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CN102670624B - Patch for treating rheumatic arthritis and preparation method thereof - Google Patents

Patch for treating rheumatic arthritis and preparation method thereof Download PDF

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Publication number
CN102670624B
CN102670624B CN201110061304.5A CN201110061304A CN102670624B CN 102670624 B CN102670624 B CN 102670624B CN 201110061304 A CN201110061304 A CN 201110061304A CN 102670624 B CN102670624 B CN 102670624B
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CN
China
Prior art keywords
patch
chloroform
preparation
sensitive adhesive
pressure sensitive
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CN201110061304.5A
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Chinese (zh)
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CN102670624A (en
Inventor
林绥
阙慧卿
彭华毅
钱丽萍
黄郑隽
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FUJIAN ACADEMY OF MEDICAL SCIENCES
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FUJIAN ACADEMY OF MEDICAL SCIENCES
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Priority to CN201110061304.5A priority Critical patent/CN102670624B/en
Publication of CN102670624A publication Critical patent/CN102670624A/en
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Expired - Fee Related legal-status Critical Current
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  • Medicinal Preparation (AREA)

Abstract

The invention discloses a patch for treating rheumatic arthritis and a preparation method thereof. The patch consists of a main medicament for treating rheumatic arthritis, a medicament solvent, a substrate and a penetrating agent, wherein the main medicament consists of triptolide and lidocaine serving as a pain-relieving medicament for relieving rheumatic arthritis pain. The patch is medical controlled-release slow release preparation, has a comprehensive pharmacological action, is used for blocking major development pathologic loops of the rheumatic arthritis disease, and has high specificity and a lasting pharmacological effect; and the preparation method is simple.

