KR20170001786A - Preparation method for pharmaceutical composition comprising Pelargonium sidoides extracts - Google Patents
Preparation method for pharmaceutical composition comprising Pelargonium sidoides extracts Download PDFInfo
- Publication number
- KR20170001786A KR20170001786A KR1020150090419A KR20150090419A KR20170001786A KR 20170001786 A KR20170001786 A KR 20170001786A KR 1020150090419 A KR1020150090419 A KR 1020150090419A KR 20150090419 A KR20150090419 A KR 20150090419A KR 20170001786 A KR20170001786 A KR 20170001786A
- Authority
- KR
- South Korea
- Prior art keywords
- pharmaceutical composition
- extract
- group
- pelagonium
- pelagonium sidoides
- Prior art date
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- 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
- A61K47/38—Cellulose; Derivatives thereof
-
- 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
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/314—Foods, ingredients or supplements having a functional effect on health having an effect on lung or respiratory system
Abstract
The present invention relates to a method for preparing a pharmaceutical composition comprising a Pelagonium sidoides extract, and more particularly, to a method for preparing a pharmaceutical composition comprising a Pelagonium sidoides extract and a pharmaceutically acceptable additive To prepare a pharmaceutical composition comprising the extract of Pelagonium sidoides which can secure the uniformity of the content and the stability of the contents by drastically reducing the size of the solid composition and improved the convenience of taking the patients having weak gelling capacity .
Description
The present invention relates to a method for preparing a pharmaceutical composition comprising Pelagonium sidoides extract, and more particularly, to a method for preparing a pharmaceutical composition comprising a Pelagonium sidoides extract, The present invention relates to a method for preparing a pharmaceutical composition comprising a Pelagonium sidoides extract having improved ease of taking for weak patients.
In general, medicines and health functional foods have been prepared in formulations such as powders, granules, syrups, liquids, pills, capsules, tablets and the like in order to take active ingredients or functional materials.
The tablet is manufactured by compressing and compressing the granular material or the mixture between two upper and lower punches filled with quantitative granules or a mixture. Unlike other formulations, it is easy to store and convenient to apply to many products Has been used.
However, when the active ingredient or the functional ingredient is in a liquid form or an oil or a low melting point solid at room temperature, it is difficult to directly process the tablets. Therefore, in order to process an active ingredient or a functional material having a liquid form, oil, or low-melting point solid, it is necessary to treat it in a stable solid form or a powder form at room temperature before compression.
In order to prepare a tablet containing a raw material ingredient of a liquid component such as a herbal medicine ingredient extract, an excipient such as calcium silicate is added and the solvent used for the preparation of the extract should be evaporated or dried to remove. In this case, since the pharmacologically active ingredient is decomposed with time to reduce the content of the active ingredient during the process of evaporation or drying, an effective amount of the pharmacologically active ingredient can be consumed in an amount greater than necessary in order to make the tablet substantially, .
In addition, it is difficult to obtain a composition in which the active ingredient is uniformly distributed by simple mixing of the herbal composition extract and the excipient as the active ingredient. In order to compensate for this, when the size of the solid composition is increased, the size of the tablet increases, Patients have difficulty swallowing tablets.
Therefore, there is a continuing need to develop a manufacturing process that can control the process more easily in commercial production, while suppressing the time-dependent decomposition of the active ingredient, thereby ensuring the content stability and the uniformity of the content.
On the other hand, Pelargonium sidoides is native to the 2300m altitude of the inland and coastal waters of South Africa. It has long been used for respiratory diseases such as diarrhea, gastrointestinal diseases, liver diseases, and cold and pulmonary tuberculosis. In particular, it is known that it is effective in the treatment of respiratory diseases by preventing spread of inflammation by preventing viruses or bacteria from adhering to mucosal cells.
Thus, Pella Swan Stadium sidoyi Death (Pelargonium sidoides ) extracts have been developed and marketed for the treatment of respiratory diseases. For example, it is sold under the names Kaloba syrup in the UK, Umckan syrup in Brazil, and umcamine syrup, umcamine syrup, umbrella syrup, and cucurbit syrup in Korea.
