CN113577079A - Preparation method and composition of phosphodiesterase inhibitor - Google Patents
Preparation method and composition of phosphodiesterase inhibitor Download PDFInfo
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
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Abstract
The invention relates to a preparation method of a phosphodiesterase inhibitor and a composition, wherein the preparation method comprises the steps of uniformly mixing tadalafil and lactose, processing by adopting a method of combining mechanical crushing and airflow crushing, and solving the problems of dissolution rate and bioavailability of a product by utilizing a surfactant solubilization technology, and is suitable for industrial mass production.
Description
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to a preparation method and a composition of a phosphodiesterase inhibitor.
Background
Tadalafil tablets are selective, reversible inhibitors of cyclic guanosine monophosphate (cGMP) specific phosphodiesterase 5(PDE5) that, when sexual stimulation results in local nitric oxide release, PDE5 is inhibited by tadalafil, resulting in elevated levels of cGMP within the corpora cavernosa, which leads to smooth muscle relaxation, blood flow into penile tissue, and erection, such as asexual stimulation.
The tadalafil solubility was: it is easily soluble in dimethyl sulfoxide, slightly soluble in acetonitrile, glacial acetic acid or dichloromethane, very slightly soluble in methanol, and hardly soluble in water or isopropanol, and BCS is classified as class II or class IV, and is a poorly soluble drug.
US6841167 discloses that tadalafil has a solubility of 2ug/ml in water at 25 c, so it has a lower dissolution rate and a lower bioavailability.
The tadalafil has the problems of poor water solubility, slow dissolution rate, low bioavailability and the like in the prior art, and the technical problems in the prior art are solved by improving the prescription and the preparation process technology.
Disclosure of Invention
According to the invention, through researching and improving the prescription and the preparation technology, the uniformity of tadalafil in vitro dissolution and in vivo absorption is ensured, and the technical problems of low dissolution speed, low bioavailability and the like of the product are solved.
In order to realize the purpose of the invention, the invention adopts the following technical scheme:
a process for preparing phosphodiesterase inhibitor includes pulverizing, sieving, weighing, mixing, granulating, total mixing, tabletting and coating.
Preferably, the preparation method of the phosphodiesterase inhibitor comprises the following steps:
1) crushing and sieving: sieving lactose, microcrystalline cellulose, binder, and disintegrating agent respectively; premixing sieved lactose and tadalafil raw materials according to a certain proportion, crushing the lactose and tadalafil raw materials in a universal crusher, and crushing the lactose and tadalafil raw materials in a jet mill for later use, wherein the jet milling air pressure is 0.4-1.0MPa, and the feeding air pressure is 0.4-0.6 MPa; the applicant finds that the heat of the crusher is serious when the tadalafil is crushed independently in the experimental process, and through a large amount of experimental researches, the lactose which is not less than one time (weight ratio) is added in the crushing process for crushing, so that the heat of the crusher is not generated, the sieving is smooth, and the efficiency is improved; the micro-powder process adopts a method that tadalafil and lactose are premixed and placed in a universal pulverizer to be pulverized for 1 time, and then the tadalafil and the lactose are pulverized for 1 time by air flow, so that the particle size distribution D90 of the raw material medicine of the pulverized tadalafil is less than 10 mu m; the premixing ratio of tadalafil to lactose is 1:1-5 (weight ratio); preferably, the pre-mixing ratio of tadalafil to lactose is 1:5 (weight ratio);
2) weighing and mixing: weighing a mixture of the crushed tadalafil and lactose according to the prescription amount, and mixing the mixture with the microcrystalline cellulose, the disintegrant, the binder and the sieved lactose according to the prescription amount in a wet mixing granulator;
3) and (3) granulating: continuously adding the wetting agent dissolved in the wetting agent into the uniformly mixed material in the step 2), uniformly stirring, granulating by a wet method, drying and finishing;
4) total mixing and tabletting: adding a lubricant with a prescribed amount into the granules in the step 3), mixing, performing tabletting operation, and tabletting;
5) coating: coating with gastric-soluble film coat.
