CN110267683A - Solid pharmaceutical preparation - Google Patents
Solid pharmaceutical preparation Download PDFInfo
- Publication number
- CN110267683A CN110267683A CN201880009378.4A CN201880009378A CN110267683A CN 110267683 A CN110267683 A CN 110267683A CN 201880009378 A CN201880009378 A CN 201880009378A CN 110267683 A CN110267683 A CN 110267683A
- Authority
- CN
- China
- Prior art keywords
- pharmaceutical preparation
- solid pharmaceutical
- tablet
- gelating agent
- uncoated tablets
- 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.)
- Pending
Links
Classifications
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K9/20—Pills, tablets, discs, rods
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Health & Medical Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- General Preparation And Processing Of Foods (AREA)
Abstract
Solid pharmaceutical preparation of the invention is the solid pharmaceutical preparation being orally ingested, according to the increased mode of the lubricity on surface is made and contacting with aqueous solution.Solid pharmaceutical preparation contains gelating agent.Gelation does not occur for solid pharmaceutical preparation above-mentioned gelating agent in the state of before taking, and by contacting with aqueous solution when taking, gelation occurs for above-mentioned gelating agent.Solid pharmaceutical preparation can be the form of tablet or capsule.The disintegration time that solid pharmaceutical preparation preferably takes water as a solvent measurement is within 60 minutes.The maximum stress that the solid pharmaceutical preparation before preferably being compared in investment water with the maximum stress of prescriptive procedure measurement similarly measures is low.
Description
Technical field
The present invention relates to a kind of solid pharmaceutical preparations.
Background technique
It is introduced with the raising of consumer health's consciousness in recent years and as the new system that food is shown functional aobvious
Show food system, it is contemplated that the market scale of Japanese healthy food, nutritional supplement also will be enlarged by from now on.In nutritional supplement,
As the preparation of oral administration, mostly using solid pharmaceutical preparations such as tablets, but big tablet or multiple tablets are taken simultaneously for not
Arrogate to oneself the people for swallowing tablet, particularly is usually difficult for the low child of function of deglutition, old man.
It is swallowed to become easy tablet, it is desirable that improve the sliding easiness of tablet, to jam difficulty of throat etc..
Multiple this technology (patent text put and studied in terms of the coating of the solid pharmaceutical preparations such as tablet of considering are reported so far
Offer 1~3).But even if tablet surface becomes easy sliding by coating, taking improves to a certain extent, but from tool
Resistance when having the larynx portion of complicated shape to pass through is still larger, swallows improvement and insufficient.
Existing technical literature
Patent document
Patent document 1: Japanese Unexamined Patent Publication 11-60472 bulletin
Patent document 2:US2010/0266687A1
Patent document 3:US2014/0294958A1
Summary of the invention
Problems to be solved by the invention
Even the purpose of the present invention is to provide one kind do not arrogate to oneself swallow the people of solid pharmaceutical preparation also can resistance be easy smallly
The solid pharmaceutical preparation taken.
Means for solving the problems
The present invention provides a kind of solid pharmaceutical preparation, is the solid pharmaceutical preparation being orally ingested, wherein its according to by with it is aqueous molten
Liquid contacts and the increased mode of the lubricity on surface is made.
Detailed description of the invention
Fig. 1 is the concept map of the measuring method of maximum stress.
Fig. 2 is electromyogram when only taking water.
Fig. 3 is electromyogram when taking the tablet manufactured in embodiment 1.
Fig. 4 is electromyogram when taking the tablet manufactured in embodiment 2.
Specific embodiment
Hereinafter, based on its preferred embodiment, the present invention will be described.
The solid pharmaceutical preparation of present embodiment is the solid pharmaceutical preparation being orally ingested, according to by contacting and table with aqueous solution
The increased mode of the lubricity in face is made.Aqueous solution mentioned here refers to that water, tea, cold drink, milk etc. are commonly used in
Liquid, saliva or their mixture drunk.Solid pharmaceutical preparation of the invention due to containing gelating agent, by with water
Property solution contact and the lubricity on surface increase.Solid pharmaceutical preparation preferably contains gelating agent in its surface element.Present embodiment
Gelation does not occur for solid pharmaceutical preparation gelating agent in the state of before taking, by being contacted with aqueous solution when taking, gelation
Gelation occurs for agent.As gelating agent, the object of lubricity is played using powdery (particle shape) and when containing aqueous solution body
Matter.In the present specification, gelation is not necessarily able to confirm that the presence of gel, as long as passing through gelating agent and aqueous solution
Contact is to play lubricity.However, it is preferred to can actually confirm the presence of gel and contacting with aqueous solution.Specifically
For, solid pharmaceutical preparation preferably is stood on plastic substrate, to every 1mm of solid pharmaceutical preparation2Surface area is added dropwise 25 DEG C with suction pipe
0.2 μ L of water, in this state keep 10~20 seconds after, be able to confirm that the presence of gel.
Gelating agent plays lubricity and contacting with aqueous solution can be by confirmation of such as getting off: for present embodiment
Solid pharmaceutical preparation, by the solid pharmaceutical preparation put into water in after maximum stress be lower than by the solid pharmaceutical preparation put into water in front of most
Big stress.Here, refer in investment water and stand solid pharmaceutical preparation on plastic substrate, to every 1mm of solid pharmaceutical preparation2Surface area
25 DEG C of 0.2 μ L of water is added dropwise with suction pipe, is kept for 10~20 seconds in this state.The determination step of maximum stress is as follows.Measurement
The schematic diagram of device is as shown in Figure 1.Appended drawing reference 1 in Fig. 1 is solid pharmaceutical preparation, appended drawing reference 2 is slit, appended drawing reference 3 is
Silicone tube.
The determination step > of < maximum stress
Using configuration along the vertical direction and the silicone tube that can movably fix along the vertical direction and in the lateral direction
Fixed a pair of of the slit of the state of the silicone tube is clipped, 1 solid pharmaceutical preparation is filled in the downside of the slit of the silicone tube, makes this
Silicone tube is moved upward along the slit, and thus measurement makes the silicone tube relative to solid pharmaceutical preparation upwards with 0.5mm/ seconds
Maximum stress when speed movement 20mm.Wherein, as silicone tube used in said determination, the sectional area ratio of silicone tube is used
The sectional area of solid pharmaceutical preparation is small and 40% big silicone tube than the sectional area of solid pharmaceutical preparation.The sectional area of solid pharmaceutical preparation relative to
The ratio of the sectional area of silicone tube is preferably 40% or more and 60% hereinafter, more preferably 45% or more and 55% or less.
In addition, for solid pharmaceutical preparation of the invention, after the solid pharmaceutical preparation measured according to above-mentioned steps is put into water most
Big stress is less than 20N, more preferably 15N hereinafter, further preferably 10N hereinafter, particularly preferably 5N or less.
Above-mentioned up and down direction refers to the direction orthogonal with horizontal plane.In addition, above-mentioned left and right directions refers to and upper and lower
To orthogonal direction.
The sectional area of above-mentioned silicone tube refers to, will be not filled with the silicone tube in the state of solid pharmaceutical preparation with its length side
The area of the part surrounded by silica gel pipe internal surface into section made of orthogonal direction cutting.
In addition, the sectional area of solid pharmaceutical preparation refers to, be filled in solid pharmaceutical preparation in the state of silicone tube with silicone tube
The area in the section in section made of the orthogonal face internal cutting off of length direction with maximum area.
In addition, the disintegration time that the solid pharmaceutical preparation of present embodiment takes water as a solvent measurement is within 60 minutes, preferably
Within 40 minutes, within further preferably 20 minutes.It is easy as the lower limit of disintegration time, such as from the manufacture of solid pharmaceutical preparation
Property is set out, and can be enumerated 1 minute or more.Disintegration time refers to the time until the sample disintegration in solvent.Disintegration time
Determination step can be according to the method for record in " the slaking test method " of " 6.09 " item in " the 15th correction Pharmacopeia of Japan ".?
In the case where using the tablet that tablet diameters are 3~15mm, tablet thickness is 4~7mm, weight is 150~500mg, as collapsing
Exerciser is solved, it is preferable to use Fushan Mountain industry companies, model: NT-400.Thickness of the solid pharmaceutical preparation of present embodiment relative to preparation
The disintegration time of degree is preferably 0.01 minute/mm or more and 25 minute/mm hereinafter, more preferably 0.05 minute/mm or more and 20
Minute/mm hereinafter, further preferably 0.1 minute/mm or more and 12 minute/mm hereinafter, still more preferably for 0.15 minute/
Mm or more and 8 minute/mm is hereinafter, most preferably 0.2 minute/mm or more and 4 minute/mm or less.
The determination step > of < disintegration time
1 solid pharmaceutical preparation is respectively put on the glass tube of the slaking test device with 6 glass tubes.Each glass tube
Upper and lower surface opening is equipped with the stainless (steel) wire that mesh is 1.8mm~2.2mm in the lower surface of glass tube.Solid system will be housed
The glass tube of agent is put into 37 ± 2 DEG C of water, and slaking test device is made to work.The glass tube in slaking test device is observed, if really
Recognize the case where solid pharmaceutical preparation starts disintegration, then the case where lifting glass tube, observe the disintegration of solid pharmaceutical preparation.The operation is repeated,
Observation is disintegrated completely to solid pharmaceutical preparation.Measurement is from making slaking test device work when 6 solid pharmaceutical preparations are all disintegrated
Time only, the time which is obtained is as disintegration time.In addition, having no the residual of solid pharmaceutical preparation completely in glass tube
Object or even if it is visible be also do not hold its shape soft substance when, be judged as solid pharmaceutical preparation be disintegrated.
