CN1188151C - Formula of injection for relieving pain and its preparation method - Google Patents
Formula of injection for relieving pain and its preparation method Download PDFInfo
- Publication number
- CN1188151C CN1188151C CNB021145407A CN02114540A CN1188151C CN 1188151 C CN1188151 C CN 1188151C CN B021145407 A CNB021145407 A CN B021145407A CN 02114540 A CN02114540 A CN 02114540A CN 1188151 C CN1188151 C CN 1188151C
- Authority
- CN
- China
- Prior art keywords
- injection
- indomethacin
- analgesia
- indometacin
- analgesic
- 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
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
The present invention relates to an injection (slow release) for analgesia, particularly to a formula of an analgesia injection and a preparation process. The traditional Chinese medicine of asarum herb and the western medicine of indometacin are made into a microencapsule injection, and the preparation process comprises: arabic gum and gelatin are used as capsule materials, the asarum herbs and the western medicine of the indometacin are made into microcapsules by a phase separation and secondary coacervation method, and the injection is prepared. The injection comprises the ingredients of 6 ml to 10 ml of asarum herb volatile oil and 8g to 14g of indometacin. The analgesia (slow release) injection has the advantages of good pain alleviation effect, long pain alleviation time, no addiction and no toxic or side effect.
Description
Affiliated technical field: the present invention relates to a kind of analgesia (slow release) injection that is used for, particularly about a kind of analgesic injection.
Background technology: existing analgesic injection is that (source: " CSTAD " MFN:175102) wait and to be several several pieces of article introductions seldom, and only limit to laboratory stage, weak point is: the medicine pain relieving weak point of holding time with indomethacin.It has compared significant difference (P＜0.05) in the intravital bioavailability of rabbit with pharmacokinetic parameters with the IMC of encapsulation after measured, and wherein the former Tmax is 1.15h, and Cmax is 1.38 μ gml
-1, t
1/2Be 4.5h, Fi:175.6%; And the latter's Tmax is 3h, Cmax:1.45 μ gml
-1, t
1/2Be 14.3h, Fi:184.28%.And existing dolantin, by adopting hot plate method that the comparative test in mice pain territory is shown, though the pain territory raising rate of dolantin is 100%, the suffering pain microencapsule injection pain territory raising rate that disappears is 97%, and analgesic effect is close substantially, but the onset time of dolantin is 3 minutes the soonest, peak time is 30 minutes, after fall after rise fast, to 2 hours, pain thresholding rate maintains between 18.52%～20%, greatly reduces.Also have a kind of analgesic effect preferably injection of morphia liquid addiction is arranged, side effect is bigger.
The purpose of this invention is to provide a kind of analgesic injection, its good analgesic effect, analgesic time is long, no addiction and any toxic and side effects.
Technical scheme of the present invention is: a kind of analgesic injection: it makes microencapsule injection together by Chinese medicine " Herba Asari " and Western medicine " indomethacin ".
It is the capsule material with arabic gum-gelatin, " Herba Asari " and Western medicine " indomethacin " are adopted be separated-complex coacervation makes microcapsule, is mixed with injection again.
Herba Asari volatile oil 6ml-10ml, indomethacin 8g-14g.
Herba Asari volatile oil 8ml, indomethacin 12g makes microcapsule, adds benzyl alcohol 4.5ml and the Aromatic water after carrying oil during dosing, is adjusted to 450ml with water for injection.
Add arabic gum-gelatin solution with the capsule core material of liquid or solid and make Emulsion, add spirit of vinegar and transfer PH3.5～4.5, put 45 ℃ of stirred in water bath and be the cohesion capsule, adding 2～4 times of amounts of 40 ℃ of water continues to stir in 45 ℃ of water-baths, dilution cohesion capsule is put stirred in water bath to 20 ℃～18 ℃, adding firming agent is 8 with sodium hydroxide accent PH, continue to stir one hour, putting into refrigerator takes out filter and does after 24 hours, wash microcapsule in right amount with distilled water and promptly do not get intermediate, dosing successively again, embedding, sterilization, inspection, finished product warehouse-in to there being the firming agent abnormal smells from the patient.
