CN104136009A - Rapidly disintegrating form of a drug and preparation method thereof - Google Patents
Rapidly disintegrating form of a drug and preparation method thereof Download PDFInfo
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- CN104136009A CN104136009A CN201380003824.8A CN201380003824A CN104136009A CN 104136009 A CN104136009 A CN 104136009A CN 201380003824 A CN201380003824 A CN 201380003824A CN 104136009 A CN104136009 A CN 104136009A
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
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Abstract
Disclosed in the present invention are a rapidly disintegrating form of a drug and a preparation method thereof, in particular relating to a form of a drug and a preparation method thereof using a membranous matrix as the skeleton structure, with the active ingredients thereof being distributed in the membranous matrix or in a gap or cavity formed by the membranous matrix and able to rapidly disintegrate in the oral cavity and other in vivo cavities. The form of a drug not only has a high strength and disintegrates rapidly, but also is suitable for loading drugs with a variety of doses, and has a good practical application value.
Description
Specification
A kind of rapidly disintegrating dosage form and preparation method thereof
Technical field
The present invention relates to a kind of rapidly disintegrating dosage form and preparation method thereof, more particularly to one kind is used as skeleton structure using membranaceous matrix, active component is distributed in the membranaceous its content or is distributed in the space or cavity that the membranaceous matrix formed, and other chambers can quickly disintegrated formulation and preparation method thereof in oral cavity and in vivo.
Background technology：
Major part medicine is all by oral administration, in numerous oral drugs, and using tablet, capsule as main flow formulation at present.But, most of Solid oral pharmaceutical based on tablet, capsule is because piece type is larger, need to be swallowed with water, for some patients, and medication is extremely inconvenient, and easily causes safety issue.For example, the patient of dysphagia, such as old man, child, the patient with cancer of the esophagus；With the patient of water inconvenient patient, such as bed position；Actively or the patient of medication, such as mental patient are not mismatched；Take medicine inconvenient patient, such as disturbances in patients with Parkinson disease, patients of senile dementia.
In order to overcome above mentioned problem, many companies release Orally disintegrated dosage form, and these formulation preparation methods are different, respectively there is advantage and disadvantage.For example, tabletting after some use direct compression methods or wet granulation, using the characteristic of super-disintegrant Fast-swelling in water, makes tablet be disintegrated rapidly.Tablet prepared by this method, because water-insoluble auxiliary material is a lot, the normal grittiness sense in mouth, and due to preparing tablet using pressed disc method, tablet inner space is minimum, and only relying on disintegrant swelling action makes tablet disintegration, therefore disintegration time limited is longer, commonly greater than one minute.The tablet prepared in the past using freeze-drying, general prepared tablet disintegration times are shorter, but intensity is smaller, fragmentation is easy to by some compressings in transport and carrying process or when shaking, it is conflict that its disintegration time, which is adjusted, with intensity, i.e. when shorten tablet disintegration time its intensity can be deteriorated more in short-term, if on the contrary, increase tablet strength will be obviously prolonged its disintegration time.For example, patent US6509040 discloses a kind of Orally disintegrated dosage form, said preparation is using modified starch as adhesive, with preferable disintegration effect.But tablet hardness prepared by this method is poor, and raw edges or radial crack phenomenon often occurs in tablet, and slice, thin piece texture is crisp, and careful operation is needed when slice, thin piece is taken out from bubble-cap, otherwise easy fragmentation is polylith.In addition, the tablet prepared using freeze-drying, the easy residual tack agglomerate on oral cavity upper wall or tongue when taking in the past, the mode such as nozzle or a small amount of drinking-water need to be licked with tongue could eliminate agglomerate sense.Inventor has carried out numerous studies to above-mentioned phenomenon, finds the easy group's of being formed heap formula excipient substance mixture in the internal microstructure of above-mentioned tablet, fragile structure, therefore, the defect of tablet internal microstructure are the key elements for causing to occur above-mentioned phenomenon.
For the defect of above-mentioned preparation method resulting dosage forms, the present invention is conducted in-depth research to tablet internal microstructure, tablet internal microstructure is adjusted by controlling auxiliary material application, can the group's of avoiding the occurrence of heap formula external morphology, and then realize dual excellent effect of the tablet in terms of disintegration and hardness.It is a discovery of the invention that when dosage form interior matrix formation membrane structure, being optimized to membranaceous matrix, not only intensity is high but also disintegration is rapid for resulting formulation, is adapted to the loading of various dose drugs.The content of the invention
The present invention collapses the defect of formulation there is provided a kind of new rapidly disintegrating dosage form for current speed, and not only intensity is high for the formulation, and disintegration is rapid, and is adapted to the loading of various dose drugs, with good actual application value.
