CN108553445B - A kind of preparation method of taxol powder spray - Google Patents
A kind of preparation method of taxol powder spray Download PDFInfo
- Publication number
- CN108553445B CN108553445B CN201810603428.3A CN201810603428A CN108553445B CN 108553445 B CN108553445 B CN 108553445B CN 201810603428 A CN201810603428 A CN 201810603428A CN 108553445 B CN108553445 B CN 108553445B
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- Prior art keywords
- taxol
- powder spray
- lactose
- preparation
- powder
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Abstract
The present invention relates to a kind of preparation methods of taxol powder spray, belong to pharmaceutical technology field.After taxol is dissolved with organic solvent first, paclitaxel solution is obtained；It in its even spraying to lactose, will obtain carrying medicine lactose again；Medicine lactose will finally be carried to be dried, then be sieved, powder is obtained.Preparation process of the present invention is simple, at low cost without complicated technology and machine, powder spray partial size is easier to control compared with the methods of conventionally spray-dried, taxol indissoluble itself, using the height of taxol powder spray dissolution rate made from the method for the present invention, dissolution rate is fast, and dissolution is complete substantially in 10min.
Description
Technical field
The present invention relates to a kind of preparation methods of taxol powder spray, belong to pharmaceutical technology field.
Background technique
Taxol is a kind of common anti-tumor drug, and anti-tumor activity with higher is usually used in treating oophoroma, cream
Gland cancer, non-small cell lung cancer, cervical carcinoma and cancer of the brain etc..However, oral administration biaavailability is lower since taxol soluble is poor,
Generally using ethyl alcohol and Emulsifier EL-60 Cremophor-EL as solvent, but the adverse reactions such as haemolysis, allergy can be generated.Cause
This, paclitaxel injection needs to use glucocorticoid and antihistamine drug in advance when in use, and then slowly injection PTX 3 is small
When, to reduce adverse reaction, great inconvenience is brought to patient, while also increasing treatment cost.Anticancer drug is passed through into lung
Portion's transmission, bioavilability with higher and less adverse reaction.And in lung field of drug delivery, powder spray sucking and mist
Change sucking compared to there are many benefit, these benefits include use of the insoluble medicine of high dose, patient breaths' stream activate inhalator,
Stability, the availability of disposable apparatus, limitation of environmental pollution of dry formulation etc..
Currently, the method for preparing powder spray is mostly spray drying process, freeze-drying, recrystallization method, micronization etc..Its
In, the hot environment in spray drying technology drying process will affect structure or be made for heat labile drug or biomolecule
It is denaturalized, in addition, suitable powder spray needs to control many kinds of parameters in order to obtain when preparing powder spray using spray drying process,
Such as inlet temperature, atomizing pressure, dry wind speed, the variation of each parameter may can influence finally obtained powder spray and produce
Product, therefore, technics comparing are complicated；The higher cost of freeze-drying, because it needs vacuum and cryogenic conditions, so vacuum refrigeration
Drying machine will configure a set of vacuum system and cryogenic system, thus investment cost and running expense are relatively high；Recrystallization method master
It is used for the delivering of hydrophobic drug, there is limitation for water soluble drug；Micronization is that acquisition drug sucking particle is most straight
Effective mode is connect, the method mostly used is the methods of fluid energy mill, ball milling, air-flow crushing, but is micronized and is difficult to control particle
Property, it is also possible to make the crystal structure of drug change during smashing, to influence the stability of powder.
Summary of the invention
Present invention aims to solve the deficiencies of the prior art, and provides a kind of a kind of preparation method of taxol powder spray, methods
Simply, without complicated technology and machine, at low cost, powder spray partial size is easy to control, and dissolution rate is high, and dissolution rate is fast.
Technical solution
A kind of preparation method of taxol powder spray, includes the following steps:
(1) after dissolving taxol with organic solvent, paclitaxel solution is obtained；
(2) it in paclitaxel solution even spraying to lactose, will obtain carrying medicine lactose；
(3) medicine lactose will be carried to be dried, then be sieved, obtain powder.
