CN111773199A - Novel fluorocalcitriol preparation and preparation method thereof - Google Patents
Novel fluorocalcitriol preparation and preparation method thereof Download PDFInfo
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- CN111773199A CN111773199A CN202010629640.4A CN202010629640A CN111773199A CN 111773199 A CN111773199 A CN 111773199A CN 202010629640 A CN202010629640 A CN 202010629640A CN 111773199 A CN111773199 A CN 111773199A
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- soft capsule
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
- A61K31/593—9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
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- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Endocrinology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a novel fluorcalcitriol preparation and a preparation method thereof, and particularly relates to the technical field of pharmaceutical preparations, wherein the preparation comprises a soft capsule filling liquid and a soft capsule shell, wherein the filling liquid consists of fluorcalcitriol, refined vegetable oil, a buffering agent and a flavoring agent; the capsule shell comprises gelatin, thickener, correctant, water, and opacifier. The prepared filling liquid of the fluocalcitriol soft capsule has stable quality, the capsule shell can not absorb water and soften, the capsule can be taken by chewing, the filling liquid is used for treating osteoporosis, rickets and the like, the disintegration time is shortest, the effect is fast, and the bioavailability is high, so that the fluocalcitriol soft capsule is obviously superior to the existing products.
Description
Technical Field
The invention relates to the technical field of pharmaceutical preparations, in particular to a novel fluocalcitriol soft capsule for treating osteoporosis and a preparation method thereof.
Background
Fluorocalcitriol, a vitamin D3 analog, is a derivative of active form of small intestine, acts by binding to receptors distributed in target tissues, can regulate calcium metabolism, resist rickets, and is used for treating hypoparathyroidism. The existing fluorocalcitriol preparation is mainly a tablet, and the fluorocalcitriol tablet is researched and developed by Nippon Sumitomo and Nippon Dazheng medicine together for sale in 4 months in the first 2001; is not marketed in other countries.
Parathyroid glands are endocrine glands located behind the thyroid side lobes in the front of the human neck, and about 80% of people have 4 parathyroid glands, and the hormone secreted by parathyroid glands is mainly parathyroid hormone, which mainly regulates calcium and phosphorus metabolism and skeletal metabolism in the human body. Hypoparathyroidism, also called as parathyroid disease, is characterized by that due to several reasons, the parathyroid hormone production is reduced or its action is deficient, so that the hypocalcemia and hyperphosphatemia are the main test abnormalities, and the patient can take the calcium preparation and vitamin D preparation for a long time to control his disease condition.
The existing fluocalcitriol preparation is mainly a tablet and has the problems of poor taste and poor patient compliance.
Disclosure of Invention
In order to overcome the above defects in the prior art, the embodiment of the invention provides a novel flucalcitriol soft capsule and a preparation method thereof, and the invention aims to solve the technical problems that: provides a kind of flucalcitriol soft capsule with high bioavailability, good patient compliance and stable quality.
In order to achieve the purpose, the invention provides the following technical scheme: a novel flucalcitriol soft capsule is characterized in that: comprises a soft capsule filling liquid and a soft capsule shell, wherein the soft capsule filling liquid comprises, by weight, 0.001-0.005 part of flucalcitriol, 30000 parts of refined vegetable oil, 50000 parts of buffering agent, 5-10 parts of flavoring agent and 8-20 parts of absolute ethyl alcohol; the soft capsule shell consists of 20-40 parts by weight of gelatin, 10-20 parts by weight of thickening agent, 10-20 parts by weight of flavoring agent, 30-50 parts by weight of water and 5-10 parts by weight of opacifier.
More preferably, the soft capsule filling liquid consists of 0.0015 part of fluorcalcitriol, 35000 parts of refined vegetable oil, 8 parts of buffering agent, 8 parts of flavoring agent and 15 parts of absolute ethyl alcohol in parts by weight; the soft capsule shell comprises 38 parts by weight of gelatin, 15 parts by weight of thickening agent, 15 parts by weight of flavoring agent, 40 parts by weight of water and 8 parts by weight of opacifier.
In the specific component formula of the soft capsule filling liquid, the refined vegetable oil is any one or more of salad oil, corn oil, peanut oil and sesame oil; the buffer is one or two of citric acid and tartaric acid; the flavoring agent is essence and sweetener.