The form of solid pharmaceutical preparation as present embodiment can enumerate tablet, capsule, pill, powder etc., preferably tablet
Or the form of capsule.In the case where any form, gelating agent is present in the most surface portion of solid pharmaceutical preparation.Most surface portion is
Refer to be located at solid pharmaceutical preparation surface side part, refer to the 0mm or more from the surface of solid pharmaceutical preparation towards center position and 1mm with
Under range.The solid pharmaceutical preparation of present embodiment has gelating agent particularly preferably in its most surface portion entirety.This specification
In, if it is possible to confirm that there are gelating agents more than at different 2 in the most surface portion of solid pharmaceutical preparation, it can be said that in most table
There is gelating agent in facial entirety.Here, surface element there are gelating agents can be by cutting the solid system of taking with scalpel etc.
Any part 30mg in most surface portion of agent or so is added suitable water and carries out gelation to confirm.Such as it is whole in most surface portion
Solid pharmaceutical preparation in body with gelating agent can be used as the tabletting object of the mixed-powder containing gelating agent and be readily derived.
The surface element of solid pharmaceutical preparation can have different structures from the part of its central side, or can also not have this
The structure of sample.For example, solid pharmaceutical preparation can be multilayered structure as core tablet.Wherein, solid pharmaceutical preparation does not have multilayer knot
Structure and when being single layer structure, be preferred from the easiness angularly of manufacture.
Solid pharmaceutical preparation can also have gelating agent at the position other than most surface portion.For example, solid pharmaceutical preparation can be most
Contain gelating agent in part (also referred to as central part) the two of surface element and its central side.As such solid pharmaceutical preparation
Example can enumerate the tablet of the uncoated tablets with single layer structure.In solid pharmaceutical preparation, the composition in most surface portion and central part
Composition can be the same or different, preferably identical from the ease of manufacturing of the tablet with uncoated tablets.In solid system
There are gelating agents for example can be cut and be taken with scalpel etc. by the way that solid pharmaceutical preparation is cut into half with cutter etc. for the central part of agent
Surface away from solid pharmaceutical preparation is more than any part 30mg or so in the central side part of 1mm, and the liquid such as suitable water Jie is added
Matter carries out gelation to confirm.It should be noted that being not included in the solidifying of the application as the ingredient that aftermentioned disintegrating agent outlines
In gelatinizing agent.
The case where solid pharmaceutical preparation to present embodiment is tablet is illustrated.
Tablet is preferably the tablet with the uncoated tablets for having gelating agent.In general, uncoated tablets (also referred to as plain piece) are
Refer to and the tablet of coatings is not formed on its surface.In the present specification, " tablet with uncoated tablets " refers in tablet
There is the part that coatings are not formed on surface, which is the tablet of the state of uncoated tablets (hereinafter, tablet table will be not formed
The part of the coatings in face is known as uncoated tablets part).In addition, in the present specification, " uncoated tablets " refer in surface essence
On be not formed coatings tablet (be coated layer covering area account for tablet surface area tablet of the ratio less than 5%).
In the present specification, " uncoated tablets " are contained within the concept of " tablet with uncoated tablets ".
The performance when the liquid mediums such as water and uncoated tablets part contact of the tablet with uncoated tablets of present embodiment
Lubricity (also referred to as sliding property).The tablet with uncoated tablets of present embodiment is preferably in the most surface of uncoated tablets part
Portion has gelating agent.Most surface portion refers to the part for being located at surface side in uncoated tablets part, refers to from uncoated tablets portion
0mm or more and 1mm below range of the surface divided towards center position.The tablet of present embodiment passes through in uncoated tablets portion
Divide, particularly the most surface portion of uncoated tablets part has gelating agent, when being contacted with liquid mediums such as water in uncoated tablets
Partial surface generates lubrication.Even if the tablet with uncoated tablets of present embodiment is not provided with coatings as a result, also it is easy
It swallows.Particularly preferably the tablet with uncoated tablets integrally has gelating agent in the most surface portion of uncoated tablets part.At this
In specification, if it is possible to confirm that there are gelating agents more than at different 2 in the most surface portion of uncoated tablets part, then may be used
To say that the most surface portion in uncoated tablets part integrally has gelating agent.Here, in surface element, there are gelating agents to lead to
It crosses and cuts any part 30mg or so for taking its most surface portion with scalpel etc., the liquid mediums such as suitable water are added and carry out gelation
To confirm.As described later, the piece with the uncoated tablets in the most surface portion entirety of uncoated tablets part with gelating agent
Agent can as the mixed-powder containing gelating agent tabletting object and be readily derived.
The above-mentioned tablet with uncoated tablets plays gelating agent and there are uncoated tablets part, therefore not
Coating tablet part is preferably in the most surface of tablet.Specifically, table shared by the uncoated tablets part of the most surface of tablet
The ratio of area is preferably 70% or more, and more preferably 90% or more, particularly preferably 95% or more.In addition, having above-mentioned
In the case that the tablet of uncoated tablets has coatings, the ratio shared in the surface area of tablet for being coated layer covering is preferred
Less than 30%, particularly preferably less than 10%, most preferably (refer to the area for being coated layer covering in tablet essentially without coatings
Surface area in shared ratio less than 5%).In addition, in the case where the above-mentioned tablet with uncoated tablets has coatings,
The thickness of coatings is preferably 3mm hereinafter, more preferably 2mm is hereinafter, spy from the surface of uncoated tablets part towards center position
It You Xuanwei not 1mm or less.By make coatings with a thickness of 1mm hereinafter, can easily play the effect of gelating agent, can
Manufacturing cost is reduced, and the enlargement of tablet can be prevented.In the case where coatings only cover tablet a part, coatings
Can be biased to partially continued presence, or island can also be dispersed into etc..As long as example, by will except gelating agent with
Outer powder (such as carbohydrate or other seasonings etc.) be coated in uncoated tablets surface and in a part of tablet surface
There are degree as coatings, then since the gelating agent for being present in uncoated tablets part plays effect, can be allowed.
In the case where the solid pharmaceutical preparation of present embodiment is capsule, the capsule is preferably by the coatings containing gelating agent
Covering.Gelating agent is preferably attached to the surface of film, capsule.For example, by will the powder containing gelating agent and soft capsule or
Hard capsule mixing, the surface of the capsule can be covered with coatings.At this point, the table with the wetting capsule such as solvent can also be passed through
Face improves adhesion.In the case where the powder containing gelating agent is not easy to be attached to the surface of soft capsule or hard capsule, lead to
The surface etc. for soaking the capsule is crossed, can be improved the adhesion of powder.As another covering method, can by soft capsule or
Hard capsule is dissolved with the solution of gelating agent by spraying to be coated to the surface of the capsule.As capsule, hard capsule can be,
But particularly preferred soft capsule.Range preferably from capsule surface product 50% or more on the surface of capsule is covered with coatings, more
It is preferred that 70% or more, further preferred 90% or more, most preferably entire surface is capped.
In the case where the solid pharmaceutical preparation of present embodiment is pill, which preferably has not wrapping containing gelating agent
Clothing pill.Such uncoated pill plays lubricity when surface and water contact.In general, uncoated pill refers to not in its table
The pill of face formation coatings.The pill especially has gel in the most surface portion of uncoated pill in uncoated pill
Agent, thus when contacting with liquid mediums such as water, uncoated pill surface generates lubrication.Even if being not provided with coatings as a result,
Also it is easy to swallow.There is energy due to the coatings for being not provided with covering its entire surface as the pill of uncoated pill
It enough prevents the enlargement of pill, reduce the advantages of manufacturing cost.
In the case where the solid pharmaceutical preparation of present embodiment is powder, preferably the powder is by the coatings containing gelating agent
Covering.For example, by the solution for containing gelating agent to the powder spray for becoming core material, a part that can obtain surface is contained
There is the powder of the coatings covering of gelating agent.
In order to realize above-mentioned lubricity and disintegration time, below used in the solid pharmaceutical preparation to present embodiment preferably at
Divide and composition is described in detail.
It is ingredient and group contained in tablet when solid pharmaceutical preparation is tablet about the ingredient and composition of solid pharmaceutical preparation below
At being ingredient and composition contained in capsule when solid pharmaceutical preparation is capsule.Particularly preferred solid pharmaceutical preparation is with uncoated tablets
Tablet and solid pharmaceutical preparation below ingredient and composition belong to constitute tablet uncoated tablets contained in ingredient and composition.
In solid pharmaceutical preparation, in order to increase the lubricity on surface and contacting with aqueous solution, cooperate gelating agent.Make
For the gelating agent contained in solid pharmaceutical preparation, lubrication is played using for powdery (particle shape) and when containing liquid mediums such as water
The substance of property.As gelating agent, can enumerate selected from such as xanthan gum, locust bean gum, guar gum, mannosan, Glucomannan,
Hyaluronic acid, agar, alginic acid, tamarind gum, plantasan, tara gum, carrageenan, acacia gum (acacia gum),
Gum arabic, bassora gum, Karaya Gum, cassia gum (cassia gum), rhamsan gum, Weilan gum, is intended greatly ghatti gum
Phoma glue (Macrophomopsis Gum), curdlan, pulullan polysaccharide, gellan gum are (deacylation fundamental mode gellan gum, natural
Type gellan gum), the natural polysaecharides such as pectin and soybean polysaccharides；The protein breakdowns object such as collagen；The polyaminoacid such as polyglutamic acid；It is poly-
It is at least one kind of in the biopolymers such as lactic acid, polyglutamic acid and their salt and derivative.Wherein, particularly preferably natural more
Carbohydrate.
