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Soluble fentanyl and its derivatives buccal film preparation and preparation method thereof

A film preparation and soluble technology, which is applied in the field of soluble fentanyl and its derivatives buccal film preparations and its preparation, can solve the problems of unsatisfactory clinical effects, slow onset of transdermal patches, and difficulty in lasting, and achieve effective Fast-acting, improved bioavailability, long-lasting effects

Active Publication Date: 2017-02-15
LP PHARM (XIAMEN) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Injection, sublingual patch, sublingual spray, and oral patch have a rapid onset of effect, but are difficult to last, while transdermal patches have a slow onset of effect, and the clinical effect is not ideal. Most of the buccal and chewable tablets have Fentanyl enters the gastrointestinal tract through saliva, producing a first-pass effect

Method used

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  • Soluble fentanyl and its derivatives buccal film preparation and preparation method thereof
  • Soluble fentanyl and its derivatives buccal film preparation and preparation method thereof
  • Soluble fentanyl and its derivatives buccal film preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The preparation of embodiment 1 fentanyl buccal instant film

[0048] prescription:

[0049]

[0050]

[0051] step:

[0052] a. Dissolve fentanyl, stevia, glycerin, lactose, menthol, and red iron oxide in 200ml of 80% ethanol solution in sequence;

[0053] b. Dissolve polyvinylpyrrolidone, hydroxymethylcellulose, and xanthan gum in solution a, stir evenly, and let stand overnight for degassing;

[0054] c. Apply liquid b evenly, with a wet film thickness of about 300-400 μm, that is, about 0.05 mg of fentanyl per square centimeter, and dry at 70°C;

[0055] d. After drying, measure the content in units of centimeters.

Embodiment 2

[0056] The preparation of embodiment 2 soluble fentanyl buccal sustained-release film

[0057] prescription:

[0058] name Prescription amount percentage Fentanyl 0.2g 0.43％ Hypromellose K15M 18g 38.54％ sucrose 2g 4.28％ Eudragit L100 12g 25.70％ triethyl citrate 7g 14.99％ microcrystalline cellulose 6g 12.85％ Polysorbate 80 1.2g 2.57％ lemon yellow 0.3g 0.64％

[0059] step:

[0060] a. Mix fentanyl, hypromellose K15M, sucrose, Eudragit L100, microcrystalline cellulose, triethyl citrate, tartrazine evenly;

[0061] b. Hot-melt extruded film-forming agent at 160°C, control the film thickness to 250μm, and contain about 0.1mg of fentanyl per square centimeter

[0062] c. Measure its content in centimeters.

experiment example 3

[0063] Preparation of experimental example 3 soluble fentanyl buccal fast-dissolving slow-release double-layer film

[0064] prescription:

[0065] Instant Film Prescription:

[0066] name Prescription amount percentage Fentanyl 0.1g 1.18％ Polyvinylpyrrolidone K30 2g 23.58％ stevia 0.2g 2.36％ sodium hydroxymethyl cellulose 1.4g 16.51％ glycerin 1.2g 14.15％ lactose 1.6g 18.87％ Menthol 0.3g 3.54％ Iron Oxide Red 0.08g 0.94％ xanthan gum 1.6g 18.87％ 80% ethanol 40ml N / A

[0067] Extended-release film prescription:

[0068] name Prescription amount percentage Fentanyl 0.2g 0.43％ Hypromellose K15M 18g 38.54％ sucrose 2g 4.28％ Eudragit L100 12g 25.70％ triethyl citrate 7g 14.99％ microcrystalline cellulose 6g 12.85％ Polysorbate 80 1.2g 2.57％ lemon yellow 0.3g 0.64％

[0069] Process:

[0070] a. Mix fentanyl, hypromellose K15M,...

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Abstract

The invention discloses soluble fentanyl, a derivative buccal membrane preparation thereof and a preparing method thereof. The soluble fentanyl and the derivative buccal membrane preparation thereof can be instant fentanyl and a derivative buccal membrane preparation thereof, can be soluble slow-release fentanyl and a derivative buccal membrane preparation thereof and also can be instant and soluble slow-release fentanyl and a derivative buccal double-layer-membrane preparation. An instant membrane can be dissolved quickly at a buccal mucosa in one minute at the oral cavity, the fentanyl and a derivative thereof are released, and the clinical effect of efficient analgesia is achieved. A slow-release membrane slowly releases medicine within four hours in the oral cavity, and effective blood concentration is maintained for a long time. An instant-slow-release double-layer membrane has a quick effect, the medicine effect is durable, and continuous analgesia can be achieved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to soluble fentanyl and its derivative buccal film preparation and a preparation method thereof. Background technique [0002] Fentanyl and its analogues, such as alfentanil, carfentanil, lofentanil, remifentanil, sufentanil, trefentanil, etc., are high-efficiency opioid analgesics. 50-100 times that of morphine. The drug effect is similar to that of morphine. In addition to the analgesic effect, it also has the effects of lowering the heart rate, inhibiting breathing, and reducing smooth muscle peristalsis. It is less addictive than morphine, and is suitable for pain relief after and during operations such as surgery and gynecology. The side effects that can be observed in this opioid as well as fentanyl are nausea, circulatory disturbance, constipation or itching and life-threatening shortness of breath, so apart from the part that needs immediate onset, sl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/70A61K31/4468A61P25/04
Inventor 苏艺杰蔡林辉凌榕槟朱海健叶英
Owner LP PHARM (XIAMEN) CO LTD
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