In a preferred embodiment, the above-mentioned soft capsule filling liquid has a formula of components, wherein the refined vegetable oil is a mixture of corn oil and peanut oil, and the ratio of the corn oil to the peanut oil is 5: 2. The buffer is a mixture of citric acid and tartaric acid, and the dosage ratio of the citric acid to the tartaric acid is 1: 3.
A novel gliflotriol soft capsule comprises a capsule shell, wherein a thickening agent is one or more of agar, guar gum, gellan gum, arabic gum, xanthan gum and locust bean gum; the flavoring agent is essence and sweetener; the opacifier is edible pigment.
Further preferably, in the above formulation of the soft capsule shell, the thickening agent is gum arabic and xanthan gum, and the ratio of gum arabic: the amount ratio of xanthan gum is 2: 1.
A novel flucalcitriol soft capsule is characterized in that: the dosage ratio of the essence and the sweetener in the flavoring agent in the soft capsule filling liquid and the soft capsule shell is 1: 1.
The invention also provides a preparation method of the novel flucalcitriol soft capsule, which comprises the following operation steps:
the method comprises the following steps: mixing fluocalcitriol, buffer and correctant, dissolving with anhydrous ethanol, and mixing with refined vegetable oil to obtain soft capsule filling solution;
step two: dissolving the sunscreen agent with a small amount of water; stirring and mixing correctant and water in a gelatin melting tank, heating in water bath, and heating to above 60 deg.C; adding gelatin and thickener, adding opacifier solution, and stirring; heating to 75 ℃, vacuumizing to a vacuum degree of-0.4 bar to-0.8 bar, and vacuumizing for 20 minutes; filtering with 100 mesh net, keeping the temperature at 60 + -5 deg.C, and removing air bubbles to obtain soft capsule shell material;
step three: making into soft capsule by soft capsule machine, and drying.
According to the fluocalcitriol soft capsule prepared by adopting the raw material formula, the soft capsule skin adopts a formula of matching gelatin, Arabic gum and xanthan gum in proportion, so that the gel hardness is reduced, the elasticity is enhanced, the strength, the thickness and the toughness of the capsule skin are proper, and different amounts of flavoring agents are added into the soft capsule skin and the soft capsule filling liquid, so that the soft capsule disclosed by the invention is good in taste and smell and good in chewiness; the soft capsule shell can not absorb water to soften or deform and be brittle, and the stability is obviously enhanced. The flucalcitriol soft capsule is a chewing soft capsule, greatly shortens the disintegration time, and has the advantages of quick response, high bioavailability and obvious advantages compared with similar products.
Detailed Description
The technical solutions in the embodiments of the present invention will be clearly and completely described below in conjunction with the embodiments of the present invention, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all of the embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.
Example 1
The soft capsule is prepared according to the method in the invention.
Example 2
The soft capsule is prepared according to the method in the invention.
Example 3
The soft capsule is prepared according to the method in the invention.
Example 4
The soft capsule is prepared according to the method in the invention.
And (3) selecting 20 persons to evaluate the samples in the embodiment, and evaluating according to the standard that 1-5 points respectively represent very poor, medium, good and good, wherein the average value is listed in table 1.
TABLE 1 sensory evaluation Table
TABLE 2 disintegration time limit
TABLE 3 Long term stability
Therefore, the chewing type fluocalcitriol soft capsule prepared by the formula provided by the invention has the advantages of good skin color, good fragrance, fast disintegration, good chewiness and good long-term stability, and can meet the requirements of consumers.
Finally, it should be noted that: although the present invention has been described in detail with reference to the general description and the specific embodiments, on the basis of the present invention, the above embodiments are only used for illustrating the technical solutions of the present invention, and not for limiting the same; while the invention has been described in detail and with reference to the foregoing embodiments, it will be understood by those skilled in the art that: the technical solutions described in the foregoing embodiments may still be modified, or some or all of the technical features may be equivalently replaced; and the modifications or the substitutions do not make the essence of the corresponding technical solutions depart from the scope of the technical solutions of the embodiments of the present invention.