As above-mentioned derivative, derivatives of hyaluronic acids, alginic acid derivative and polyglutamic acid derivative etc. can be enumerated.
In addition, alginate, hyaluronate, polyglutamate etc. can be enumerated as above-mentioned salt.As derivatives of hyaluronic acids,
Hyaluronic acid ester, acetylation hyaluronic acid etc. can be enumerated.As alginic acid derivative, alginic acid ester etc. can be enumerated.As poly- paddy
Threonine derivative can enumerate polyglutamic acid esters etc..As alginate, can enumerate sodium alginate, potassium alginate, ammonium alginate and
Calcium alginate etc..As hyaluronate, Sodium Hyaluronate and potassium hyaluronate etc. can be enumerated.As polyglutamate, can lift
Polyglutamic acid sodium and polyglutamic acid potassium etc. out.Gelating agent can only be used alone a kind, two or more can also be applied in combination.
The angle being disintegrated in vivo is easy after intake, preferably gelating agent contains poly- selected from locust bean gum, sweet dew
Sugar, Glucomannan, hyaluronic acid, agar, tamarind gum, plantasan, tara gum, cassia gum, gum arabic, India tree
Glue, bassora gum, Karaya Gum, cassia gum, rhamsan gum, Weilan gum, big Phomopsis glue, curdlan, Propiram are more
Sugar, gellan gum, polyaminoacid, polylactic acid and one or more of their salt and derivative are (hereinafter also referred to as specific solidifying
Gelatinizing agent), the angle that disintegration and lubricity are taken into account also is played with high level from other than the disintegration easiness after intake is excellent
Degree sets out, and particularly preferably contains locust bean gum.
In addition, from the viewpoint of the angle for seeking disintegration and lubricity to take into account, from the viewpoint of manufacturing, preferably combine 2 kinds with
On gelating agent, further preferably combine specific gelating agent with the gelating agent in addition to specific gelating agent.
Specifically, it is preferable that by as the locust bean gum of specific gelating agent and as the gelation in addition to specific gelating agent
The combination such as xanthan gum, guar gum, alginic acid, carrageenan of agent.For example, by combining locust bean in xanthan gum or guar gum
Glue can effectively improve and swallow easiness brought by lubrication sense.In addition, by combining locust bean gum in guar gum, it can
With the solid pharmaceutical preparation that intracorporal disintegration after being taken in is excellent.
In solid pharmaceutical preparation, lubrication sense when being contacted to fully generate with liquid mediums such as water, preferably gelating agent
Ratio is 0.01 mass % or more.In addition, from the dissolution easiness angularly of effective component, it is solidifying preferably in solid pharmaceutical preparation
The ratio of gelatinizing agent is 70 mass % or less.From these angles, in solid pharmaceutical preparation, the ratio of gelating agent is more preferably
0.1 mass % or more and 60 mass % hereinafter, further preferably 1 mass % or more and 50 mass % hereinafter, further it is excellent
3 mass % or more are selected as and 30 mass % hereinafter, most preferably 5 mass % or more and 20 mass % or less.Present embodiment
Solid pharmaceutical preparation in solid pharmaceutical preparation containing at least one kind of in above-mentioned specific gelating agent in the case where, as solid system
The preferred scope of the gross mass of above-mentioned specific gelating agent in agent, can enumerate identical as the preferred scope of above-mentioned gelating agent
Range.At least one kind of gross mass said here in above-mentioned specific gelating agent refers to, contains only in solid pharmaceutical preparation
It is a kind of the quality in the case where a kind in above-mentioned specific gelating agent, contains 2 in these in solid pharmaceutical preparation
Kind or more in the case where be their gross mass.
In the case that solid pharmaceutical preparation of the invention contains specific gelating agent and gelating agent in addition to this, solid system
The former in agent: the ratio of the latter is from the viewpoint of taking into account lubricity and disintegration, relative to 100 mass parts of the latter, the former
It is special more than further preferably 15 mass parts and 900 below the mass more than preferably 10 mass parts and 1000 below the mass
It You Xuanwei not more than 20 mass parts and 800 below the mass.
For example, in the case that solid pharmaceutical preparation of the invention contains xanthan gum and locust bean gum, the former in solid pharmaceutical preparation: after
The ratio of person is from the angle for the content for improving lubricity and effective component, based on 100 mass parts of xanthan gum, locust bean
Glue is more preferably 10 mass parts or more 1000 below the mass, more than further preferably 15 mass parts and 900 below the mass,
More than particularly preferably 20 mass parts and 800 below the mass.
In addition, in the case that solid pharmaceutical preparation of the invention contains guar gum and locust bean gum, the former in solid pharmaceutical preparation: after
The ratio of person is from the angle for the content for improving lubricity and effective component, relative to 100 mass parts of guar gum, locust bean gum
More than more preferably 10 mass parts and 1000 below the mass, more than further preferably 15 mass parts and 900 below the mass,
More than particularly preferably 20 mass parts and 800 below the mass.
Solid pharmaceutical preparation preferably also containing selected from sugar alcohol, monosaccharide, disaccharides, oligosaccharide, cellulose, cellulose derivative,
One or more of starch, starch derivatives and starch decomposition product (are also referred to as specific excipient) below.By that will coagulate
Gelatinizing agent and these specific excipient compositions, can be obtained that lubricity is excellent, disintegration time also short solid pharmaceutical preparation.
As specific excipient, as set forth above, it is possible to comprising selected from (A) monosaccharide, (B) disaccharides, (C) oligosaccharide,
(D) one or more of cellulose, (E) cellulose derivative, (F) starch, (G) starch derivatives and (H) starch decomposition product, but
From the angle for seeking disintegration and lubricity to take into account, will preferably belong to not in the ingredient recorded in two or more (A)~(H)
It is generic at subassembly.Specifically, can for example enumerate the combination of disaccharides and cellulose, disaccharides and reduction maltose
The combination of combination, disaccharides and starch.In addition, will further preferably belong to not in the ingredient recorded in 3 kinds or more (A)~(H)
It is generic at subassembly.Specifically, the combination of disaccharides, starch and cellulose can be for example enumerated, disaccharides, reduction malt
Sugar and the combination of cellulose etc..
As sugar alcohol, the alcohol of monosaccharide, the alcohol of disaccharides, alcohol more than trisaccharide can be enumerated.As the alcohol of monosaccharide, can enumerate for example
The tetritol such as antierythrite, D- threitol, L- threitol, the pentitols such as D-arabinose alcohol, xylitol, D- iditol, half
The hexitols such as lactitol (dulcitol), D-Glucose alcohol (D-sorbite), the cyclic alcohol such as inositol, mannitol, volemitol, core
Sugar alcohol, avocado sugar, D- erythro form-D- galactolipin-octose alcohol etc..In addition, the alcohol as disaccharides, such as reduction maltose can be enumerated
(maltitol), galactitol, isomalt (Palatinitol) etc..In addition, wheat can be enumerated as alcohol more than trisaccharide
Bud trisugar alcohol, Isomaltotriose alcohol, pine camphor etc..As sugar alcohol, combined from using used in the present invention with gelating agent
It is particularly preferably at least one kind of in the alcohol selected from disaccharides from the perspective of the manufacturing of hardness to the tablet of special tabletting etc.,
It is particularly preferably at least one kind of in reduction maltose and isomalt.
As monosaccharide, glucose, galactolipin, fructose, mannose can be enumerated.Wherein, from seek being easy to get property, disintegration
The angle that property and lubricity are taken into account is set out, preferably glucose.
As disaccharides, sucrose, maltose, lactose, trehalose, turanose, cellobiose can be enumerated.Wherein, from disintegration
From the perspective of property, be preferably selected from one or more of trehalose, sucrose, maltose, from seek being easy to get property, disintegration and
From the perspective of lubricity is taken into account, more preferable sucrose, maltose.The present invention can be obtained in the case where containing lactose
Effect, but from the viewpoint of seeking disintegration and lubricity to take into account, as disaccharides, more preferably in addition to lactose two
Carbohydrate.
As oligosaccharide, trisaccharide or more and 20 sugar sugar below can be enumerated, preferably more than trisaccharide and ten sugar are below
Sugar, more preferably more than trisaccharide and six sugar are hereinafter, specifically, raffinose, maltotriose, Song Santang, gentianose, A Kabo
Sugar, stachyose, galactose oligosaccharides, oligofructose, mannosan, isomalto-oligosaccharide (Isomaltotriose, panose), oligomeric wood
Sugar, soyabean oligosaccharides, aspergillus niger oligosaccharide, newborn fructo-oligose.Especially from seeking being easy to get property, disintegration and lubricity simultaneous
The angle of Gu is set out, it is preferable to use isomalto-oligosaccharide or oligofructose.
In addition to other than the angle of the masking of taste, also from the angle for promoting salivary secretion, further preferably solid pharmaceutical preparation
Contain any one of monosaccharide, disaccharides, oligosaccharide.Especially solid pharmaceutical preparation preferably contains these carbohydrates in surface element.