It is an object of the invention to provide a kind of using space between membranaceous matrix and membranaceous matrix and/or cavity as the quick of principal character
Disintegrated dosage form, the formulation contains the auxiliary material of at least one active component and one or more, the auxiliary material forms membranaceous matrix in dosage form interior, membranaceous stromal surface can be with porous or complete non-porous, space or cavity are formed between membranaceous matrix, the active component is distributed in the membranaceous its content or is distributed in the space or cavity that the membranaceous matrix formed, and the ratio that the cumulative volume of the space or cavity accounts for the formulation cumulative volume is 10%-98%.Because the thickness of the membranaceous matrix of dosage form interior has vital effect for formulation intensity and disintegration ability, found by researching and developing, when the membranaceous matrix average thickness is 0.05 μ ι η -20 μ ι η, prepared formulation does not only have larger mechanical strength, and disintegration time is short.It is preferred that membranaceous matrix average thickness is 0.05 μ τ η -5 μ ι η.It is further preferred that the membranaceous matrix average thickness is 0.05 μ π ι -0.5 μ π ι.The thickness that the speed being made up of the membranaceous matrix collapses formulation can be lmm-10mm.The speed, which collapses formulation upper surface and can bear maximum pressure, is not less than 0.0051N/cm2, the speed collapses formulation in friability experiment without fragmentation or capping, weightless less than 0.8%, and the disintegration rate that the speed collapses formulation is less than 30 seconds.The membranaceous stromal thickness, which is determined, uses reflective spectral measure method, is calculated using genetic annealing algorithms（Chu Dong, plural layers thickness measure [J] the photoelectric projects of the based on genetic annealing algorithms, 2010,2 (37) such as palace excitement:45-49)；The porosity measurement method calculates (Xiao Xin, experimental study [J] the food industry science and technology of the freeze-dried material interior porosity influence factors such as Taole benevolence, 2007,3 (28) using the imaging of micro- CT scan, Image Reconstruction and software analysis:78-81)；The speed collapses the maximum pressure that formulation upper surface can bear（Unit is N/cm2, the N is newton）Calculated by following methods：The speed is collapsed into formulation to be flat on desktop, take a glass bar to be placed in the speed to collapse directly over formulation, glass bar does the movement of falling object in different height respectively, calculate the minimum constructive height that glass bar makes the speed collapse formulation deformation, the speed, which is calculated, according to F=mgh collapses the unilateral suffered power of formulation, then divided by lifting surface area（Glass bar cross-sectional area）Produce, wherein m is glass bar weight, g is acceleration of gravity, h is the height of freely falling body, speed of the present invention, which collapses the upper surface that formulation deformed finger formulation contacts with glass bar, to be occurred being recessed or crackle.The friability is with reference to Chinese Pharmacopoeia two annex X G (annex page 89 of version in 2010）It is measured, the disintegration time assay method is placed in 10ml beakers to take said preparation 1（2ml water is previously added, temperature is 37 ± Γ Ο, and timing is started with stopwatch, until tablet is disintegrated completely, records complete disintegration time.
Rapidly disintegrating dosage form provided by the present invention, its internal membranaceous matrix includes the auxiliary material for serving as filmogen and film reinforcing agent, and the characteristic such as the film forming of membranaceous matrix and whole formulation outward appearance, intensity and disintegrating property and the supplementary product consumption such as the filmogen and film reinforcing agent are directly related.The filmogen can be selected from, but not limited to, one or more kinds of compositions in following raw material：Sesbania gum, Indian gum, furcellaran, peach gum, preferably sesbania gum.The film reinforcing agent is selected from, but not limited to, one or more kinds of compositions in following raw material：Xylitol, glycine, serine, mannitol, sorbierite, trehalose, dextrin, sodium chloride or alumina silicate, preferably xylitol.The membranaceous matrix also includes the one or more in suspending agent, sweetener, essence, antioxidant, defoamer.Suspending agent can both play a part of suspending during formulation is prepared, and can also play a part of film reinforcing agent.The one or more that suspending agent may be selected from but be not limited in following raw material：Chitin, chitose, sesbania gum, tara gum, Indian gum, furcellaran, western tragacanth, glue is drawn in red match, tamarind gum, Karaya Gum, converted starch, alginic acid, propylene glycol alginate, sodium alginate, hydroxyethylmethylcellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, glucan, polyvinyl alcohol, xanthans, konjac glucomannan, Arabic gum, algin, melon bean gum, agar, hydroxymethyl cellulose, ethylhydroxyethylcellulose, methylcellulose, carbomer, carrageenan, pectin, locust bean gum, polyvinylpyrrolidone, sodium carboxymethylcellulose, dextrin, it is preferred that xanthans or konjac glucomannan.
