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A kind of method for measuring the dissolution of besarotene soft capsules with enzyme

A technology of soft capsule and dissolution medium, applied in the field of medicine, can solve the problems of unbreakable swelling of preparations, difficult to release, cross-linking and combination of soft capsules, etc., and achieve the effect of overcoming the reduction of in vitro release degree

Active Publication Date: 2022-04-22
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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  • A kind of method for measuring the dissolution of besarotene soft capsules with enzyme
  • A kind of method for measuring the dissolution of besarotene soft capsules with enzyme
  • A kind of method for measuring the dissolution of besarotene soft capsules with enzyme

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Experimental program
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Effect test

Embodiment 1

[0031] Example 1: The method for measuring the dissolution of besarotene soft capsules with enzyme

[0032] (1) Preparation of 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, and adjust the pH to 7.5±0.05 with phosphoric acid or sodium hydroxide;

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

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

[0035] (2) run the dissolution apparatus: the setting condition is 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 into the dissolution vessel, run the instrument to 37°C, ad...

Embodiment 2

[0046] Example 2: Dissolution Methodology Study

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

[0048] Table 1 The results of the step-by-step addition of the dissolution speed and the dissolution medium

[0049]

[0050] The results showed that the soft capsules did not diss...

Embodiment 3

[0059] Example 3: HPLC method validation

[0060] 1. Linear

[0061] 1.1 Preparation of reference stock solution

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

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

[0064] Table 4 Pipetting of 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 capsules were randomly selected, and the dis...

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Abstract

The invention discloses a method for measuring the dissolution of besarotene soft capsules with enzymes. The method mainly includes the preparation of dissolution medium, the preparation of test solution, the preparation and measurement of reference solution. This method more realistically reflects the dissolution and release behavior of Besarotene soft capsules in vivo, overcomes the problem of reduced in vitro release due to the cross-linking of gelatin in the capsule material, and objectively reflects the actual dissolution and release behavior of Besarotene soft capsules. formulation quality.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a method for measuring the dissolution of besarotene soft capsules with enzymes. Background technique [0002] Besarotene is a new type of retinoic acid analog, a new generation of drugs acting on the RXR receptor, 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), with 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 can be developed by combining besarotene and software capsules, which can improve drug stability and reduce the dosage of patients. [0003] However, the software capsule is affected by the environment such as temperature, humidity, oxidation, heat sensitivity, U...

Claims

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Application Information

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Patent Type & Authority Patents(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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