As cellulose, cellulose powder, avicel cellulose can be enumerated.Avicel cellulose refers to will be from fibrous plant
The alpha-cellulose acid moieties obtained with pulp form ground substance obtained from depolymerization, purification.For example, can enumerate, " the 15th changes
Positive Pharmacopeia of Japan solution is told a story " (wide river book shop development row) middle substance for belonging to avicel cellulose recorded.Avicel cellulose can be with
It is divided into avicel cellulose powder and avicel cellulose compound, but either of which can be used in solid pharmaceutical preparation of the invention
Kind.
As cellulose derivative, carboxymethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose and first can be enumerated
Base cellulose.Carboxymethyl cellulose is from the angle of the angle of accessibility, lubricity and disintegration time taken into account, preferably
Degree of etherification falling is 0.2mol/C6~1.0mol/C6, further preferably 0.5mol/C6~0.8mol/C6.Even if containing inside
In the case where being crosslinked with the croscarmellose sodium of sodium carboxymethylcellulose, low degree of substitution hydroxypropyl cellulose, it can also obtain
To effect of the invention, but from the viewpoint of seeking disintegration and lubricity to take into account, as cellulose derivative, more preferably
Cellulose derivative in addition to croscarmellose sodium and low degree of substitution hydroxypropyl cellulose.
As starch, native starch can be enumerated.As the source of starch, corn, potato, pueraria lobata, cassava, sweet can be enumerated
Potato, rice, wheat, wheat, barley, Chinese yam, taro etc..In the case where cooperating starch, especially from seeking disintegration and lubrication
The angle that property is taken into account is set out, and is particularly preferably cooperated with sugar alcohol compositions.
As starch derivatives, can enumerate chemical starch, oxidized starch, enzyme treated starch and alphalysed starch, starch phosphate,
Di(2-ethylhexyl)phosphate starch, amylcose acetate, octenyl succinic acid starch, two starch of glycerol, carboxymethyl starch, hydroxypropul starch, crosslinking are formed sediment
Powder, soluble starch, graft starch, sodium carboxymethyl starch, from the angle for taking into account lubricity and disintegration time, preferably αization
Starch.In the case where cooperating starch derivatives, from the angle for seeking disintegration and lubricity to take into account, particularly preferably with sugar
Alcohol combines to cooperate.It should be noted that effect of the invention can be obtained containing sodium carboxymethyl starch
Fruit, but from the viewpoint of seeking disintegration and lubricity to take into account, as starch derivatives, more preferably remove sodium carboxymethyl starch
Starch derivatives in addition.
As starch decomposition product, dextrin can be enumerated, can preferably enumerate the dextrin that DE is 8~9.5.
The content of specific excipient in solid pharmaceutical preparation is from further increasing and with gelating agent and specific excipient
The angle of effect set out, be 10 mass parts or more preferably with respect to 100 mass parts of gelating agent in uncoated tablets, from raising
The angle of the content of effective component is set out, and the amount of specific excipient is preferably with respect to 100 matter of gelating agent in uncoated tablets
Measuring part is 3000 below the mass.From these angles, the amount of the specific excipient in solid pharmaceutical preparation is preferably with respect to solid
100 mass parts of gelating agent in body preparation be 10 mass parts or more and 3000 below the mass, more preferably 20 mass parts with
It is upper and 2500 below the mass, more than particularly preferably 30 mass parts and 2000 below the mass.
In addition, the amount of excipient preferably with respect to 100 mass parts of solid pharmaceutical preparation be 1 mass parts more than and 90 mass parts with
Under, more than more preferably 2 mass parts and 80 below the mass, more than most preferably 3 mass parts and 70 below the mass.Especially
From the angle of disintegration, specific excipient preferably accounts for 40 mass % or more, more preferably 50 matter in solid pharmaceutical preparation
% or more, further preferably 60 mass % or more are measured, can also be 70 mass % or more.In addition, as specific excipient
Amount the upper limit, from the angle containing gelating agent, preferably in solid pharmaceutical preparation for 95 mass % hereinafter, more preferably 90
Quality % or less.
The angle high from lubricity, the preferably solid pharmaceutical preparation in the present invention contain the list in specific excipient
One or more of carbohydrate, disaccharides, oligosaccharide, starch derivatives (especially alphalysed starch) and starch decomposition product, more preferably contain
There are monosaccharide, disaccharides, oligosaccharide or starch decomposition product.
From the viewpoint of in addition to lubricity disintegration it is also excellent, particularly preferred solid pharmaceutical preparation is as specific excipient
Containing monosaccharide, disaccharides, oligosaccharide, sugar alcohol, avicel cellulose or cellulose derivative (especially carboxymethyl cellulose), into
One step preferably comprises monosaccharide, disaccharides, oligosaccharide, sugar alcohol or carboxymethyl cellulose.
In addition, obtaining from the caking property for the raw material powder for improving solid pharmaceutical preparation, when solid pharmaceutical preparation is tablet through tabletting
The easiness of the preparation of the hardness of tablet etc., the angle of screening effect for the unpleasant taste for obtaining effective component are set out, also excellent
Choosing contains sugar alcohol, disaccharides.
Most preferably monosaccharide, disaccharides, oligosaccharide, sugar alcohol, avicel cellulose and carboxymethyl cellulose are specific as accounting for
Main component in excipient, the ingredient specifically as the 50 mass % or more in specific excipient contain.
In addition, preferably solid pharmaceutical preparation is as specific excipient composition from the angle that disintegration and lubricity improve
Containing one or more of disaccharides, oligosaccharide, sugar alcohol, cellulose derivative, starch and starch decomposition product is selected from, particularly preferably
The combination of disaccharides and oligosaccharide or cellulose derivative.Uncoated tablets contain disaccharides and its as specific excipient composition
When his specific excipient, from the viewpoint of taking into account lubricity and disintegration, other specific excipient are relative to disaccharides
100 mass parts, more than more preferably 1 mass parts and 1000 below the mass, more than further preferably 5 mass parts and 300 matter
Part is measured hereinafter, more than particularly preferably 5 mass parts and 100 below the mass.
In addition, preferably solid pharmaceutical preparation is as specific excipient composition from the angle for improving disintegration and lubricity
Contain sugar alcohol and starch or alphalysed starch.From the viewpoint of taking into account lubricity and disintegration, solid pharmaceutical preparation is as specific figuration
When agent combination contains sugar alcohol and starch or alphalysed starch, starch or alphalysed starch are relative to 100 mass parts of sugar alcohol, more preferably 10 matter
Part or more and 1000 below the mass is measured, more than further preferably 30 mass parts and 700 below the mass, particularly preferably 50
More than mass parts and 500 below the mass.
In present embodiment, easy solid system is swallowed from the balance for being easier to obtain hardness and degree of gelation is good
The angle of agent is set out, and preferably comprises starch, starch derivatives or starch decomposition product and by itself and xanthan gum, locust bean gum and melon
That glue and their salt and derivative, particularly locust bean gum combination.
In addition, as described later, from being easier to obtain hardness, swallow easiness and sliding easiness is excellent, swallows readily
The angle of solid pharmaceutical preparation is set out, further preferably in the particle containing sugar alcohol and gelating agent for being gelled agent covering without containing surface
Under conditions of, by sugar alcohol and at least one kind of group in xanthan gum, locust bean gum and guar gum and their salt and derivative
It closes.In addition, as described later, under conditions of being free of the coating of gelating agent, also preferably containing by selected from starch and xanthan
The gelating agent and reduction wheat that at least one or more in glue, locust bean gum or guar gum and their salt and derivative is constituted
The solid pharmaceutical preparation of bud sugar.
Solid pharmaceutical preparation preferably contains specific excipient in most surface portion, and then is with uncoated tablets in solid pharmaceutical preparation
In the case where tablet, preferably also contain specific excipient in central part.
3. other compositions
Solid pharmaceutical preparation preferably comprises silica etc. as flow improver.As silica, particle two can be enumerated
Silica and light silicon anhydride.In the case where containing silica, the amount of silica is preferably with respect to 100 matter of solid pharmaceutical preparation
Measuring part is 0.01 mass parts or more and 2 below the mass, more than more preferably 0.1 mass parts and 1.8 below the mass, further
More than preferably 0.5 mass parts and 1.7 below the mass, more than most preferably 1 mass parts and 1.5 below the mass.
The angle of (preventing pestle adhesion when tabletting) is improved from manufacturing, solid pharmaceutical preparation preferably comprises lubricant.Make
For lubricant, magnesium stearate, calcium stearate can be enumerated.In the case where containing lubricant, ratio is in solid system of the invention
It is preferably 0.1 mass % or more and 20 mass % in agent hereinafter, more preferably 0.5 mass % or more and 10 mass % or less.
Solid pharmaceutical preparation can contain effective component.Effective component described herein can be medicament, be also possible to except medicament
Functional components, plant or animal in addition, microbe-derived processed material etc..Solid pharmaceutical preparation in addition to above-mentioned effective component,
It, can also tune containing adhesive, in addition to carbohydrate other than specific excipient, silica, disintegrating agent, lubricant, carbohydrate
Taste substance, emulsifier, fragrance etc..In addition, the solid pharmaceutical preparation of present embodiment be it is oral use, it is i.e. interior take, and be to swallow to use piece
Agent.The solid pharmaceutical preparation of present embodiment can certainly be used as nutritional supplement, healthy food, trophic function food, functionality
Show that food, specific health food and drug use.