However, since the above-mentioned medicines are manufactured and sold in the form of liquid such as syrup, Pelargonium ( Pelargonium) In addition to the extract of sidoides , a glycerin mixture is added. As a result, the water absorption rate of the active ingredient is decreased, and compared with the case of using a solid preparation, Pelargonium sidoides < / RTI > extract. In addition, there is a problem in stability such as short shelf life and sedimentation as compared with a solid preparation, and sugar components and the like are added for sweet taste, so that they may be contaminated and altered by microorganisms after opening. In addition, since it is sold in a separate container, it is less convenient to move than a solid preparation, and it is inconvenient because a separate tool such as a spoon or a cup is required for taking it, and it is difficult to take the same amount every time, There is a risk of breaking.
In the prior art related to the present invention, Korean Patent No. 10-1497508 discloses a solid preparation comprising Pelagonium sidoides extract and a silicate compound and a method for producing the same, but the technical composition is different from that of the present invention .
Accordingly, it is an object of the present invention to provide a method for preparing a pharmaceutical composition comprising Pelagonium sidoides extract having excellent content uniformity and content stability.
The present invention also provides a pharmaceutical composition comprising a Pelagonium sidoides extract prepared by the above method.
To achieve these and other advantages and in accordance with the purpose of the present invention, as embodied and broadly described herein, there is provided a method for preparing a granule, comprising: spraying a Pelagonium sidoides extract on a surface of a carrier to form granules; And mixing the dried granule with a pharmaceutically acceptable additive. The present invention also provides a method for preparing a pharmaceutical composition comprising a Pelagonium sidoides extract.
According to one embodiment of the present invention, the Pelagonium sidoides extract is obtained by extracting one or a mixture of two or more selected from the group consisting of water, methanol, ethanol, propanol and butanol as a solvent.
According to another embodiment of the present invention, the carrier is selected from the group consisting of? -Cyclodextrin,? -Cyclodextrin and? -Cyclodextrin.
According to another embodiment of the present invention, the mass ratio of the Pelagonium sidoides extract to the carrier is 1: 1 to 9: 1.
According to another embodiment of the present invention, the step of forming the granules is carried out in a fluidized bed granulator.
According to another embodiment of the present invention, the inlet air temperature of the fluidized bed granulator is 60 ° C to 100 ° C.
According to another embodiment of the present invention, the injection nozzle position of the fluidized bed granulator is an upper and a lower side.
According to another embodiment of the present invention, the pharmaceutically acceptable additive is selected from the group consisting of a sweetener, a flavoring agent, a coloring agent, a disintegrant, a binder, a lubricant, a thickener, a stabilizer and a surfactant .
According to another embodiment of the present invention, the disintegrant is selected from the group consisting of low-substituted hydroxypropyl cellulose, natural starch, modified starch, pregelatinized starch, partially pregelatinized starch, pregelatinized starch, , Crospovidone, sodium starch glyconate, croscarmellose sodium, carboxymethylcellulose sodium and carboxymethylcellulose calcium.
According to another embodiment of the present invention, the lubricant is selected from the group consisting of talc, sodium benzonate, sodium stearyl fumarate (Pruv), calcium stearate, magnesium stearate the composition is selected from the group consisting of magnesium stearate, zinc stearate, glyceryl behenate, stearic acid and glyceryl monostearate.
The present invention also provides a pharmaceutical composition comprising a Pelagonium sidoides extract prepared by the above method.
According to one embodiment of the present invention, the pharmaceutical composition is characterized in that it is formulated as a tablet or a capsule, and the tablet may be a coated tablet.
According to another embodiment of the present invention, the pharmaceutical composition may be used for the treatment of respiratory diseases, and the respiratory diseases are selected from the group consisting of cold, cough, asthma, tonsillitis, sore throat, pulmonary tuberculosis and chronic bronchitis. .
According to the present invention, a pharmaceutical composition comprising a Pelagonium sidoides extract capable of ensuring uniformity and content stability of epicatechin as an index component showing the functionality of Pelagonium sidoides extract can be prepared by a simple method .
Fig. 1 is a photograph of a section of the tablet of Example 2 of the present invention and Comparative Example. Fig.
The present inventors have found that the extract of Pelagonium sidoides contains about 10 to 13% of alcohol, and the step of removing the solvent used in the preparation of the extract to solid formulate the liquid Pelagonium sidoides extract And it has been found that epicatechin, which is an active ingredient, is decomposed with time in the process of removing the solvent by evaporation or drying, so that the uniformity of content and the stability of content are not ensured, and the present invention has been devised.
