Method for determining enzyme dissolution of bexarotene softgel

A technology of soft capsules and dissolution media, applied in the field of medicine, can solve the problems of unbreakable swelling of preparations, affecting the measurement of capsule preparations, cross-linking of soft capsules, etc., and achieve the effect of overcoming the reduction of in vitro release

Active Publication Date: 2019-11-15
HUMANWELL PURACAP PHARM WUHAN CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, software capsules are affected by environmental factors such as temperature, humidity, oxidation, heat sensitivity, and UV light, which easily lead to chemical interactions between the gelatin in the capsule shell and the contents. Shaped substances, it is difficult to release or not rupture, that is, the phenomenon of cross-linking and bonding of soft capsules occurs, making the preparations swell without breaking, limiting the release of drugs, and affecting the determination of the dissolution rate of capsule preparations in vitro

Method used

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  • Method for determining enzyme dissolution of bexarotene softgel
  • Method for determining enzyme dissolution of bexarotene softgel
  • Method for determining enzyme dissolution of bexarotene softgel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: the method for measuring the dissolution of besarotene soft capsule plus enzyme

[0032] (1) Prepare phosphate buffer solution: prepare 2100ml of 0.05M potassium dihydrogen phosphate solution and 450ml of 0.2M sodium hydroxide solution, add water to 6 liters, adjust pH to 7.5±0.05 with phosphoric acid or sodium hydroxide;

[0033] Prepare dissolution medium A with the above-mentioned phosphate buffer solution: add 80.0 mg of trypsin to 4 liters of phosphate buffer solution and stir evenly;

[0034] Prepare dissolution medium B with the above-mentioned phosphate buffer solution: add 30g HDTMA to 2 liters of phosphate buffer solution and stir at 37°C for 1 hour;

[0035] (2) Run the dissolution apparatus: the setting conditions are the slurry method, the dissolution speed is 75rpm / min, the temperature is 37°C, and the dissolution time is 45 minutes;

[0036] (3) Preparation of the test solution: add 600ml of dissolution medium A to the dissolution cup, run ...

Embodiment 2

[0046] Embodiment 2: Dissolution methodological research

[0047] 1. Dissolution speed and dissolution medium are added step by step: when the amount of trypsin in dissolution medium A is 20mg / L, the dissolution time is 45min, the dissolution volume is 900ml, and the speed is 50rpm / min, 75rpm / min, and 100rpm / min, the dissolution The dissolution rate of medium A and dissolution medium B mixed and added and added step by step, the results are shown in Table 1, wherein 900ml (A+B) refers to the addition of dissolution medium in one step, which includes the phosphate buffer solution of the present invention , trypsin and HDTMA, the preparation method is: add 80mg of trypsin and 30g of HDTMA to 6L of phosphate buffer, stir at 37°C for 1h.

[0048] Table 1 The results of dissolution speed and dissolution medium added step by step

[0049]

[0050] The result shows that directly adding 900ml dissolution medium, the soft capsule does not dissolve. Add in steps, and when the disso...

Embodiment 3

[0059] Embodiment 3: HPLC methodology verification

[0060] 1. Linear

[0061] 1.1 Preparation of reference substance stock solution

[0062] Weigh 80mg of besarotene compound standard into a 100ml volumetric flask (concentration is 800ug / mL), first dissolve it with 30ml of methanol, and then use the dissolution medium (the volume ratio of dissolution medium A to dissolution medium B is 2:1) Volume.

[0063] 1.2 Precisely pipette the reference substance stock solution according to Table 4

[0064] The pipetting of table 4 reference substance stock solution

[0065] sample Volume of control stock solution constant volume Concentration (ug / mL) 1 2mL 100mL 16 2 4mL 100mL 32 3 4mL 50mL 64 4 5mL 50mL 80 5 15mL 100mL 120

[0066] 1.3 The linearity measured by HPLC is y=26835.929x+6749.964, R 2 = 1.000.

[0067] 2. Precision

[0068] According to the dissolution method of the present invention, 6 besarotene soft ...

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Abstract

The invention discloses a method for determining enzyme dissolution of a bexarotene softgel. The method mainly comprises preparation of a dissolution medium, preparation of a tested solution, preparation of a contrast solution and determination. The method can more effectively reflect dissolution and release in the enzyme dissolution of bexarotene softgel, overcomes the problem of reduction of in-vitro release degree due to gelatin crosslinking in the capsule material, and can objectively reflect the practical dissolution and the preparation quality of the softgel.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a method for measuring the dissolution of bexarotene soft capsules plus enzymes. Background technique [0002] Bexarotene is a new type of retinoic acid analogue, a new generation of drugs that act on RXR receptors, and is mainly used for the treatment of cutaneous T-cell lymphoma, non-small cell lung cancer, breast cancer and psoriasis. However, it belongs to the class II compound of the biopharmaceutical classification system (BCS), and has poor solubility and low bioavailability. In view of the characteristics of high stability, anti-oxidation, convenient administration, and high bioavailability of soft capsules, Besarotene soft capsules were developed by combining besarotene with soft capsules, which can improve drug stability and reduce dosage for patients. [0003] However, software capsules are affected by environmental factors such as temperature, humidity, oxidation, heat sensit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G01N30/02
CPCG01N30/02
Inventor 李琳刘波高婷文学智刘丽蔡波涛叶翔
Owner HUMANWELL PURACAP PHARM WUHAN CO LTD
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