The solid pharmaceutical preparation of present embodiment is by containing seasoning and/or fragrance in addition to carbohydrate, energy in most surface portion
Promote salivary secretion when enough in oral cavity containing solid pharmaceutical preparation, increase the supplies of the liquid mediums to the solid pharmaceutical preparation such as water.As
Sweetener, acid etc. can be used in the seasoning.As sweetener, sucrose derivative, the A Si of Sucralose can be used
The peptides system sweeteners such as Ba Tian, alitame (alitame), neotame (neotame), glycyrrhizin, STEVIA REBAUDIANA (stevia), Radix Glycyrrhizae
Deng.As acid, organic acid can be used, as its example, citric acid, malic acid, tartaric acid etc. can be enumerated.As perfume (or spice)
Material can also use the essence etc. of fruit class other than the citrus flavors such as grapefruit flavours, lemon extract, orange taste essence.
The solid pharmaceutical preparation of present embodiment can contain disintegrating agent.As disintegrating agent, such as it can enumerate and can be used as food additive
Add the sodium bicarbonate (sodium bicarbonate) of object, magnesium carbonate, calcium carboxymethylcellulose, Explotab etc., crospovidone, carboxymethyl
Sodium starch, croscarmellose sodium, low-substituted hydroxypropyl cellulose.It can also be played even if in the case where containing disintegrating agent
Effect of the invention, but from the viewpoint of lubricity is excellent, the content of disintegrating agent is preferably few, specifically, disintegrating agent is matched
Resultant is preferably with respect to 100 parts by weight of solid pharmaceutical preparation for 9.9 parts by weight hereinafter, more preferably 9 parts by weight are hereinafter, further preferably
For 6 parts by weight hereinafter, particularly preferably 3 parts by weight hereinafter, particularly preferably 1 parts by weight hereinafter, be most preferably do not contain.
In above-mentioned disintegrating agent, from the viewpoint of lubricity is excellent, it is preferably selected from crospovidone, carboxymethyl starch
The disintegrating agent of one or more of sodium, croscarmellose sodium or low-substituted hydroxypropyl cellulose (is also referred to as below
Specific disintegrating agent) content it is few.Specifically, relative to 100 parts by weight of solid pharmaceutical preparation, the use level of disintegrating agent is preferably
9.9 parts by weight hereinafter, more preferably 9 parts by weight hereinafter, further preferably 6 parts by weight hereinafter, still more preferably be 3 weight
Part hereinafter, highly preferred is 1 below the mass, not contain most preferably.It should be noted that low-substituted hydroxypropyl cellulose refers to
The cellulose for reacting propylene oxide with alkali cellulose at high temperature and manufacturing is to contain 5.0 after drying 1 hour at 105 DEG C
The cellulose of~16.0% hydroxypropyl.
The solid pharmaceutical preparation of present embodiment can be gelled containing surface agent covering containing sugar alcohol and gelating agent
Particle.This can also be played even if in the case where being gelled the particle containing sugar alcohol and gelating agent of agent covering comprising surface
What The effect of invention, but from the viewpoint of disintegration is excellent, preferably surface were gelled agent covering contains sugar alcohol and gelation
The content of the particle of agent is few, and surface is gelled the compounding amount of the particle containing sugar alcohol and gelating agent of agent covering relative to solid
100 parts by weight of body preparation, below preferably 10 parts by weight, below more preferably 5 parts by weight, further preferably 3 parts by weight with
Under, still more preferably for below 1 parts by weight, be most preferably not contain.What surface was gelled agent covering contains sugar alcohol and solidifying
The particle of gelatinizing agent to particle spray gelating agent containing sugar alcohol etc. by forming.In the present invention, by making solid pharmaceutical preparation
In without containing surface be gelled agent covering the particle containing sugar alcohol and gelating agent and make its gelating agent with specifically
The state that excipient equably mixes is easy further to shorten disintegration time.
The particle containing sugar alcohol and gelating agent for being gelled agent covering without containing surface for example can be by with TOF-
The distribution of gelating agent in SIMS cross-section imaging research solid pharmaceutical preparation confirms.At this point, if not observing gelating agent
Locally layer present in collection, gelating agent are uniformly dispersed in solid pharmaceutical preparation, it can be said that solid pharmaceutical preparation of the invention is not
The particle containing sugar alcohol and gelating agent of agent covering is gelled containing surface.
For solid pharmaceutical preparation, it is contemplated that the easiness swallowed, for example, in the case where the tablet of collar plate shape, 1 weight
Preferably 100mg or more and 500mg hereinafter, more preferably 120mg or more and 450mg hereinafter, most preferably 150mg or more and
400mg or less.Diameter is preferably 5mm or more and 12mm hereinafter, more preferably 5.5mm or more and 11mm are hereinafter, most preferably 6mm
Above and 10mm or less.Thickness is preferably 2mm or more and 10mm hereinafter, more preferably 2.5mm or more and 9mm are hereinafter, most preferably
For 3mm or more and 8mm or less.Hardness be preferably 3kgf or more and 20kgf hereinafter, more preferably 4kgf or more and 18kgf hereinafter,
Most preferably 5kgf or more and 16kgf or less.Diameter, thickness, hardness can be measured by aftermentioned method.
Hereinafter, being further illustrated to the preferred manufacturing method of the solid pharmaceutical preparation of present embodiment.
The manufacturing method of present embodiment preferably to containing gelating agent be selected from sugar alcohol, monosaccharide, disaccharides, oligomeric
One or more of sugar, cellulose, cellulose derivative, starch, starch derivatives and starch decomposition product (specific excipient)
Raw material powder carries out tabletting, manufactures tablet by this method, particularly with the tablet of uncoated tablets.
As gelating agent, sugar alcohol, monosaccharide, disaccharides, oligosaccharide, cellulose, cellulose derivative, starch, starch
Derivative and starch decomposition product, can enumerate above-mentioned substance.In addition, as in the powder containing gelating agent and specific excipient
The ingredient in addition to gelating agent and specific excipient, the above-mentioned excipient enumerated, disintegrating agent, adhesive, profit can be enumerated
Lubrication prescription, emulsifier, effective component, seasoning, fragrance etc..The preferred scope of the mass ratio of gelating agent in raw material powder,
The preferred mass ratio of the preferred mass ratio of preferred gelating agent ingredient and specific excipient, silica,
Disintegrating agent, the preferred mass ratio of lubricant are identical as their the preferred mass ratio in above-mentioned solid pharmaceutical preparation.
In addition, as described above, as raw material powder, the raw material powder of any core will be contained in the case where tablet has core
Tabletting.
Raw material powder containing gelating agent and specific excipient can be powdered gelating agent and powdered
Specific excipient and the powdered mixture of other compositions contained as needed itself, or being also possible to will be powdered
Gelating agent and powdered specific excipient and the powdered other compositions contained as needed mixture pelleting
Obtained from prilling powder.
As prilling process, can be not particularly limited to make using when manufacturing tablet orally by granulation method
Well known prilling process.
The preferred manufacturing method of the solid pharmaceutical preparation of present embodiment is preferably comprised by the powder of gelating agent and selected from sugar
1 in alcohol, monosaccharide, disaccharides, oligosaccharide, cellulose, cellulose derivative, starch, starch derivatives and starch decomposition product
Kind or more powder mixing process, and by obtained mixed-powder not by spraying dissolved with gelating agent aqueous solution and carry out
The process of tabletting.This is because as described above, with by surface be gelled agent covering containing sugar alcohol and gelating agent
Particle carries out solid pharmaceutical preparation obtained from tabletting and compares, and without such coating, gelating agent and specific excipient are equal
The solid pharmaceutical preparation, particularly uncoated tablets mixed evenly is excellent in terms of disintegration and lubricity, particularly disintegration.
As described above, the solid pharmaceutical preparation of present embodiment is by the mixed-powder containing gelating agent and specific excipient
Tabletting object, particularly will be to the mixed-powder tabletting obtained from the not spraying aqueous solution containing gelating agent of the mixed-powder
Made of tabletting object, it is excellent due to that can be readily derived in its surface element entirety there are the solid pharmaceutical preparation of gelating agent
Choosing.It obtains " the tabletting object of the mixed-powder containing gelating agent and specific excipient " and " not spraying containing gelating agent
Aqueous solution and obtain mixed-powder (containing gelating agent and specific excipient), by tabletting obtained from the mixed-powder tabletting
Object " though statement in comprising manufacturing method, compared with the content recorded in this specification, in more detail determine uncoated tablets in
Gelating agent, the existing way of specific excipient and unrealistic, there is the case where having to using such statement.
The solid pharmaceutical preparation of present embodiment is the solid pharmaceutical preparation being orally ingested, by contacting and the profit on surface with aqueous solution
Slip increases.Especially as it was noted above, in the case where solid pharmaceutical preparation is the tablet with uncoated tablets, as described above, by
Contain gelating agent in uncoated tablets, is to be not different with having the tablet of the uncoated tablets without gelating agent in keeping
Hard character, but when taking, by being contacted with liquid mediums such as water, surface gelling and there is lubrication sense, flexibility
And elasticity, it becomes easy and swallows.In addition, the shape of uncoated tablets part is kept in the case where contacting with liquid mediums such as water,
It is present in effective component of uncoated tablets part etc. to be suppressed in intraoral dissolution.In this way, the solid system of present embodiment
Agent, which has, to be swollen in the liquid mediums such as water and generates the feature of lubrication sense on the surface of uncoated tablets.
As described above, the preferred embodiment as tablet of the invention, such as mode below can be enumerated.
