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.