Described capsule core material is volatile oil and " indomethacin " respectively first emulsive mixture that Herba Asari extracts; Described capsule material the best is arabic gum-gelatin, can also be Resina persicae, cellulose acetate-phthalate, carboxymethyl cellulose, ethyl cellulose, can also be carboxyl-ethyl polymer, beta cyclodextrin or pectin, gelatin.
During described " microcapsule " gelling, adopt 5%～10% acetic acid, also can adopt 5%～10% hydrochloric acid; Firming agent is a glutaraldehyde, can also be formaldehyde.
Described technical parameter is: the best colostrum time is about 10 minutes, and bath temperature is 40 ℃～45 ℃, and mixing time is 15～30 minutes in the water-bath, and PH is 3.8～4 during gelling; Can also be to be 15～25 minutes the colostrum time, bath temperature be 45 ℃～60 ℃, and mixing time is 40～60 minutes in the water-bath, and PH is 3.5～4.5 during gelling.
During curing, best PH is 5.5～6.5, can also be that PH is 6.5～8.
Described dosing is that Aromatic water and the water for injection behind the Herba Asari extraction volatile oil adds an amount of benzyl alcohol again, and certain antiinflammation is arranged, and can also adopt benzoic acid, three potassium sorbates etc. in addition.
Characteristics of the present invention are:
1, it is made up of Herba Asari and two kinds of medicines of indomethacin, wherein Herba Asari be the aristolochiaceae plant Herba Asari (the dry herb of Asarum hetero tropoides Fr.Schmidt var.mandshuricum (maxim.) K:tag., have dispel the wind, cold expelling, analgesic effect; Indomethacin (Indomethacin) has another name called indometacin, is a kind of NSAID (non-steroidal anti-inflammatory drug), and its molecular formula is: C
19H
16ClNO
4, have analgesic, analgesia, antiinflammation, mechanism: suppress prostaglandin (PG) synzyme, thereby precursor-arachidonic acid synthesis of prostaglandins of blocking-up PG is removed the proinflammatory effect of endogenous PG.
2, its preparation technology is: with two kinds of medicines with arabic gum-gelatin be the capsule material be separated-complex coacervation makes microcapsule, is mixed with injection again.And " microcapsule " a kind of intermediate dosage form that to be RECENT DEVELOPMENTS get up, it can be prepared to multiple dosage form as required and use.Because medicine is wrapped in the small spherical capsule, can play the raising medicine stability; Cover bad stink; Improve medicine to gastral reaction, reduce side effect; Multiple effects such as prolong drug curative effect are a kind of rising dosage forms.Just be based on this reason, thisly make microencapsule injection together by Chinese medicine " Herba Asari " and Western medicine " indomethacin " and improved medicine stability, avoid digestive tract reaction, keep long action time, be a kind of in, the collaborative compatibility of Western medicine, the efficient pain relieving newtype drug of prescription.This medicine mature preparation process, quality is more stable, and through clinical confirmation, analgesic effect is compared with dolantin, and diversity is remarkable (P＞0.05) not, and effective percentage reaches 99.7%.Especially these product more possess dolantin two places innovations characteristic can't be obtained: pain relieving is held time and is reached more than 8 hours, and elder can reach 24 hours; No dependence and other toxic and side effects.So this project is expected to become the replacement dolantin, the efficient analgesic that has no side effect has very huge potential social benefit and economic benefit.
3, it and injection indomethacin are relatively: the injection indomethacin analgesic effect weak point of holding time, it has compared significant difference (P＜0.05) in the intravital bioavailability of rabbit with pharmacokinetic parameters with the IMC of encapsulation after measured, wherein the former Tmax is 1.15h, and Cmax is 1.38 μ gml
-1, t
1/2Be 4.5h, Fi:175.6%; And the latter's Tmax is 3h, Cmax:1.45 μ gml
-1, t
1/2Be 14.3h, Fi:184.28%.Data result shows the novel form that this microencapsule injection is expected to become the bioavailability height and has sustained-release analgesia, and it is long more than indomethacin to hold time.