Description

A kind of 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 and a kind ofly treat rheumatoid arthritis patch having topical pain relief concurrently and preparation method thereof.
Background technology
Patch sticks the thin slice stratiform preparation in human body skin, and wherein percutaneous drug absorption enters the general designation of local target tissue or systemic circulation system, includes the patch of local skin transmission and transdermal delivery.Patch belongs to transdermal delivery system, is the pharmaceutical preparation with better usefulness row, and blood drug level can be kept to be stabilized in the Valid concentration for the treatment of; Owing to avoiding the first pass effect of drug oral through gastrointestinal tract and liver, more stably directly enter blood flow than oral administration, can improve medicine in vivo predictability; Improve safety; Improve the advantages such as the compliance of patient.
Radix Tripterygii Wilfordii lactone alcohol (triptolide) is the chemical composition extracted from Celastraceae tripterygium plant Radix Tripterygii Wilfordii.From pharmacological action: (1) Radix Tripterygii Wilfordii lactone alcohol had both had non-specific antiinflammatory immunity function, have again to suppress the immunization for main.(2) all there is obvious inhibitory action to Acute and chronic inflammation, and with hypophysis--system is relevant, mainly cause ACTH to discharge by hypophysis, adrenal cortex reinforcing secretory function.(3) research being applied to adjuvant arthritis shows: have obvious inhibitory action to rat assist agent arthritis, and rat assist agent arthritis is the animal model of research antirheumatic, and its histopathologic change is very similar to the rheumatoid arthritis of people.In a word, the pharmacological action of Radix Tripterygii Wilfordii lactone alcohol is comprehensive, just blocks the main pathology link of rheumatoid arthritis disease development, with strong points, evident in efficacy.It not only has the dual function of remission and disease amelioration 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, alleviate the misery of patient.
At present, about the research report of patch and patent existing many, but not have for the 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 one to treat rheumatoid arthritis patch, and this patch is the slow releasing preparation of medicine controlled releasing, and principal agent can sustained release for a long time, and pharmacological effect is lasting, and formula is simple.
A kind of patch technologies scheme for the treatment of rheumatoid arthritis is:
One treats rheumatoid arthritis patch, principal agent wherein containing treatment rheumatoid arthritis, drug solvent, binding agent, patch substrate and Transdermal absorption penetrating agent, the principal agent for the treatment of rheumatoid arthritis is Radix Tripterygii Wilfordii lactone alcohol and the analgesic lidocaine hydrochloride alleviating rheumatoid arthritis pain, and the feature of this patch is the slow releasing preparation of medicine controlled releasing.
Described a kind of optimum weight proportioning for the treatment of each composition of rheumatoid arthritis patch is: principal agent (1): principal agent (2): Transdermal absorption penetrating agent: binding agent and patch substrate and solvent=0.1 ~ 1 ‰: 2 ‰: 1 ~ 10%: 65 ~ 95%.
The present invention also provides a kind of formula for the treatment of rheumatoid arthritis patch: Radix Tripterygii Wilfordii lactone alcohol (triptolide, triptolide) 481.5mg, lidocaine hydrochloride 2.4g, polyisobutylene oppanol B 10031.2g, polyisobutylene Oppanol B 1262.5g, lanoline 5.0g, liquid paraffin 15g, Borneolum Syntheticum 12g, 80% ethanol 9g, add chloroform to 1200g.
The present invention provides a kind of preparation method for the treatment of rheumatoid arthritis patch simultaneously, the first step: get high molecular weight polyisobutylene oppanol B 10031.2g and low-molecular-weight polyisobutylene Oppanol B 1262.5g, add chloroform to 1000g, until high and low molec weight polyisobutylene dissolves (pressure sensitive adhesive) for subsequent use completely. second step: dissolve Radix Tripterygii Wilfordii lactone alcohol with appropriate chloroform, dropwise slowly be added in 5g lanoline, limit edged stirs. the 3rd step: get 12g Borneolum Syntheticum and lidocaine hydrochloride 2.4g adds in beaker, dissolve with appropriate 80% ethanol and chloroform.4th step: the lanoline containing medicine is dropwise slowly added to limit edged in pressure sensitive adhesive and stirs.5th step: the dropwise containing 12g Borneolum Syntheticum and lidocaine hydrochloride is slowly added to limit edged in pressure sensitive adhesive and stirs, and add chloroform to 1200g.6th step: the pressure sensitive adhesive electric blender all having added medicine is stirred 1h, places 12h, then stirs 1h by electric blender, places 1-5h, to bubble-free, in impouring TB-300 type composite coating machine, is paved into the patch that thickness is 0.45mm.
Beneficial effect:
This patch:
(1) percutaneous drug absorption, directly enters body circulation, avoids medicine to be subject to liver sausage first-pass effect;
(2) not by the impact of gastrointestinal tract various factors, also directly stimulation or other adverse effect are not caused to gastrointestinal tract;
(3) this patch is the slow releasing preparation of medicine controlled releasing, has slow release long-acting feature, can reach 24 hours, and every day only need be administered once;
(4) extremely easy to use, without the need to oral or injection;
(5) safety, the toxic reaction of almost medication as none, particularly avoids the toxicity of Radix Tripterygii Wilfordii lactone alcohol;
(6) if in use there is untoward reaction, also can wipe immediately, stop administration.
This patch preparation method is simple, small investment, need not purchase main equipment and adopt complicated technique.
Detailed description of the invention
A kind of rheumatoid arthritis patch for the treatment of forms by treating the principal agent of rheumatoid arthritis, drug solvent, binding agent, substrate and Transdermal absorption penetrating agent, and principal agent is Radix Tripterygii Wilfordii lactone alcohol and the analgesic lidocaine hydrochloride alleviating rheumatoid arthritis pain.
Drug solvent is chloroform.
Binding agent and patch substrate are high molecular weight polyisobutylene oppanol B 100with low-molecular-weight polyisobutylene Oppanol B 12.
Transdermal absorption penetrating agent is lauryl alcohol, laurocapram (azone), Borneolum Syntheticum, Camphora, isopropyl myristate (IPM) wherein a kind or 2 kinds.
A kind of optimum weight proportioning for the treatment of each composition of rheumatoid arthritis patch is: principal agent (1): principal agent (2): Transdermal absorption penetrating agent: binding agent and patch substrate and solvent=0.1 ~ 1 ‰: 2 ‰: 1 ~ 10%: 65 ~ 95%.
A kind of formula for the treatment of rheumatoid arthritis patch is:
A kind of preparation method for the treatment of rheumatoid arthritis patch is: the preparation of (1) pressure sensitive adhesive: get high molecular weight polyisobutylene oppanol B 10031.2g and low-molecular-weight polyisobutylene Oppanol B 1262.5g, adds chloroform to 1000g, until high and low molec weight polyisobutylene dissolves for subsequent use completely.(2) dissolve Radix Tripterygii Wilfordii lactone alcohol with appropriate chloroform, be dropwise slowly added in 5g lanoline, limit edged stirs.(3) get 12g Borneolum Syntheticum and lidocaine hydrochloride 2.4g adds in beaker, dissolve with appropriate 80% ethanol and chloroform.(4) lanoline containing medicine is dropwise slowly added to limit edged in pressure sensitive adhesive to stir.(5) dropwise containing 12g Borneolum Syntheticum and lidocaine hydrochloride is slowly added to limit edged in pressure sensitive adhesive to stir, and adds chloroform to 1200g.(6) the pressure sensitive adhesive electric blender all having added medicine is stirred 1h, place 12h, then stir 1h by electric blender, place 1-5h, to bubble-free, in impouring TB-300 type composite coating machine, be paved into the patch that thickness is 0.45mm.
In the present invention, if necessary, suitably can also add and can be used for 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 surfactant such as shrink pears sugar alcohol fatty acid ester, fatty acid glyceride, polyoxyethylene hydrogenation Semen Ricini, polyoxyethylene stearyl base ether, polyoxyethanyl lauryl ether, sodium lauryl sulfate; Lanoline, paraffin, olive pull 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.
Patch of the present invention, can adopt the general method adopted in patch preparing technical field to prepare.
Special regulation is had to the container that dress patch uses: medicinal carton or medicinal plastic bag or aluminium foil bag in the present invention.