In order to prepare the above-mentioned rapidly disintegrating dosage form using membranaceous matrix as skeletal support, it can be prepared using freeze-drying, boulton process, low temperature drying method, wherein freeze-drying comprises the following steps：（A) preparation of matrix liquid：Will
Active constituents of medicine, filmogen, film reinforcing agent and other auxiliary materials are added in the suspending agent aqueous solution fully dissolved, form matrix liquid；（B) deaerate：To above-mentioned（A) matrix liquid that step is prepared is de-gassed；（C) injection molding：By step（B) matrix liquid Jing Guo degassing process is by certain volume injection mould；（D) pre-freeze：By step（C) mould that matrix liquid is marked with carries out pre-freeze；（E) freezing thousand is dry：Will（D) the preparation freeze-drying obtained, removes solvent, produces.In preparation process, described solvent is water or volatile organic solvent, preferably water, methanol, ethanol, acetone, ethyl acetate or dimethyl sulfoxide (DMSO).The step（C) note sample volume is 0.1 ~ 2.0ml, preferably 0.4ml in.In the preparation steps of matrix liquid, the matrix liquid include weight ratio be 0 ~ 75.0% active constituents of medicine, weight ratio be 1.0% ~ 10.0% filmogen, weight ratio be 1.0% ~ 10.0% film reinforcing agent, 0 ~ 5% other auxiliary materials, surplus is water.The matrix liquid include weight ratio be 0 ~ 25% active constituents of medicine, weight ratio be 2.5% ~ 5.0% filmogen, weight ratio be 2.5%-5.0% film reinforcing agents, 0 ~ 5% other auxiliary materials, surplus is water.In step（D) in, the pre-freezing temperature is less than the eutectic temperature of the matrix liquid, and selection pre-freezing temperature is-40-150 °C, is preferably-60-120 °C.In step（E) in, primary drying temperature is less than the eutectic temperature of the matrix liquid in the freezing dry process, or the product temperature is less than the matrix liquid eutectic temperature.
There is no particular limitation for the main ingredient that the present invention relates to, and is not only suitable for slightly molten, slightly soluble, almost soluble,very slightly, insoluble or insoluble medicine, also is adapted for water soluble drug, can be selected from, but not limited to, the composition of a kind of following medicine or several drugses.
Chemicals-antipyretic-antalgic anti-inflammatory agent, such as aspirin, Diflunisal, salsalate, paracetamol, Indomethacin, brufen, naproxen, Ketoprofen, pirprofen, suprofen, Flurbiprofen, piroxicam, Meloxicam, aulin, Benzbromarone.
Central stimulant, such as pemoline, adrafinil, Piracetam.
Treat migraine agent, such as Sumatriptan succinate.
Antalgesic, such as rotundin, buprenorphine, pentazocine, naloxone.
Anti-parkinson and treatment senile dementia medicine, such as levodopa, compound carbidopa, compound benserazide, amantadine hydrochloride, piribedil, phenolicamine, donepezil, huperzine are first-class.
Psychotolytic, such as chlorpromazine, fenazil, pethidine, thioridazine, Chlorprothixene, Clozapine, Sulpiride, Tai Bili, penfluridol, Risperidone.
Antiepileptic and anticonvulsive drug, such as dilantin sodium, carbamazepine, Primidone, Gabapentin, Lamotrigine, sodium vedproate, Clonazepam.
Hypnotic sedative agent, dissolves such as diazepam, the husky west of nitrazepam, Austria, Lorazepam, phenobarbital.
Cholinesterase inhibitor, such as hyoscine.
Antiarrhymic, such as third pyridine, tocainide, mexiletine, aetmozine, dilantin sodium, Propafenone, amiodarone.
Antianginal and antiatherosclerotic, such as Propranolol, nifedipine, Gemfibrozil, Bezafibrate, Lovastatin, Simvastatin, Pravastatin.
Antihypertensive, such as Enalapril, captopril, Hydrochioro, Amlodipine.
Adrenoceptor blocking agents, such as acebutolol, alprenolol.
Cortex class medicine, such as betamethasone, cortisone acetate.
Antidiabetic, such as Repaglinide.
Antithyroid drug, such as propylthiouracil (PTU), Carbimazole, methimazole.
