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Fluorouracil rectal temperature-sensitive emulsion having bio-adhesion and preparation method of emulsion

A fluorouracil and bioadhesion technology, which can be applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problem of low absorption efficiency of fluorouracil, poor patient compliance, and uneven drug distribution. and other problems to achieve the effect of reducing adverse reactions, slow absorption, and increasing strength

Active Publication Date: 2016-06-01
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0032] The technical problem to be solved by the present invention is aimed at the short residence time of the existing rectal drug preparations in the rectum, uneven drug distribution, large local irritation, poor drug absorption and low bioavailability, poor patient compliance, and the treatment of colorectal To address the problems of low absorption efficiency of cancer drug fluorouracil through mucosa, short biological half-life, and large mucosal irritation, a bioadhesive fluorouracil temperature-sensitive emulsion for rectal use is provided, and a preparation method thereof

Method used

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  • Fluorouracil rectal temperature-sensitive emulsion having bio-adhesion and preparation method of emulsion
  • Fluorouracil rectal temperature-sensitive emulsion having bio-adhesion and preparation method of emulsion
  • Fluorouracil rectal temperature-sensitive emulsion having bio-adhesion and preparation method of emulsion

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Experimental program
Comparison scheme
Effect test

preparation example Construction

[0105] The preparation of test sample: the proportioning of fixed P407 / P188 is respectively (19.0 / 10.0; 17.0 / 15.0) in this embodiment, and drug microemulsion is respectively (55ml, 66ml, 77ml), and adhesive agent is respectively (0.2%, 0.3%, 0.4%), that is, 100mL temperature-sensitive emulsion contains P40717.0g, 19.0g, P18815.0g, 10.0g respectively, and fluorouracil microemulsion is (55ml: of which fluorouracil 0.83g, soybean oil 18.3mL, Span804.2mL, Tween800.83mL, 1.2-propanediol 4.2mL, 66ml: of which fluorouracil 1g, soybean oil 22mL, Span805mL, Tween801mL, 1.2-propanediol 5mL, 66ml: of which fluorouracil 1.1g, soybean oil 25.7mL, Span805.7mL, Tween801.1mL, 1.2 -Propylene glycol 5.7mL,), adhesive agent is respectively 0.2g, 0.3g, 0.4g.

[0106] The gel temperature measurement method is as described above.

[0107] Selection requirements: the phase transition temperature is more suitable in the range of 10-20 °C.

[0108] Table 2 Effect table of bioadhesives and drug micro...

Embodiment 1

[0135] Embodiment 1: Prescription 1

[0136] Prescription: 1

[0137]

[0138]

[0139] Add distilled water to 100mL.

[0140] (1) Mix soybean oil, Span80, Tween80 and 1.2-propanediol in a certain proportion, keep stirring at 45°C and 2000 rpm, add an appropriate amount of 5-FU aqueous solution drop by drop, and continue stirring for 10 minutes to obtain a white microemulsion .

[0141] (2) Preparation of temperature sensitive emulsion

[0142] Mix Poloxamer 407 and Poloxamer 188 with water and store in a refrigerator at 4-10°C to form a clear solution;

[0143] The carbomer is evenly sprinkled into water under full stirring to make it fully swell to obtain a bioadhesive material solution.

[0144] Then fully mix fluorouracil microemulsion, poloxamer solution, and bioadhesive material solution at 4°C, then add water to make the content of each component reach a predetermined concentration, and slowly rise to room temperature to obtain bioadhesive fluorouracil Temper...

Embodiment 2-9

[0145] Embodiment 2-9: Prescription 2-9

[0146] Table 7 Prescriptions 2-9

[0147]

[0148] Add distilled water to 100mL.

[0149] (1) Mix soybean oil, Span80, Tween80 and 1.2-propanediol in a certain proportion, keep stirring at 45°C and 2000 rpm, add an appropriate amount of 5-FU aqueous solution drop by drop, and continue stirring for 10 minutes to obtain a white microemulsion .

[0150] (2) Preparation of temperature sensitive emulsion

[0151] Mix Poloxamer 407 and Poloxamer 188 with water and store in a refrigerator at 4-10°C to form a clear solution;

[0152] Sprinkle polycarbofil into water evenly under full stirring to make it fully swell to obtain a bioadhesive material solution.

[0153] Then fully mix fluorouracil microemulsion, poloxamer solution, and bioadhesive material solution at 4°C, then add water to make the content of each component reach a predetermined concentration, and slowly rise to room temperature to obtain bioadhesive fluorouracil Temperatur...

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Abstract

The invention provides a fluorouracil micro-emulsion as well as a rectal emulsion having bio-adhesion and temperature sensitivity and a preparation method of the emulsion. The micro-emulsion is prepared from the fluorouracil and a temperature-sensitive material and a bio-adhesion material are added into the micro-emulsion so that the rectal emulsion is prepared. The preparation is in the form of a solid under a room-temperature storage state, so that the stability of the preparation is enhanced; the preparation, which is refrigerated at 10 DEG C within a short time before being used, can be transformed into an emulsion which can flow freely, and the emulsion, after being used, can rapidly spread and cure in a rectum; the characteristics of a solid preparation and a liquid preparation are integrated; the emulsion is large in contact area between medicines and rectum surface, good in biocompatibility and excellent in strength and bio-adhesion force, and the emulsion can be firmly attached to rectal mucosa, so that an action time is prolonged; the medicine micro-emulsion carried in the preparation is high in transmucosal absorption efficiency; and the medicines are prevented from directly contacting mucosal tissues, so that irritation of the medicines to the rectal mucosa is relieved, the bioavailability and the treatment effect of the medicines are improved, and adverse reactions are reduced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a fluorouracil microemulsion and a bioadhesive temperature-sensitive emulsion for rectum containing the same and a preparation method thereof. Background technique [0002] Colorectal cancer is a malignant tumor with increasing incidence. Because it penetrates deep into the pelvis, surgery is difficult, and the postoperative recurrence and metastasis rates are high. The current treatment is mainly radical resection, supplemented by comprehensive treatment of radiotherapy and chemotherapy. Fluorouracil (also known as 5-fluorouracil, 5-FU) is an antimetabolite antineoplastic drug that can inhibit thymidine deoxynucleotide synthetase and hinder DNA synthesis. It is the basic drug for the treatment of colorectal cancer. For injection and oral administration. 5-FU has a short biological half-life and a narrow range of drug safety. Its main adverse reactions are ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/513A61K47/34A61K47/38A61K47/36A61K47/32A61P35/00
Inventor 王璐璐郑稳生陈少华相莉张秀立张宇佳魏曼张楠
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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