4, with dolantin relatively, the pain relieving of the present invention length of holding time.Though by adopt hot plate method with two kinds of injection to mice bitterly the pain territory raising rate of the comparative test demonstration dolantin in territory be 100%, injection pain territory raising rate of the present invention is 97%, analgesic effect is close substantially, but the onset time of dolantin is 3 minutes the soonest, peak time is 30 minutes, after fall after rise fast, to 2 hours, pain thresholding rate maintains between 18.52%～20%, greatly reduces.And this injection onset peak time is 2 hours, then falls after rise gently, and pain thresholding rate maintains 80%, to more than 24 hours.And have no side effect and dependency.Test shows that the dolantin toxic and side effects is 20.37%, dependency 100%; This injection toxic and side effects is 0.29%, and dependency is 0.
5, it and liniment Tongbining for cold-type arthralgia are relatively: dosage form differs, route of administration difference, bioavailability difference.Relation between medicament and the curative effect is very close, and it depends on multiple factor, but having the greatest impact to drug absorption.Drug absorption is from fast to slow successively: vein＞suction＞muscle＞subcutaneous＞rectum or Sublingual＞oral＞skin.Medicament of the present invention absorbs by muscle, and liniment Tongbining for cold-type arthralgia passes through skin absorbs, and visible injection bioavailability of the present invention is peaceful far above arthralgia aggravated by cold, and their prescription differences, has any different on the effect.Liniment Tongbining for cold-type arthralgia is made up of 15 kinds of Chinese medicine and western medicine such as Semen Strychni (processed)s, be adapted to rheumatism, rheumatoid, scapulohumeral periarthritis, hyperosteogeny, sprain and partial gall that various strain causes, injection of the present invention is made up of Herba Asari, indomethacin, is adapted to anal fistula, tumor and other postoperative pain, headache, toothache, rheumatic arthritis etc.Herba Asari volatile oil mixes behind the colostrum respectively with indomethacin, makes microcapsule again, and this also meets a kind of method of microcapsule preparation technology, be that medicated powder is scattered in the vegetable oil, and Herba Asari volatile oil have anti-inflammatory analgesic action, it and indomethacin composing prescription preparation, to learn from other's strong points to offset one's weaknesses, strengthen synergism.
The present invention will be further described below in conjunction with embodiment.
Get Herba Asari volatile oil 8ml and use arabic gum colostrum 4 minutes; Indomethacin 12g, both are mixed into Emulsion after 6 minutes with the gelatin grinding, reuse adds spirit of vinegar and transfers PH4, put 45 ℃ of stirred in water bath and be the cohesion capsule, adding 3 times of amounts of 40 ℃ of water continues to stir 30 minutes in 45 ℃ of water-baths, dilution cohesion capsule is put stirred in water bath to 20 ℃～18 ℃, add firming agent and transfer PH8 with sodium hydroxide, continue to stir one hour, putting refrigerator takes out filter and does after 24 hours, wash microcapsule in right amount with distilled water and promptly do not get intermediate, then with the Aromatic water behind the extraction volatile oil to there being the firming agent abnormal smells from the patient, 4.5ml the benzyl alcohol dosing, water for injection is adjusted 450ml embedding again, sterilization, check, the finished product warehouse-in.
Claims (2)
1, a kind of analgesic injection is characterized in that it is that active part is made with Herba Asari volatile oil 6ml-10ml and indomethacin 8g-14g.