In order to solve the above problems, the present invention provides a method for preparing a pharmaceutical composition comprising a Pelargonium sidoides extract comprising the following steps.
1) spray drying Pelagonium sidoides extract on the surface of the carrier to form granules; And
2) mixing the dried granulate with a pharmaceutically acceptable additive.
As used herein, the term "Pella Konishi Titanium sidoyi des (Pelargonium sidoides "is also known as a plant native to the inland and coastal highlands of South Africa and is also named as kaloba, umcka or zucol. And the extract can be used as a preparation for oral administration for deep sea or dwarf, including the extract thereof. The above-mentioned Pelagonium sidoides can be commercially purchased, collected from nature or cultivated, It does not.
In the present invention, the term "Pelagonium sidoides extract" means an extract obtained by extracting the above-mentioned Pelagonium sidoides. The extraction site is not particularly limited, but roots are preferable. The Pelagonium sidoides extract is prepared by dissolving the Pelagonium sidoides pulverized product in water, an alcohol of various carbon numbers such as an alcohol of 1 to 4 carbon atoms (C 4 ) or a mixed solvent thereof as an extraction solvent And may be obtained by extraction. The alcohol may be, but is not limited to, methanol, ethanol, propanol or butanol. In addition, the above extract may be an extract extracted using an extraction method such as hot water extraction, cold extraction, reflux cooling extraction, ultrasonic extraction, etc., but is not limited thereto and includes all of the extract, the diluted solution of the extract or the concentrated solution.
In one embodiment of the present invention, the Pelagonium sidoides extract is prepared by cutting dry roots of Pelargonium sidoides (Geraniaceae) to an appropriate size (10 mm or less and 95% or more) followed by 35% ethanol (2 minutes) And then extracted with 5.3% ethanol (8 min). The filtrate was heated at 120 to 121 ° C for 30 sec., And the extract of Pelagonium obtained from about 1 g of Pelagonium sidoides dried root was extracted with 8 to 10 g of extract. Death 11% ethanol extract (1 → 8 ~ 10) was used (Examples 1 to 4).
The above step 1) is a step of spraying the extract of Pelagonium sidoides, which is a pharmacologically active substance, on the surface of the carrier to coat the active substance and form granules by drying.
The carrier to be used in the present invention is not particularly limited as long as the active substance is easily spray-coated and is a pharmaceutically acceptable substance that is easily granulated. Specific examples of the carrier include? -Cyclodextrin,? -Cyclodextrin,? -Cyclodextrin, And mixtures thereof.
In one embodiment of the present invention, the content of epicatechin, an indicator component of Pelagonium sidoides extract, was measured by mixing and storing the Pelagonium sidoides extract and each carrier substance. As a result, when the cyclodextrin was used, It was confirmed that the additive was the most stable additive (Example 1, Table 1).
In one embodiment of the present invention, the mass ratio of the active ingredient Pelagonium sidoides extract to the carrier is in the range of 1: 1 to 9: 1, and when the active ingredient and the carrier particle are within the above range, The content of the components is maximized and the efficiency of the process is improved by suppressing the loss of the active component from the carrier and the active ingredient sticking to the inner wall of the granule during the spray coating and granulation process.
In one embodiment of the present invention, spray coating and granulation of the active material is carried out in a fluidized bed granulator. In the fluidized bed granulator, the active substance Pelagonium sidoides extract is spray coated onto the carrier particles at a controlled rate and injection pressure. The carrier particles are kept in motion by mechanical or airflow stirring during the spray coating step, and the carrier particles coated with the active material are agglomerated by the agitation to form granules.
Wherein the air used for fluidization is heated to the desired temperature due to the air heater disposed at the inlet portion of the apparatus. In one embodiment of the present invention, the spray drying temperature which did not affect the degradation of Pelagonium sidoides extract was experimentally confirmed. As a result, when the inlet air temperature of the fluidized bed granulator was set to 60 to 100 ° C It was confirmed that almost no disappearance of the surface component was observed even after 14 hours of exposure at that temperature (Experimental Example 1, Table 4). At a spray drying temperature lower than the above range, it takes a long time to dry the Pelagonium sidoides extract to cause over-agglomeration of the particles, making it difficult to prepare a pharmaceutical composition having a uniform content of Pelagonium sidoides extract, The decomposition of the surface component occurs and the stability of the content is not ensured.