(1) a kind of tablet with uncoated tablets, contains:
Gelating agent, and
Selected from sugar alcohol, monosaccharide, disaccharides, oligosaccharide, cellulose, cellulose derivative, starch, starch derivatives and shallow lake
One or more of powder decomposition product.
(2) tablet according to (1), wherein the uncoated tablets contain selected from sugar alcohol, monosaccharide, disaccharides, oligomeric
One or more of sugar and starch decomposition product.
(3) tablet according to (1) or (2), wherein the gelating agent is selected from xanthan gum, locust bean gum, Guar
Glue, mannosan, Glucomannan, hyaluronic acid, agar, alginic acid, tamarind gum, plantasan, tara gum, carrageenan, gold
Silk tree natural gum, gum arabic, ghatti gum, bassora gum, Karaya Gum, cassia gum, rhamsan gum, Weilan gum, stem quasi- greatly
The mould category glue of point, curdlan, pulullan polysaccharide, gellan gum (deacylation fundamental mode gellan gum, natural type gellan gum), pectin and soybean are more
The polysaccharides such as carbohydrate；The protein breakdowns object such as gelatin, collagen；The polyaminoacid such as polyglutamic acid；The biology such as polylactic acid, polyglutamic acid is poly-
It is at least one kind of in conjunction object and their salt and derivative.
(4) tablet according to any one of (1)~(3), wherein except will be by by spraying dissolved with gelating agent
The particle that aqueous solution is granulated carries out tablet obtained from tabletting.
(5) tablet according to any one of (1)~(4), wherein except contain crospovidone, carboxymethyl starch
The tablet of sodium, croscarmellose sodium or low degree of substitution hydroxypropyl cellulose.
(6) tablet according to any one of (1)~(5), with uncoated tablets, the uncoated tablets contain gel
Agent and one or more of selected from monosaccharide, disaccharides, oligosaccharide, alphalysed starch and starch decomposition product.
(7) tablet according to any one of (1)~(6), with uncoated tablets, the uncoated tablets contain:
Selected from locust bean gum, mannosan, Glucomannan, hyaluronic acid, agar, tamarind gum, plantasan, he draw
It is glue, cassia gum, gum arabic, ghatti gum, bassora gum, Karaya Gum, acacia gum, rhamsan gum, Weilan gum, big
Phomopsis glue, curdlan, pulullan polysaccharide, gellan gum, polyaminoacid, polylactic acid and their salt and derivative
One or more of, and
Selected from one or more of monosaccharide, disaccharides, oligosaccharide, alphalysed starch and starch decomposition product.
(8) tablet according to any one of (1)~(7), with uncoated tablets, the uncoated tablets contain:
Selected from locust bean gum, mannosan, Glucomannan, hyaluronic acid, agar, tamarind gum, plantasan, he draw
It is glue, cassia gum, gum arabic, ghatti gum, bassora gum, Karaya Gum, acacia gum, rhamsan gum, Weilan gum, big
Phomopsis glue, curdlan, pulullan polysaccharide, gellan gum, polyaminoacid, polylactic acid and their salt and derivative
One or more of,
Selected from one or more of xanthan gum, guar gum, alginic acid, carrageenan, and
Selected from one or more of monosaccharide, disaccharides, oligosaccharide, alphalysed starch and starch decomposition product.
(9) tablet according to any one of (1)~(8), with uncoated tablets, the uncoated tablets contain:
Gelating agent,
Disaccharides, and
Selected from one or more of oligosaccharide, sugar alcohol, cellulose derivative, starch, starch decomposition product.
(10) tablet according to any one of (1)~(9), contains:
Gelating agent,
Sugar alcohol, and
Selected from one or more of starch, alphalysed starch,
And the coating of gelating agent is not contained.
Embodiment
Hereinafter, enumerate embodiment illustrates the present invention in further detail.But the scope of the present invention be not limited to it is described
Embodiment.Wherein, as the material recorded in table 1~3, commercially available product is used respectively.Especially as isomalto-oligosaccharide,
Use the Palatinitol 900P of Showa Sangyo Co., Ltd..In addition, using Nippon Paper strain formula meeting as avicel cellulose
The KC Flock W-400G of society's manufacture.It is fine using the carboxymethyl that degree of etherification falling is 0.5~0.7mol/C6 as carboxymethyl cellulose
Tie up plain calcium.As starch powder, FREUND Industry Co., Ltd パ ー Off ィ ラ ー 102 is used.As alphalysed starch, use
Sanwa Cornstarch Co., Ltd. NON-GMO corn α-Y.As dextrin, SongGu Chemical Industrial Co., Ltd マ ッ is used
クス1000。
1. the evaluation of lubricity
(embodiment 1)
As raw material powder, according to the match ratio of table 1, the various raw materials that 400 amounts are mixed in polybag (remove stearic acid
Outside calcium) after, sieving, and then add, mixing calcium stearate.Directly with rotary tablet machine (chrysanthemum water makes institute) by the mixed-powder
Tabletting obtains the uncoated tablets of collar plate shape.The uncoated tablets measured with Si Shi (schleuniger) tablet hardness tester it is hard
Degree.In addition, with digital vernier slide calliper rule (digital display calliper CD-15AX；Three rich (Mitutoyo)) the obtained piece of uncoated tablets of measurement
Agent diameter, tablet thickness, as a result hardness be 7.4kgf, tablet diameters 10mm, tablet thickness 3.52mm.In addition, measuring
The weight of 1 uncoated tablets arrived, result 270mg.It should be noted that hardness, tablet diameters, tablet thickness and weight are
The average value of 3 respective measured values.
(embodiment 2)
According to the match ratio of table 1, the compounding ratio of raw material powder is changed, in addition to this, is obtained similarly to Example 1
Uncoated tablets.Measurement similarly to Example 1 is carried out to obtained uncoated tablets, as a result hardness is 7.7kgf, tablet diameters are
10mm, tablet thickness 3.50mm, weight 270mg.
(evaluations of Examples 1 and 2)
For uncoated tablets obtained in Examples 1 and 2, implement the myoelectric potential of larynx when taking with single blind cross-over experiment method
Measure and take sense questionnaire survey.
In addition, determining inclined-plane in order to evaluate the sliding easiness of tablet and sliding the time.
The instructions of taking of uncoated tablets
About subject, select consciously to exist and do not arrogate to oneself the normal adults 6 for swallowing tablet (men and women's ratio is 2:4).It takes
Method sucks uncoated tablets 4 as object first, then sucks 22 DEG C of water 20mL, uncoated tablets are taken together with water
With.
Myoelectricity position-finding
Myoelectricity position-finding has used myoelectric apparatus (AM science Co. Ltd. system is wireless myoelectricity measurement-analysis system " Lateo ").
Measuring method carries out as follows according to the subsidiary operation manual of myoelectric apparatus, specifically.The electrode of myoelectric apparatus is installed on throat, is
It is accustomed to larynx, the water 20mL of equivalent when subject being made to take and take uncoated tablets.Then, larynx when taking water 20mL is measured
Myoelectric potential.Then, after sucking uncoated tablets 4, the myoelectricity of larynx when being taken with 20mL water is measured respectively for each trial zone
Position.Flesh activity is that the integrated value calculated based on obtained myoelectric potential (unit volt (V)) is found out only to take flesh when water
Relative value when meat activity is 100 (%).Value that is everyone primary relative value is total, obtaining divided by number is living as muscle
Momentum (%).Wherein, in FIG. 1 to FIG. 3,1 is counted as 1/200 second.
It should be noted that the time of having a rest that the measurement of each trial zone separates about 5 minutes carries out, the suitable of uncoated tablets is taken
Sequence is changed by each testee.
Questionnaire survey
For sliding easiness, using by when taking tablet jam, do not enter larynx degree it is fricton-tight and be not easy to gulp down
Under situation be denoted as minimum evaluation (- 3 point), will not feel rub throat without jam to larynx degree be easy slide simultaneously
Be easy the case where swallowing be evaluated as highest evaluation (3 points) 7 grades evaluated.
It is using the degree that tongue, larynx portion are felt to attachment tacky and be not easy the case where swallowing for tacky
It is evaluated as minimum evaluation (- 3 points), will not be adhered in tongue or larynx portion, with only feeling the degree lubricated without tacky and appearance
7 grades that the case where easily swallowing is evaluated as highest evaluation (3 points) are evaluated.
Inclined-plane slides the time
It (is when viewing from the side linear, logical from upper part of channel to the aluminium channel that 30 ° of fixed sections are U-shaped is tilted
Road length is 90cm, width 1.2cm) water per minute for supplying 150ml.In this state, make 1 uncoated tablets from than channel
The low 10cm in upper end position at slidably flow, the time needed for being measured to the 80cm slided to lower end (second).Carry out 5
Secondary test calculates 5 average value, slides time (second) as inclined-plane.
The muscle activity amount (%) of the larynx obtained by myoelectricity position-finding is shown in table 1, representative myoelectricity is illustrated in
Fig. 2~Fig. 4.
About the evaluation score obtained by questionnaire survey, the average value of 6 people and inclined-plane are slid to the measurement of time (second)
As a result shown in table 1.Wherein, in table 1, the unit of uncoated tablets composition is mass parts.
Table 1
By table 1 and Fig. 2~Fig. 4 it is found that compared with the case where only taking water, the flesh of the larynx of the uncoated tablets of Examples 1 and 2
Meat activity is controlled as 1.5 times or so of increase, be not required to when taking firmly, be difficult to feel to swallow the easy-to-swallow of pressure
Uncoated tablets.Also known by questionnaire survey, feel sliding easiness while, tongue, larynx portion uncoated tablets not
Meeting is tacky and adheres to, is easy to swallow.