Antithistamine, such as Cetirizine Hydrochloride, Loratadine.
Autacoid, such as dinoprostone, Alprostadil, Betahistine.
Digestive system surgical procedures, such as scopolamine butylbromide, Granisetron Hydrochloride.
Hematological system medicine, such as EPO, cobamamide.
Urinary system medicine, such as azosemide, frusemide.
Reproductive system medicine, such as estrogen, Nandrolone Phenylpropionate.
Antiparasitic agent, such as albendazole, cambendazole.
Antineoplastic, such as aminoglutethimide, amsacrine.
Antimicrobial, such as ampicillin, sulbenicillin sodium.
Tri-Biocin, such as Amoxicillin, cefalexin, Cefprozil, CEFUROXIME AXETIL, ROX, Erythromycin Ethylsuccinate, josamycin.
Effective component of chinese medicine monomer, such as：Breviscapinun, qinghaosu etc..
Single medicinal material material extract, such as：Tanshinone, root of red-rooted salvia phenolic acid etc..
Compound Chinese medicine extract, such as：Composite salvia dropping extract of bolus, cow-bezoar bolus compound extract etc..
Sumatriptan succinate, Topiramate, Lamotrigine, atomoxetine, duloxetine hydrochloride, PIOGITAZONE HYDROCHLORIDE, Atorvastatin, fenofibrate, Valsartan, olmesartan medoxomil, Irbesartan, Carvedilol, quetiapine fumarate, esomeprazole magnesium, Lansoprazole, sildenafil citrate, sulfuric acid atazanavir, Raloxifene, erlotinib Hydrochloride, Ritonavir, darunavir, Sunitinib malate, Sebivo, capecitabine, Gefitinib, imatinib mesylate, Dipyridamole, bisulfate clopidogrel, voriconazole and Risperidone.
Rapidly disintegrating dosage form prepared by the present invention is not limited only to apply the oral agents agent of the discharge active component in oral cavity, applies also for the administration of other body cavitys, including rectum, vagina, intranasal, eye.It is not limited only to apply in human drugs, cosmetics, health products, food, animal-use drug product can also be applied to.
Rapidly disintegrating dosage form prepared by the present invention, compared with prior art, disintegration rate faster, can not only make the formulation of film-form, can also make the formulation of any feasible shapes according to the size and shape of mould.
Embodiment
Illustrate the present invention in further detail by the following examples, but these embodiments are the citing of the present invention, and the present invention is not restricted to this.It should be noted that the various details for the present invention can be changed arbitrarily, but certainly, these modifications are fallen within protection scope of the present invention.
Each active component, auxiliary material and the quantity listed according to table 1 prepare said preparation, and preparation method is as follows：Weigh each material according to the recipe quantity in table 1, it is dry-mixed it is uniform after, add purified water, addition is as shown in Table, after stirring, homogeneous in mulser, 2500 revs/min are placed in, homogeneous 15min, after homogeneous is finished, decoction is transferred in bottle,suction, vacuum outgas 30min, decoction is sub-packed in circular-cap again, is the fast disintegrating preparations that can obtain circular or similar round using vacuum drying or freeze-drying or low temperature drying.
Table 1
Implement
8 embodiment of embodiment 1 embodiment, 4 embodiment, 5 embodiment, 6 EXAMPLE Example 923
Nitrogen difficult to understand nitrogen Olanzapine hydrochloric acid department difficult to understand carrys out Olanzapine Olanzapine
Hydrochloric acid department comes the flat 5g of the flat 5g of Olanzapine Olanzapine, 5g, sesbania n 5g, sesbania 5g, sesbania
Locate 5g, sesbania
5g, sesbania sesbania sesbania gum lg, wooden 0.625g, field glue 0.8g, red glue 1.2g, print
Square 0.625g, field glue 1.5g, peach gum lg, wood glue lg, glue lg sugar alcohol 5g cyanines glue lg, phycocolloid degree glue
Group cyanines glue lg, wood glue 0.5g, sugar alcohol 5g xylose xylose glycine xylitol 0.2g, wooden 0.4g, wood
Into sugar alcohol 5g xylitol water 89g alcohol 5g, alcohol 5g 0.05g, water 5g, molasses sugar alcohol 5g sugar alcohols 5g
Water 93.375g 6g, water 87g water 89g water 89g 88.95g 93.375g water 89g water 88.4g
System
It is standby
500 500 500 500 500 500 500 500 500 total
Amount
System
Freeze low temperature
Standby 30 vacuum 30,30 °C of vacuum 30'C vacuum freeze dryings, 30 °C of vacuum vacuum 30 vacuum drying drying
The dry 4h in side dries 4h drying 4h 4h dryings 4h and dries 4h dryings 4h
4h 10h
Method
Film
Shape
0.25μ 0.50μ
The μ η ι -20 μ η ι matter m m of 0.37 μ π ι, 1.00 μ η ι, 0.33 μ π ι, 0.05 μ η ι 0.26
It is thick
Degree
Hole