In addition, in order to maximize the content of the Pelagonium sidoides extract attached on the carrier, it is preferable that the injection nozzle of the fluidized bed granulator is located on the upper and lower sides. This is because, when the injection nozzle is located at the bottom, the content of Pelagonium sidoides extract adhered to the inner wall surface of the granulator lowers and becomes uneven.
In one embodiment of the present invention, it was confirmed that the tablets containing the Pelagonium sidoides extract prepared according to the production method of the present invention were more excellent in the content stability than the commercial tablets prepared by the general mixing method ( Experimental Example 2, Table 5).
The step 2) is a step of preparing a pharmaceutical composition by mixing a pharmaceutically acceptable additive with the granules prepared through step 1).
The pharmaceutical composition of the present invention may contain a pharmaceutically acceptable additive for the purpose of enhancing compliance and improving formulation and stability within a range not to impair the effects of the present invention, A sweetening agent, a flavoring agent, a coloring agent, a disintegrating agent, a binder, a lubricant, a thickening agent, a stabilizer, a surfactant, and the like, and other conventional excipients known in the art may also be included.
The disintegrant of the present invention plays a role in accelerating the decomposition of the preparation when placed in an aqueous environment, and examples of the disintegrant that can be used in the preparation method of the present invention include low-substituted hydroxypropyl cellulose cellulose, L-HPC), natural starch, modified starch, pregelatinized starch, partially gelatinized starch, pregelatinized starch and crospovidone, preferably low-substituted hydroxypropylcellulose have. The low-substituted hydroxypropyl cellulose means hydroxypropyl cellulose having a relatively low degree of substitution with a hydroxypropoxyl group (-OCH 2 CHOHCH 3) in cellulose.
The lubricant is an excipient that provides fluidity and helps to formulate, for example, talc, sodium benzonate, sodium stearyl fumarate (Pruv), calcium stearate calcium stearate, magnesium stearate, zinc stearate, glyceryl behenate, stearic acid, and glyceryl monostearate. Magnesium stearate and talc may be used.
The present invention also provides a pharmaceutical composition comprising the extract of Pelagonium sidoides prepared by the above-mentioned method.
The pharmaceutical composition may be formulated for administration by any suitable means. For example, the composition may be compressed into tablets or filled into capsules to form capsules. Such formulations may include pharmaceutically acceptable excipients, including swelling agents, lubricants, disintegrants, binders, and the like, which are commonly used in the compositions.
In one embodiment of the invention, tablets comprising Pelagonium sidoides extract may be formulated in a coating tablet. Since the extract of Pelagonium sidoides which is a herbal ingredient is unstable to heat and moisture, stability can be maintained even over a long period of time by forming a coating layer with an appropriate coating material in a tabular state containing a Pelagonium sidoides extract.
The coating material may be any of the commonly used tablet coating materials, such as polymeric coatings, pigments, plasticizers, solubilizing agents, and the like. Suitable coatings include hydroxypropylmethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose phthalate, and the like. Polyethylene glycol may be included as a plasticizer in the film coating composition. In addition, additional plasticizers such as diethyl citrate and triethyl citrate may also be included in the film coating composition. Suitable solubilizing agents include polyoxyethylene sorbitan fatty acid esters, in particular polysorbate 80. Suitable pigments include titanium dioxide and various iron oxides. The coating material may be dispersed in an appropriate solvent, for example, water, and applied to the tablet using conventional fan coating or spray coating techniques.
The pharmaceutical composition of the present invention inhibits the spread of inflammation by preventing the adhesion of viruses or bacteria to mucosal cells, thereby preventing the spread of inflammation and preventing the infectious diseases such as acute chronic infections, bronchitis, sinusitis, tonsillitis, nasopharyngitis, otitis media, cough, runny nose, Can be used for the same respiratory disease treatment.
Hereinafter, the present invention will be described in detail with reference to Examples.
However, the following examples are intended to illustrate the contents of the present invention, but the scope of the present invention is not limited by the following examples.
< Example 1> Pelagonium Tryidis Selection of additive with excellent stability of extract
2 g of Pelagonium sidoides extract and 2 g of each additive were stored at 40 ° C for 3 months, and then the content of epicatechin was measured by an analysis of the amount of epicatechin approved by the Food and Drug Administration (Table 1).
