CN102085199B - Percutaneous absorption biological patch for treating rheumatoid arthritis and preparing method thereof - Google Patents

Percutaneous absorption biological patch for treating rheumatoid arthritis and preparing method thereof Download PDF

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Publication number
CN102085199B
CN102085199B CN200910112919.9A CN200910112919A CN102085199B CN 102085199 B CN102085199 B CN 102085199B CN 200910112919 A CN200910112919 A CN 200910112919A CN 102085199 B CN102085199 B CN 102085199B
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China
Prior art keywords
rheumatoid arthritis
water
biological
percutaneous absorption
biological patch
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CN200910112919.9A
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CN102085199A (en
Inventor
林绥
彭华毅
邓思珊
黄郑隽
阙慧卿
钱丽萍
连建清
郭舜民
齐一萍
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FUJIAN ACADEMY OF MEDICAL SCIENCES
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FUJIAN ACADEMY OF MEDICAL SCIENCES
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Abstract

The invention relates to a percutaneous absorption biological patch for treating rheumatoid arthritis and preparing method thereof. The biological patch consists of basic remedy treating for the rheumatoid arthritis, medicament solvent, adhesive, biological plaster matrix and percutaneous absorption penetration enhancer. The basic remedies treating for the rheumatoid arthritis include triptolide and analgesics lidocaine hydrochloride alleviating the pain of the rheumatoid arthritis. The biological plaster has comprehensive pharmacological effect, exactly blocks up the main pathology link of development of rheumatoid arthritis, has strong pertinency and lasting pharmacological effect; and can be prepared by using a general method in biological plaster preparing technology field; and the preparing method is simple.