The rate of gap 65.6% 80% 43.4% 60% 69.9% 98% -70.2% 10%
It is crisp
Broken 0.62% -- 0.54% 0.51 % 0.8% ---degree
Most
Greatly
Hold the IN/c 0.014N/C 0.015N/C 0.014N/c of 0.014N/c 0.015N/c Ο Ο Ι Ν/c 0.005
2
By m2 m2 m m2 m2 m2 m2Pressure
By force
9
IZT000/C10ZN3/X3d nnzimoz OAV
Claims (18)
- Claims1. a kind of speed collapses formulation, auxiliary material containing at least one active component and the membranaceous matrix of formation, space or cavity can be formed between wherein membranaceous matrix, the active component is distributed in the membranaceous its content or is distributed in the space or cavity that the membranaceous matrix formed, the ratio that the cumulative volume of the space or cavity accounts for the formulation cumulative volume is 10%-98%, and the speed, which collapses formulation upper surface and can bear maximum pressure, is not less than 0.0051N/cm2。2. speed according to claim 1 collapses formulation, it is characterised in that the speed collapses formulation in friability experiment without fragmentation or capping, and weightlessness is less than 0.8%.3. speed according to claim 1 collapses formulation, it is characterised in that the disintegration rate that the speed collapses formulation is less than 30 seconds.4. speed according to claim 1 collapses formulation, it is characterised in that the ratio that the cumulative volume of the space or cavity accounts for the formulation cumulative volume is 60-80%.5. speed according to claim 1 collapses formulation, it is characterised in that the membranaceous stromal surface is porous or complete non-porous.6. the speed according to any claim in claim 1-5 collapses formulation, it is characterised in that the membranaceous matrix average thickness is 0.05 μ π ι -20 μ ι η.7. speed according to claim 6 collapses formulation, it is characterised in that the membranaceous matrix average thickness is 0.05 μ ι η -1 μ ι η.8. speed according to claim 7 collapses formulation, it is characterised in that the membranaceous matrix average thickness is 0.05 μ ι η -0.5 μ ι η.9. the speed according to any claim in claim 1-8 collapses formulation, it is characterised in that the auxiliary material of the membranaceous matrix of formation comprises at least a kind of filmogen.10. speed according to claim 9 collapses formulation, it is characterised in that the auxiliary material of the membranaceous matrix of formation at least also includes at least one film reinforcing agent.U. speed according to claim 9 collapses formulation, it is characterised in that one or more kinds of compositions of the filmogen in sesbania gum, Indian gum, furcellaran and peach gum.12. speed according to claim 9 collapses formulation, it is characterised in that the filmogen is sesbania gum.13. speed according to claim 10 collapses formulation, characterized in that, one or more kinds of compositions of the film reinforcing agent in xylitol, glycine, serine, mannitol, sorbierite, trehalose, dextrin, sodium chloride or alumina silicate.14. the speed according to claim 13 collapses formulation, it is characterised in that the film reinforcing agent is xylitol.15. the speed according to any claim in claim 1-14 collapses formulation, it is characterised in that the auxiliary material of the membranaceous matrix of formation also includes the one or more in suspending agent, sweetener, essence, antioxidant, defoamer.16. the speed according to any claim in claim 1-15 collapses formulation, it is characterized in that, the speed collapses the oral agents agent that formulation is not limited only to apply the discharge active component in oral cavity, applies also for the administration of other body cavitys, including rectum, vagina, intranasal, eye.17. the speed according to any claim in claim 1-15 collapses formulation, it is characterised in that the speed collapses formulation and is not limited only to apply in human drugs, cosmetics, health products, food, animal-use drug product can also be applied to.18. the speed according to any claim in claim 1-15 collapses formulation, it is characterised in that the thickness that the speed collapses formulation is lmm- l Omni o19. a kind of prepare the preparation method that speed described in claim 1 collapses formulation, it is characterised in that comprises the following steps：（A) prepare to include and form the auxiliary material of membranaceous matrix and the solution of active component or suspension（B) solution or suspension are sub-packed in bubble-cap, are dried using vacuum drying or low temperature drying or freeze-drying method.
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