As shown in Table 1, when the Pelagonium sidoides extract and the cyclodextrin were mixed, the change in the content of the indicator component was minimized and the cyclodextrin was confirmed to be the most stable additive.
< Example 2 to 4 and Comparative Example > Pelagonium Tryidis Preparation of Tablets Containing Extracts
Tablets containing Pelagonium sidoides extract were prepared by the compositions and spray drying described in Table 2 below. That is, the extract of Pelagonium sidoides was spray-dried on the surface of the carrier in a fluidized bed granulator using cyclodextrin selected as a preferred additive in Example 1 as a carrier to form granules. Low-substituted hydroxypropylcellulose and magnesium stearate were added to the granules and mixed at 18 rpm for 10 minutes. The resulting mixture was set in a circular punch of 8.0 mm and then tableted to a reference amount of 235 mg. The obtained tablets were placed in a coater (SFC 30, Sejong Pharmatech) and coated with 5 mg of Opadry II white coater. As a comparative example, Umka Minjung which was co-marketed by Hanwha Pharm and Yuyu Pharm was used.
Spray drying
(1 → 8 ~ 10)
Commercial tablets
mix
The granulation conditions of the fluidized bed granulator were prepared as shown in Table 3, except that the positions of the spray nozzles were different.
< Experimental Example 1> Spray drying Temperature dependent Pelagonium Tryidis Measurement of the content of extract
In order to establish the spray drying and supply temperature range to ensure the stability of epicatechin, the content index of Pelagonium sidoides extract, Pelagonium sidoides extract was exposed to the corresponding temperatures in Table 4 for 14 hours, and then the Food and Drug Administration The content of epicatechin was determined by the amount of the approved epicatechin.
As shown in Table 4, at the spray temperature of 60 to 100 ° C, there was almost no change in the content of the index component of Pelagonium sidoides, but it was confirmed that the content stability was not ensured at temperatures exceeding that.
< Experimental Example 2> Pelagonium Tryidis Determination of the content stability of tablets containing extracts
Dissolve the tablets of Examples 2 to 4 and Comparative Example in an ethanol diluent (96% ethanol: purified water = 1: 3) to make 20 mL. Take 0.5 mL of the solution and add 10 mL of ethanol dilution, 1.5 mL of Folin ciocateus phenol reagent and 10 mL of sodium carbonate solution Appear in a 25 mL volumetric flask and add water to make 25 mL. This solution was left at room temperature for 20 minutes and then centrifuged to obtain the supernatant, and the content of epicatechin was analyzed by UV.
(Acceleration condition: 40 DEG C, 75% RH)
As shown in Table 5, the tablets of Examples 2 and 3 of the present invention exhibited a better content stability and a uniform content than the tablets of the comparative example, in that the Example was carried out by spray drying Pelagonium sidoides extract on the carrier While the comparative example is comparatively low in uniformity because Pelagonium sidoides is mixed with maltodextrin, and it is considered that the size of the solid composition is increased in order to compensate the uniformity. The solid compositions of the examples are 235 mg each, while the comparative example is about 400 mg.
In addition, as shown in Fig. 1, the tablets (Example 2) according to the present invention had a smaller size of the solid composition than the commercial tablets of the comparative example, and the Pelagonium sidoides extract was uniformly distributed, It was confirmed that the composition size was larger than those of the examples and that the dried Pelagonium sidoides was distributed unevenly.
The lower content of Example 4 compared to the tablets of Examples 2 and 3 is judged to be the result of the Pelagonium sidoides extract attached to the inner wall of the fluidized bed granulator.
In this example, the content stability and content uniformity were secured, and the size of the solid composition was drastically reduced, thereby improving the convenience of taking the patients having weak gelling capacity.
Claims (15)
And mixing the dried granules with a pharmaceutically acceptable additive. ≪ Desc / Clms Page number 20 >
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| WO2020009394A1 (en) * | 2018-07-03 | 2020-01-09 | 한국유나이티드제약 주식회사 | Pharmaceutical composition containing extract of pelargonium sidoides, and preparation method therefor |
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| WO2020009394A1 (en) * | 2018-07-03 | 2020-01-09 | 한국유나이티드제약 주식회사 | Pharmaceutical composition containing extract of pelargonium sidoides, and preparation method therefor |
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