Description

Percutaneous absorption biological patch for the treatment of rheumatoid arthritis and preparation method thereof
Technical field
The present invention relates to field of pharmaceutical preparations and formulation method, especially relate to a kind of rheumatoid arthritis for the treatment of and have percutaneous absorption biological patch of topical pain relief and preparation method thereof concurrently.
Background technology
Radix Tripterygii Wilfordii lactone alcohol (triptolide) is the chemical composition of extracting from Celastraceae tripterygium plant Radix Tripterygii Wilfordii.From pharmacological action: (1) Radix Tripterygii Wilfordii lactone alcohol had both had non-specific antiinflammatory immunity function, having again to suppress is main immunization.(2) Acute and chronic inflammation is all had to obvious inhibitory action, and with hypophysis--system is relevant, be mainly to cause that by hypophysis ACTH discharges, adrenal cortex reinforcing secretory function.(3) research that is applied to adjuvant arthritis shows: rat assist agent arthritis is had to obvious inhibitory action, and rat assist agent arthritis is the animal model of research antirheumatic, and its histopathology changes very similar to people's rheumatoid arthritis.In a word, the pharmacological action of Radix Tripterygii Wilfordii lactone alcohol is comprehensive, just blocks the main pathology link of rheumatoid arthritis disease progression, with strong points, evident in efficacy.It not only has the dual function that remission and the state of an illness are alleviated concurrently, also there is the effect of parahormone sample and immunoregulation effect, but it is non-hormone again, multiple the acting on all over the body of collection multiclass medicine, is that two class resisting rheumatoid arthritis Western medicine and amcinonide are incomparable.Lignocaine is widely used Bangesic clinically, can play the symptom of rheumatoid arthritis patient pain, alleviates patient's misery.
At present, existing many about research report and the patent of patch, but do not have for the biological patch of Radix Tripterygii Wilfordii lactone alcohol and lignocaine specially, therefore there is no its preparation method yet.
Summary of the invention
The object of the invention is to provide a kind of percutaneous absorption biological patch for the treatment of rheumatoid arthritis, the principal agent of this biological patch sustained release for a long time, and pharmacological effect is lasting, and formula is simple.
The percutaneous absorption biological for the treatment of rheumatoid arthritis pastes technical scheme:
A kind of percutaneous absorption biological patch for the treatment of rheumatoid arthritis, wherein contain principal agent, drug solvent, binding agent, biological patch substrate and the Transdermal absorption penetrating agent for the treatment of rheumatoid arthritis, the principal agent for the treatment of rheumatoid arthritis is Radix Tripterygii Wilfordii lactone alcohol and the analgesic lidocaine hydrochloride of alleviating rheumatoid arthritis pain.
The optimum weight proportioning that the percutaneous absorption biological of described treatment rheumatoid arthritis pastes each composition is: principal agent (1): principal agent (2): drug solvent: Transdermal absorption penetrating agent: binding agent and biological paste substrate: solvent=0.01~0.2 ‰: 1~2 ‰: 3~8%: 1~10%: 13~18%: 65~81%.
The present invention also provides a kind of formula of percutaneous absorption biological patch for the treatment of rheumatoid arthritis, is Radix Tripterygii Wilfordii lactone alcohol 6.0mg, lidocaine hydrochloride 1.2g, sodium polyacrylate 0.25g, PVA-124 3.0g, gelatin 3.0g, lanoline 5.0g, white vaseline 2.5g, glycerol 7.5g, azone 1.0g, Kaolin 1g, azone 1.0g, distilled water 45ml.
The present invention provides a kind of preparation method of percutaneous absorption biological patch for the treatment of rheumatoid arthritis simultaneously, and (1) dissolves 0.25g sodium polyacrylate and places 24h with 10ml distilled water; (2) Radix Tripterygii Wilfordii lactone alcohol 6mg is dissolved in to 2ml dehydrated alcohol, in water-bath, is heated to dissolve, then is dissolved in 5.0g lanoline, in water-bath, be heated to dissolve; (3) add white vaseline 2.5g, mix; (3) lidocaine hydrochloride of use 10ml water dissolution 1.2g; (4) with the PVA-124 of 20ml distilled water dissolving 3.0g, in water-bath, heat about 10min and dissolve; (5) with the gelatin of 15ml distilled water dissolving 3.0g, in water-bath, heat about 5min and dissolve; (6) grind Kaolin with a small amount of water; (7) all substrate is mixed, add lidocaine hydrochloride aqueous solution, heat about 10min, add 7.5g glycerol, add 1.0g azone, stir 1h, obtain biological patch 60g, coating.
Beneficial effect:
This percutaneous absorption biological patch:
(1) percutaneous drug absorption, directly enters body circulation, avoids medicine to be subject to liver sausage first-pass effect;
(2) be not subject to the impact of gastrointestinal tract various factors, yet directly gastrointestinal tract do not caused and stimulated or other adverse effect;
(3) have slow release long-acting feature, can reach 24 hours, only need be administered once every day;
(4) extremely easy to use, without oral or injection;
(5) safety, the almost toxic reaction of medication as none, has particularly avoided the toxicity of Radix Tripterygii Wilfordii lactone alcohol;
(6) if in use there is untoward reaction, also can wipe immediately, stop administration.
This percutaneous absorption biological patch preparation method is simple, and small investment need not be purchased main equipment and adopt complicated technique.
The specific embodiment
The percutaneous absorption biological patch for the treatment of rheumatoid arthritis is made up of principal agent, drug solvent, binding agent, biological paste substrate and the Transdermal absorption penetrating agent for the treatment of rheumatoid arthritis, and principal agent is Radix Tripterygii Wilfordii lactone alcohol and the analgesic lidocaine hydrochloride of alleviating rheumatoid arthritis pain.
Drug solvent be from monohydric alcohol, dihydroxylic alcohols, trihydroxylic alcohol, esters, select a kind or 2 kinds and more than.
Drug solvent is a kind or 2 kinds in ethanol, propylene glycol, glycerol, 1,2 propylene glycol, Polyethylene Glycol, isopropyl alcohol, 2-octyldodecanol, ketopyrrolidine, METHYLPYRROLIDONE.
Binding agent and biological paste substrate are a kind or 2 kinds or 3 kinds in PVAC polyvinylalcohol-124, PVAC polyvinylalcohol-1788, PVAC polyvinylalcohol-0588, PVA-1750, PVP, CMC-Na, HPMC, lanoline, white vaseline, Kaolin, Polyethylene Glycol PEG-400, gelatin, Carbomer-940, sodium polyacrylate, silicone rubber, zein, polyvinyl butyral resin, polyacrylic resin III.
Transdermal absorption penetrating agent is wherein a kind or 2 kinds of lauryl alcohol, laurocapram (azone), Borneolum Syntheticum, Camphora, isopropyl myristate (IPM).
The optimum weight proportioning of the each composition of percutaneous absorption biological patch for the treatment of rheumatoid arthritis is: principal agent (1): principal agent (2): drug solvent: Transdermal absorption penetrating agent: binding agent and biological paste substrate: solvent=0.01~0.2 ‰: 1~2 ‰: 3~8%: 1~10%: 13~18%: 65~81%.
Take treatment rheumatoid arthritis percutaneous absorption biological patch formula as:
Radix Tripterygii Wilfordii lactone alcohol 6.0mg
Lidocaine hydrochloride 1.2g
Lanoline 5.0g
Sodium polyacrylate 0.25g
PVA-124 3.0g
Gelatin 3.0g
White vaseline 2.5g
Glycerol 7.5g
Kaolin 1.0g
Azone 1.0g
Distilled water 45ml
60g coating
The percutaneous absorption biological patch that the present invention treats rheumatoid arthritis can adopt the general method adopting in biological paste preparing technical field to prepare, and method is: (1) dissolves 0.25g sodium polyacrylate and places 24h with 10ml distilled water; (2) Radix Tripterygii Wilfordii lactone alcohol 6mg is dissolved in to 2ml dehydrated alcohol, in water-bath, is heated to dissolve, then is dissolved in 5.0g lanoline, in water-bath, be heated to dissolve; (3) add white vaseline 2.5g, mix; (3) lidocaine hydrochloride of use 10ml water dissolution 1.2g; (4) with the PVA-124 of 20ml distilled water dissolving 3.0g, in water-bath, heat about 10min and dissolve; (5) with the gelatin of 15ml distilled water dissolving 3.0g, in water-bath, heat about 5min and dissolve; (6) grind Kaolin with a small amount of water; (7) all substrate is mixed, add lidocaine hydrochloride aqueous solution, heat about 10min, add 7.5g glycerol, add 1.0g azone, stir 1h, obtain biological patch 60g, coating.
The container in the present invention, dress biological paste being used has special regulation: carton or medicinal plastic bag.
In the present invention, if necessary, can also suitably add and can be used for biological patch or operable additive, as PH regulators such as malic acid, phosphoric acid, citric acid, tartaric acid, lactic acid, diethanolamine, triethanolamine, diisopropanolamine (DIPA)s; The surfactants such as shrink pears sugar alcohol fatty acid ester, fatty acid glyceride, polyoxyethylene hydrogenation Semen Ricini, polyoxyethylene stearyl base ether, polyoxy ethyl lauryl ether, sodium lauryl sulfate; Lanoline, paraffin, olive are pulled oil, almond oil, polyisoprene, propylene glycol, colza wet goods softening agent; The astringent such as zinc oxide, aluminum sulfate; The antiseptic such as propyl p-hydroxybenzoate.

