Semen Cassiae Soft Capsule High Active Ingredient Concentration

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Solution Overview

Problem

Current soft capsule preparations for lowering blood lipids and weight have low solid-state active ingredient content, leading to reduced efficacy and the need for higher dosages, and use vegetable oil as a dispersion medium, limiting the application due to low solubility of aqueous and ethanol-soluble drug ingredients.

Innovation Solution

A Semen Cassiae soft capsule formulation incorporating ethanol soluble extract powder of Semen Cassiae, aqueous soluble extract powder of Radix Glycyrrhizae, evening primrose oil, sea buckthorn seed oil, and beeswax, where the ethanol soluble extract powder is dissolved in ethanol and beeswax, mixed with evening primrose oil and Radix Glycyrrhizae extract, and then encapsulated with sea buckthorn seed oil to enhance solubility and efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If vegetable oil is used as dispersion medium in soft capsule preparations, then the soft capsule can be manufactured with conventional technology, but the concentration of aqueous and ethanol soluble drug ingredients is low

Engineering Contradiction:
ImprovemanufacturabilityVSAvoidconcentration of active ingredients
Core Design Contradiction:
Ease of manufactureVSQuantity of substance

Solution Approach 1:

The patent uses a composite dispersion medium system combining vegetable oil with ethanol and water to create a multi-phase system. This allows both lipid-soluble and water-soluble active ingredients to be simultaneously dispersed at high concentrations, resolving the contradiction between ease of manufacture and active ingredient concentration.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent changes the physical and chemical parameters of the dispersion medium by introducing ethanol and water into the vegetable oil system. This creates a cosolvent system that can dissolve both hydrophobic and hydrophilic active ingredients, thereby increasing the overall concentration of active ingredients while maintaining manufacturability.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If higher dosage is used to compensate for low efficacy, then the active ingredient content per capsule remains low, but the treatment effect is insufficient

Engineering Contradiction:
Improveactive ingredient contentVSAvoidefficacy
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent changes the solubility parameters of the formulation by using a multi-phase dispersion medium system. This allows significantly higher concentrations of both water-soluble and ethanol-soluble active ingredients to be incorporated into each capsule, thereby increasing the effective dose per capsule and improving treatment efficacy without requiring patients to take excessive numbers of capsules.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS8859006B2Semen cassiae soft capsule for reducing fat and losing weight and preparation method thereof
Publication Date: 2014.10.14 MA JIANZHONG

AI summary

A Semen Cassiae soft capsule for lowering blood lipids and losing weight and the preparation method thereof. The content of the soft capsule consist of the following components by weight part: 10-60 parts of ethanol soluble extract powder of Semen Cassiae, 2-10 parts of aqueous soluble extract powder of Radix Glycyrrhizae, 10-30 parts of evening primrose oil, 5-20 parts of sea buckthorn seed oil and 2-10 parts of beeswax. The preparation method includes the following steps: preparing all the components respectively; dissolving the ethanol soluble extract powder of Semen Cassiae in ethanol, adding 50% of the total weight of beeswax, heating in a water bath at 75 degrees Celsius to obtain a liquid mixture of Semen Cassiae and beeswax; heating the remainder beeswax with evening primrose oil, adding the liquid mixture of Semen Cassiae and beeswax while continuously stirring, adding aqueous soluble extract powder of Radix Glycyrrhizae, cooling the mixture by circulation water, adding sea buckthorn seed oil and continuously stirring to obtain the content for soft capsules, encapsulating soft capsules by conventional method to obtain the Semen Cassiae soft capsule.