CN104414974A - Neferine sublingual spraying agent and preparation method thereof - Google Patents
Neferine sublingual spraying agent and preparation method thereof Download PDFInfo
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- CN104414974A CN104414974A CN201310381125.9A CN201310381125A CN104414974A CN 104414974 A CN104414974 A CN 104414974A CN 201310381125 A CN201310381125 A CN 201310381125A CN 104414974 A CN104414974 A CN 104414974A
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- neferine
- spraying agent
- sublingual
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- sublingual spraying
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides a neferine sublingual spraying agent and a preparation method thereof. The neferine sublingual spraying agent can be quickly absorbed by the sublingual mucosa, can directly enter the blood, is free from liver first-pass effect, is convenient to take, causes less adverse reaction and has a good treatment effect.
Description
Technical field
The invention belongs to technical field of traditional Chinese pharmacology, relate to the pharmaceutical dosage form of Neferine in Plumula Nelumbinis, especially undertongue spraying agent and preparation method thereof.
Background technology
(-)-Neferine (neferine, Nef) is a kind of bisbenzylisoquinoline alkaloid (the molecular formula C extracted from the green plumule of nymphaeaceae plant lotus (Nelumbo nucifera Gaertn) mature seed
38h
44n
2O6).Prove that it has blood pressure lowering, arrhythmia, anticoagulant, antioxidation and scavenging capacity free radical, resists myocardial ischemia through pharmacological evaluation and clinical application, relaxing smooth muscle, heart tonifying, anticancer, to the protection of cerebral ischemia, improve the effect such as acute lung injury and pulmonary fibrosis, CNS inhibition, blood sugar lowering; can be used as antiarrhythmic drug quick acting clinically, be therefore suitable for being prepared into quick-effective preparation (as sublingual formulation, the preparation etc. that can supply injection).
Present stage, antiarrhythmic drug conventional clinically is often prepared into oral formulations, and generally speaking oral formulations is all by gastrointestinal tract mucous absorption, for unstable, the irritant and obvious medicine of first pass effect in the gastrointestinal tract, and should not oral administration; And these medicines generally adopt drug administration by injection in the past, long-term prescription can cause very large misery and inconvenience to patient.But medicine can avoid first pass effect through part mucosa absorption, improve bioavailability, the object of whole body therapeutic can be reached.Therefore, the present invention proposes and the (-)-Neferine in Plumula Nelumbinis is prepared into undertongue spraying agent, to reach safe and effective therapeutic purposes.
(-)-Neferine is a class poorly water-soluble, but the lipotropy Organic substance that Determination of oil-water partition coefficient is higher.Although this material has lower dissolubility in physiological solution, there is in body higher transmucosal effect.(-)-Neferine is a class fat-soluble medicine, and oil/water partition coefficient, about 245, can meet the condition of Sublingual or buccal administration.
(-)-Neferine undertongue spraying agent of the present invention does not need disintegrate and stripping, decrease because of involuntary salivation and the impact of swallowing sublingual administration routes usefulness, simultaneously because droplet volume is little, advantage is more easily absorbed fast by mucosa with mucosal contact area is large etc., is more suitable for clinically as anti-arrhythmic.
Summary of the invention
The object of this invention is to provide a kind of (-)-Neferine undertongue spraying agent, it passes through scientific formula, be spray by (-)-Neferine Polymer materialspreparation, it can solve the bioavailability that prior art exists clinically lower, use inconvenience, shortcoming that patient is difficult to accept, have gastrointestinal tract certain side effect.
The present invention is achieved by the following technical solutions: the (-)-Neferine crude drug and the correctives that take recipe quantity, add the solubilizing agent of recipe quantity, be prepared into microsphere or microcapsule, shake up, ultrasonic promotion is dissolved, the EtOH Sonicate or the vibration that add recipe quantity again are extremely dissolved completely, filter, standardize solution, shake up, be sub-packed in 3 ~ 10 mL sublingual spraying bottles, sealing screw capping, puts shady and cool place and keeps in Dark Place.