Another object of the present invention is to provide a novel phosphodiesterase inhibitor composition: the prescription of the composition comprises the following components in percentage by weight: 4 to 6 percent of tadalafil, 71 to 73 percent of lactose, 12 to 14.5 percent of microcrystalline cellulose, 7 to 9 percent of disintegrant, 0.5 to 1 percent of adhesive, 0.29 to 0.35 percent of solubilizer and 0.5 to 1 percent of lubricant.
Further preferably, the composition formula comprises the following weight percentages: 4% tadalafil, 73% lactose, 14.5% microcrystalline cellulose, 7% disintegrant, 0.6% binder, 0.3% solubilizer, 0.6% lubricant.
Preferably, the solubilizer is sodium lauryl sulfate, the disintegrant is croscarmellose sodium, the binder is high-substituted hydroxypropyl cellulose, and the lubricant is magnesium stearate.
Compared with the prior art, the invention has the following advantages:
(1) solves the problem of difficult dissolution of the raw material medicine, and leads the in vitro dissolution to be consistent with the original research.
(2) The invention overcomes the problems of serious heat generation and difficult sieving of tadalafil raw material medicaments when the tadalafil raw material medicaments are crushed by improving the preparation process.
(3) The invention adopts a method combining mechanical grinding and air flow grinding in the aspect of micronization process, easily ensures that 90 percent of particles of the tadalafil raw material medicine have the particle size of less than 10 mu m, and combines a surfactant solubilization technology, effectively solves the problem of difficult dissolution of the raw material medicine, and improves the bioavailability.
Detailed Description
The present invention will be further described by way of the following examples, but the present invention is not limited to the following examples, which do not limit the scope of the present invention in any way. Certain changes and modifications within the scope of the claims, which may be made by one skilled in the art, are also considered to be within the scope of the invention.
Example 1
Prescription:
the preparation method comprises the following steps:
1) crushing and sieving: sieving lactose, microcrystalline cellulose, high-substituted hydroxypropyl cellulose, and croscarmellose sodium respectively; taking the sieved lactose and tadalafil raw material medicines according to the mass ratio of 1:1, premixing in proportion, crushing the mixture for 1 time by a universal crusher, crushing the mixture for 1 time by an airflow crusher (the air pressure of the airflow crusher is 0.4-1.0Mpa, and the feeding air pressure is 0.4-0.6Mpa), measuring the particle size by a Malvern laser particle size analyzer, sampling and measuring the content, wherein the particle size distribution D90 of the tadalafil raw material is less than 10 mu m;
2) weighing and mixing: weighing a mixture of the crushed tadalafil and lactose according to the prescription amount, and mixing the mixture with the microcrystalline cellulose, the croscarmellose sodium, the high-substituted hydroxypropyl cellulose and the sieved lactose according to the remaining prescription amount in a wet mixing granulator;
3) and (3) granulating: continuously adding the sodium dodecyl sulfate dissolved in the purified water into the uniformly mixed material in the step 2), uniformly stirring, granulating by a wet method, drying and finishing;
4) total mixing and tabletting: adding magnesium stearate with the prescription amount into the granules in the step 3), mixing, performing tabletting operation, and tabletting;
5) coating: coating with gastric-soluble film coat.
Example 2
Prescription:
the preparation method comprises the following steps:
1) crushing and sieving: sieving lactose, microcrystalline cellulose, high-substituted hydroxypropyl cellulose, and croscarmellose sodium respectively; taking the sieved lactose and tadalafil raw material medicines according to the mass ratio of 1: 3, premixing in proportion, crushing the mixture for 1 time by using a universal crusher, crushing the mixture for 1 time by using an airflow crusher (the air pressure of the airflow crusher is 0.4-1.0Mpa, and the feeding air pressure is 0.4-0.6Mpa), measuring the particle size by using a Malvern laser particle size analyzer, wherein the particle size distribution D90 of the tadalafil raw material medicine is less than 10 mu m, and sampling to measure the content for later use;
2) weighing and mixing: weighing a mixture of the crushed tadalafil and lactose according to the prescription amount, and mixing the mixture with the microcrystalline cellulose, the croscarmellose sodium, the high-substituted hydroxypropyl cellulose and the sieved lactose according to the remaining prescription amount in a wet mixing granulator;
3) and (3) granulating: continuously adding the sodium dodecyl sulfate dissolved in the purified water into the uniformly mixed material in the step 2), uniformly stirring, granulating by a wet method, drying and finishing;
4) total mixing and tabletting: adding magnesium stearate with the prescription amount into the granules in the step 3), mixing, performing tabletting operation, and tabletting;
5) coating: coating with gastric-soluble film coat.