Claims (9)
1. A novel flucalcitriol soft capsule is characterized in that: comprises a soft capsule filling liquid and a soft capsule shell, wherein the soft capsule filling liquid comprises, by weight, 0.001-0.005 part of flucalcitriol, 30000 parts of refined vegetable oil, 50000 parts of buffering agent, 5-10 parts of flavoring agent and 8-20 parts of absolute ethyl alcohol; the soft capsule shell consists of 20-40 parts by weight of gelatin, 10-20 parts by weight of thickening agent, 10-20 parts by weight of flavoring agent, 30-50 parts by weight of water and 5-10 parts by weight of opacifier.
2. The novel flucalcitriol soft capsule according to claim 1, characterized in that: the soft capsule filling liquid consists of 0.0015 part of fluocalcitriol, 35000 parts of refined vegetable oil, 8 parts of buffering agent, 8 parts of flavoring agent and 15 parts of absolute ethyl alcohol in parts by weight; the soft capsule shell comprises 38 parts by weight of gelatin, 15 parts by weight of thickening agent, 15 parts by weight of flavoring agent, 40 parts by weight of water and 8 parts by weight of opacifier.
3. The novel flucalcitriol soft capsule according to claim 1 or 2, characterized in that: in the component formula of the soft capsule filling liquid, the refined vegetable oil is any one or more of salad oil, corn oil, peanut oil and sesame oil; the buffer is one or two of citric acid and tartaric acid; the flavoring agent is essence and sweetener.
4. The novel flucalcitriol soft capsule according to claim 1 or 2, characterized in that: in the component formula of the soft capsule shell, the thickening agent is one or more of agar, guar gum, gellan gum, arabic gum, xanthan gum and locust bean gum; the flavoring agent is essence and sweetener; the opacifier is edible pigment.
5. The novel flucalcitriol soft capsule according to claim 3, characterized in that: in the formula of the components of the soft capsule filling liquid, the refined vegetable oil is a mixture of corn oil and peanut oil, and the dosage ratio of the corn oil to the peanut oil is 5: 2.
6. The novel flucalcitriol soft capsule according to claim 3, characterized in that: in the component formula of the soft capsule filling liquid, the buffering agent is a mixture of citric acid and tartaric acid, and the dosage ratio of the citric acid to the tartaric acid is 1: 3.
7. The novel flucalcitriol soft capsule according to claim 4, characterized in that: in the formula of the soft capsule shell, the thickening agent is acacia and xanthan gum, and the ratio of the acacia: the amount ratio of xanthan gum is 2: 1.
8. A novel flucalcitriol soft capsule according to claims 1 to 3, characterized in that: the dosage ratio of the essence and the sweetener in the flavoring agent in the soft capsule filling liquid and the soft capsule shell is 1: 1.
9. A preparation method of a novel fluocalcitriol soft capsule is characterized in that: the method specifically comprises the following operation steps:
the method comprises the following steps: mixing fluocalcitriol, buffer and correctant, dissolving with anhydrous ethanol, and mixing with refined vegetable oil to obtain soft capsule filling solution;
step two: dissolving the sunscreen agent with a small amount of water; stirring and mixing correctant and water in a gelatin melting tank, heating in water bath, and heating to above 60 deg.C; adding gelatin and thickener, adding opacifier solution, and stirring; heating to 75 ℃, vacuumizing to a vacuum degree of-0.4 bar to-0.8 bar, and vacuumizing for 20 minutes; filtering with 100 mesh net, keeping the temperature at 60 + -5 deg.C, and removing air bubbles to obtain soft capsule shell material;
step three: making into soft capsule by soft capsule machine, and drying.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202010629640.4A CN111773199A (en) | 2020-07-03 | 2020-07-03 | Novel fluorocalcitriol preparation and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202010629640.4A CN111773199A (en) | 2020-07-03 | 2020-07-03 | Novel fluorocalcitriol preparation and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN111773199A true CN111773199A (en) | 2020-10-16 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202010629640.4A Withdrawn CN111773199A (en) | 2020-07-03 | 2020-07-03 | Novel fluorocalcitriol preparation and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN111773199A (en) |
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2020
- 2020-07-03 CN CN202010629640.4A patent/CN111773199A/en not_active Withdrawn
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Application publication date: 20201016 |