(-)-Neferine undertongue spraying agent prepared by the present invention, correctives can comprise in citric acid, Mentholum, stevioside, glycyrrhizin, sucralose, glucide one or more; Solubilizing agent can be buffer, cyclodextrin (hydroxypropyl--cyclodextrin, sulphur butyl--cyclodextrin), surfactant (tween 80,20,40, PEG1000, succinate gathers glucoside grease etc.); For increasing the stability of prescription Chinese medicine, also can add cosolvent, it can comprise ethanol, 1,2-PD (PG), glycerol, isopropyl alcohol and Polyethylene Glycol (PEG) etc.
The present invention finds in the process of development (-)-Neferine undertongue spraying agent, and regulating the pH value of solution that insoluble drug is dissociated is a kind of simple and effective solubilization method.And sublingual mucosa is easy damaged not, repair function is strong again, and pH value can 1 ~ 10.The soda acid that adjust ph is commonly used has: citric acid (pKa=3.13,4.46,6.40), lactic acid (pKa=3.13), acetic acid (pKa=4.76) and phosphate (pKa=2.15,7.20,12.33) etc.
Detailed description of the invention
By following (-)-Neferine crude drug and the Mentholum of getting recipe quantity (see table 1), add the solubilizing agent of recipe quantity, be prepared into microsphere or microcapsule, shake up, ultrasonic promotion is dissolved, the EtOH Sonicate or the vibration that add recipe quantity again are extremely dissolved completely, filter, standardize solution, shake up, be sub-packed in 3 mL sublingual spraying bottles, sealing screw capping, puts shady and cool place and keeps in Dark Place.
The formula of table 3 (-)-Neferine spray
(-)-Neferine spray Formulation prepared by the present invention is reasonable, and preparation technology is easy, can guarantee product quality.Doser is advanced, and quantitatively accurately, favorable reproducibility, container closure, for the successful exploitation of dosage changing form provides guarantee.
Claims (3)
1. the undertongue spraying agent containing (-)-Neferine, is characterized in that this medicine contains the (-)-Neferine extracted from Plumula Nelumbinis and the adjuvant prepared needed for this spray.
2. (-)-Neferine undertongue spraying agent according to claim 1 refers to and directly can enter blood by sublingual mucosal absorption, completes the pharmaceutical dosage form of absorption process.
3. (-)-Neferine water solublity is unstable, becomes microcapsule or microsphere, then make spray with Polymer materialspreparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310381125.9A CN104414974A (en) | 2013-08-29 | 2013-08-29 | Neferine sublingual spraying agent and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310381125.9A CN104414974A (en) | 2013-08-29 | 2013-08-29 | Neferine sublingual spraying agent and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN104414974A true CN104414974A (en) | 2015-03-18 |
Family
ID=52965801
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310381125.9A Pending CN104414974A (en) | 2013-08-29 | 2013-08-29 | Neferine sublingual spraying agent and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN104414974A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1537538A (en) * | 2003-04-16 | 2004-10-20 | 郑向黎 | Method for preparing compound flavone spray |
| CN1634565A (en) * | 2004-11-30 | 2005-07-06 | 深圳市海王英特龙生物技术股份有限公司 | Protein medicine microcapsule and inhalational aerosol thereof |
-
2013
- 2013-08-29 CN CN201310381125.9A patent/CN104414974A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1537538A (en) * | 2003-04-16 | 2004-10-20 | 郑向黎 | Method for preparing compound flavone spray |
| CN1634565A (en) * | 2004-11-30 | 2005-07-06 | 深圳市海王英特龙生物技术股份有限公司 | Protein medicine microcapsule and inhalational aerosol thereof |
Non-Patent Citations (2)
| Title |
|---|
| 柳伟，等: "莲子心总生物碱滴丸的制备工艺及含量测定", 《中国中药杂志》 * |
| 温博栋: "《半固体及其他制剂技术》", 31 January 2009 * |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20150318 |
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| WD01 | Invention patent application deemed withdrawn after publication |