Example 3
Prescription:
the preparation method comprises the following steps:
1) crushing and sieving: sieving lactose, microcrystalline cellulose, high-substituted hydroxypropyl cellulose, and croscarmellose sodium respectively; taking the sieved lactose and tadalafil raw material medicines according to the mass ratio of 1:5, premixing in proportion, crushing the mixture for 1 time by a universal crusher, crushing the mixture for 1 time by an airflow crusher (the air pressure of the airflow crusher is 0.4-1.0Mpa, and the feeding air pressure is 0.4-0.6Mpa), measuring the particle size by a Malvern laser particle size analyzer, sampling and measuring the content, wherein the particle size distribution D90 of the tadalafil raw material is less than 10 mu m;
2) weighing and mixing: weighing a mixture of the crushed tadalafil and lactose according to the prescription amount, and mixing the mixture with the microcrystalline cellulose, the croscarmellose sodium, the high-substituted hydroxypropyl cellulose and the sieved lactose according to the remaining prescription amount in a wet mixing granulator;
3) and (3) granulating: continuously adding the sodium dodecyl sulfate dissolved in the purified water into the uniformly mixed material in the step 2), uniformly stirring, granulating by a wet method, drying and finishing;
4) total mixing and tabletting: adding magnesium stearate with the prescription amount into the granules in the step 3), mixing, performing tabletting operation, and tabletting;
5) coating: coating with gastric-soluble film coat.
Comparative example 1
Prescription: same as in example 3.
The preparation method comprises the following steps:
1) crushing and sieving: sieving lactose, microcrystalline cellulose, high-substituted hydroxypropyl cellulose, and croscarmellose sodium respectively; crushing the sieved tadalafil raw material medicine for 1 time by a universal crusher, determining the particle size by using a Malvern laser particle size analyzer, wherein the particle size distribution D90 of the tadalafil raw material medicine is less than 10 mu m, and sampling to determine the content for later use;
2) weighing and mixing: weighing the tadalafil crushed according to the prescription amount, mixing the tadalafil crushed according to the prescription amount with the microcrystalline cellulose, the croscarmellose sodium, the highly substituted hydroxypropyl cellulose and the screened lactose according to the prescription amount in a wet mixing granulator;
3) and (3) granulating: continuously adding the sodium dodecyl sulfate dissolved in the purified water into the uniformly mixed material in the step 2), uniformly stirring, granulating by a wet method, drying and finishing;
4) total mixing and tabletting: adding magnesium stearate with the prescription amount into the granules in the step 3), mixing, performing tabletting operation, and tabletting;
5) coating: coating with gastric-soluble film coat.
Comparative example 2
Prescription: same as in example 3.
The preparation method comprises the following steps:
1) crushing and sieving: sieving lactose, microcrystalline cellulose, high-substituted hydroxypropyl cellulose, and croscarmellose sodium respectively; crushing the sieved tadalafil raw material for 1 time by using an airflow crusher (the air pressure of the airflow crusher is 0.4-1.0Mpa, and the feeding air pressure is 0.4-0.6Mpa), measuring the particle size by using a Malvern laser particle size analyzer, wherein the particle size distribution D90 of the tadalafil raw material is less than 10 mu m, sampling and measuring the content for later use;
2) weighing and mixing: weighing the tadalafil crushed according to the prescription amount, and mixing the tadalafil crushed according to the prescription amount with the microcrystalline cellulose, the croscarmellose sodium, the highly substituted hydroxypropyl cellulose and the sieved lactose in a wet mixing granulator;
3) and (3) granulating: continuously adding the sodium dodecyl sulfate dissolved in the purified water into the uniformly mixed material in the step 2), uniformly stirring, granulating by a wet method, drying and finishing;
4) total mixing and tabletting: adding magnesium stearate with the prescription amount into the granules in the step 3), mixing, performing tabletting operation, and tabletting;
5) coating: coating with gastric-soluble film coat.