It should be noted that being combined with crospovidone, sodium carboxymethyl starch, crosslinking carboxylic first compared with embodiment 1 or 2
The sliding easiness of the uncoated tablets of base sodium cellulosate or low-substituted hydroxypropyl cellulose and it is not easy tackiness reduction.
In addition, being compared to the inclined-plane landing time, as shown in table 1, embodiment 1,2, can also due to sliding at 2 seconds or less
Know that the uncoated tablets of embodiment are easy sliding and contacting with water, therefore is easy to swallow.
It should be noted that being combined with crospovidone, sodium carboxymethyl starch, crosslinking carboxylic first compared with embodiment 1 or 2
The inclined-plane of the uncoated tablets of base sodium cellulosate or low-substituted hydroxypropyl cellulose landing property reduces.
To sum up, in the case where the uncoated tablets containing gelating agent and specific excipient (sugar alcohol, alphalysed starch), i.e.,
Make to be not arrogate to oneself the people for swallowing tablet, resistance also less, can easily take.
2. the evaluation of disintegration
(embodiment 3~6)
According to the match ratio of following table 1, hardness is changed to 9kgf, tablet diameters are changed to 9mm, becomes tablet thickness
More 4.81~5.08mm (embodiment 3 is 4.81mm, embodiment 4 and 6 is 4.89mm, embodiment 5 is 5.08mm), weight is become
More 300mg has obtained uncoated tablets in addition to this similarly to Example 1.
By following methods, obtained uncoated tablets are carried out with the measurement of disintegration time.Show the result in table 2.
Disintegration time
The method recorded in " slaking test method " according to " 6.09 " item in " the 15th correction Pharmacopeia of Japan ", uses
Slaking test device (Fushan Mountain Industry Co., Ltd, model: NT-40H) measures disintegration time with n=6.Wherein, solution uses water.
Unit in the composition of table 2 is mass parts.
Table 2
As shown in Table 2, gelating agent and specific disintegrating agent (sugar alcohol, cellulose, cellulose derivative, starch) are combined with
Uncoated tablets disintegration time it is short.In addition, even if in the case where having cooperated specific disintegrating agent (crospovidone), and not
The case where cooperation, is compared, and disintegration time also shortens 2 into left and right.
3. the evaluation of lubricity and disintegration time
(embodiment 7~14,16~21, comparative example 1)
It according to the match ratio of following Table 3, operates similarly with example 1, has obtained uncoated tablets.Obtained embodiment 7
~14,16~21, the hardness of the uncoated tablets of comparative example 1, tablet diameters, tablet thickness be identical journey with embodiment 3~5
Degree, weight 300mg.
(embodiment 15)
57.1 mass parts of D-sorbite, 30.0 mass parts of maltose are put into fluidized bed pelletizer, and (fluidized bed is granulated dry
Dry coating machine, model: FD-LAB-1 type, Powrex company) in, it, further will be yellow after the suspension of spray crystallization cellulose
The dilution of virgin rubber hot water, the suspension that 0.1% (w/v) is made, are sprayed, are then granulated, obtained by D-sorbite
The particle surface constituted with the mixed-powder of maltose is formed with the particle composition of xanthan gum coating, and (surface is gelled agent
The particle containing sugar alcohol and gelating agent of covering).
After mixing 0.5 mass parts of calcium stearate in obtained particle composition, using rotary tablet machine, (chrysanthemum water is made
Institute) tabletting is carried out, having obtained hardness, tablet diameters, tablet thickness is same degree, weight 300mg with embodiment 3~5
Uncoated tablets.The amount of avicel cellulose and xanthan gum in uncoated tablets is to measure shown in table 1.
For uncoated tablets obtained in embodiment 7~21, comparative example 1, by method same as embodiment 3~6 into
The measurement of row disintegration time.Show the result in table 3.
And then following methods are utilized, the maximum stress of uncoated tablets obtained in measurement embodiment 7~21, comparative example 1.
The determination step > of < maximum stress
Uncoated tablets are statically placed on plastic substrate, every 1mm of uncoated tablets2Surface area is added dropwise 25 DEG C with suction pipe
0.2 μ L of water is kept for 15 seconds in this state.
Using consistently being configured along up and down direction according to length direction and up and down direction and that can move along the vertical direction
The fixed internal diameter of dynamic mode is 9mm, the silicone tube that outer diameter is 11mm and to clip the state of the silicone tube in the lateral direction
Fill 1 above-mentioned uncoated tablets (tablet diameters 9mm) in the downside of fixed a pair of of slit, the slit in the silicone tube.
Make the silicone tube along the gap relative to the uncoated tablets using Yama Co., Ltd.'s electricity creepmeter (RE2-33005C) measurement
Maximum stress when 20mm mobile with 0.5mm/ seconds speed upwards.The sectional area of silicone tube used in measurement is uncoated
The 50% of the sectional area of piece.In the case where stress is more than 20, terminate to measure at the moment.As silicone tube, Japan rubber is used
Glue industry companies transparent organic silicon square tube.As slit, fixture (AT- is squeezed out using the special cylinder of Yama Co., Ltd.'s electricity
43446), it is fixed in the position that mutual minimum interval is 2mm.
Maximum stress is found out with 3 average value even.
Unit in the composition of table 3 is mass parts.
By the embodiment 7~21 in table 3 compared with comparative example 1 it is found that relative to only contain specific excipient without
The uncoated tablets of comparative example 1 containing gelating agent, the embodiment 7~21 containing gelating agent and specific excipient are not wrapped
The maximum stress of garment piece is greatly reduced.
In addition, by the result of embodiment 7~14 it is found that in specific excipient, including monosaccharide, disaccharides, low
In the case where the uncoated tablets of glycan or starch decomposition product, maximum stress is especially low.
In addition, from the comparison of embodiment 15 and 16 it is found that with by surface be gelled agent covering containing sugar alcohol and gel
Uncoated tablets obtained from the particle tabletting of agent are compared, sugar alcohol is mixed with gelating agent and uncoated tablets that tabletting obtains
Disintegration time shortens, and maximum stress is lower.
It should be noted that with by surface be gelled agent covering the particle tabletting containing sugar alcohol and gelating agent and obtain
To uncoated tablets compare, sugar alcohol is mixed with gelating agent and the disintegration time for the uncoated tablets that tabletting obtains shortens, it is maximum
The tendency that stress is lower is not only when using D-sorbite as sugar alcohol as it can be seen that in the sugar alcohol (erythrose in addition to D-sorbite
Alcohol, mannitol etc.) when also show.
In addition, by the result of embodiment 17~21 it is found that in the case where using locust bean gum as gelating agent, especially
It is that disintegration time shortens, maximum stress is lower, therefore for gelating agent, from the sight for seeking disintegration and lubricity to take into account
Point sets out, and locust bean gum is especially excellent.
It operates similarly with example 1, manufactures uncoated tablets below (Formulation Example 1~41).Any uncoated tablets are all
The excellent uncoated tablets of lubricity, disintegration.It especially combines there are two types of the uncoated tablets of above gelating agent, containing being selected from
The uncoated tablets of one or more of monosaccharide, disaccharides, oligosaccharide, starch derivatives and starch decomposition product, combination contain 2 kinds
The uncoated tablets of the ingredient to belong to a different category in the above specific excipient, combination have disaccharides and selected from oligosaccharide, sugar alcohol,
Lubricity, the disintegration of the uncoated tablets of one or more of cellulose derivative, starch and starch decomposition product are excellent.In addition, right
Sucrose is sprinkled on the uncoated tablets that make in Formulation Example 1~41, according to being coated the ratio of layer covering in tablet in having
Shared ratio is prepared in surface area for 20% mode more than and less than 30% (makes sucrose attachment adjust ratio by using water
Example) the obtained tablet of uncoated tablets is also the excellent tablet of lubricity, disintegration.Similarly, for covering according to being coated layer
The ratio of lid ratio shared in the surface area of tablet is that uncoated tablets prepared by 5% mode more than and less than 10% are also
The excellent uncoated tablets of lubricity, disintegration.
Formulation Example 42
Prepare content liquid (safflower oil is 95 mass %, beeswax is 5 mass %), be filled in glycerol be 16.4 mass %,
The film, capsule that the ratio that Purified Water is 36.8 mass %, gelatin is 43.3 mass % and caramel colorant is 3.5 mass % contains
In (weight before drying), soft capsule is thus made.Encapsulated following progress: by prolonging film, capsule liquid stream and filming,
And it internally fills content liquid and is sealed, keep molding soft capsule dry (every 1 300mg).For 1 soft capsule,
Soft capsule is mixed with locust bean gum in such a way that the weight of locust bean gum (powder) reaches 5mg, adheres to locust bean gum.It is logical
The process is crossed, a part for obtaining surface is attached with the soft capsule of gelating agent.
Industrial availability
Solid pharmaceutical preparation of the invention due to it is easy-to-swallow and do not need carry out entire surface coating, can be to avoid packet
Enlargement caused by clothing, in addition, manufacturing cost can also be reduced by without coating.In addition, the disintegration after intake is easy
Property is also excellent.Therefore, solid pharmaceutical preparation of the invention can be used as or manufacture nutritional supplement, healthy food, trophic function food, function
Energy property shows food, specific health food and drug etc., is useful.
