteride soft capsules. The inventors have found through research that the reasons for the lower dissolution rate of dutasteride soft capsules on the market are not only the poor water solubility of dutasteride original drug itself, but also the quality difference with dutasteride soft capsules during the storage period. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K47/14A61K47/10A61K47/18A61K31/58A61P13/08
CPCA61K9/4808A61K9/4816A61K9/4825A61K9/4858A61K31/58
Inventor 郑朝武吴至录唐凤来
Owner HAINAN HUALON PHARM
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