Further, in step (1), the organic solvent is selected from dehydrated alcohol, acetone, methylene chloride, chloroform or second
Any one in acetoacetic ester.
Further, in step (1), the concentration of paclitaxel solution is 1~10mg/ml.
Further, in step (2), the partial size of the lactose is 5 μm hereinafter, the weight ratio of taxol and lactose is 1:100
~2000.
Further, in step (3), drying temperature is 60~90 DEG C.
Further, in step (3), the sieving referred to 120 mesh~1200 meshes.
It further, further include step (4): by powder filled into capsule.
The beneficial effects of the present invention are: preparation process of the present invention is simple, it is at low cost without complicated technology and machine, with
The methods of conventionally spray-dried is easier to control compared to powder spray partial size, taxol indissoluble itself, is made using the method for the present invention
Taxol powder spray dissolution rate it is high, dissolution rate is fast, and dissolution is complete substantially in 10min.
Detailed description of the invention
Fig. 1 is the scanning electron microscope (SEM) photograph of taxol powder spray made from embodiment 1；
Fig. 2 is the In Vitro Dissolution figure of taxol powder spray made from embodiment 1；
Fig. 3 is the scanning electron microscope (SEM) photograph of taxol powder spray made from embodiment 3；
Fig. 4 is the In Vitro Dissolution figure of taxol powder spray made from embodiment 3.
Specific embodiment
Present invention will be further explained below with reference to the attached drawings and examples.
Remarks: in following embodiments, the test of the Emptying Rate, active component deposition, In Vitro Dissolution of taxol powder spray
It is carried out referring to 2015 editions Chinese Pharmacopoeias.
Embodiment 1
A kind of preparation method of taxol powder spray, includes the following steps:
(1) after dissolving 2mg taxol with 1ml dehydrated alcohol, paclitaxel solution is obtained；
(2) nano-spray instrument (model: KH1080, producer: bright spot Science and Technology Ltd.) is selected, paclitaxel solution is uniform
It is sprayed on 3.3g lactose, obtains carrying medicine lactose；
(3) load medicine lactose is put into vacuum oven and is dried, drying temperature is 80 DEG C, time 2h, then is distinguished
120 meshes and 240 meshes are crossed, powder is obtained；
The scanning electron microscope (SEM) photograph of powder is shown in Fig. 1, and taxol powder adsorption is in surface of lactose；Use Malvern Mastersizer
2000 instruments are measured the partial size of powder, and measuring partial size is 2.6 ± 0.1 μm.
(4) by powder filled into capsule.
The Emptying Rate of the powder spray is measured 90% or more, meets regulation；The active component deposition for measuring powder spray is
27.4 ± 2.3%, 20% is required higher than general；It is measured using In Vitro Dissolution of the Rotating shaker to powder spray, dissolution result is shown in
Fig. 2, it can be seen that the taxol powder spray sample of embodiment 1 is almost dissolved out in 10min.
Embodiment 2
A kind of preparation method of taxol powder spray, includes the following steps:
(1) after dissolving 5mg taxol with 1ml dehydrated alcohol, paclitaxel solution is obtained；
(2) nano-spray instrument (model: KH1080, producer: bright spot Science and Technology Ltd.) is selected, paclitaxel solution is uniform
It is sprayed on 3g lactose, obtains carrying medicine lactose；
(3) load medicine lactose is put into vacuum oven and is dried, drying temperature is 70 DEG C, time 7h, then is distinguished
120 meshes and 240 meshes are crossed, powder is obtained；
The partial size of powder is measured using 2000 instrument of Malvern Mastersizer, measuring partial size is 2.8 ± 0.2
μm。
(4) by powder filled into capsule.
Embodiment 3
A kind of preparation method of taxol powder spray, includes the following steps:
(1) by after 3mg taxol 1ml acetone solution, paclitaxel solution is obtained；
(2) nano-spray instrument (model: KH1080, producer: bright spot Science and Technology Ltd.) is selected, paclitaxel solution is uniform
It is sprayed on 3g lactose, obtains carrying medicine lactose；
(3) load medicine lactose is put into baking oven and is dried, drying temperature is 80 DEG C, time 2h, then crosses 120 mesh respectively
Sieve and 240 meshes, obtain powder；
The scanning electron microscope (SEM) photograph of powder is shown in Fig. 3, and taxol powder adsorption is in surface of lactose；Use Malvern Mastersizer
2000 instruments are measured the partial size of powder, and measuring partial size is 3.1 ± 0.1 μm.