Claims (5)
1. a kind of solid pharmaceutical preparation is the solid pharmaceutical preparation being orally ingested, according to by being contacted and the profit on surface with aqueous solution
The increased mode of slip is made.
2. solid pharmaceutical preparation according to claim 1, wherein
The solid pharmaceutical preparation is the solid pharmaceutical preparation containing gelating agent,
Gelation does not occur for solid pharmaceutical preparation gelating agent in the state of before taking,
When taking by contacting with aqueous solution, gelation occurs the solid pharmaceutical preparation for the gelating agent.
3. solid pharmaceutical preparation according to claim 1 or 2, wherein
It is within 60 minutes using water as the disintegration time that solvent measures.
4. solid pharmaceutical preparation described in any one of claim 1 to 3 is the solid pharmaceutical preparation being orally ingested, wherein
Solid pharmaceutical preparation is stood on plastic substrate, to every 1mm of solid pharmaceutical preparation225 DEG C of water 0.2 is added dropwise with suction pipe for surface area
μ L, after being kept for 10~20 seconds in this state, the maximum stress that measures as steps described below with to before investment water this is solid
The maximum stress that body preparation equally measures compares low, the determination step > of < maximum stress
Using configuration along the vertical direction and the silicone tube that can movably fix along the vertical direction and to clip in the lateral direction
Fixed a pair of of the slit of the state of the silicone tube fills 1 solid pharmaceutical preparation in the downside of the slit of the silicone tube, makes this
Silicone tube is moved upward along the slit, and thus measurement makes the silicone tube relative to the solid pharmaceutical preparation upwards with 0.5mm/
Maximum stress when the speed movement 20mm of second,
In the measurement, the sectional area of silicone tube is smaller than the sectional area of solid pharmaceutical preparation and is greater than the sectional area of solid pharmaceutical preparation
40%.
5. the solid pharmaceutical preparation according to any one of claim 3~4, wherein
The solid pharmaceutical preparation is the form of tablet or capsule.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2017-018883 | 2017-02-03 | ||
| JP2017018883 | 2017-02-03 | ||
| JP2017-072905 | 2017-03-31 | ||
| JP2017072905 | 2017-03-31 | ||
| PCT/JP2018/003640 WO2018143423A1 (en) | 2017-02-03 | 2018-02-02 | Solid preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110267683A true CN110267683A (en) | 2019-09-20 |
Family
ID=63040182
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880009378.4A Pending CN110267683A (en) | 2017-02-03 | 2018-02-02 | Solid pharmaceutical preparation |
Country Status (4)
| Country | Link |
|---|---|
| JP (5) | JP7096593B2 (en) |
| KR (1) | KR102329377B1 (en) |
| CN (1) | CN110267683A (en) |
| WO (1) | WO2018143423A1 (en) |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997016172A1 (en) * | 1995-11-03 | 1997-05-09 | Edward Mendell Co., Inc. | Controlled release formulation (albuterol) |
| US5648092A (en) * | 1990-07-19 | 1997-07-15 | Merck Patent Gesellschaft Mit Beschrankter Haftung | Sucralfate chewable tablet |
| JP2002275054A (en) * | 2001-03-19 | 2002-09-25 | Dainippon Pharmaceut Co Ltd | Easily administrable solid preparation |
| WO2017002803A1 (en) * | 2015-06-29 | 2017-01-05 | 株式会社ダイセル | Composition for outer layer of solid preparation, and easy-to-take solid preparation including said composition for outer layer |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6080427A (en) | 1997-04-17 | 2000-06-27 | Bristol-Myers Squibb Company | Cefadroxil monohydrate tablet formulation |
| CA2317021A1 (en) | 1997-12-29 | 1999-07-08 | The Procter & Gamble Company | Tablet composition |
| US6572887B2 (en) | 2000-05-01 | 2003-06-03 | National Starch And Chemical Investment Holding Corporation | Polysaccharide material for direct compression |
| BRPI0417123A (en) | 2003-12-12 | 2007-08-21 | Penwest Pharmaceutical Co | prolonged release torsemide formulation |
| JP2006117626A (en) | 2004-09-24 | 2006-05-11 | Nisshin Pharma Inc | Method for producing coenzyme q10-blended composition |
| US20070005933A1 (en) | 2005-06-29 | 2007-01-04 | Kopec Brian J | Preventing multiple translation lookaside buffer accesses for a same page in memory |
| WO2007091856A1 (en) | 2006-02-10 | 2007-08-16 | Lg Household & Health Care Ltd. | In-situ melting and gelling tablet composition for oral care |
| CL2008003230A1 (en) | 2007-11-01 | 2009-11-27 | Sanofi Aventis Healthcare Pty Ltd | Tablet coating composition comprising cellulosic polymer, plasticizer, sweetener and powder flavor composition which comprises flavor associated with solid carrier; tablet coating fluid comprising said composition; pharmaceutical tablet; process of preparing said tablet. |
| JP5909851B2 (en) | 2010-02-24 | 2016-04-27 | 大正製薬株式会社 | Easy-to-swallow tablets |
| AU2012334035A1 (en) | 2011-11-10 | 2014-03-27 | Dpx Holdings B.V. | Lubricious coatings |
| JP6045237B2 (en) | 2012-07-27 | 2016-12-14 | 旭化成株式会社 | Tablet-type thickener |
| JP6045238B2 (en) | 2012-07-27 | 2016-12-14 | 旭化成株式会社 | Tablet containing thickening polysaccharide |
| JP6998210B2 (en) * | 2015-09-30 | 2022-01-18 | 株式会社ダイセル | Particle composition for easy-to-take solid preparation and easy-to-take solid preparation containing the particle composition |
-
2018
- 2018-02-02 JP JP2018566136A patent/JP7096593B2/en active Active
- 2018-02-02 JP JP2018017267A patent/JP7390695B2/en active Active
- 2018-02-02 WO PCT/JP2018/003640 patent/WO2018143423A1/en active Application Filing
- 2018-02-02 CN CN201880009378.4A patent/CN110267683A/en active Pending
- 2018-02-02 KR KR1020197024029A patent/KR102329377B1/en active IP Right Grant
-
2022
- 2022-06-16 JP JP2022097646A patent/JP7390750B2/en active Active
-
2023
- 2023-11-13 JP JP2023192726A patent/JP2023184766A/en active Pending
- 2023-11-13 JP JP2023193144A patent/JP2023184779A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5648092A (en) * | 1990-07-19 | 1997-07-15 | Merck Patent Gesellschaft Mit Beschrankter Haftung | Sucralfate chewable tablet |
| WO1997016172A1 (en) * | 1995-11-03 | 1997-05-09 | Edward Mendell Co., Inc. | Controlled release formulation (albuterol) |
| JP2002275054A (en) * | 2001-03-19 | 2002-09-25 | Dainippon Pharmaceut Co Ltd | Easily administrable solid preparation |
| WO2017002803A1 (en) * | 2015-06-29 | 2017-01-05 | 株式会社ダイセル | Composition for outer layer of solid preparation, and easy-to-take solid preparation including said composition for outer layer |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2023184779A (en) | 2023-12-28 |
| KR102329377B1 (en) | 2021-11-19 |
| JP2023184766A (en) | 2023-12-28 |
| JP7096593B2 (en) | 2022-07-06 |
| JP7390695B2 (en) | 2023-12-04 |
| JP2022120168A (en) | 2022-08-17 |
| KR20190105631A (en) | 2019-09-17 |
| WO2018143423A1 (en) | 2018-08-09 |
| JP7390750B2 (en) | 2023-12-04 |
| JP2018158917A (en) | 2018-10-11 |
| JPWO2018143423A1 (en) | 2019-11-21 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN103721264B (en) | A kind of for helping the gel swallowing oral solid pharmaceutical formulation | |
| Alvani et al. | Use of carbohydrates, including dextrins, for oral delivery | |
| WO2006082842A1 (en) | Hard capsule having improved solubility | |
| TWI733650B (en) | Disintegrable particle composition containing microfibrous cellulose | |
| JPWO2013115171A1 (en) | Orally disintegrating tablets containing bitter mask granules | |
| JP5665372B2 (en) | Fast disintegrating solid preparation | |
| TWI714536B (en) | Disintegrable particle composition containing crushed lactose or granulated lactose | |
| KR20200006594A (en) | Disintegrating tablet composition comprising microfibrous cellulose and active ingredient | |
| CN103826660A (en) | Orally disintegrating tablet containing hydroxyalkyl cellulose fine particles | |
| AU2006263068B2 (en) | Orally disintegrating powder comprising cilostazol and mannitol | |
| CN110267683A (en) | Solid pharmaceutical preparation | |
| JP6104038B2 (en) | Composite composition of crystalline cellulose | |
| TW202011943A (en) | Easy-to-take granular preparation, and method for producing same | |
| JP5918584B2 (en) | Taste masking method | |
| CN116270515B (en) | Preparation method for improving quality of beraprost sodium tablet product | |
| JP6029874B2 (en) | Sol pharmaceutical composition containing itraconazole | |
| JP2016117731A (en) | Oral agent, production method for oral agent, coating composition for oral solid formulation | |
| JP2023119660A (en) | Base material for tablet, composition promoting collapse of tablet, texture and/or food taste improving composition of oral tablet and manufacturing method of tablet | |
| JP2010173966A (en) | Disintegrable solid preparation | |
| JPH02221232A (en) | Readily drinkable medicine composition | |
| MX2008000114A (en) | Orally disintegrating powder comprising cilostazol and mannitol. |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 40009530 Country of ref document: HK |