Claims (2)

1. a percutaneous absorption biological patch for the treatment of rheumatoid arthritis, is characterized in that: the formula of this biological patch is: Radix Tripterygii Wilfordii lactone alcohol 6.0mg, lidocaine hydrochloride 1.2g, sodium polyacrylate 0.25g, PVA-124 3.0g, gelatin 3.0g, lanoline 5.0g, white vaseline 2.5g, glycerol 7.5g, azone 1.0g, Kaolin 1g, distilled water 45ml.
2. a preparation method for the treatment of the percutaneous absorption biological patch of rheumatoid arthritis, is characterized in that: (1) dissolves 0.25g sodium polyacrylate and places 24h with 10ml distilled water; (2) Radix Tripterygii Wilfordii lactone alcohol 6mg is dissolved in to 2ml dehydrated alcohol, in water-bath, is heated to dissolve, then is dissolved in 5.0g lanoline, in water-bath, be heated to dissolve; (3) add white vaseline 2.5g, mix; (4) lidocaine hydrochloride of use 10ml water dissolution 1.2g; (5) with the PVA-124 of 20ml distilled water dissolving 3.0g, in water-bath, heat 10min and dissolve; (6) with the gelatin of 15ml distilled water dissolving 3.0g, in water-bath, heat 5min and dissolve; (7) grind Kaolin with a small amount of water; (8) all substrate is mixed, add lidocaine hydrochloride aqueous solution, heating 10min, adds 7.5g glycerol, adds 1.0g azone, stirs 1h, obtains biological patch 60g, coating.
CN200910112919.9A 2009-12-08 2009-12-08 Percutaneous absorption biological patch for treating rheumatoid arthritis and preparing method thereof Expired - Fee Related CN102085199B (en)

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Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102018696B (en) * 2010-11-22 2013-07-03 北京泰德制药股份有限公司 Skin external preparation containing lidocaine or pharmaceutical salt thereof
CN105434446B (en) * 2015-11-21 2018-03-02 中南大学湘雅医院 Triptolide traditional Chinese medicine compound film coating agent and preparation method and application thereof
CN113398101B (en) * 2021-07-30 2022-06-28 温州医科大学附属眼视光医院 Compound lidocaine gel patch

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1095278A (en) * 1993-05-14 1994-11-23 安庆市余良卿制药厂 Tripterygium wilfordii plaster
CN1634033A (en) * 2004-11-10 2005-07-06 广州市瑞迅生物科技有限公司 Triptolide nano lipsome gelling agent of external use and its preparation method
WO2009075094A1 (en) * 2007-12-11 2009-06-18 Medrx Co., Ltd. Tape preparation comprising etodolac in ionic liquid form

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1095278A (en) * 1993-05-14 1994-11-23 安庆市余良卿制药厂 Tripterygium wilfordii plaster
CN1634033A (en) * 2004-11-10 2005-07-06 广州市瑞迅生物科技有限公司 Triptolide nano lipsome gelling agent of external use and its preparation method
WO2009075094A1 (en) * 2007-12-11 2009-06-18 Medrx Co., Ltd. Tape preparation comprising etodolac in ionic liquid form

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