2, a kind of analgesic injection according to claim 1 is characterized in that it is that active part is made with Herba Asari volatile oil 8ml and indomethacin 12g.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021145407A CN1188151C (en) | 2002-04-25 | 2002-04-25 | Formula of injection for relieving pain and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021145407A CN1188151C (en) | 2002-04-25 | 2002-04-25 | Formula of injection for relieving pain and its preparation method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1380083A CN1380083A (en) | 2002-11-20 |
| CN1188151C true CN1188151C (en) | 2005-02-09 |
Family
ID=4743150
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB021145407A Expired - Fee Related CN1188151C (en) | 2002-04-25 | 2002-04-25 | Formula of injection for relieving pain and its preparation method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1188151C (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100381120C (en) * | 2003-10-17 | 2008-04-16 | 昆明紫健生物技术有限公司 | Fibrauretine powder for injection and its production process |
| CN1302767C (en) * | 2005-06-13 | 2007-03-07 | 广州中医药大学第一附属医院 | Apoplexy treating injection |
| CN103301791A (en) * | 2013-07-09 | 2013-09-18 | 吉林大学 | Quercetin microcapsule and preparation method thereof |
| CN115350658B (en) * | 2022-10-24 | 2023-03-21 | 江西天佳生物工程股份有限公司 | Optimization method of thymol essential oil coating granulation process |
-
2002
- 2002-04-25 CN CNB021145407A patent/CN1188151C/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN1380083A (en) | 2002-11-20 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US20170348276A1 (en) | Nasal cannabidiol compositions | |
| JP6445002B2 (en) | Soft tablet containing turmeric extract | |
| Panigrahi et al. | Extract of Sesbania grandiflora Ameliorates Hyperglycemia in High Fat Diet‐Streptozotocin Induced Experimental Diabetes Mellitus | |
| CN1188151C (en) | Formula of injection for relieving pain and its preparation method | |
| WO2020057029A1 (en) | Compatible composition of masticinic acid and myrrh terpene, preparation method therefor, and use thereof | |
| US10357530B2 (en) | Combination of valerian root extract and lavender oil for use in the treatment of sleep disorders | |
| Lugo-Lugo et al. | Antinociceptive local activity of 4-allyl-1-hydroxy-2-methoxybenzene (eugenol) by the formalin test: an anti-inflammatory effect | |
| CN102284015A (en) | Integrated novel form preparation technology for powder with marvellous effect and production method thereof | |
| CN102100894A (en) | Preparation technology of new integrative formulation of free wanderer powder and production method thereof | |
| US20210188797A1 (en) | Heat and oxidation resistant a9 tetrahydrocannobinol (thc) and cannabiniol (cbd) compound and method of manufacturing the same | |
| US20030096024A1 (en) | Methods and compositions for the treatment of benign prostatic hypertrophy | |
| CN106551915A (en) | Enteric-coated composition and preparation method thereof | |
| CN1253018A (en) | Nm-class insulin particles and their preparing process | |
| US20130072577A1 (en) | Vaporized Medicants and Methods of Use | |
| CN101249063B (en) | Calciparine/sodium salt nano oral preparation and preparation technique thereof | |
| Maskare et al. | Novel formulation for treatment of mouth ulcer | |
| CN103028095A (en) | Preparation technology and production method of integrated new dosage form of dry ginger and Radix aconiti lateralis preparata decoction | |
| AU2021103679A4 (en) | Neem (Azadirachita indica) Gum Based in Situ Gelling System for Targeted Delivery of Simvastatin into Stomach | |
| Overby | Exploring Novel Anti-Obesity Strategies: Nutritional and Pharmacological Interventions to Induce Browning and Brown Adipogenesis | |
| CN101104064A (en) | Traditional Chinese medicine special for treating fishbone stuck in throat | |
| RU2236860C2 (en) | Ointment "orien" with analgetic and anti-inflammatory effect | |
| JP2012512869A (en) | Delivery system for delivery of substances into the oral cavity | |
| CN1915242A (en) | Exterior coating medication for treating ulcer in the oral cavity, and preparation method | |
| JPS60501904A (en) | Sustained release methods and products | |
| CN101152225A (en) | Traditional Chinese medicine for treating ancylostomiasis |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20050209 Termination date: 20160425 |