Claims (2)

1. treat a patch for rheumatoid arthritis, it is characterized in that: the formula of this patch is: triptolide 481.5mg, lidocaine hydrochloride 2.4g, polyisobutylene oppanol B 10031.2g, polyisobutylene oppanol B 1262.5g, lanoline 5g, Borneolum Syntheticum 12g, 80% ethanol 9g, add chloroform to 1200g.
2. treat a preparation method for rheumatoid arthritis patch as claimed in claim 1, it is characterized in that: the first step: get high molecular weight polyisobutylene oppanol B 10031.2g and polyisobutylene oppanol B 1262.5g, adds chloroform to 1000g, until high and low molec weight polyisobutylene dissolves completely, obtains pressure sensitive adhesive for subsequent use; Second step: dissolve triptolide with appropriate chloroform, be dropwise slowly added in 5g lanoline, limit edged stirs; 3rd step: get 12g Borneolum Syntheticum and lidocaine hydrochloride 2.4g adds in beaker, dissolves with appropriate 80% ethanol and chloroform; 4th step: the lanoline containing medicine is dropwise slowly added in pressure sensitive adhesive, limit edged stirs; 5th step: the dropwise containing Borneolum Syntheticum and lidocaine hydrochloride is slowly added to limit edged in pressure sensitive adhesive and stirs, and add chloroform to 1200g; 6th step: the pressure sensitive adhesive electric blender all having added medicine is stirred 1h, places 12 h, then stir 1h by electric blender, places 1-5h, to bubble-free, in impouring TB-300 type composite coating machine, is paved into the patch that thickness is 0.45mm;
Described patch is generally aluminium foil bag or plastic bag packaging, and outsourcing is carton.
CN201110061304.5A 2011-03-14 2011-03-14 Patch for treating rheumatic arthritis and preparation method thereof Expired - Fee Related CN102670624B (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201110061304.5A CN102670624B (en) 2011-03-14 2011-03-14 Patch for treating rheumatic arthritis and preparation method thereof

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Application Number Priority Date Filing Date Title
CN201110061304.5A CN102670624B (en) 2011-03-14 2011-03-14 Patch for treating rheumatic arthritis and preparation method thereof

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CN102670624A CN102670624A (en) 2012-09-19
CN102670624B true CN102670624B (en) 2015-04-15

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Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109125733A (en) * 2018-10-30 2019-01-04 成都先手生物科技有限公司 A kind of composition for the treatment of of arthritis and its application
CN109908112B (en) * 2019-04-19 2022-04-19 内蒙古科尔沁药业有限公司 Non-allergic rubber plaster and preparation method thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101618030A (en) * 2009-08-10 2010-01-06 沈阳亿灵医药科技有限公司 Triptolide transdermal patch and preparation method thereof
CN102086199A (en) * 2010-12-28 2011-06-08 广济药业(孟州)有限公司 Method for self-extracting recycled riboflavin from liquid waste

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101618030A (en) * 2009-08-10 2010-01-06 沈阳亿灵医药科技有限公司 Triptolide transdermal patch and preparation method thereof
CN102086199A (en) * 2010-12-28 2011-06-08 广济药业(孟州)有限公司 Method for self-extracting recycled riboflavin from liquid waste

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