Comparative example 3
Prescription:
the preparation method comprises the following steps:
1) crushing and sieving: sieving lactose, microcrystalline cellulose, high-substituted hydroxypropyl cellulose, and croscarmellose sodium respectively; taking the sieved lactose and tadalafil raw material medicines according to the mass ratio of 1:5, premixing in proportion, crushing the mixture for 1 time by a universal crusher, crushing the mixture for 1 time by an airflow crusher (the air pressure of the airflow crusher is 0.4-1.0Mpa, and the feeding air pressure is 0.4-0.6Mpa), measuring the particle size by a Malvern laser particle size analyzer, sampling and measuring the content, wherein the particle size distribution D90 of the tadalafil raw material is less than 10 mu m;
2) weighing and mixing: weighing a mixture of the crushed tadalafil and lactose according to the prescription amount, and mixing the mixture with the microcrystalline cellulose, the croscarmellose sodium, the high-substituted hydroxypropyl cellulose and the sieved lactose according to the remaining prescription amount in a wet mixing granulator;
3) and (3) granulating: adding purified water into the uniformly mixed material in the step 2), uniformly stirring, performing wet granulation, drying and finishing;
4) total mixing and tabletting: adding magnesium stearate with the prescription amount into the granules in the step 3), mixing, performing tabletting operation, and tabletting;
5) coating: coating with gastric-soluble film coat.
Comparative example 4
Prescription:
the preparation method comprises the following steps:
1) crushing and sieving: sieving lactose, microcrystalline cellulose, high-substituted hydroxypropyl cellulose, and croscarmellose sodium respectively; taking the sieved lactose and tadalafil raw material medicines according to the mass ratio of 1:5, premixing in proportion, crushing the mixture for 1 time by a universal crusher, crushing the mixture for 1 time by an airflow crusher (the air pressure of the airflow crusher is 0.4-1.0Mpa, and the feeding air pressure is 0.4-0.6Mpa), measuring the particle size by a Malvern laser particle size analyzer, sampling and measuring the content, wherein the particle size distribution D90 of the tadalafil raw material is less than 10 mu m;
2) weighing and mixing: weighing a mixture of the crushed tadalafil and lactose according to the prescription amount, and mixing the mixture with the microcrystalline cellulose, the croscarmellose sodium, the high-substituted hydroxypropyl cellulose and the sieved lactose according to the remaining prescription amount in a wet mixing granulator;
3) and (3) granulating: continuously adding the sodium dodecyl sulfate dissolved in the purified water into the uniformly mixed material in the step 2), uniformly stirring, granulating by a wet method, drying and finishing;
4) total mixing and tabletting: adding magnesium stearate with the prescription amount into the granules in the step 3), mixing, performing tabletting operation, and tabletting;
5) coating: coating with gastric-soluble film coat.
Experimental example 1
The change in particle size data before and after the treatments of examples 1 to 3 and comparative examples 1 to 2 was measured, and the results are shown in Table 1.
Table 1: particle size detection data comparison
Experimental example 2
Tadalafil tablets prepared in examples 1-3 of the present invention, tablets prepared in comparative examples 1-4, and the original research
The dissolution rate of tadalafil tablets (purchased commercially) was measured by high performance liquid chromatography in 0.25% sodium dodecyl sulfate solution as dissolution medium according to the standard of 'Chinese pharmacopoeia' 2015 edition, and the experimental results are shown in table 2.
TABLE 2 dissolution data comparison
As shown in Table 2, the dissolution rate of Tadalafil tablets prepared by the invention is higher than that of the original research
The tablets dissolve out substantially consistently.
