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Compound tablet of dapoxetine hydrochloride and tadalafil and preparation method thereof

A technology of dapoxetine hydrochloride and tadalafil, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., and can solve the problem of affecting the release speed of sustained-release or immediate-release pellets , inaccurate drug dosage, micro-pill structure damage and other problems, to achieve good synergy, prevent micro-pill structure damage, and low crushing brittleness

Active Publication Date: 2022-07-26
SHANDONG HUBBLE KISEN BIOLOGICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dapoxetine hydrochloride and tadalafil have been made into pellets and capsules in the prior art, but there is still the problem of inaccurate drug dosage
Compared with capsules, tablets have the advantages of convenient division of drug dosage, accurate drug dosage, and stable quality. However, during the tableting process of making pellets into tablets, it is easy to squeeze and deform the pellets, which will damage the structure of the pellets. In turn affecting the release rate of sustained-release or immediate-release pellets

Method used

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  • Compound tablet of dapoxetine hydrochloride and tadalafil and preparation method thereof
  • Compound tablet of dapoxetine hydrochloride and tadalafil and preparation method thereof
  • Compound tablet of dapoxetine hydrochloride and tadalafil and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Weigh out 1 mmol γ-CD and 4 mmol K 2 CO 3 , 8 mmol NaOH or 8 mmol KOH, add 20 mL of pure water respectively, after ultrasonication to complete dissolution, use 0.8 pum water system to filter and filter to obtain the mother liquor for standby; Water methanol is placed in a closed container, heated in a water bath at 60 °C until the white turbidity is completely dissolved, and heating is continued for 20 min; immediately after taking out, add an equal volume of anhydrous methanol with a certain amount of PEG20000 dissolved, shake evenly, room temperature Let stand at 4000 rpm for 5 min, then pour off the supernatant, wash the precipitate twice with anhydrous ethanol and twice with anhydrous methanol, and dry the final solid at 40°C under vacuum overnight to obtain Nanoscale K 2 CO 3 -γ-CD-MOF, NaOH-γ-CD-MOF, KOH-γ-CD-MOF organic framework materials.

[0065] K prepared by the above method respectively 2 CO 3 - γ-CD-MOF, NaOH-γ-CD-MOF, KOH-γ-CD-MOF, γ-CD-MOF and CD a...

Embodiment 2

[0067] Example 2 Compression hardness test of drug-loaded matrix material

[0068] The matrix tablet was prepared by powder direct compression method. Weigh the excipients according to the prescribed amount, mix them evenly, pass through an 80-mesh sieve, mix with the sieve 3 times, dry in an oven at 40°C for 30 min, take out, add the prescribed amount of magnesium stearate, mix well, and press a 11 mm shallow arc The hardness test results are shown in Table 1.

[0069] Prescription: 18 g of drug-loaded matrix material, adding ELF Pharm and HPMC with a mass ratio of 1:1:1 K15M , Lactose powder, a total of 62 g.

[0070]

[0071] From the results in Table 1, the hardness of NaOH-γ-CD-MOF and KOH-γ-CD-MOF framework materials loaded with dapoxetine hydrochloride, and the hardness of KOH-γ-CD-MOF framework materials loaded with tadalafil Better, it can reach more than 20 kg, the compressibility is good, and there is no sticking and punching phenomenon, and it is suitable as ...

Embodiment 3

[0073] Add an appropriate amount of ultrapure aqueous solution to the centrifuge tube, add NaOH-γ-CD-MOF and KOH-γ-CD-MOF framework materials loaded with dapoxetine hydrochloride in excess, and KOH-γ- For CD-MOF skeleton material, place the centrifuge tube in an air-bath thermostatic shaker at 37°C, 100 r / min, shake well for 24 h, take the supernatant, and filter with a 0.22 μm membrane. The drug loading in the drug-loaded matrix material was tested. Precisely weigh 1 mg of each drug-loaded matrix material, dissolve them in 1 mL of ultrapure water, and filter them with a 0.22 μm filter membrane to determine the drug-loading amount. The results are shown in Table 2.

[0074]

[0075] From Table 2, it can be seen that the drug loading of NaOH-γ-CD-MOF framework materials loaded with dapoxetine hydrochloride is higher than that of KOH-γ-CD-MOF, so NaOH-γ-CD-MOF was selected as the next study. skeleton material.

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Abstract

The invention provides a dapoxetine hydrochloride and tadalafil composite tablet and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The compound tablet comprises dapoxetine hydrochloride pellets, tadalafil pellets, a tabletting aid and a lubricant, and by virtue of the arrangement of a coating structure, tadalafil with a relatively long half-life period and dapoxetine hydrochloride with a relatively short half-life period can act synchronously, so that a relatively good synergistic effect is achieved, and the treatment effect is improved.

Description

technical field [0001] The application relates to the field of pharmaceutical preparations, in particular to a composite tablet of dapoxetine hydrochloride and tadalafil and a preparation method thereof. Background technique [0002] Premature ejaculation (PE) is the most common ejaculation dysfunction, manifested as persistent or repeated penile penetration due to minimal sexual stimulation before, during, or shortly after penetration of the penis, and before sexual gratification. ejaculate. Premature ejaculation is a common sexual dysfunction disease in men, with a clinical incidence of about 30%. It can be divided into four types: secondary, primary, premature ejaculation-like ejaculation dysfunction and natural variability. At present, there are many clinical treatment methods, including drugs, surgery and behavioral therapy. Among them, dapoxetine hydrochloride is the only clinically approved drug for premature ejaculation. Dapoxetine hydrochloride is a serotonin reu...

Claims

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Application Information

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IPC IPC(8): A61K9/26A61K31/4985A61K47/44A61K47/38A61K47/32A61K47/40A61P15/08A61P15/10A61K31/138A61K9/50
CPCA61K31/138A61K31/4985A61K9/2081A61K9/2013A61K9/2027A61K9/2054A61K9/205A61P15/08A61P15/10A61K9/5073A61K2300/00
Inventor 王成张震王维剑武海军张家婧
Owner SHANDONG HUBBLE KISEN BIOLOGICAL TECH CO LTD
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