(4) by powder filled into capsule.
The Emptying Rate of the powder spray is measured 90% or more, meets regulation；The active component deposition for measuring powder spray is
28.4 ± 2.4%, 20% is required higher than general；It is measured using In Vitro Dissolution of the Rotating shaker to powder spray, dissolution result is shown in
Fig. 4, it can be seen that the taxol powder spray sample of embodiment 3 is almost dissolved out in 10min.
Comparative example 1
A kind of preparation method of taxol powder spray: being dissolved in 3ml DMSO using 2mg taxol and 100mg, super using 2L
Pure water dialysed overnight, 2000g are centrifuged 5 minutes obtained carrier micelles, and leucine (weight ratio 20%) and mannitol (weight is then added
Amount is spray-dried than 75%), obtains taxol powder spray.
It measures 80% needs of taxol powder spray release 24 hours or more.And the taxol powder spray of the embodiment of the present invention
Sample is almost dissolved out in 10min, therefore taxol powder spray dissolution of the invention is very fast and complete.
Claims (5)
1. a kind of preparation method of taxol powder spray, which comprises the steps of:
(1) after dissolving taxol with organic solvent, paclitaxel solution is obtained；
(2) it in paclitaxel solution even spraying to lactose, will obtain carrying medicine lactose；
(3) medicine lactose will be carried to be dried, then be sieved, obtain powder；
In step (2), the weight ratio of taxol and lactose is 1:100~2000；
In step (3), the sieving referred to 120 mesh~1200 meshes.
2. the preparation method of taxol powder spray as described in claim 1, which is characterized in that in step (1), the organic solvent
Any one in dehydrated alcohol, acetone, methylene chloride, chloroform or ethyl acetate.
3. the preparation method of taxol powder spray as described in claim 1, which is characterized in that in step (1), paclitaxel solution
Concentration is 1~10mg/ml.
4. the preparation method of taxol powder spray as described in claim 1, which is characterized in that in step (3), drying temperature 60
~90 DEG C.
5. the preparation method of taxol powder spray as described in any one of Claims 1-4, which is characterized in that the preparation method
It further include step (4): by powder filled into capsule.
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| CN100428938C (en) * | 2005-09-28 | 2008-10-29 | 天津药业研究院有限公司 | Glucocorticoid capsule type inhaling atomized powder and preparation method |
| US20080276935A1 (en) * | 2006-11-20 | 2008-11-13 | Lixiao Wang | Treatment of asthma and chronic obstructive pulmonary disease with anti-proliferate and anti-inflammatory drugs |
| CN100459976C (en) * | 2007-02-15 | 2009-02-11 | 黄成安 | Compound paclitaxel preparation containing phospholipid dispersant and its preparation method |
| CN101919865B (en) * | 2009-06-09 | 2013-04-03 | 上海信谊百路达药业有限公司 | Capsule type budesonide dry powder inhalation and preparation process thereof |
| CN102232926A (en) * | 2010-04-23 | 2011-11-09 | 湖南易能生物医药有限公司 | Oral taxol nanoparticles and preparation method thereof |
| CN103110584A (en) * | 2013-01-29 | 2013-05-22 | 青岛大学 | Tiotropium bromide powder inhalation and preparation method thereof |
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| CN104188941B (en) * | 2014-09-02 | 2016-11-16 | 重庆和平制药有限公司 | A kind of method preparing clenbuterol hydrochloride inhaling powder mist agent |
| CN104398497B (en) * | 2014-10-29 | 2017-11-24 | 中山大学 | Itraconazole inhalation powder spray and preparation method thereof |
| CN105796534B (en) * | 2014-12-31 | 2019-06-28 | 深圳翰宇药业股份有限公司 | A kind of Dapagliflozin inhalation powder spray and preparation method thereof |
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