Experimental example 3
Tadalafil tablets prepared by the invention and original grinding
The tablets were subjected to beagle pharmacokinetic experiments, and the experimental results are shown in table 3.
Table 3: comparison of pharmacokinetic experiments
And (4) conclusion: AUC and Cmax data show that the bioavailability and the peak concentration of the tadalafil tablet prepared by the invention are improved and are superior to those of the tadalafil tablet prepared by the prior art (original product).
Claims (9)
1. A preparation method of a phosphodiesterase inhibitor comprises the steps of crushing, sieving, weighing, mixing, granulating, total mixing, tabletting and coating, and is characterized in that the crushing process adopts mechanical crushing, and then the airflow crushing treatment is carried out on the crushed material.
2. The method of preparing a phosphodiesterase inhibitor according to claim 1, comprising the steps of:
1) crushing and sieving: sieving lactose, microcrystalline cellulose, binder, and disintegrating agent respectively; premixing the sieved lactose and the tadalafil raw material medicine according to a certain proportion, crushing the premixed lactose and the tadalafil raw material medicine by a universal crusher, and crushing the crushed tadalafil raw material medicine by an airflow crusher for later use;
2) weighing and mixing: weighing a mixture of the crushed tadalafil and lactose according to the prescription amount, and mixing the mixture with the microcrystalline cellulose, the disintegrant, the binder and the sieved lactose according to the prescription amount in a wet mixing granulator;
3) and (3) granulating: adding a solubilizer into the uniformly mixed material obtained in the step 2), uniformly stirring, performing wet granulation, drying and finishing;
4) total mixing and tabletting: adding a lubricant with a prescribed amount into the granules in the step 3), mixing, performing tabletting operation, and tabletting;
5) coating: coating with gastric-soluble film coat.
3. The method of claim 2, wherein the gas stream crushing pressure in step 1) is 0.4 to 1.0Mpa, and the feed gas pressure is 0.4 to 0.6 Mpa.
4. The method of preparing a phosphodiesterase inhibitor according to claim 2, wherein the pre-mixing ratio of tadalafil to lactose in step 1) is 1: 1-5.
5. The method of preparing a phosphodiesterase inhibitor according to claim 4, wherein the pre-mixing ratio of tadalafil to lactose in step 1) is 1: 5.
6. The method for preparing a phosphodiesterase inhibitor according to claim 2, wherein the granulation process in the step 3) is performed by dissolving the solubilizer in the wetting agent and continuously adding the dissolved solubilizer to the material for wet granulation.
7. The composition prepared by any of the preparation methods of claims 1-6, wherein the composition is formulated in the following weight percentages: 4 to 6 percent of tadalafil, 71 to 73 percent of lactose, 12 to 14.5 percent of microcrystalline cellulose, 7 to 9 percent of disintegrant, 0.5 to 1 percent of adhesive, 0.29 to 0.35 percent of solubilizer and 0.5 to 1 percent of lubricant.
8. The composition of claim 7, wherein the composition is formulated in the following weight percentages: 4% tadalafil, 73% lactose, 14.5% microcrystalline cellulose, 7% disintegrant, 0.6% binder, 0.3% solubilizer, 0.6% lubricant.
9. The composition according to claim 7 or 8, wherein the solubilizer is sodium lauryl sulfate, the disintegrant is croscarmellose sodium, the binder is highly substituted hydroxypropylcellulose, and the lubricant is magnesium stearate.
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| CN114366721A (en) * | 2021-12-27 | 2022-04-19 | 海南卓力制药有限公司 | Tadalafil-containing pharmaceutical composition tablet and preparation method thereof |
| CN117482057A (en) * | 2023-11-30 | 2024-02-02 | 福安药业集团宁波天衡制药有限公司 | Stable granisetron hydrochloride tablet and preparation method thereof |
| CN117482057B (en) * | 2023-11-30 | 2024-07-26 | 福安药业集团宁波天衡制药有限公司 | Stable granisetron hydrochloride tablet and preparation method thereof |
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